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Sample records for non-inflammatory microspheres inhibits

  1. Characterization of unsaturated fatty acid sustained-release microspheres for long-term algal inhibition.

    Science.gov (United States)

    Ni, Lixiao; Jie, Xiaoting; Wang, Peifang; Li, Shiyin; Hu, Shuzhen; Li, Yiping; Li, Yong; Acharya, Kumud

    2015-02-01

    The unsaturated fatty acid (linoleic acid) sustained-release microspheres were prepared with linoleic acid (LA) using alginate-chitosan microcapsule technology. These LA sustained-release microspheres had a high encapsulation efficiency (up to 62%) tested by high performance liquid chromatography with a photo diode array. The dry microspheres were characterized by a scanning electron microscope, X-ray diffraction measurement, dynamic thermogravimetric analysis and Fourier transform infrared spectral analysis. The results of characterization showed that the microspheres had good thermal stability (decomposition temperature of 236°C), stable and temperature independent release properties (release time of more than 40 d). Compared to direct dosing of LA, LA sustained-released microspheres could inhibit Microcystis aeruginosa growth to the non-growth state. The results of this study suggested that the LA sustained-release microspheres may be a potential candidate for algal inhibition. Copyright © 2014 Elsevier Ltd. All rights reserved.

  2. Biocompatibility, Inflammatory Response, and Recannalization Characteristics of Nonradioactive Resin Microspheres: Histological Findings

    International Nuclear Information System (INIS)

    Bilbao, Jose I.; Martino, Alba de; Luis, Esther de; Diaz-Dorronsoro, Lourdes; Alonso-Burgos, Alberto; Martinez de la Cuesta, Antonio; Sangro, Bruno; Garcia de Jalon, Jose A.

    2009-01-01

    Intra-arterial radiotherapy with yttrium-90 microspheres (radioembolization) is a therapeutic procedure exclusively applied to the liver that allows the direct delivery of high-dose radiation to liver tumors, by means of endovascular catheters, selectively placed within the tumor vasculature. The aim of the study was to describe the distribution of spheres within the precapillaries, inflammatory response, and recannalization characteristics after embolization with nonradioactive resin microspheres in the kidney and liver. We performed a partial embolization of the liver and kidney vessels in nine white pigs. The left renal and left hepatic arteries were catheterized and filled with nonradioactive resin microspheres. Embolization was defined as the initiation of near-stasis of blood flow, rather than total occlusion of the vessels. The hepatic circulation was not isolated so that the effects of reflux of microspheres into stomach could be observed. Animals were sacrificed at 48 h, 4 weeks, and 8 weeks, and tissue samples from the kidney, liver, lung, and stomach evaluated. Microscopic evaluation revealed clusters of 10-30 microspheres (15-30 μm in diameter) in the small vessels of the kidney (the arciform arteries, vasa recti, and glomerular afferent vessels) and liver. Aggregates were associated with focal ischemia and mild vascular wall damage. Occlusion of the small vessels was associated with a mild perivascular inflammatory reaction. After filling of the left hepatic artery with microspheres, there was some evidence of arteriovenous shunting into the lungs, and one case of cholecystitis and one case of marked gastritis and ulceration at the site of arterial occlusion due to the presence of clusters of microspheres. Beyond 48 h, microspheres were progressively integrated into the vascular wall by phagocytosis and the lumen recannalized. Eight-week evaluation found that the perivascular inflammatory reaction was mild. Liver cell damage, bile duct injury, and

  3. Fiber-optic microsphere-based antibody array for the analysis of inflammatory cytokines in saliva.

    Science.gov (United States)

    Blicharz, Timothy M; Siqueira, Walter L; Helmerhorst, Eva J; Oppenheim, Frank G; Wexler, Philip J; Little, Frédéric F; Walt, David R

    2009-03-15

    Antibody microarrays have emerged as useful tools for high-throughput protein analysis and candidate biomarker screening. We describe here the development of a multiplexed microsphere-based antibody array capable of simultaneously measuring 10 inflammatory protein mediators. Cytokine-capture microspheres were fabricated by covalently coupling monoclonal antibodies specific for cytokines of interest to fluorescently encoded 3.1 microm polymer microspheres. An optical fiber bundle containing approximately 50,000 individual 3.1 microm diameter fibers was chemically etched to create microwells in which cytokine-capture microspheres could be deposited. Microspheres were randomly distributed in the wells to produce an antibody array for performing a multiplexed sandwich immunoassay. The array responded specifically to recombinant cytokine solutions in a concentration-dependent fashion. The array was also used to examine endogenous mediator patterns in saliva supernatants from patients with pulmonary inflammatory diseases such as asthma and chronic obstructive pulmonary disease (COPD). This array technology may prove useful as a laboratory-based platform for inflammatory disease research and diagnostics, and its small footprint could also enable integration into a microfluidic cassette for use in point-of-care testing.

  4. Polymer based microspheres of aceclofenac as sustained release parenterals for prolonged anti-inflammatory effect

    Energy Technology Data Exchange (ETDEWEB)

    Kaur, Manpreet; Sharma, Sumit; Sinha, VR, E-mail: sinha_vr@rediffmail.com

    2017-03-01

    Poly(lactic-co-glycolic acid) (PLGA) (75:25) and polycaprolactone (PCL) microspheres were fabricated for prolonged release of aceclofenac by parenteral administration. Microspheres encapsulating aceclofenac were designed to release the drug at controlled rate for around one month. Biodegradable microspheres were prepared by solvent emulsification evaporation method in different polymer:drug ratios (1:1, 2:1 and 3:1). After drug loading, PLGA and PCL microspheres showed a controlled size distribution with an average size of 11.75 μm and 3.81 μm respectively and entrapment efficiency in the range of 90 ± 0.72% to 91.06 ± 4.01% with PLGA and 83.01 ± 2.13% to 90.4 ± 2.11% with PCL. Scanning electron microscopy has confirmed good spherical structures of microspheres. The percent yield of biodegradable polymeric microspheres ranged between 30.95 ± 10.14% to 92.84 ± 3.15% and 47.33 ± 4.72% to 80 ± 3.60% for PLGA and PCL microspheres respectively. PLGA microspheres followed Higuchi release pattern while Korsmeyer-Peppas explained the release pattern of PCL microspheres. Stability studies of microspheres were also carried out by storing the preparations at 2-8 °C for 30, 60 and 90 days and evaluating them for entrapment efficiency, residual drug content and polymer drug compatability. In-vivo studies showed significant anti-inflammatory activity of microspheres upto 48 hours using the carrageenan induced rat paw oedema model. - Highlights: • PLGA and PCL polymeric microspheres for parenteral prolonged drug delivery system were formulated. • Polymeric microspheres were characterized physically and drug excipient incompatability. • Three months accelerated stability studies were carried for drug loaded polymeric microspheres. • Pharmacodynamic studies prove the rationality of sustained therapeutic effect of designed drug delivery system.

  5. Solvent/Non-Solvent Sintering To Make Microsphere Scaffolds

    Science.gov (United States)

    Laurencin, Cato T.; Brown, Justin L.; Nair, Lakshmi

    2011-01-01

    A solvent/non-solvent sintering technique has been devised for joining polymeric microspheres to make porous matrices for use as drug-delivery devices or scaffolds that could be seeded with cells for growing tissues. Unlike traditional sintering at elevated temperature and pressure, this technique is practiced at room temperature and pressure and, therefore, does not cause thermal degradation of any drug, protein, or other biochemical with which the microspheres might be loaded to impart properties desired in a specific application. Also, properties of scaffolds made by this technique are more reproducible than are properties of comparable scaffolds made by traditional sintering. The technique involves the use of two miscible organic liquids: one that is and one that is not a solvent for the affected polymer. The polymeric microspheres are placed in a mold having the size and shape of the desired scaffold, then the solvent/non-solvent mixture is poured into the mold to fill the void volume between the microspheres, then the liquid mixture is allowed to evaporate. Some of the properties of the resulting scaffold can be tailored through choice of the proportions of the liquids and the diameter of the microspheres.

  6. Pharmacodynamics of diclofenac from novel Eudragit entrapped microspheres.

    Science.gov (United States)

    Momoh, M A; Kenechukwu, F C; Adedokun, M O; Odo, C E; Attama, A A

    2014-05-01

    Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations. The objective of this study was to evaluate Eudragit® RS100/RL100 microspheres formulated by the solvent-evaporation technique for improved delivery of diclofenac. Three batches of (DF1, DF2 and DF3) microspheres were prepared using different ratios of Eudragit RS-100 and RL-100 polymers based on the solvent-evaporation method. The microspheres were characterized based on morphological properties, particle size analysis and encapsulation efficiency (EE%). In vitro release of DS was investigated in both 0.1 N HCl (pH 1.2) and phosphate-buffered saline (pH 7.4), while anti-inflammatory studies were evaluated in the rat model. Maximum EE% of 86.61 ± 0.11, 88.14 ± 0.16 and 85.50 ± 0.21 was obtained for DF1, DF2 and DF3, respectively. Discrete, smooth and brownish microspheres of size range 437 ± 0.01-479 ± 0.21 µm were obtained. Release of DS from the formulation depends on the polymer ratio. All the batches exhibited good anti-inflammatory activities. Microsphere formulations based on Eudragit® polymers would likely offer a reliable and alternative means of delivering DS orally.

  7. Synthesis, characterisation and biomedical applications of curcumin conjugated chitosan microspheres.

    Science.gov (United States)

    Saranya, T S; Rajan, V K; Biswas, Raja; Jayakumar, R; Sathianarayanan, S

    2018-04-15

    Curcumin is a diaryl heptanoid of curcuminoids class obtained from Curcuma longa. It possesses various biological activities like anti-inflammatory, hypoglycemic, antioxidant, wound-healing, and antimicrobial activities. Chitosan is a biocompatible, biodegradable and non-toxic natural polymer which enhances the adhesive property of the skin. Chemical conjugation will leads to sustained release action and to enhance the bioavailability. This study aims to synthesis and characterize biocompatible curcumin conjugated chitosan microspheres for bio-medical applications. The Schiff base reaction was carried out for the preparation of curcumin conjugated chitosan by microwave method and it was characterised using FTIR and NMR. Curcumin conjugated chitosan microspheres (CCCMs) were prepared by wet milling solvent evaporation method. SEM analysis showed these CCCMs were 2-5μm spherical particles. The antibacterial activities of the prepared CCCMs were studied against Staphylococcus aureus and Escherichia coli, the zone of inhibition was 28mm and 23mm respectively. Antioxidant activity of the prepared CCCMs was also studied by DPPH and H 2 O 2 method it showed IC 50 esteem value of 216μg/ml and 228μg/ml, and anti-inflammatory activity results showed that CCCMs having IC 50 value of 45μg/ml. The results conclude that the CCCMs having a good antibacterial, antioxidant and anti-inflammatory activities. This, the prepared CCCMs have potential application in preventing skin infections. Copyright © 2017. Published by Elsevier B.V.

  8. TRI Microspheres prevent key signs of dry eye disease in a murine, inflammatory model.

    Science.gov (United States)

    Ratay, Michelle L; Balmert, Stephen C; Acharya, Abhinav P; Greene, Ashlee C; Meyyappan, Thiagarajan; Little, Steven R

    2017-12-13

    Dry eye disease (DED) is a highly prevalent, ocular disorder characterized by an abnormal tear film and ocular surface. Recent experimental data has suggested that the underlying pathology of DED involves inflammation of the lacrimal functional unit (LFU), comprising the cornea, conjunctiva, lacrimal gland and interconnecting innervation. This inflammation of the LFU ultimately results in tissue deterioration and the symptoms of DED. Moreover, an increase of pathogenic lymphocyte infiltration and the secretion of pro-inflammatory cytokines are involved in the propagation of DED-associated inflammation. Studies have demonstrated that the adoptive transfer of regulatory T cells (Tregs) can mediate the inflammation caused by pathogenic lymphocytes. Thus, as an approach to treating the inflammation associated with DED, we hypothesized that it was possible to enrich the body's own endogenous Tregs by locally delivering a specific combination of Treg inducing factors through degradable polymer microspheres (TRI microspheres; TGF-β1, Rapamycin (Rapa), and IL-2). This local controlled release system is capable of shifting the balance of Treg/T effectors and, in turn, preventing key signs of dry eye disease such as aqueous tear secretion, conjunctival goblet cells, epithelial corneal integrity, and reduce the pro-inflammatory cytokine milieu in the tissue.

  9. Solvent/non-solvent sintering: a novel route to create porous microsphere scaffolds for tissue regeneration.

    Science.gov (United States)

    Brown, Justin L; Nair, Lakshmi S; Laurencin, Cato T

    2008-08-01

    Solvent/non-solvent sintering creates porous polymeric microsphere scaffolds suitable for tissue engineering purposes with control over the resulting porosity, average pore diameter, and mechanical properties. Five different biodegradable biocompatible polyphosphazenes exhibiting glass transition temperatures from -8 to 41 degrees C and poly (lactide-co-glycolide), (PLAGA) a degradable polymer used in a number of biomedical settings, were examined to study the versatility of the process and benchmark the process to heat sintering. Parameters such as: solvent/non-solvent sintering solution composition and submersion time effect the sintering process. PLAGA microsphere scaffolds fabricated with solvent/non-solvent sintering exhibited an interconnected porosity and pore size of 31.9% and 179.1 mum, respectively which was analogous to that of conventional heat sintered PLAGA microsphere scaffolds. Biodegradable polyphosphazene microsphere scaffolds exhibited a maximum interconnected porosity of 37.6% and a maximum compressive modulus of 94.3 MPa. Solvent/non-solvent sintering is an effective strategy for sintering polymeric microspheres, with a broad spectrum of glass transition temperatures, under ambient conditions making it an excellent fabrication route for developing tissue engineering scaffolds and drug delivery vehicles. (c) 2007 Wiley Periodicals, Inc.

  10. Continuous delivery of propranolol from liposomes-in-microspheres significantly inhibits infantile hemangioma growth

    Directory of Open Access Journals (Sweden)

    Guo XN

    2017-09-01

    Full Text Available Xiaonan Guo,1,* Xiaoshuang Zhu,1,* Dakan Liu,1 Yubin Gong,1 Jing Sun,2 Changxian Dong1 1Department of Hemangioma and Vascular Malformation, Henan Provincial People’s Hospital, Zhengzhou, People’s Republic of China; 2Department of Pharmacy, Second Military Medical University, Shanghai, People’s Republic of China *These authors contributed equally to this work Purpose: To reduce the adverse effects and high frequency of administration of propranolol to treat infantile hemangioma, we first utilized propranolol-loaded liposomes-in-microsphere (PLIM as a novel topical release system to realize sustained release of propranolol.Methods: PLIM was developed from encapsulating propranolol-loaded liposomes (PLs in microspheres made of poly(lactic-co-glycolic acid-b-poly(ethylene glycol-b-poly(lactic-co-glycolic acid copolymers (PLGA-PEG-PLGA. The release profile of propranolol from PLIM was evaluated, and its biological activity was investigated in vitro using proliferation assays on hemangioma stem cells (HemSCs. Tumor inhibition was studied in nude mice bearing human subcutaneous infantile hemangioma.Results: The microspheres were of desired particle size (~77.8 µm and drug encapsulation efficiency (~23.9% and achieved sustained drug release for 40 days. PLIM exerted efficient inhibition of the proliferation of HemSCs and significantly reduced the expression of two angiogenesis factors (vascular endothelial growth factor-A [VEGF-A] and basic fibroblast growth factor [bFGF] in HemSCs. Notably, the therapeutic effect of PLIM in hemangioma was superior to that of propranolol and PL in vivo, as reflected by significantly reduced hemangioma volume, weight, and microvessel density. The mean hemangioma weight of the PLIM-treated group was significantly lower than that of other groups (saline =0.28 g, propranolol =0.21 g, PL =0.13 g, PLIM =0.03 g; PLIM vs saline: P<0.001, PLIM vs propranolol: P<0.001, PLIM vs PL: P<0.001. The mean microvessel density of

  11. Fiber-optic array using molecularly imprinted microspheres for antibiotic analysis.

    Science.gov (United States)

    Carrasco, Sergio; Benito-Peña, Elena; Walt, David R; Moreno-Bondi, María C

    2015-05-01

    In this article we describe a new class of high-density optical microarrays based on molecularly imprinted microsphere sensors that directly incorporate specific recognition capabilities to detect enrofloxacin (ENRO), an antibiotic widely used for both human and veterinary applications. This approach involves the preparation of highly cross-linked polymer microspheres by thermal precipitation-polymerization in the presence and absence of the target analyte ENRO to generate either molecularly imprinted (MIP) or non-imprinted polymer (NIP) microspheres, respectively. Each polymer type of tailor-made microsphere is fluorescently encoded with either coumarin-30 or tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(ii) dichloride [Ru(dip) 3 ]Cl 2 to enable the microspheres to be distinguished. The new MIP-based sensing platform utilizes an optical fiber bundle containing approximately 50 000 individual 3.1 μm diameter fibers that are chemically etched to create microwells in which MIP and NIP microspheres can be deposited and imaged using an epi-fluorescence microscope. The method enables multiplexed detection by independently addressing both types of beads through their separate light channels. The unique response to the presence of ENRO is manifested on the basis of a competitive immunoassay. A red-fluorescent dye-tagged ENRO, labeled with BODIPY® TR Cadaverine, competes with ENRO for specific binding sites. The developed immuno-like assay displayed a limit of detection (LOD) of 0.04 μM (10% binding inhibition) and a dynamic range of 0.29-21.54 μM (20-80% binding inhibition). The selectivity of the assay was evaluated by measuring the cross-reactivity of other fluoroquinolones (ciprofloxacin, norfloxacin, danofloxacin, and flumequine) and non-related antibiotics (penicillin G and doxycycline). This work demonstrates, for the first time, the applicability of MIPs, as an alternative to biomolecule receptors, for the development of multiplexed detection fiber

  12. Porous PLGA microspheres tailored for dual delivery of biomolecules via layer-by-layer assembly.

    Science.gov (United States)

    Go, Dewi P; Palmer, Jason A; Mitchell, Geraldine M; Gras, Sally L; O'Connor, Andrea J

    2015-05-01

    Tissue engineering is a complex and dynamic process that requires varied biomolecular cues to promote optimal tissue growth. Consequently, the development of delivery systems capable of sequestering more than one biomolecule with controllable release profiles is a key step in the advancement of this field. This study develops multilayered polyelectrolyte films incorporating alpha-melanocyte stimulating hormone (α-MSH), an anti-inflammatory molecule, and basic fibroblast growth factor (bFGF). The layers were successfully formed on macroporous poly lactic-co-glycolic acid microspheres produced using a combined inkjet and thermally induced phase separation technique. Release profiles could be varied by altering layer properties including the number of layers and concentrations of layering molecules. α-MSH and bFGF were released in a sustained manner and the bioactivity of α-MSH was shown to be preserved using an activated macrophage cell assay in vitro. The system performance was also tested in vivo subcutaneously in rats. The multilayered microspheres reduced the inflammatory response induced by a carrageenan stimulus 6 weeks after implantation compared to the non-layered microspheres without the anti-inflammatory and growth factors, demonstrating the potential of such multilayered constructs for the controlled delivery of bioactive molecules. © 2014 Wiley Periodicals, Inc.

  13. LYATK1 potently inhibits LPS-mediated pro-inflammatory response

    Energy Technology Data Exchange (ETDEWEB)

    Xi, Feng [Department of Intensive Care Unit, Taixing People" ' s Hospital, Taixing, Jiangsu Province, 225400 (China); Liu, Yuan [Department of Ophthalmology, Nanjing First Hospital, Nanjing Medical University, Nanjing (China); Wang, Xiujuan; Kong, Wei [Department of Intensive Care Unit, Taixing People" ' s Hospital, Taixing, Jiangsu Province, 225400 (China); Zhao, Feng, E-mail: taixingzhaofeng163@163.com [Department of Intensive Care Unit, Taixing People" ' s Hospital, Taixing, Jiangsu Province, 225400 (China)

    2016-01-29

    Lipopolysaccharide (LPS)-primed monocytes/macrophages produce pro-inflammatory cytokines, which could lead to endotoxin shock. TGF-β-activated kinase1 (TAK1) activation is involved in the process. In the current study, we studied the potential effect of a selective TAK1 inhibitor, LYTAK1, on LPS-stimulated response both in vitro and in vivo. We demonstrated that LYTAK1 inhibited LPS-induced mRNA expression and production of several pro-inflammatory cytokines [interleukin 1β (IL-1β), tumor necrosis factor-α (TNFα) and interleukin-6 (IL-6)] in RAW 264.7 macrophages. LYTAK1's activity was almost nullified with TAK1 shRNA-knockdown. Meanwhile, in both primary mouse bone marrow derived macrophages (BMDMs) and human peripheral blood mononuclear cells (PBMCs), LPS-induced pro-inflammatory cytokine production was again attenuated with LYTAK1 co-treatment. Molecularly, LYTAK1 dramatically inhibited LPS-induced TAK1-nuclear factor kappa B (NFκB) and mitogen-activated protein kinase (Erk, Jnk and p38) activation in RAW 264.7 cells, mouse BMDMs and human PBMCs. In vivo, oral administration of LYTAK1 inhibited LPS-induced activation of TAK1-NFκB-p38 in ex-vivo cultured PBMCs, and cytokine production and endotoxin shock in mice. Together, these results demonstrate that LYTAK1 inhibits LPS-induced production of several pro-inflammatory cytokines and endotoxin shock probably through blocking TAK1-regulated signalings. - Highlights: • LYTAK1 inhibits LPS-induced pro-inflammatory cytokine production in RAW 264.7 cells. • The effect by LYTAK1 is more potent than other known TAK1 inhibitors. • LYTAK1 inhibits LPS-induced cytokine production in primary macrophages/monocytes. • LYTAK1 inhibits LPS-induced TAK1-NFκB and MAPK activation in macrophages/monocytes. • LYTAK1 gavage inhibits LPS-induced endotoxin shock and cytokine production in mice.

  14. LYATK1 potently inhibits LPS-mediated pro-inflammatory response

    International Nuclear Information System (INIS)

    Xi, Feng; Liu, Yuan; Wang, Xiujuan; Kong, Wei; Zhao, Feng

    2016-01-01

    Lipopolysaccharide (LPS)-primed monocytes/macrophages produce pro-inflammatory cytokines, which could lead to endotoxin shock. TGF-β-activated kinase1 (TAK1) activation is involved in the process. In the current study, we studied the potential effect of a selective TAK1 inhibitor, LYTAK1, on LPS-stimulated response both in vitro and in vivo. We demonstrated that LYTAK1 inhibited LPS-induced mRNA expression and production of several pro-inflammatory cytokines [interleukin 1β (IL-1β), tumor necrosis factor-α (TNFα) and interleukin-6 (IL-6)] in RAW 264.7 macrophages. LYTAK1's activity was almost nullified with TAK1 shRNA-knockdown. Meanwhile, in both primary mouse bone marrow derived macrophages (BMDMs) and human peripheral blood mononuclear cells (PBMCs), LPS-induced pro-inflammatory cytokine production was again attenuated with LYTAK1 co-treatment. Molecularly, LYTAK1 dramatically inhibited LPS-induced TAK1-nuclear factor kappa B (NFκB) and mitogen-activated protein kinase (Erk, Jnk and p38) activation in RAW 264.7 cells, mouse BMDMs and human PBMCs. In vivo, oral administration of LYTAK1 inhibited LPS-induced activation of TAK1-NFκB-p38 in ex-vivo cultured PBMCs, and cytokine production and endotoxin shock in mice. Together, these results demonstrate that LYTAK1 inhibits LPS-induced production of several pro-inflammatory cytokines and endotoxin shock probably through blocking TAK1-regulated signalings. - Highlights: • LYTAK1 inhibits LPS-induced pro-inflammatory cytokine production in RAW 264.7 cells. • The effect by LYTAK1 is more potent than other known TAK1 inhibitors. • LYTAK1 inhibits LPS-induced cytokine production in primary macrophages/monocytes. • LYTAK1 inhibits LPS-induced TAK1-NFκB and MAPK activation in macrophages/monocytes. • LYTAK1 gavage inhibits LPS-induced endotoxin shock and cytokine production in mice.

  15. Microsphere erosion in outer hydrogel membranes creating macroscopic porosity to counter biofouling-induced sensor degradation.

    Science.gov (United States)

    Vaddiraju, S; Wang, Y; Qiang, L; Burgess, D J; Papadimitrakopoulos, F

    2012-10-16

    Biofouling and tissue inflammation present major challenges toward the realization of long-term implantable glucose sensors. Following sensor implantation, proteins and cells adsorb on sensor surfaces to not only inhibit glucose flux but also signal a cascade of inflammatory events that eventually lead to permeability-reducing fibrotic encapsulation. The use of drug-eluting hydrogels as outer sensor coatings has shown considerable promise to mitigate these problems via the localized delivery of tissue response modifiers to suppress inflammation and fibrosis, along with reducing protein and cell absorption. Biodegradable poly (lactic-co-glycolic) acid (PLGA) microspheres, encapsulated within a poly (vinyl alcohol) (PVA) hydrogel matrix, present a model coating where the localized delivery of the potent anti-inflammatory drug dexamethasone has been shown to suppress inflammation over a period of 1-3 months. Here, it is shown that the degradation of the PLGA microspheres provides an auxiliary venue to offset the negative effects of protein adsorption. This was realized by: (1) the creation of fresh porosity within the PVA hydrogel following microsphere degradation (which is sustained until the complete microsphere degradation) and (2) rigidification of the PVA hydrogel to prevent its complete collapse onto the newly created void space. Incubation of the coated sensors in phosphate buffered saline (PBS) led to a monotonic increase in glucose permeability (50%), with a corresponding enhancement in sensor sensitivity over a 1 month period. Incubation in serum resulted in biofouling and consequent clogging of the hydrogel microporosity. This, however, was partially offset by the generated macroscopic porosity following microsphere degradation. As a result of this, a 2-fold recovery in sensor sensitivity for devices with microsphere/hydrogel composite coatings was observed as opposed to similar devices with blank hydrogel coatings. These findings suggest that the use of

  16. [Non-selective and selective non-steroidal anti-inflammatory drugs, administration in pregnancy and breast feeding].

    Science.gov (United States)

    Fardet, Laurence; Nizard, Jacky; Généreau, Thierry

    2002-09-28

    THE FACTS: Non steroidal anti-inflammatory drugs (NSAI), except aspirin, are classically contraindicated during pregnancy. Nevertheless, they are widely used, in particular by the obstetricians. During pregnancy, the potential toxicity of these drugs is double, maternal and fetal. The maternal toxicity is comparable to that, already known in adults, with however, some particularities at the time of labor and delivery. The fetal toxicity is mainly renal and cardiovascular, with the NSAI responsible for oligoamniosis and premature closure of the arterial canal of the fetus. On the other hand, the use of these molecules during breast-feeding does not seem source of adverse events, notably in the newborn. THE VARIOUS MOLECULES: Among the family of non-selective non-steroidal anti-inflammatories, indications and adverse events of the various molecules differ considerably. Moreover, whereas the majority of these molecules are non-selective, i.e. inhibiting the two isoforms of cyclooxygenase, new therapeutics, specifically inhibiting cyclooxygenase-2, are now available. Few studies have been published concerning their prescription during pregnancy and breast-feeding and their maternal and fetal side effects remain ignored by most of the practitioners.

  17. Polymer-coated albumin microspheres as carriers for intravascular tumour targeting of cisplatin.

    Science.gov (United States)

    Verrijk, R; Smolders, I J; McVie, J G; Begg, A C

    1991-01-01

    We used a poly-lactide-co-glycolide polymer (PLAGA 50:50) to formulate cisplatin (cDDP) into microspheres designed for intravascular administration. Two systems were developed. PLAGA-coated albumin microspheres and microspheres consisting of PLAGA only. PLAGA-coated microspheres displayed a mean diameter of 31.8 +/- 0.9 microns and a payload of 7.5% cDDP (w/w). Solid PLAGA microspheres exhibited a mean diameter of 19.4 +/- 0.6 microns and a payload of 20% cDDP. Release characteristics and in vitro effects on L1210 leukemia and B16 melanoma cell lines were investigated. Both types of microsphere overcame the initial rapid release of cDDP (burst effect), and PLAGA-coated albumin microspheres also showed a lag phase of approximately 30 min before cDDP release began. PLAGA-coated albumin microspheres released most of their payload through diffusion, and the coating eventually cracked after 7 days' incubation in saline supplemented with 0.1% Tween at 37 degrees C, enabling the release of any cDDP remaining. Effects of platinum, pre-released from PLAGA-coated albumin microspheres on the in vitro growth of L1210 cells were comparable with those of standard formulations (dissolved) of cDDP. Material released from non-drug-loaded PLAGA microspheres had no effect on L1210 cell growth, suggesting the absence of cytotoxic compounds in the matrix. The colony-forming ability of B16 cells was also equally inhibited by standard cDDP and pre-released drug. These studies show that formulation of cDDP in PLAGA-based microspheres prevents the rapid burst effect of cDDP seen in previous preparations and offers an improved system of administration for hepatic artery infusion or adjuvant therapy, enabling better clinical handling and the promise of a higher ratio of tumour tissue to normal tissue.

  18. Synthesis and anti-angiogenic effect of conjugates between serum albumin and non-steroidal anti-inflammatory drugs

    DEFF Research Database (Denmark)

    Kjær, Birgitte; Struve, Casper; Friis, Tina

    2010-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit tumor growth and angiogenesis. Covalent linkage of naproxen to human serum albumin (HSA) has been shown to target it efficiently to the liver and this may potentially be exploited for liver-selective inhibition of angiogenesis. With the aim...... effect on endothelial cells at or above the level of the non-conjugated NSAIDs in an in vitro angiogenesis assay....

  19. Dual Drug Loaded Biodegradable Nanofibrous Microsphere for Improving Anti-Colon Cancer Activity

    Science.gov (United States)

    Fan, Rangrang; Li, Xiaoling; Deng, Jiaojiao; Gao, Xiang; Zhou, Liangxue; Zheng, Yu; Tong, Aiping; Zhang, Xiaoning; You, Chao; Guo, Gang

    2016-06-01

    One of the approaches being explored to increase antitumor activity of chemotherapeutics is to inject drug-loaded microspheres locally to specific anatomic sites, providing for a slow, long term release of a chemotherapeutic while minimizing systemic exposure. However, the used clinically drug carriers available at present have limitations, such as their low stability, renal clearance and residual surfactant. Here, we report docetaxel (DOC) and curcumin (CUR) loaded nanofibrous microspheres (DOC + CUR/nanofibrous microspheres), self-assembled from biodegradable PLA-PEO-PPO-PEO-PLA polymers as an injectable drug carrier without adding surfactant during the emulsification process. The obtained nanofibrous microspheres are composed entirely of nanofibers and have an open hole on the shell without the assistance of a template. It was shown that these DOC + CUR/nanofibrous microspheres could release curcumin and docetaxel slowly in vitro. The slow, sustained release of curcumin and docetaxel in vivo may help maintain local concentrations of active drug. The mechanism by which DOC + CUR/nanofibrous microspheres inhibit colorectal peritoneal carcinomatosis might involve increased induction of apoptosis in tumor cells and inhibition of tumor angiogenesis. In vitro and in vivo evaluations demonstrated efficacious synergistic antitumor effects against CT26 of curcumin and docetaxel combined nanofibrous microspheres. In conclusion, the dual drug loaded nanofibrous microspheres were considered potentially useful for treating abdominal metastases of colorectal cancer.

  20. Inhibition of Pro-inflammatory Mediators and Cytokines by Chlorella Vulgaris Extracts.

    Science.gov (United States)

    Sibi, G; Rabina, Santa

    2016-01-01

    The aim of this study was to determine the in vitro anti-inflammatory activities of solvent fractions from Chlorella vulgaris by inhibiting the production of pro-inflammatory mediators and cytokines. Methanolic extracts (80%) of C. vulgaris were prepared and partitioned with solvents of increasing polarity viz., n-hexane, chloroform, ethanol, and water. Various concentrations of the fractions were tested for cytotoxicity in RAW 264.7 cells using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, and the concentrations inducing cell growth inhibition by about 50% (IC50) were chosen for further studies. Lipopolysaccharide (LPS) stimulated RAW 264.7 cells were treated with varying concentrations of C. vulgaris fractions and examined for its effects on nitric oxide (NO) production by Griess assay. The release of prostaglandin E2 (PGE2), tumor necrosis factor-α (TNF-α), and interleukin 6 (IL-6) were quantified using enzyme-linked immunosorbent assay using Celecoxib and polymyxin B as positive controls. MTT assay revealed all the solvent fractions that inhibited cell growth in a dose-dependent manner. Of all the extracts, 80% methanolic extract exhibited the strongest anti-inflammatory activity by inhibiting NO production (P < 0.01), PGE2 (P < 0.05), TNF-α, and IL-6 (P < 0.001) release in LPS induced RAW 264.7 cells. Both hexane and chloroform fractions recorded a significant (P < 0.05) and dose-dependent inhibition of LPS induced inflammatory mediators and cytokines in vitro. The anti-inflammatory effect of ethanol and aqueous extracts was not significant in the study. The significant inhibition of inflammatory mediators and cytokines by fractions from C. vulgaris suggests that this microalga would be a potential source of developing anti-inflammatory agents and a good alternate for conventional steroidal and nonsteroidal anti-inflammatory drugs. C. vulgaris extracts have potential anti-inflammatory activitySolvent extraction using methanol

  1. Beat frequency ultrasonic microsphere contrast agent detection system

    Science.gov (United States)

    Pretlow, III, Robert A. (Inventor); Yost, William T. (Inventor); Cantrell, Jr., John H. (Inventor)

    1997-01-01

    A system for and method of detecting and measuring concentrations of an ultrasonically-reflective microsphere contrast agent involving detecting non-linear sum and difference beat frequencies produced by the microspheres when two impinging signals with non-identical frequencies are combined by mixing. These beat frequencies can be used for a variety of applications such as detecting the presence of and measuring the flow rates of biological fluids and industrial liquids, including determining the concentration level of microspheres in the myocardium.

  2. Inhibition of amyloidogenesis by non-steroidal anti-inflammatory drugs and their hybrid nitrates

    Science.gov (United States)

    Schiefer, Isaac T.; Abdul-Hay, Samer; Wang, Huali; Vanni, Michael; Qin, Zhihui; Thatcher, Gregory R. J.

    2011-01-01

    Poor blood-brain barrier penetration of non-steroidal anti-inflammatory drugs (NSAIDs) has been blamed for the failure of the selective amyloid lowering agent (SALA) R-flurbiprofen in phase 3 clinical trials for Alzheimer’s disease (AD). NO-donor NSAIDs (NO-NSAIDs) provide an alternative, gastric-sparing approach to NSAID SALAs, which may improve bioavailability. NSAID analogs were studied for anti-inflammatory activity and for SALA activity in N2a neuronal cells transfected with human amyloid precursor protein (APP). Flurbiprofen (1) analogs were obtained with enhanced anti-inflammatory and anti-amyloidogenic properties compared to 1, however, esterification led to elevated Aβ1–42 levels. Hybrid nitrate prodrugs possessed superior anti-inflammatory activity and reduced toxicity relative to the parent NSAIDs, including clinical candidate, CHF5074. Although hybrid nitrates elevated Aβ1–42 at higher concentration, SALA activity was observed at low concentrations (≤ 1 µM): both Aβ1–42 and the ratio of Aβ1–42/Aβ1–40 were lowered. This biphasic SALA activity was attributed to the intact nitrate drug. For several compounds the selective modulation of amyloidogenesis was tested using an immunoprecipitation MALDI-TOF approach. These data support the development of NO-NSAIDs as an alternative approach towards a clinically useful SALA. PMID:21405086

  3. The Ayurvedic plant Bacopa monnieri inhibits inflammatory pathways in the brain.

    Science.gov (United States)

    Nemetchek, Michelle D; Stierle, Andrea A; Stierle, Donald B; Lurie, Diana I

    2017-02-02

    Bacopa monnieri (L) Wettst (common name, bacopa) is a medicinal plant used in Ayurveda, the traditional system of medicine of India, as a nootropic. It is considered to be a "medhya rasayana", an herb that sharpens the mind and the intellect. Bacopa is an important ingredient in many Ayurvedic herbal formulations designed to treat conditions such as memory loss, anxiety, poor cognition and loss of concentration. It has also been used in Ayurveda to treat inflammatory conditions such as arthritis. In modern biomedical studies, bacopa has been shown in animal models to inhibit the release of the pro-inflammatory cytokines TNF-α and IL-6. However, less is known regarding the anti-inflammatory activity of Bacopa in the brain. The current study examines the ability of Bacopa to inhibit the release of pro-inflammatory cytokines from microglial cells, the immune cells of the brain that participate in inflammation in the CNS. The effect of Bacopa on signaling enzymes associated with CNS inflammatory pathways was also studied. Various extracts of Bacopa were prepared and examined in the N9 microglial cell line in order to determine if they inhibited the release of the proinflammatory cytokines TNF-α and IL-6. Extracts were also tested in cell free assays as inhibitors of caspase-1 and matrix metalloproteinase-3 (enzymes associated with inflammation) and caspase-3, which has been shown to cleave protein Tau, an early event in the development of Alzheimer's disease. The tea, infusion, and alkaloid extracts of bacopa, as well as Bacoside A significantly inhibited the release of TNF-α and IL-6 from activated N9 microglial cells in vitro. In addition, the tea, infusion, and alkaloid extracts of Bacopa effectively inhibited caspase 1 and 3, and matrix metalloproteinase-3 in the cell free assay. Bacopa inhibits the release of inflammatory cytokines from microglial cells and inhibits enzymes associated with inflammation in the brain. Thus, Bacopa can limit inflammation in the

  4. The Ayurvedic plant Bacopa Monnieri inhibits inflammatory pathways in the brain

    Science.gov (United States)

    Nemetchek, Michelle D.; Stierle, Andrea A.; Stierle, Donald B.; Lurie, Diana I.

    2016-01-01

    Ethnopharmacological Relevance Bacopa monnieri (L) Wettst (common name, bacopa) is a medicinal plant used in Ayurveda, the traditional system of medicine of India, as a nootropic. It is considered to be a “medhya rasayana”, an herb that sharpens the mind and the intellect. Bacopa is an important ingredient in many Ayurvedic herbal formulations designed to treat conditions such as memory loss, anxiety, poor cognition and loss of concentration. It has also been used in Ayurveda to treat inflammatory conditions such as arthritis. In modern biomedical studies, bacopa has been shown in animal models to inhibit the release of the pro-inflammatory cytokines TNF-α and IL-6. However, less is known regarding the anti-inflammatory activity of Bacopa in the brain. Aim Of The Study The current study examines the ability of Bacopa to inhibit the release of pro-inflammatory cytokines from microglial cells, the immune cells of the brain that participate in inflammation in the CNS. The effect of Bacopa on signaling enzymes associated with CNS inflammatory pathways was also studied. Materials And Methods Various extracts of Bacopa were prepared and examined in the N9 microglial cell line in order to determine if they inhibited the release of the proinflammatory cytokines TNF-α and IL-6. Extracts were also tested in cell free assays as inhibitors of caspase-1 and matrix metalloproteinase-3 (enzymes associated with inflammation) and caspase-3, which has been shown to cleave protein Tau, an early event in the development of Alzheimer's disease. Results The tea, infusion, and alkaloid extracts of bacopa, as well as Bacoside A significantly inhibited the release of TNF-α and IL-6 from activated N9 microglial cells in vitro. In addition, the tea, infusion, and alkaloid extracts of Bacopa effectively inhibited caspase 1 and 3, and matrix metalloproteinase-3 in the cell free assay. Conclusions Bacopa inhibits the release of inflammatory cytokines from microglial cells and inhibits

  5. Inhibition of inflammatory mediators contributes to the anti-inflammatory activity of KYKZL-1 via MAPK and NF-κB pathway

    International Nuclear Information System (INIS)

    Xu, Guang-Lin; Du, Yi-Fang; Cheng, Jing; Huan, Lin; Chen, Shi-Cui; Wei, Shao-Hua; Gong, Zhu-Nan; Cai, Jie; Qiu, Ting; Wu, Hao; Sun, Ting; Ao, Gui-Zhen

    2013-01-01

    KYKZL-1, a newly synthesized compound with COX/5-LOX dual inhibition, was subjected to the anti-inflammatory activity test focusing on its modulation of inflammatory mediators as well as intracellular MAPK and NF-κB signaling pathways. In acute ear edema model, pretreatment with KYKZL-1 (p.o.) dose-dependently inhibited the xylene-induced ear edema in mice with a higher inhibition than diclofenac. In a three-day TPA-induced inflammation, KYKZL-1 also showed significant anti-inflammatory activity with inhibition ranging between 20% and 64%. In gastric lesion test, KYKZL-1 elicited markedly fewer stomach lesions with a low index of ulcer as compared to diclofenac in rats. In further studies, KYKZL-1 was found to significantly inhibit the production of NO, PGE 2 , LTB 4 in LPS challenged RAW264.7, which is parallel to its attenuation of the expression of iNOS, COX-2, 5-LOX mRNAs or proteins and inhibition of phosphorylation of p38 and ERK MAPKs and activation of NF-κB. Taken together, our data indicate that KYKZL-1 comprises dual inhibition of COX and 5-LOX and exerts an obvious anti-inflammatory activity with an enhanced gastric safety profile via simultaneous inhibition of phosphorylation of p38 and ERK MAPKs and activation of NF-κB. - Highlights: • KYKZL-1 is designed to exhibit COX/5-LOX dual inhibition. • KYKZL-1 inhibits NO, PGE 2 and LTB 4 and iNOS, COX-2 and 5-LOX mRNAs and MAPKs. • KYKZL-1 inhibits phosphorylation of MAPKs. • KYKZL-1 inactivates NF-κB pathway

  6. Inhibition of inflammatory mediators contributes to the anti-inflammatory activity of KYKZL-1 via MAPK and NF-κB pathway

    Energy Technology Data Exchange (ETDEWEB)

    Xu, Guang-Lin [Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Science, Nanjing Normal University, Nanjing (China); Department of Pharmacology, University of Michigan, Ann Arbor (United States); Du, Yi-Fang; Cheng, Jing; Huan, Lin [Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Science, Nanjing Normal University, Nanjing (China); Chen, Shi-Cui [Jinhu Food and Drug Administration, Jiangsu (China); Wei, Shao-Hua [College of Chemistry and Materials Science, Nanjing Normal University, Nanjing (China); Gong, Zhu-Nan, E-mail: biopharmacology@126.com [Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Science, Nanjing Normal University, Nanjing (China); Cai, Jie; Qiu, Ting; Wu, Hao; Sun, Ting [Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Science, Nanjing Normal University, Nanjing (China); Ao, Gui-Zhen [Department of Medicinal Chemistry, School of Pharmacy, Soochow University, Jiangsu (China)

    2013-10-01

    KYKZL-1, a newly synthesized compound with COX/5-LOX dual inhibition, was subjected to the anti-inflammatory activity test focusing on its modulation of inflammatory mediators as well as intracellular MAPK and NF-κB signaling pathways. In acute ear edema model, pretreatment with KYKZL-1 (p.o.) dose-dependently inhibited the xylene-induced ear edema in mice with a higher inhibition than diclofenac. In a three-day TPA-induced inflammation, KYKZL-1 also showed significant anti-inflammatory activity with inhibition ranging between 20% and 64%. In gastric lesion test, KYKZL-1 elicited markedly fewer stomach lesions with a low index of ulcer as compared to diclofenac in rats. In further studies, KYKZL-1 was found to significantly inhibit the production of NO, PGE{sub 2}, LTB{sub 4} in LPS challenged RAW264.7, which is parallel to its attenuation of the expression of iNOS, COX-2, 5-LOX mRNAs or proteins and inhibition of phosphorylation of p38 and ERK MAPKs and activation of NF-κB. Taken together, our data indicate that KYKZL-1 comprises dual inhibition of COX and 5-LOX and exerts an obvious anti-inflammatory activity with an enhanced gastric safety profile via simultaneous inhibition of phosphorylation of p38 and ERK MAPKs and activation of NF-κB. - Highlights: • KYKZL-1 is designed to exhibit COX/5-LOX dual inhibition. • KYKZL-1 inhibits NO, PGE{sub 2} and LTB{sub 4} and iNOS, COX-2 and 5-LOX mRNAs and MAPKs. • KYKZL-1 inhibits phosphorylation of MAPKs. • KYKZL-1 inactivates NF-κB pathway.

  7. Protective effects of alginate–chitosan microspheres loaded with alkaloids from Coptis chinensis Franch. and Evodia rutaecarpa (Juss. Benth. (Zuojin Pill against ethanol-induced acute gastric mucosal injury in rats

    Directory of Open Access Journals (Sweden)

    Wang QS

    2015-11-01

    Full Text Available Qiang-Song Wang,1,2,* Xiao-Ning Zhu,1,* Heng-Li Jiang,1,* Gui-Fang Wang,3 Yuan-Lu Cui1 1Tianjin State Key Laboratory of Modern Chinese Medicine, Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, 2Institute of Biomedical Engineering, Chinese Academy of Medical Science & Peking Union Medical College, 3Pharmacy Department, Baokang Hospital, Tianjin University of Traditional Chinese Medicine, Tianjin, People’s Republic of China *These authors contributed equally to this work Abstract: Zuojin Pill (ZJP, a traditional Chinese medicine formula, consists of Coptis chinensis Franch. and Evodia rutaecarpa (Juss. Benth. in a ratio of 6:1 (w/w and was first recorded in “Danxi’s experiential therapy” for treating gastrointestinal disorders in the 15th century. However, the poor solubility of alkaloids from ZJP restricted the protective effect in treating gastritis and gastric ulcer. The aim of the study was to investigate the protective mechanism of mucoadhesive microspheres loaded with alkaloids from C. chinensis Franch. and E. rutaecarpa (Juss. Benth. on ethanol-induced acute gastric mucosal injury in rats. Surface morphology, particle size, drug loading, encapsulation efficiency, in vitro drug release, mucoadhesiveness, and fluorescent imaging of the microspheres in gastrointestinal tract were studied. The results showed that the mucoadhesive microspheres loaded with alkaloids could sustain the release of drugs beyond 12 hours and had gastric mucoadhesive property with 82.63% retention rate in vitro. The fluorescence tracer indicated high retention of mucoadhesive microspheres within 12 hours in vivo. The mucoadhesive microspheres loaded with alkaloids could reduce the gastric injury by decreasing the mucosal lesion index, increasing the percentage of inhibition and increasing the amount of mucus in the gastric mucosa in an ethanol-induced gastric mucosal injury rat model. Moreover, the

  8. Thunbergia alata inhibits inflammatory responses through the inactivation of ERK and STAT3 in macrophages.

    Science.gov (United States)

    Cho, Young-Chang; Kim, Ye Rang; Kim, Ba Reum; Bach, Tran The; Cho, Sayeon

    2016-11-01

    Thunbergia alata (Acanthaceae) has been used traditionally to treat various inflammatory diseases such as fever, cough and diarrhea in East African countries including Uganda and Kenya. However, systemic studies elucidating the anti-inflammatory effects and precise mechanisms of action of T. alata have not been conducted, to the best of our knowledge. To address these concerns, we explored the anti-inflammatory effects of a methanol extract of T. alata (MTA) in macrophages. Non-cytotoxic concentrations of MTA (≤300 µg/ml) inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)‑stimulated RAW 264.7 macrophages by transcriptional regulation of inducible NO synthase in a dose-dependent manner. The expression of cyclooxygenase-2, the enzyme responsible for the production of prostaglandin E2, was unchanged by MTA at the mRNA and protein levels. MTA treatment inhibited interleukin (IL)-6 production and decreased the mRNA expression of pro‑inflammatory cytokines, including IL-6 and IL-1β. Tumor necrosis factor-α production and mRNA expression were not regulated by MTA treatment. The decreased production of inflammatory mediators by MTA was followed by the reduced phosphorylation of extracellular signal‑regulated kinase (ERK) and signal transducer and activator of transcription 3 (STAT3). MTA treatment had no effect on activity of other mitogen‑activated protein kinases (MAPKs), p38, c-Jun N-terminal kinase (JNK), and nuclear factor-κB (NF-κB). These results indicate that MTA selectively inhibits the excessive production of inflammatory mediators in LPS-stimulated murine macrophages by reducing the activity of ERK and STAT3, suggesting that MTA plays an important inhibitory role in the modulation of severe inflammation.

  9. Low threshold lasing of bubble-containing glass microspheres by non-whispering gallery mode excitation over a wide wavelength range

    Energy Technology Data Exchange (ETDEWEB)

    Kumagai, Tsutaru, E-mail: kumagai.t.af@m.titech.ac.jp; Kishi, Tetsuo; Yano, Tetsuji [Department of Chemistry and Materials Science, Tokyo Institute of Technology, 2-12-1 Ookayama, Meguro-ku, Tokyo 152-8550 (Japan)

    2015-03-21

    Bubble-containing Nd{sup 3+}-doped tellurite glass microspheres were fabricated by localized laser heating technique to investigate their optical properties for use as microresonators. Fluorescence and excitation spectra measurements were performed by pumping with a tunable CW-Ti:Sapphire laser. The excitation spectra manifested several sharp peaks due to the conventional whispering gallery mode (WGM) when the pumping laser was irradiated to the edge part of the microsphere. However, when the excitation light was irradiated on the bubble position inside the microsphere, “non-WGM excitation” was induced, giving rise to numerous peaks at a broad wavelength range in the excitation spectra. Thus, efficient excitation was achieved over a wide wavelength range. Lasing threshold excited at the bubble position was much lower than that for the excitation at the edges of the microsphere. The lowest value of the laser threshold was 34 μW for a 4 μm sphere containing a 0.5 μm bubble. Efficiency of the excitation at the bubble position with broadband light was calculated to be 5 times higher than that for the edge of the microsphere. The bubble-containing microsphere enables efficient utilization of broadband light excitation from light-emitting diodes and solar light.

  10. Histological Comparison of Kidney Tissue Following Radioembolization with Yttrium-90 Resin Microspheres and Embolization with Bland Microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Suresh de, E-mail: suresh.desilva@unsw.edu.au [Southern Radiology Group, Radiology Department Sutherland Hospital (Australia); Mackie, Simon [Western General Hospital, Department of Urology (United Kingdom); Aslan, Peter [St George Hospital, Department of Urology (Australia); Cade, David [Sirtex Technology Pty Ltd (Australia); Delprado, Warick [Douglass Hanly Moir Pathology (Australia)

    2016-12-15

    BackgroundIntra-arterial brachytherapy with yttrium-90 ({sup 90}Y) resin microspheres (radioembolization) is a procedure to selectively deliver high-dose radiation to tumors. The purpose of this research was to compare the radioembolic effect of {sup 90}Y-radioembolization versus the embolic effect of bland microspheres in the porcine kidney model.MethodsIn each of six pigs, ~25–33 % of the kidney volume was embolized with {sup 90}Y resin microspheres and an equivalent number of bland microspheres in the contralateral kidney. Kidney volume was estimated visually from contrast-enhanced fluoroscopy imaging. Morphologic and histologic analysis was performed 8–9 weeks after the procedure to assess the locations of the microspheres and extent of tissue necrosis from {sup 90}Y-radioembolization and bland embolization. A semi-quantified evaluation of the non-acute peri-particle and perivascular tissue reaction was conducted. All guidelines for the care and use of animals were followed.ResultsKidneys embolized with {sup 90}Y-radioembolization decreased in mass by 30–70 % versus the contralateral kidney embolized with bland microspheres. These kidneys showed significant necrosis/fibrosis, avascularization, and glomerular atrophy in the immediate vicinity of the {sup 90}Y resin microspheres. By contrast, glomerular changes were not observed, even with clusters of bland microspheres in afferent arterioles. Evidence of a foreign body reaction was recorded in some kidneys with bland microspheres, and subcapsular scarring/infarction only with the highest load (4.96 × 10{sup 6}) of bland microspheres.ConclusionThis study showed that radioembolization with {sup 90}Y resin microspheres produces localized necrosis/fibrosis and loss of kidney mass in a porcine kidney model. This result supports the study of {sup 90}Y resin microspheres for the localized treatment of kidney tumors.

  11. Histological Comparison of Kidney Tissue Following Radioembolization with Yttrium-90 Resin Microspheres and Embolization with Bland Microspheres

    International Nuclear Information System (INIS)

    Silva, Suresh de; Mackie, Simon; Aslan, Peter; Cade, David; Delprado, Warick

    2016-01-01

    BackgroundIntra-arterial brachytherapy with yttrium-90 ("9"0Y) resin microspheres (radioembolization) is a procedure to selectively deliver high-dose radiation to tumors. The purpose of this research was to compare the radioembolic effect of "9"0Y-radioembolization versus the embolic effect of bland microspheres in the porcine kidney model.MethodsIn each of six pigs, ~25–33 % of the kidney volume was embolized with "9"0Y resin microspheres and an equivalent number of bland microspheres in the contralateral kidney. Kidney volume was estimated visually from contrast-enhanced fluoroscopy imaging. Morphologic and histologic analysis was performed 8–9 weeks after the procedure to assess the locations of the microspheres and extent of tissue necrosis from "9"0Y-radioembolization and bland embolization. A semi-quantified evaluation of the non-acute peri-particle and perivascular tissue reaction was conducted. All guidelines for the care and use of animals were followed.ResultsKidneys embolized with "9"0Y-radioembolization decreased in mass by 30–70 % versus the contralateral kidney embolized with bland microspheres. These kidneys showed significant necrosis/fibrosis, avascularization, and glomerular atrophy in the immediate vicinity of the "9"0Y resin microspheres. By contrast, glomerular changes were not observed, even with clusters of bland microspheres in afferent arterioles. Evidence of a foreign body reaction was recorded in some kidneys with bland microspheres, and subcapsular scarring/infarction only with the highest load (4.96 × 10"6) of bland microspheres.ConclusionThis study showed that radioembolization with "9"0Y resin microspheres produces localized necrosis/fibrosis and loss of kidney mass in a porcine kidney model. This result supports the study of "9"0Y resin microspheres for the localized treatment of kidney tumors.

  12. Over Expression of Long Non-Coding RNA PANDA Promotes Hepatocellular Carcinoma by Inhibiting Senescence Associated Inflammatory Factor IL8.

    Science.gov (United States)

    Peng, Chuanhui; Hu, Wendi; Weng, Xiaoyu; Tong, Rongliang; Cheng, Shaobing; Ding, Chaofeng; Xiao, Heng; Lv, Zhen; Xie, Haiyang; Zhou, Lin; Wu, Jian; Zheng, Shusen

    2017-06-23

    It has been reported that long non-coding RNA PANDA was disregulated in varieties types of tumor, but its expression level and biological role in hepatocellular carcinoma (HCC) remains contradictory. We detected PANDA expression in two independent cohorts (48 HCC patients following liver transplantation and 84 HCC patients following liver resection), and found that PANDA was down-regulated in HCC. Thereafter we explored its function in cancer biology by inversing its low expression. Surprisingly, overexpression of PANDA promoted HCC proliferation and carcinogenesis in vitro and in vivo. Mechanistically, PANDA repressed transcriptional activity of senescence associated inflammatory factor IL8, which leaded to inhibition of cellular senescence. Therefore, our research help to better understand the complex role of PANDA in HCC, and suggest more thoughtful strategies should be applied before it can be treated as a potential therapeutic target.

  13. Leflunomide biodegradable microspheres intended for intra-articular administration: Development, anti-inflammatory activity and histopathological studies.

    Science.gov (United States)

    El-Setouhy, Doaa Ahmed; Abdelmalak, Nevine Shawky; Anis, Shady E; Louis, Dina

    2015-11-30

    Leflunomide, the disease-modifying anti-rheumatic drug was formulated as microspheres for prolonged drug release in the form of intraarticular injection. Eight formulations were developed using three biodegradable PDLG polymers (lactide/glycolide copolymer) and polycaprolactone (PLC) at two drug:polymer ratios (1:2 and 1:4). Solvent evaporation method was employed using polyvinyl alcohol or hydropxypropyl methylcellulose as stabilizers. Formulations were assessed for encapsulation efficiency, yield, particle size, release pattern and SEM. F6 (PDLG 5010), with appropriate particle size and prolonged drug release, was chosen for in-vivo studies using arthritis induced rats, which were intrarticularly injected with F6 or took oral Avara(®). Nuclear factor-kappa B measurements and histopathologic studies were conducted. There was significant reduction of inflammation caused by both F6 and oral Avara(®). Histopathologic studies showed minimal infiltration by chronic inflammatory cells and no angiogenesis in F6 compared to Avara(®). Results also revealed biocompatibility of the polymer used. Copyright © 2015 Elsevier B.V. All rights reserved.

  14. Investigation of control conditions of uranium dioxide pellets sinterability through microspheres

    International Nuclear Information System (INIS)

    Assis, Gino de.

    1996-01-01

    Promotion or inhibition of ceramic powders sinterability, the decisive question in ceramic processing is approached in this dissertation. Each high density microsphere has been considered as a solid inclusion in a low density microspheres matrix, generating big pores. Such pores make it difficult for the pellets density due the fact that they are difficult to be eliminated. A master mixture, allowing the pellet densification in the projected range has been reached. Batches of microspheres have been observed sometimes with high apparent density and sometimes with low apparent density. This apparent density variation was attributed to changing the oxygen partial pressure during calcination under air atmosphere. It is evident that the control of the apparent density of the microspheres needs a further research in order to adjust the sinterability of the microspheres on the desired level.It was demonstrated that the produced microspheres do not have impurities levels that can promote its sinterability or avoid their use in nuclear area

  15. Inhibition of lipase and inflammatory mediators by Chlorella lipid extracts for antiacne treatment.

    Science.gov (United States)

    Sibi, G

    2015-01-01

    Acne vulgaris is a chronic inflammatory disease, and its treatment is challenging due to the multifactorial etiology and emergence of antibiotic-resistant Propionibacterium acnes strains. This study was focused to reduce antibiotics usage and find an alternate therapeutic source for treating acne. Lipid extracts of six Chlorella species were tested for inhibition of lipase, reactive oxygen species (ROS) production, cytokine production using P. acnes (Microbial Type Culture Collection 1951). Lipase inhibitory assay was determined by dimercaprol Tributyrate - 5, 5'- dithiobis 2-nitrobenzoic acid method and ROS production assay was performed using nitro-blue tetrazolium test. The anti-inflammatory activity of algal lipid extracts was determined by in vitro screening method based on inhibition of pro-inflammatory cytokines, tumor necrosis factor-alpha (TNF-α) produced by human peripheral blood mononuclear cells. Minimum inhibitory concentration (MIC) values of lipid extracts were determined by microdilution method, and the fatty acid methyl esters (FAME) were analyzed by gas chromatography-mass spectroscopy. Chlorella ellipsoidea has the highest lipase inhibitory activity with 61.73% inhibition, followed by Chlorella vulgaris (60.31%) and Chlorella protothecoides (58.9%). Lipid extracts from C. protothecoides and C. ellipsoidea has significantly reduced the ROS production by 61.27% and 58.34% respectively. Inhibition of pro-inflammatory cytokines TNF-α showed the inhibition ranging from 58.39% to 78.67%. C. vulgaris has exhibited the MICvalue of 10 μg/ml followed by C. ellipsoidea, C. protothecoides and Chlorella pyrenoidosa (20 μg/ml). FAME analysis detected 19 fatty acids of which 5 were saturated fatty acids, and 14 were unsaturated fatty acids ranging from C14 to C24. The results suggest that lipid extracts of Chlorella species has significant inhibitory activity on P. acnes by inhibiting lipase activity. Further, anti-inflammatory reaction caused by the

  16. Inhibition of lipase and inflammatory mediators by Chlorella lipid extracts for antiacne treatment

    Directory of Open Access Journals (Sweden)

    G Sibi

    2015-01-01

    Full Text Available Acne vulgaris is a chronic inflammatory disease, and its treatment is challenging due to the multifactorial etiology and emergence of antibiotic-resistant Propionibacterium acnes strains. This study was focused to reduce antibiotics usage and find an alternate therapeutic source for treating acne. Lipid extracts of six Chlorella species were tested for inhibition of lipase, reactive oxygen species (ROS production, cytokine production using P. acnes (Microbial Type Culture Collection 1951. Lipase inhibitory assay was determined by dimercaprol Tributyrate - 5, 5′- dithiobis 2-nitrobenzoic acid method and ROS production assay was performed using nitro-blue tetrazolium test. The anti-inflammatory activity of algal lipid extracts was determined by in vitro screening method based on inhibition of pro-inflammatory cytokines, tumor necrosis factor-alpha (TNF-α produced by human peripheral blood mononuclear cells. Minimum inhibitory concentration (MIC values of lipid extracts were determined by microdilution method, and the fatty acid methyl esters (FAME were analyzed by gas chromatography-mass spectroscopy. Chlorella ellipsoidea has the highest lipase inhibitory activity with 61.73% inhibition, followed by Chlorella vulgaris (60.31% and Chlorella protothecoides (58.9%. Lipid extracts from C. protothecoides and C. ellipsoidea has significantly reduced the ROS production by 61.27% and 58.34% respectively. Inhibition of pro-inflammatory cytokines TNF-α showed the inhibition ranging from 58.39% to 78.67%. C. vulgaris has exhibited the MICvalue of 10 μg/ml followed by C. ellipsoidea, C. protothecoides and Chlorella pyrenoidosa (20 μg/ml. FAME analysis detected 19 fatty acids of which 5 were saturated fatty acids, and 14 were unsaturated fatty acids ranging from C14 to C24. The results suggest that lipid extracts of Chlorella species has significant inhibitory activity on P. acnes by inhibiting lipase activity. Further, anti-inflammatory reaction caused

  17. Biodegradable polymeric microsphere-based drug delivery for inductive browning of fat

    Directory of Open Access Journals (Sweden)

    Chunhui eJiang

    2015-11-01

    Full Text Available Brown and beige adipocytes are potent therapeutic agents to increase energy expenditure and reduce risks of obesity and its affiliated metabolic symptoms. One strategy to increase beige adipocyte content is through inhibition of the evolutionarily conserved Notch signaling pathway. However, systemic delivery of Notch inhibitors is associated with off-target effects and multiple dosages of application further faces technical and translational challenges. Here, we report the development of a biodegradable polymeric microsphere-based drug delivery system for sustained, local release of a Notch inhibitor, DBZ. The microsphere-based delivery system was fabricated and optimized using an emulsion/solvent evaporation technique to encapsulate DBZ into poly(lactide-co-glycolide (PLGA, a commonly used biodegradable polymer for controlled drug release. Release studies revealed the ability of PLGA microspheres to release DBZ in a sustained manner. Co-culture of white adipocytes with and without DBZ-loaded PLGA microspheres demonstrated that the released DBZ retained its bioactivity, and effectively inhibited Notch and promoted browning of white adipocytes. Injection of these DBZ-loaded PLGA microspheres into mouse inguinal white adipose tissue (WAT depots resulted in browning in vivo. Our results provide the encouraging proof-of-principle evidence for the application of biodegradable polymers as a controlled release platform for delivery of browning factors, and pave the way for development of new translational therapeutic strategies for treatment of obesity.

  18. Current knowledge on biodegradable microspheres in drug delivery.

    Science.gov (United States)

    Prajapati, Vipul D; Jani, Girish K; Kapadia, Jinita R

    2015-08-01

    Biodegradable microspheres have gained popularity for delivering a wide variety of molecules via various routes. These types of products have been prepared using various natural and synthetic biodegradable polymers through suitable techniques for desired delivery of various challenging molecules. Selection of biodegradable polymers and technique play a key role in desired drug delivery. This review describes an overview of the fundamental knowledge and status of biodegradable microspheres in effective delivery of various molecules via desired routes with consideration of outlines of various compendial and non-compendial biodegradable polymers, formulation techniques and release mechanism of microspheres, patents and commercial biodegradable microspheres. There are various advantages of using biodegradable polymers including promise of development with different types of molecules. Biocompatibility, low dosage and reduced side effects are some reasons why usage biodegradable microspheres have gained in popularity. Selection of biodegradable polymers and formulation techniques to create microspheres is the biggest challenge in research. In the near future, biodegradable microspheres will become the eco-friendly product for drug delivery of various genes, hormones, proteins and peptides at specific site of body for desired periods of time.

  19. Methyl salicylate lactoside inhibits inflammatory response of fibroblast-like synoviocytes and joint destruction in collagen-induced arthritis in mice.

    Science.gov (United States)

    Xin, Wenyu; Huang, Chao; Zhang, Xue; Xin, Sheng; Zhou, Yiming; Ma, Xiaowei; Zhang, Dan; Li, Yongjie; Zhou, Sibai; Zhang, Dongming; Zhang, Tiantai; Du, Guanhua

    2014-07-01

    Methyl salicylate 2-O-β-d-lactoside (MSL), whose chemical structure is similar to that of salicylic acid, is a natural product derivative isolated from a traditional Chinese herb. The aim of this study was to investigate the therapeutic effect of MSL in mice with collagen-induced arthritis (CIA) and explore its underlying mechanism. The anti-arthritic effects of MSL were evaluated on human rheumatoid fibroblast-like synoviocytes (FLS) in vitro and CIA in mice in vivo by obtaining clinical scores, measuring hind paw thickness and inflammatory cytokine levels, radiographic evaluations and histopathological assessments. Treatment with MSL after the onset of arthritis significantly prevented the progression and development of rheumatoid arthritis (RA) in CIA mice without megascopic gastric mucosa damage. In addition, MSL inhibited the production of pro-inflammatory mediators, the phosphorylation and translocation of NF-κB, and cell proliferation induced by TNF-α in FLS. MSL non-selectively inhibited the activity of COX in vitro, but was a more potent inhibitor of COX-2 than COX-1. MSL also inhibited the phosphorylation of inhibitor of NF-κB kinase, IκBα and p65, thus blocking the nuclear translocation of NF-κB in TNF-α-stimulated FLS. MSL exerts therapeutic effects on CIA mice, suppressing the inflammatory response and joint destruction by non-selectively inhibiting the activity of COX and suppressing activation of the NF-κB signalling pathway, but without damaging the gastric mucosa. Therefore, MSL has great potential to be developed into a novel therapeutic agent for the treatment of RA. © 2014 The British Pharmacological Society.

  20. Myositis non-inflammatory mechanisms: An up-dated review.

    Science.gov (United States)

    Manole, Emilia; Bastian, Alexandra E; Butoianu, Niculina; Goebel, Hans H

    2017-01-01

    Idiopathic inflammatory myopathies (IIM) represent a heterogeneous group of rare muscular diseases, with no clearly known causes. IIM frequently have an incomplete response to treatment due to the difficulty in distinguishing between IIM forms, and due to neglect their non-inflammatory causes. Important data concerning non-immune mechanisms in IIM pathology have been recently accumulated. There is a correlation between inflammatory and non-inflammatory mechanisms, but their involvement in IIM pathogenesis is still unknown. Here we review some of the most important data regarding the non-immune IIM pathology, highlighting possible future therapeutic targets: endoplasmic reticulum stress, ATP metabolism, ROS generation, autophagy, and microRNAs disturbances.

  1. Laser emission in Nd3+ doped barium–titanium–silicate microspheres under continuous and chopped wave pumping in a non-coupled pumping scheme

    International Nuclear Information System (INIS)

    Martín, L L; Pérez-Rodríguez, C; Martín, I R; Navarro-Urrios, D; Ferrarese-Lupi, F; Garrido, B; Montserrat, J; Dominguez, C; Capuj, N

    2013-01-01

    Laser action using non-coupled excitation and detection of microspheres made of Nd 3+ doped barium–titanium–silicate glass has been demonstrated and measured. The microspheres have also been successfully deposited over Si 3 N 4 strip waveguides with a SiO 2 separation layer, thus enabling the laser emission extraction onto a CMOS compatible photonic circuit. The dynamics of the lasing wavelength and intensity has been studied as a function of the pump power and interpreted in terms of thermal effects generated through non-radiative recombination of the excited ions. (paper)

  2. Biocompatibility of Bletilla striata Microspheres as a Novel Embolic Agent

    Directory of Open Access Journals (Sweden)

    ShiHua Luo

    2015-01-01

    Full Text Available We have prepared Chinese traditional herb Bletilla striata into microspheres as a novel embolic agent for decades. The aim of this study was to evaluate the biocompatibility of Bletilla striata microspheres (BSMs. After a thermal test of BSMs in vitro, the cell biocompatibility of BSMs was investigated in mouse fibroblasts and human umbilical vein endothelial cells using the methyl tetrazolium (MTT assay. In addition, blood biocompatibility was evaluated. In vivo intramuscular implantation and renal artery embolization in rabbits with BSMs were used to examine the inflammatory response. The experimental rabbits did not develop any fever symptoms after injection of BSMs, and BSMs exhibited no cytotoxicity in cultured mouse fibroblasts and human umbilical vein endothelial cells. Additionally, BSMs exhibited high compatibility with red blood cells and no hemolysis activity. Intramuscular implantation with BSMs resulted in a gradually lessened mild inflammatory reaction that disappeared after eight weeks. The occlusion of small renal vessels was associated with a mild perivascular inflammatory reaction without significant renal and liver function damage. In conclusion, we believe that BSMs exhibit high biocompatibility and are a promising embolic agent.

  3. BIOCOMPATIBLE FLUORESCENT MICROSPHERES: SAFE PARTICLES FOR MATERIAL PENETRATION STUDIES

    Energy Technology Data Exchange (ETDEWEB)

    Farquar, G; Leif, R

    2009-07-15

    Biocompatible polymers with hydrolyzable chemical bonds have been used to produce safe, non-toxic fluorescent microspheres for material penetration studies. The selection of polymeric materials depends on both biocompatibility and processability, with tailored fluorescent properties depending on specific applications. Microspheres are composed of USFDA-approved biodegradable polymers and non-toxic fluorophores and are therefore suitable for tests where human exposure is possible. Micropheres were produced which contain unique fluorophores to enable discrimination from background aerosol particles. Characteristics that affect dispersion and adhesion can be modified depending on use. Several different microsphere preparation methods are possible, including the use of a vibrating orifice aerosol generator (VOAG), a Sono-Tek atomizer, an emulsion technique, and inkjet printhead. Applications for the fluorescent microspheres include challenges for biodefense system testing, calibrants for biofluorescence sensors, and particles for air dispersion model validation studies.

  4. Perilipin 1 Mediates Lipid Metabolism Homeostasis and Inhibits Inflammatory Cytokine Synthesis in Bovine Adipocytes.

    Science.gov (United States)

    Zhang, Shiqi; Liu, Guowen; Xu, Chuang; Liu, Lei; Zhang, Qiang; Xu, Qiushi; Jia, Hongdou; Li, Xiaobing; Li, Xinwei

    2018-01-01

    Dairy cows with ketosis displayed lipid metabolic disorder and high inflammatory levels. Adipose tissue is an active lipid metabolism and endocrine tissue and is closely related to lipid metabolism homeostasis and inflammation. Perilipin 1 (PLIN1), an adipocyte-specific lipid-coated protein, may be involved in the above physiological function. The aim of this study is to investigate the role of PLIN1 in lipid metabolism regulation and inflammatory factor synthesis in cow adipocytes. The results showed that PLIN1 overexpression upregulated the expression of fatty acid and triglyceride (TAG) synthesis molecule sterol regulator element-binding protein-1c (SREBP-1c) and its target genes, diacylglycerol acyltransferase (DGAT) 1, and DGAT2, but inhibited the expression of lipolysis enzymes hormone-sensitive lipase (HSL) and CGI-58 for adipose triglyceride lipase (ATGL), thus augmenting the fatty acids and TAG synthesis and inhibiting lipolysis. Importantly, PLIN1 overexpression inhibited the activation of the NF-κB inflammatory pathway and decreased the expression and content of tumor necrosis factor alpha (TNF-α), interleukin 1 beta (IL-1β), and interleukin 6 (IL-6) induced by lipopolysaccharide. Conversely, PLIN1 silencing inhibited TAG synthesis, promoted lipolysis, and overinduced the activation of the NF-κB inflammatory pathway in cow adipocytes. In ketotic cows, the expression of PLIN1 was markedly decreased, whereas lipid mobilization, NF-κB pathway, and downstream inflammatory cytokines were overinduced in adipose tissue. Taken together, these results indicate that PLIN1 can maintain lipid metabolism homeostasis and inhibit the NF-κB inflammatory pathway in adipocytes. However, low levels of PLIN1 reduced the inhibitory effect on fat mobilization, NF-κB pathway, and inflammatory cytokine synthesis in ketotic cows.

  5. Perilipin 1 Mediates Lipid Metabolism Homeostasis and Inhibits Inflammatory Cytokine Synthesis in Bovine Adipocytes

    Directory of Open Access Journals (Sweden)

    Shiqi Zhang

    2018-03-01

    Full Text Available Dairy cows with ketosis displayed lipid metabolic disorder and high inflammatory levels. Adipose tissue is an active lipid metabolism and endocrine tissue and is closely related to lipid metabolism homeostasis and inflammation. Perilipin 1 (PLIN1, an adipocyte-specific lipid-coated protein, may be involved in the above physiological function. The aim of this study is to investigate the role of PLIN1 in lipid metabolism regulation and inflammatory factor synthesis in cow adipocytes. The results showed that PLIN1 overexpression upregulated the expression of fatty acid and triglyceride (TAG synthesis molecule sterol regulator element-binding protein-1c (SREBP-1c and its target genes, diacylglycerol acyltransferase (DGAT 1, and DGAT2, but inhibited the expression of lipolysis enzymes hormone-sensitive lipase (HSL and CGI-58 for adipose triglyceride lipase (ATGL, thus augmenting the fatty acids and TAG synthesis and inhibiting lipolysis. Importantly, PLIN1 overexpression inhibited the activation of the NF-κB inflammatory pathway and decreased the expression and content of tumor necrosis factor alpha (TNF-α, interleukin 1 beta (IL-1β, and interleukin 6 (IL-6 induced by lipopolysaccharide. Conversely, PLIN1 silencing inhibited TAG synthesis, promoted lipolysis, and overinduced the activation of the NF-κB inflammatory pathway in cow adipocytes. In ketotic cows, the expression of PLIN1 was markedly decreased, whereas lipid mobilization, NF-κB pathway, and downstream inflammatory cytokines were overinduced in adipose tissue. Taken together, these results indicate that PLIN1 can maintain lipid metabolism homeostasis and inhibit the NF-κB inflammatory pathway in adipocytes. However, low levels of PLIN1 reduced the inhibitory effect on fat mobilization, NF-κB pathway, and inflammatory cytokine synthesis in ketotic cows.

  6. Inhibition by local bupivacaine-releasing microspheres of acute postoperative pain from hairy skin incision.

    Science.gov (United States)

    Ohri, Rachit; Wang, Jeffrey Chi-Fei; Blaskovich, Phillip D; Pham, Lan N; Costa, Daniel S; Nichols, Gary A; Hildebrand, William P; Scarborough, Nelson L; Herman, Clifford J; Strichartz, Gary R

    2013-09-01

    Acute postoperative pain causes physiological deficits and slows recovery. Reduction of such pain by local anesthetics that are delivered for several days postoperatively is a desirable clinical objective, which is approached by a new formulation and applied in animal studies reported here. We subcutaneously injected a new formulation of poly-lactic-co-glycolic acid polymer microspheres, which provides steady drug release for 96+ hours into rats at the dorsal region 2 hours before surgery. A single 1.2-cm-long skin incision was followed by blunt dissection of skin away from the underlying fascia, and closed by 2 sutures, followed by 14 days of testing. Microspheres containing 5, 10, 20, and 40 mg bupivacaine were injected locally 2 hours before surgery; bupivacaine-free microspheres were the vehicle control, and bupivacaine HCl solution (0.5%), the positive control. Mechanical sensitivity was determined by the frequency of local muscle contractions to repeated pokes with nylon monofilaments (von Frey hairs) exerting 4 and 15 g forces, testing, respectively, allodynia and hyperalgesia, and by pinprick. Injection of bupivacaine microspheres (40 mg drug) into intact skin reduced responses to 15 g von Frey hairs for 6 hours and to pinprick for 36 hours. Respective reductions from bupivacaine HCl lasted for 3 and 2 hours. Skin incision and dissection alone caused mechanical allodynia and hyperalgesia for 14 days. Microspheres containing 20 or 40 mg bupivacaine suppressed postoperative hypersensitivity for up to 3 days, reduced integrated allodynia (area under curve of response versus time) over postoperative days 1 to 5 by 51% ± 20% (mean ± SE) and 78% ± 12%, and reduced integrated hyperalgesia by 55% ± 13% and 64% ± 11%, for the respective doses. Five and ten milligrams bupivacaine in microspheres and the 0.5% bupivacaine solution were ineffective in reducing postoperative hypersensitivity, as were 40 mg bupivacaine microspheres injected contralateral to the

  7. Microradiographic microsphere manipulator

    International Nuclear Information System (INIS)

    Singleton, R.M.

    1980-01-01

    A method and apparatus are provided for radiographic characterization of small hollow spherical members (microspheres), constructed of either optically transparent or opaque materials. The apparatus involves a microsphere manipulator which holds a batch of microspheres between two parallel thin plastic films for contact microradiographic characterization or projection microradiography thereof. One plastic film is translated to relative to and parallel to the other to roll the microspheres through any desired angle to allow different views of the microspheres

  8. [Anti-inflammatory, analgesic and anti-pyretic activities of a non-steroidal anti-inflammatory drug, etofenamate, in experimental animals].

    Science.gov (United States)

    Nakamura, H; Motoyoshi, S; Imazu, C; Ishii, K; Yokoyama, Y; Seto, Y; Kadokawa, T; Shimizu, M

    1982-08-01

    Anti-inflammatory, analgesic, and anti-pyretic activities of orally administered etofenamate, the diethylene glycol ester of flufenamic acid, were investigated in experimental animals. Against acetic acid-induced vascular permeability in mice and ultra-violet light-induced erythema in guinea pigs, etofenamate produced a dose related inhibition at doses of 40--320 mg/kg and 5--20 mg/kg, respectively. In rats, felt-pellet-induced granuloma formation and adjuvant-induced arthritis were significantly inhibited by repeated administration of etofenamate at doses of 20 mg/kg/day for 5 days and 40 mg/kg/day for 21 days, respectively. Etofenamate showed an inhibitory activity on the squeak response caused by flexing and extending the silver nitrate-induced arthritic joint in rats; and it produced a dose related anti-writhing activity at doses of 50--300 mg/kg and 10--80 mg/kg in mice and rats, respectively, in the acetic acid-induced writhing test. Etofenamate showed a significant anti-pyretic activity at doses of 0.2 mg/kg or more. These potencies of etofenamate were 0.5 to 1.6 times those of flufenamic acid. In particular, the anti-erythema, anti-arthritis, and anti-pyretic activities of etofenamate were approximately equivalent to or superior to those of flufenamic acid. From these results, it was suggested that etofenamate given orally, like other non-steroidal anti-inflammatory drugs, showed anti-inflammatory, analgesic, and anti-pyretic activities in experimental animals.

  9. Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits type I-IV allergic inflammation and pro-inflammatory enzymes.

    Science.gov (United States)

    Lee, Ji Yun; Kim, Chang Jong

    2010-06-01

    We previously reported that arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan isolated from Forsythia koreana, exhibits anti-inflammatory, antioxidant, and analgesic effects in animal models. In addition, arctigenin inhibited eosinophil peroxidase and activated myeloperoxidase in inflamed tissues. In this study, we tested the effects of arctigenin on type I-IV allergic inflammation and pro-inflammatory enzymes in vitro and in vivo. Arctigenin significantly inhibited the heterologous passive cutaneous anaphylaxis induced by ovalbumin in mice at 15 mg/kg, p.o., and compound 48/80-induced histamine release from rat peritoneal mast cells at 10 microM. Arctigenin (15 mg/kg, p.o.) significantly inhibited reversed cutaneous anaphylaxis. Further, arctigenin (15 mg/kg, p.o.) significantly inhibited the Arthus reaction to sheep's red blood cells, decreasing the hemolysis titer, the hemagglutination titer, and the plaque-forming cell number for SRBCs. In addition, arctigenin significantly inhibited delayed type hypersensitivity at 15 mg/kg, p.o. and the formation of rosette-forming cells at 45 mg/kg, p.o. Contact dermatitis induced by picrylchloride and dinitrofluorobenzene was significantly (p arctigenin (0.3 mg/ear). Furthermore, arctigenin dose-dependently inhibited pro-inflammatory enzymes, such as cyclooxygenase-1 and 2, 5-lipoxygenase, phospholipase A2, and phosphodiesterase. Our results show that arctigenin significantly inhibited B- and T-cell mediated allergic inflammation as well as pro-inflammatory enzymes.

  10. Metformin inhibits inflammatory response via AMPK–PTEN pathway in vascular smooth muscle cells

    International Nuclear Information System (INIS)

    Kim, Sun Ae; Choi, Hyoung Chul

    2012-01-01

    Highlights: ► PTEN was induced by metformin and inhibited by compound C and AMPK siRNA. ► Metformin suppressed TNF-α-induced COX-2 and iNOS mRNA expression. ► Compound C and bpv (pic) increased iNOS and COX-2 protein expression. ► NF-κB activation was restored by inhibiting AMPK and PTEN. ► AMPK and PTEN regulated TNF-α-induced ROS production in VSMCs. -- Abstract: Atherosclerosis is a chronic inflammation of the coronary arteries. Vascular smooth muscle cells (VSMCs) stimulated by cytokines and chemokines accelerate the inflammatory response and migrate to the injured endothelium during the progression of atherosclerosis. Activation of AMP activated protein kinase (AMPK), a key sensor maintaining metabolic homeostasis, suppresses the inflammatory response. However, how AMPK regulates the inflammatory response is poorly understood. To identify the mechanism of this response, we focused on phosphatase and tensin homolog (PTEN), which is a negative regulator of inflammation. We investigated that activation of AMPK-induced PTEN expression and suppression of the inflammatory response through the AMPK–PTEN pathway in VSMCs. We treated with the well-known AMPK activator metformin to induce PTEN expression. PTEN was induced by metformin (2 mM) and inhibited by compound C (10 μM) and AMPK siRNA. Tumor necrosis factor-alpha (TNF-α) was used to induce inflammation. The inflammatory response was confirmed by cyclooxygenase (COX)-2, inducible nitric oxide synthase (iNOS) expression, and activation of nuclear factor (NF)-κB. Metformin suppressed COX-2 and iNOS mRNA and protein expression dose dependently. Treatment with compound C and bpv (pic) in the presence of metformin, iNOS and COX-2 protein expression increased. NF-κB activation decreased in response to metformin and was restored by inhibiting AMPK and PTEN. Inhibiting AMPK and PTEN restored ROS levels stimulated with TNF-α. Taken together, PTEN could be a possible downstream regulator of AMPK, and the

  11. A binding site for non-steroidal anti-inflammatory drugs in FAAH

    Science.gov (United States)

    Bertolacci, Laura; Romeo, Elisa; Veronesi, Marina; Magotti, Paola; Albani, Clara; Dionisi, Mauro; Lambruschini, Chiara; Scarpelli, Rita; Cavalli, Andrea; Vivo, Marco De; Piomelli, Daniele; Garau, Gianpiero

    2013-01-01

    In addition to inhibiting the cyclooxygenasemediated biosynthesis of prostanoids, various widely used non-steroidal anti-inflammatory drugs (NSAIDs) enhance endocannabinoid signaling by blocking the anandamidedegrading membrane enzyme, fatty acid amide hydrolase (FAAH). The X-ray structure of FAAH in complex with the NSAID carprofen, along with studies of site-directed mutagenesis, enzyme activity assays, and nuclear magnetic resonance, now reveal the molecular details of this interaction, providing information that may guide the design of dual FAAH-cyclooxygenase inhibitors with superior analgesic efficacy. PMID:23240907

  12. Mechanism of inhibition of myeloperoxidase by anti-inflammatory drugs.

    Science.gov (United States)

    Kettle, A J; Winterbourn, C C

    1991-05-15

    Hypochlorous acid (HOCl) is the most powerful oxidant produced by human neutrophils, and should therefore be expected to contribute to the damage caused by these inflammatory cells. It is produced from H2O2 and Cl- by the heme enzyme myeloperoxidase (MPO). We used a H2O2-electrode to assess the ability of a variety of anti-inflammatory drugs to inhibit conversion of H2O2 to HOCl. Dapsone, mefenamic acid, sulfapyridine, quinacrine, primaquine and aminopyrine were potent inhibitors, giving 50% inhibition of the initial rate of H2O2 loss at concentrations of about 1 microM or less. Phenylbutazone, piroxicam, salicylate, olsalazine and sulfasalazine were also effective inhibitors. Spectral investigations showed that the inhibitors acted by promoting the formation of compound II, which is an inactive redox intermediate of MPO. Ascorbate reversed inhibition by reducing compound II back to the active enzyme. The characteristic properties that allowed the drugs to inhibit MPO reversibly were ascertained by determining the inhibitory capacity of related phenols and anilines. Inhibition increased as substituents on the aromatic ring became more electron withdrawing, until an optimum reduction potential was reached. Beyond this optimum, their inhibitory capacity declined. The best inhibitor was 4-bromoaniline which had an I50 of 45 nM. An optimum reduction potential enables inhibitors to reduce MPO to compound II, but prevents them from reducing compound II back to the active enzyme. Exploitation of this optimum reduction potential will help in targeting drugs against HOCl-dependent tissue damage.

  13. BIOCOMPATIBLE FLUORESCENT MICROSPHERES: SAFE PARTICLES FOR MATERIAL PENETRATION STUDIES

    Energy Technology Data Exchange (ETDEWEB)

    farquar, G; Leif, R

    2008-09-12

    Biocompatible polymers with hydrolyzable chemical bonds are being used to produce safe, non-toxic fluorescent microspheres for material penetration studies. The selection of polymeric materials depends on both biocompatibility and processability, with tailored fluorescent properties depending on specific applications. Microspheres are composed of USFDA-approved biodegradable polymers and non-toxic fluorophores and are therefore suitable for tests where human exposure is possible. Micropheres are being produced which contain unique fluorophores to enable discrimination from background aerosol particles. Characteristics that affect dispersion and adhesion can be modified depending on use. Several different microsphere preparation methods are possible, including the use of a vibrating orifice aerosol generator (VOAG), a Sono-Tek atomizer, an emulsion technique, and inkjet printhead. The advantages and disadvantages of each method will be presented and discussed in greater detail along with fluorescent and charge properties of the aerosols. Applications for the fluorescent microspheres include challenges for biodefense system testing, calibrants for biofluorescence sensors, and particles for air dispersion model validation studies.

  14. Resonant microsphere gyroscope based on a double Faraday rotator system.

    Science.gov (United States)

    Xie, Chengfeng; Tang, Jun; Cui, Danfeng; Wu, Dajin; Zhang, Chengfei; Li, Chunming; Zhen, Yongqiu; Xue, Chenyang; Liu, Jun

    2016-10-15

    The resonant microsphere gyroscope is proposed based on a double Faraday rotator system for the resonant microsphere gyroscope (RMSG) that is characterized by low insertion losses and does not destroy the reciprocity of the gyroscope system. Use of the echo suppression structure and the orthogonal polarization method can effectively inhibit both the backscattering noise and the polarization error, and reduce them below the system sensitivity limit. The resonance asymmetry rate dropped from 34.2% to 2.9% after optimization of the backscattering noise and the polarization noise, which greatly improved the bias stability and the scale factor linearity of the proposed system. Additionally, based on the optimum parameters for the double Faraday rotator system, a bias stability of 0.04°/s has been established for an integration time of 10 s in 1000 s in a resonator microsphere gyroscope using a microsphere resonator with a diameter of 1 mm and a Q of 7.2×106.

  15. 188Re-microspheres of albumin - the potential preparation for radiotherapy

    International Nuclear Information System (INIS)

    Dyomin, D.N.; Petriev, V.M.

    2000-01-01

    In this paper author describe preparation the albumin microspheres labelled with rhenium-188. We undertake an attempt to develop kits to the generator of rhenium-188 on the basis of albumin microspheres for radiotherapy of both oncological and non-oncological diseases. Microspheres, rhenium-188 with sizes 1 0-20 micron for treatment of rheumatoid arthritis (damage of large and intermediate joints), intraperitoneal administration and intrapleural administration at metastases covering a cavity. Microspheres, Re-188 with sizes 40-60 micron for treatment of disseminated kidney cancer (intraarterial, selectively), intratumoral administration to damaged nodules less than 2-3 cm. Microspheres, Re-188 with sizes 80-100 micron for large neoplasms and metastases of liver (intraarterial, selectively), intratumoral administration to damaged nodules with sizes over 3 cm. Preparation of albumin microspheres is carried out by thermal denaturation of protein in vegetable oil. Microspheres are obtained with the necessary range of sizes by ultrasonic fractionation. At our laboratory the method of preparation of albumin microspheres with any sizes of particles (from 5 -10 up to 800 -1000 microns) has been developed. (authors)

  16. Glass microspheres for medical applications

    Science.gov (United States)

    Conzone, Samuel David

    Radioactive dysprosium lithium borate glass microspheres have been developed as biodegradable radiation delivery vehicles for the radiation synovectomy treatment of rheumatoid arthritis. Once injected into a diseased joint, the microspheres deliver a potent dose of radiation to the diseased tissue, while a non-uniform chemical reaction converts the glass into an amorphous, porous, hydrated dysprosium phosphate reaction product. The non-radioactive, lithium-borate component is dissolved from the glass (up to 94% weight loss), while the radioactive 165Dy reacts with phosphate anions in the body fluids, and becomes "chemically" trapped in a solid, dysprosium phosphate reaction product that has the same size as the un-reacted glass microsphere. Ethylene diamine tetraacetate (EDTA) chelation therapy can be used to dissolve the dysprosium phosphate reaction product after the radiation delivery has subsided. The dysprosium phosphate reaction product, which formed in vivo in the joint of a Sprague-Dawley rat, was dissolved by EDTA chelation therapy in 100 Gy) of localized beta radiation to a treatment site within the body, followed by complete biodegradability. The non-uniform reaction process is a desirable characteristic for a biodegradable radiation delivery vehicle, but it is also a novel material synthesis technique that can convert a glass to a highly porous materials with widely varying chemical composition by simple, low-temperature, glass/solution reaction. The reaction product formed by nonuniform reaction occupies the same volume as the un-reacted glass, and after drying for 1 h at 300°C, has a specific surface area of ≈200 m2/g, a pore size of ≈30 nm, and a nominal crushing strength of ≈10 MPa. Finally, rhenium glass microspheres, composed of micron-sized, metallic rhenium particles dispersed within a magnesium alumino borate glass matrix were produced by sintering ReO2 powder and glass frit at 1050°C. A 50 mg injection of radioactive rhenium glass

  17. Bioactive Extract from Moringa oleifera Inhibits the Pro-inflammatory Mediators in Lipopolysaccharide Stimulated Macrophages

    Science.gov (United States)

    Fard, Masoumeh Tangestani; Arulselvan, Palanisamy; Karthivashan, Govindarajan; Adam, Siti Khadijah; Fakurazi, Sharida

    2015-01-01

    Introduction: Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. Objectives: The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS) - stimulated macrophages. Materials and Methods: The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO) production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Results: Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E2, tumor necrosis factor alpha, interleukin (IL)-6, and IL-1β. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. Conclusion: These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders. SUMMARY Hydroethanolic extracts of Moringa oleifera effectively inhibit the NO production in LPS induced inflammatory model.M. oleifera crude extracts successfully modulate the production of pro-inflammatory mediators in LPS stimulated macrophages.M. oleifera extracts suppressed the expression of inflammatory mediators in LPS stimulated macrophages. PMID:27013794

  18. Flexible Microsphere-Embedded Film for Microsphere-Enhanced Raman Spectroscopy.

    Science.gov (United States)

    Xing, Cheng; Yan, Yinzhou; Feng, Chao; Xu, Jiayu; Dong, Peng; Guan, Wei; Zeng, Yong; Zhao, Yan; Jiang, Yijian

    2017-09-27

    Dielectric microspheres with extraordinary microscale optical properties, such as photonic nanojets, optical whispering-gallery modes (WGMs), and directional antennas, have drawn interest in many research fields. Microsphere-enhanced Raman spectroscopy (MERS) is an alternative approach for enhanced Raman detection by dielectric microstructures. Unfortunately, fabrication of microsphere monolayer arrays is the major challenge of MERS for practical applications on various specimen surfaces. Here we report a microsphere-embedded film (MF) by immersing a highly refractive microsphere monolayer array in the poly(dimethylsiloxane) (PDMS) film as a flexible MERS sensing platform for one- to three-dimensional (1D to 3D) specimen surfaces. The directional antennas and wave-guided whispering-gallery modes (WG-WGMs) contribute to the majority of Raman enhancement by the MFs. Moreover, the MF can be coupled with surface-enhanced Raman spectroscopy (SERS) to provide an extra >10-fold enhancement. The limit of detection is therefore improved for sensing of crystal violet (CV) and Sudan I molecules in aqueous solutions at concentrations down to 10 -7 M. A hybrid dual-layer microsphere enhancer, constructed by depositing a MF onto a microsphere monolayer array, is also demonstrated, wherein the WG-WGMs become dominant and boost the enhancement ratio >50-fold. The present work opens up new opportunities for design of cost-effective and flexible MERS sensing platforms as individual or associated techniques toward practical applications in ultrasensitive Raman detection.

  19. Metformin inhibits inflammatory response via AMPK-PTEN pathway in vascular smooth muscle cells

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Sun Ae [Department of Pharmacology, Aging-Associated Vascular Disease Research Center, College of Medicine, Yeungnam University, Daegu 705-717 (Korea, Republic of); Choi, Hyoung Chul, E-mail: hcchoi@med.yu.ac.kr [Department of Pharmacology, Aging-Associated Vascular Disease Research Center, College of Medicine, Yeungnam University, Daegu 705-717 (Korea, Republic of)

    2012-09-07

    Highlights: Black-Right-Pointing-Pointer PTEN was induced by metformin and inhibited by compound C and AMPK siRNA. Black-Right-Pointing-Pointer Metformin suppressed TNF-{alpha}-induced COX-2 and iNOS mRNA expression. Black-Right-Pointing-Pointer Compound C and bpv (pic) increased iNOS and COX-2 protein expression. Black-Right-Pointing-Pointer NF-{kappa}B activation was restored by inhibiting AMPK and PTEN. Black-Right-Pointing-Pointer AMPK and PTEN regulated TNF-{alpha}-induced ROS production in VSMCs. -- Abstract: Atherosclerosis is a chronic inflammation of the coronary arteries. Vascular smooth muscle cells (VSMCs) stimulated by cytokines and chemokines accelerate the inflammatory response and migrate to the injured endothelium during the progression of atherosclerosis. Activation of AMP activated protein kinase (AMPK), a key sensor maintaining metabolic homeostasis, suppresses the inflammatory response. However, how AMPK regulates the inflammatory response is poorly understood. To identify the mechanism of this response, we focused on phosphatase and tensin homolog (PTEN), which is a negative regulator of inflammation. We investigated that activation of AMPK-induced PTEN expression and suppression of the inflammatory response through the AMPK-PTEN pathway in VSMCs. We treated with the well-known AMPK activator metformin to induce PTEN expression. PTEN was induced by metformin (2 mM) and inhibited by compound C (10 {mu}M) and AMPK siRNA. Tumor necrosis factor-alpha (TNF-{alpha}) was used to induce inflammation. The inflammatory response was confirmed by cyclooxygenase (COX)-2, inducible nitric oxide synthase (iNOS) expression, and activation of nuclear factor (NF)-{kappa}B. Metformin suppressed COX-2 and iNOS mRNA and protein expression dose dependently. Treatment with compound C and bpv (pic) in the presence of metformin, iNOS and COX-2 protein expression increased. NF-{kappa}B activation decreased in response to metformin and was restored by inhibiting AMPK

  20. Inhibition of nitric oxide and inflammatory cytokines in LPS-stimulated murine macrophages by resveratrol, a potent proteasome inhibitor

    Directory of Open Access Journals (Sweden)

    Qureshi Asaf A

    2012-07-01

    Full Text Available Abstract Background Altered immune function during ageing results in increased production of nitric oxide (NO and other inflammatory mediators. Recently, we have reported that NO production was inhibited by naturally-occurring proteasome inhibitors (quercetin, δ-tocotrienol, and riboflavin in lipopolysaccharide (LPS-stimulated RAW264.7 cells, and thioglycolate-elicited peritoneal macrophages from C57BL/6 mice. In a continuous effort to find more potent, non-toxic, commercially available, naturally-occurring proteasome inhibitors that suppress inflammation, the present study was carried out to describe the inhibition of NF-κB activation and NO, TNF-α, IL-6, IL-1β, and iNOS expression by trans-resveratrol, trans-pterostilbene, morin hydrate, and nicotinic acid in LPS-induced RAW 264.7 cells and thioglycolate-elicited peritoneal macrophages from C57BL/6 and BALB/c mice. Results The present results indicate that resveratrol, pterostilbene, and morin hydrate caused significant inhibition (>70% to 90%; P 40%; P 60%; P 40%; P P  Conclusions The present results clearly demonstrate that resveratrol and pterostilbene are particularly potent proteasome inhibitors that suppress expression of genes, and production of inflammatory products in LPS-stimulated RAW 264.7 cells, and macrophages from C57BL/6 and BALB/c mice. Resveratrol and pterostilbene which are present in grapes, blueberries, and red wine, have been implicated as contributing factors to the lower incidence of cardiovascular disease in the French population, despite their relatively high dietary fat intake. Consequently, it appears likely that the beneficial nutritional effects of resveratrol and pterostilbene are due at least in part, to their ability to inhibit NF-κB activation by the proteasome, thereby suppressing activation of pro-inflammatory cytokines and iNOS genes, resulting in decreased secretion of TNF-α, IL-1β, IL-6, and NO levels, in response to inflammatory stimuli

  1. Sirtuin inhibition attenuates the production of inflammatory cytokines in lipopolysaccharide-stimulated macrophages

    International Nuclear Information System (INIS)

    Fernandes, Cláudia A.; Fievez, Laurence; Neyrinck, Audrey M.; Delzenne, Nathalie M.; Bureau, Fabrice; Vanbever, Rita

    2012-01-01

    Highlights: ► Lipopolysaccharide-stimulated macrophages were treated with cambinol and sirtinol. ► Cambinol and sirtinol decreased lipopolysaccharide-induced cytokines. ► Cambinol decreased NF-κB activity but had no impact on p38 MAPK activation. ► Sirtuins are an interesting target for the treatment of inflammatory diseases. -- Abstract: In several inflammatory conditions such as rheumatoid arthritis or sepsis, the regulatory mechanisms of inflammation are inefficient and the excessive inflammatory response leads to damage to the host. Sirtuins are class III histone deacetylases that modulate the activity of several transcription factors that are implicated in immune responses. In this study, we evaluated the impact of sirtuin inhibition on the activation of lipopolysaccharide (LPS)-stimulated J774 macrophages by assessing the production of inflammatory cytokines. The pharmacologic inhibition of sirtuins decreased the production of tumour necrosis factor-alpha (TNF-α) interleukin 6 (IL-6) and Rantes. The reduction of cytokine production was associated with decreased nuclear factor kappa B (NF-κB) activity and inhibitor kappa B alpha (IκBα) phosphorylation while no impact was observed on the phosphorylation status of p38 mitogen-activated kinase (p38 MAPK). This work shows that sirtuin pharmacologic inhibitors are a promising tool for the treatment of inflammatory conditions.

  2. Selective removal of 2,4-dichlorophenol from contaminated water using non-covalent imprinted microspheres

    International Nuclear Information System (INIS)

    Li Ying; Li Xin; Li Yuqi; Qi Jingyao; Bian Jiang; Yuan Yixing

    2009-01-01

    A molecularly imprinted polymer (MIP) for selective removal of 2,4-dichlorophenol (2,4-DCP) in water was prepared as microspheres by the reverse microemulsion polymerization method based on the non-covalent interactions between 2,4-DCP, oleic acid, and divinylbenzene in acetonitrile. Microspheres have been characterized by Fourier transform infrared spectrometer (FTIR) and energy dispersive X-ray spectrometer (EDS) studies with evidence of 2,4-DCP linkage in polymer particles and scanning electron microscopy (SEM) to study their morphological properties. The proper adsorption and selective recognition ability of the MIP were studied by an equilibrium-adsorption method. The MIP showed outstanding affinity towards 2,4-DCP in aqueous solution and the optimum pH value for binding has been found around the neutral range. The molecular recognition of 2,4-DCP was analyzed in detail by using molecular modeling software. In addition, by investigating the variation in the adsorption ability of the MIP, it clearly showed excellent reproducibility. - Molecular imprinting has potential as a remediation technology in water treatment.

  3. Effect of gamma-irradiation on biodegradable microspheres loaded with rasagiline mesylate

    International Nuclear Information System (INIS)

    Fernandez, Marcos; Barcia, Emilia; Negro, Sofia

    2016-01-01

    In the present study, the influence of gamma-irradiation was evaluated on the physicochemical characteristics and in vitro release of rasagiline mesylate (RM), a selective MAO-B inhibitor used in Parkinson's disease, from poly(D,L-lactide-co-glycolide) (PLGA) microspheres. Microspheres were prepared using PLGA 50:50 by the solvent evaporation technique (O/W emulsion). Microspheres were sterilized by gamma-irradiation and their influence was assessed by scanning electron microscopy (SEM), laser light diffraction, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gel permeation chromatography (GPC), encapsulation efficiency (EE) and in vitro drug release. Gamma-irradiation of RM-loaded microspheres did not affect EE, DSC and XRD patterns. After gamma-irradiation, changes on the surface were observed by SEM, but no significant difference in mean particle size was observed. GPC measurements showed a decrease in molecular weight of the polymer after five days of in vitro release. The similarity factor value between irradiated and non-irradiates microspheres was <50, indicating the non-similarity of the release profiles. The sterilization technique had an effect on the integrity of polymeric system, significantly affecting in vitro release of RM from PLGA microspheres. Therefore, from our results we conclude that gamma-irradiation is not a suitable sterilization procedure for this formulation

  4. Consistent inhibition of cyclooxygenase drives macrophages towards the inflammatory phenotype.

    Directory of Open Access Journals (Sweden)

    Yi Rang Na

    Full Text Available Macrophages play important roles in defense against infection, as well as in homeostasis maintenance. Thus alterations of macrophage function can have unexpected pathological results. Cyclooxygenase (COX inhibitors are widely used to relieve pain, but the effects of long-term usage on macrophage function remain to be elucidated. Using bone marrow-derived macrophage culture and long-term COX inhibitor treatments in BALB/c mice and zebrafish, we showed that chronic COX inhibition drives macrophages into an inflammatory state. Macrophages differentiated in the presence of SC-560 (COX-1 inhibitor, NS-398 (COX-2 inhibitor or indomethacin (COX-1/2 inhibitor for 7 days produced more TNFα or IL-12p70 with enhanced p65/IκB phosphoylation. YmI and IRF4 expression was reduced significantly, indicative of a more inflammatory phenotype. We further observed that indomethacin or NS-398 delivery accelerated zebrafish death rates during LPS induced sepsis. When COX inhibitors were released over 30 days from an osmotic pump implant in mice, macrophages from peritoneal cavities and adipose tissue produced more TNFα in both the basal state and under LPS stimulation. Consequently, indomethacin-exposed mice showed accelerated systemic inflammation after LPS injection. Our findings suggest that macrophages exhibit a more inflammatory phenotype when COX activities are chronically inhibited.

  5. Caffeoyl glucosides from Nandina domestica inhibit LPS-induced endothelial inflammatory responses.

    Science.gov (United States)

    Kulkarni, Roshan R; Lee, Wonhwa; Jang, Tae Su; Lee, JungIn; Kwak, Soyoung; Park, Mi Seon; Lee, Hyun-Shik; Bae, Jong-Sup; Na, MinKyun

    2015-11-15

    Endothelial dysfunction is a key pathological feature of many inflammatory diseases, including sepsis. In the present study, a new caffeoyl glucoside (1) and two known caffeoylated compounds (2 and 3) were isolated from the fruits of Nandina domestica Thunb. (Berberidaceae). The compounds were investigated for their effects against lipopolysaccharide (LPS)-mediated endothelial inflammatory responses. At 20 μM, 1 and 2 inhibited LPS-induced hyperpermeability, adhesion, and migration of leukocytes across a human endothelial cell monolayer in a dose-dependent manner suggesting that 1 and 2 may serve as potential scaffolds for the development of therapeutic agents to treat vascular inflammatory disorders. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Neuroprotection of Scutellarin is mediated by inhibition of microglial inflammatory activation.

    Science.gov (United States)

    Wang, S; Wang, H; Guo, H; Kang, L; Gao, X; Hu, L

    2011-06-30

    Inhibition of microglial over-reaction and the inflammatory processes may represent a therapeutic target to alleviate the progression of neurological diseases, such as neurodegenerative diseases and stroke. Scutellarin is the major active component of Erigeron breviscapus (Vant.) Hand-Mazz, a herbal medicine in treatment of cerebrovascular diseases for a long time in the Orient. In this study, we explored the mechanisms of neuroprotection by Scutellarin, particularly its anti-inflammatory effects in microglia. We observed that Scutellarin inhibited lipopolysaccharide (LPS)-induced production of proinflammatory mediators such as nitric oxide (NO), tumor necrosis factor α (TNFα), interleukin-1β (IL-1β) and reactive oxygen species (ROS), suppressed LPS-stimulated inducible nitric oxide synthase (iNOS), TNFα, and IL-1β mRNA expression in rat primary microglia or BV-2 mouse microglial cell line. Scutellarin inhibited LPS-induced nuclear translocation and DNA binding activity of nuclear factor κB (NF-κB). It repressed the LPS-induced c-Jun N-terminal kinase (JNK) and p38 phosphorylation without affecting the activity of extracellular signal regulated kinase (ERK) mitogen-activated protein kinase. Moreover, Scutellarin also inhibited interferon-γ (IFN-γ)-induced NO production, iNOS mRNA expression and transcription factor signal transducer and activator of transcription 1α (STAT1α) activation. Concomitantly, conditioned media from Scutellarin pretreated BV-2 cells significantly reduced neurotoxicity compared with conditioned media from LPS treated alone. Together, the present study reported the anti-inflammatory activity of Scutellarin in microglial cells along with their underlying molecular mechanisms, and suggested Scutellarin might have therapeutic potential for various microglia mediated neuroinflammation. Copyright © 2011 IBRO. Published by Elsevier Ltd. All rights reserved.

  7. A short history of anti-rheumatic therapy. III. Non steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    P. Marson

    2011-06-01

    Full Text Available The chemical advances of the 20th century led to the synthesis of non steroidal anti-inflammatory drugs (NSAIDs, beginning from phenylbutazone and indomethacin and continuing with other new drugs, including ibuprofen, diclofenac, naproxen, piroxicam and, more recently, the highly selective COX-2 inhibitors (coxibs. This progress derived from the discovery of the mechanism of action of these drugs: the inhibition of synthesis of prostaglandins due to the cycloxigenase enzyme system, according to the experimental contributions of John R. Vane.

  8. Sirtuin inhibition attenuates the production of inflammatory cytokines in lipopolysaccharide-stimulated macrophages

    Energy Technology Data Exchange (ETDEWEB)

    Fernandes, Claudia A. [Universite catholique de Louvain, Louvain Drug Research Institute (LDRI), Pharmaceutics and Drug Delivery Research Group, Brussels B-1200 (Belgium); Fievez, Laurence [University of Liege, GIGA-Research, Laboratory of Cellular and Molecular Immunology, Liege B-4000 (Belgium); Neyrinck, Audrey M.; Delzenne, Nathalie M. [Universite catholique de Louvain, LDRI, Metabolism and Nutrition Research Group, Brussels B-1200 (Belgium); Bureau, Fabrice [University of Liege, GIGA-Research, Laboratory of Cellular and Molecular Immunology, Liege B-4000 (Belgium); Vanbever, Rita, E-mail: rita.vanbever@uclouvain.be [Universite catholique de Louvain, Louvain Drug Research Institute (LDRI), Pharmaceutics and Drug Delivery Research Group, Brussels B-1200 (Belgium)

    2012-04-20

    Highlights: Black-Right-Pointing-Pointer Lipopolysaccharide-stimulated macrophages were treated with cambinol and sirtinol. Black-Right-Pointing-Pointer Cambinol and sirtinol decreased lipopolysaccharide-induced cytokines. Black-Right-Pointing-Pointer Cambinol decreased NF-{kappa}B activity but had no impact on p38 MAPK activation. Black-Right-Pointing-Pointer Sirtuins are an interesting target for the treatment of inflammatory diseases. -- Abstract: In several inflammatory conditions such as rheumatoid arthritis or sepsis, the regulatory mechanisms of inflammation are inefficient and the excessive inflammatory response leads to damage to the host. Sirtuins are class III histone deacetylases that modulate the activity of several transcription factors that are implicated in immune responses. In this study, we evaluated the impact of sirtuin inhibition on the activation of lipopolysaccharide (LPS)-stimulated J774 macrophages by assessing the production of inflammatory cytokines. The pharmacologic inhibition of sirtuins decreased the production of tumour necrosis factor-alpha (TNF-{alpha}) interleukin 6 (IL-6) and Rantes. The reduction of cytokine production was associated with decreased nuclear factor kappa B (NF-{kappa}B) activity and inhibitor kappa B alpha (I{kappa}B{alpha}) phosphorylation while no impact was observed on the phosphorylation status of p38 mitogen-activated kinase (p38 MAPK). This work shows that sirtuin pharmacologic inhibitors are a promising tool for the treatment of inflammatory conditions.

  9. Potassium humate inhibits complement activation and the production of inflammatory cytokines in vitro

    Energy Technology Data Exchange (ETDEWEB)

    van Rensburg, C.E.J.; Naude, P.J. [University of Pretoria, Pretoria (South Africa)

    2009-08-15

    The effects of brown coal derived potassium humate on lymphocyte proliferation, cytokine production and complement activation were investigated in vitro. Potassium humate increased lymphocyte proliferation of phytohaemaglutinin A (PHA) and pokeweed mitogen (PWM) stimulated mononuclear lymphocytes (MNL) in vitro from concentrations of 20 to 80 {mu} g/ml, in a dose dependant manner. On the other hand potassium humate, at 40 {mu} g/ml, significantly inhibited the release of TNF-alpha, IL-1 beta, IL-6 and IL-10 by PHA stimulated MNL. Regarding complement activation it was found that potassium humate inhibits the activation of both the alternative and classical pathways without affecting the stability of the red blood cell membranes. These results indicate that the anti-inflammatory potential of potassium humate could be partially due to the inhibition of pro-inflammatory cytokines responsible for the initiation of these reactions as well as inhibition of complement activation. The increased lymphocyte proliferation observed, might be due to increased IL-2 production as previously been documented.

  10. Structure-Based Design and Synthesis of a Small Molecule that Exhibits Anti-inflammatory Activity by Inhibition of MyD88-mediated Signaling to Bacterial Toxin Exposure.

    Science.gov (United States)

    Alam, Shahabuddin; Javor, Sacha; Degardin, Melissa; Ajami, Dariush; Rebek, Mitra; Kissner, Teri L; Waag, David M; Rebek, Julius; Saikh, Kamal U

    2015-08-01

    Both Gram-positive and Gram-negative pathogens or pathogen-derived components, such as staphylococcal enterotoxins (SEs) and endotoxin (LPS) exposure, activate MyD88-mediated pro-inflammatory cellular immunity for host defense. However, dysregulated MyD88-mediated signaling triggers exaggerated immune response that often leads to toxic shock and death. Previously, we reported a small molecule compound 1 mimicking BB-loop structure of MyD88 was capable of inhibiting pro-inflammatory response to SEB exposure in mice. In this study, we designed a dimeric structure compound 4210 covalently linked with compound 1 by a non-polar cyclohexane linker which strongly inhibited the production of pro-inflammatory cytokines in human primary cells to SEB (IC50 1-50 μm) or LPS extracted from Francisella tularensis, Escherichia coli, or Burkholderia mallei (IC50 10-200 μm). Consistent with cytokine inhibition, in a ligand-induced cell-based reporter assay, compound 4210 inhibited Burkholderia mallei or LPS-induced MyD88-mediated NF-kB-dependent expression of reporter activity (IC50 10-30 μm). Furthermore, results from a newly expressed MyD88 revealed that 4210 inhibited MyD88 dimer formation which is critical for pro-inflammatory signaling. Importantly, a single administration of compound 4210 in mice showed complete protection from lethal toxin challenge. Collectively, these results demonstrated that compound 4210 inhibits toxin-induced inflated pro-inflammatory immune signaling, thus displays a potential bacterial toxin therapeutic. © 2014 John Wiley & Sons A/S.

  11. Bilobalide, a unique constituent of Ginkgo biloba, inhibits inflammatory pain in rats.

    Science.gov (United States)

    Goldie, Michelle; Dolan, Sharron

    2013-08-01

    Standardized Ginkgo biloba extract EGb 761 has been shown to inhibit inflammatory hyperalgesia in rats; however, the mechanism of action is not known. This study set out to investigate the anti-inflammatory and analgesic potential of bilobalide, a unique G. biloba constituent, in three well-characterized models of acute inflammatory pain. The effect of oral, intraplantar or intrathecal administration of bilobalide or drug-vehicle (0.25% agar; 10% ethanol in H2O) on responses to noxious thermal and mechanical stimulation of the hindpaw, and paw oedema were assessed in adult male Wistar rats before and after intradermal hindpaw injection of carrageenan (3%; 50 μl) or capsaicin (10 μg; 50 μl) or after hindpaw incision (n=6-8/group). Oral administration of bilobalide (10-30 mg/kg) significantly inhibited thermal hyperalgesia in response to carrageenan, capsaicin and paw incision, independent of dose, with an efficacy similar to that of diclofenac. In the carrageenan model, mechanical hypersensitivity and paw oedema were also significantly reduced after treatment with bilobalide (10-30 mg/kg). Intrathecal administration of bilobalide (0.5-1 μg) inhibited carrageenan-induced thermal hyperalgesia, but had no effect on mechanical hypersensitivity or paw oedema (application≥2 μg induced adverse effects, precluding testing of higher doses). Intraplantar administration of bilobalide (30-100 μg) had no effect. These data show that bilobalide is a potent anti-inflammatory and antihyperalgesic agent, the therapeutic effects of which are mediated in part through a central site of action, and may account for the therapeutic action of the whole extract G. biloba.

  12. The antioxidants curcumin and quercetin inhibit inflammatory processes associated with arthritis.

    Science.gov (United States)

    Jackson, J K; Higo, T; Hunter, W L; Burt, H M

    2006-04-01

    Curcumin and quercetin are antioxidant molecules with anti-proliferative, anti-inflammatory and immunosuppressive activities. The objective of this study was to investigate the inhibitory activity of these agents using four assays of inflammatory aspects of arthritis. Crystal-induced neutrophil activation was measured by luminol-dependent chemiluminescence. Synoviocyte proliferation was measured by an MTS assay using HIG-82 rabbit synoviocytes in cell culture. Chondrocyte (cultured primary cells) expression of the matrix metalloproteinases collagenase and stromelysin was measured by Northern Blot analysis. Angiogenesis was measured using the chorioallantoic membrane of the chick embryo. Both agents inhibited neutrophil activation, synoviocyte proliferation and angiogenesis. Curcumin strongly inhibited collagenase and stromelysin expression at micromolar concentrations whereas quercetin had no effect in this assay. These studies suggest that curcumin and to a lesser extent quercetin may offer therapeutic potential for the treatment of crystal-induced arthritis or rheumatoid arthritis.

  13. Aloin Suppresses Lipopolysaccharide-Induced Inflammatory Response and Apoptosis by Inhibiting the Activation of NF-κB

    Directory of Open Access Journals (Sweden)

    Xuan Luo

    2018-02-01

    Full Text Available Numerous herbal-derived natural products are excellent anti-inflammatory agents. Several studies have reported that aloin, the major anthraquinone glycoside obtained from the Aloe species, exhibits anti-inflammatory activity. However, the molecular mechanism of this activity is not well understood. In this report, we found that aloin suppresses lipopolysaccharide-induced pro-inflammatory cytokine secretion and nitric oxide production, and downregulates the expression of tumor necrosis factor alpha (TNF-α, interleukin 6 (IL-6, inducible nitric oxide synthase (iNOS, and cyclooxygenase-2 (COX-2. Aloin inhibits the phosphorylation and acetylation of the NF-κB p65 subunit by suppressing the upstream kinases p38 and Msk1, preventing LPS-induced p65 translocation to the nucleus. We have also shown that aloin inhibits LPS-induced caspase-3 activation and apoptotic cell death. Collectively, these findings suggest that aloin effectively suppresses the inflammatory response, primarily through the inhibition of NF-κB signaling.

  14. Paracrine action of mesenchymal stromal cells delivered by microspheres contributes to cutaneous wound healing and prevents scar formation in mice.

    Science.gov (United States)

    Huang, Sha; Wu, Yan; Gao, Dongyun; Fu, Xiaobing

    2015-07-01

    Accumulating evidence suggests that mesenchymal stromal cells (MSCs) participate in wound healing to favor tissue regeneration and inhibit fibrotic tissue formation. However, the evidence of MSCs to suppress cutaneous scar is extremely rare, and the mechanism remains unidentified. This study aimed to demonstrate whether MSCs-as the result of their paracrine actions on damaged tissues-would accelerate wound healing and prevent cutaneous fibrosis. For efficient delivery of MSCs to skin wounds, microspheres were used to maintain MSC potency. Whether MSCs can accelerate wound healing and alleviate cutaneous fibrosis through paracrine action was investigated with the use of a Transwell co-culture system in vitro and a murine model in vivo. MSCs cultured on gelatin microspheres fully retained their cell surface marker expression profile, proliferation, differentiation and paracrine potential. Co-cultures of MSCs and fibroblasts indicated that the benefits of MSCs on suppressing fibroblast proliferation and its fibrotic behavior induced by inflammatory cytokines probably were caused by paracrine actions. Importantly, microspheres successfully delivered MSCs into wound margins and significantly accelerated wound healing and concomitantly reduced the fibrotic activities of cells within the wounds and excessive accumulation of extracellular matrix as well as the transforming growth factor-β1/transforming growth factor-β3 ratio. This study provides insight into what we believe to be a previously undescribed, multifaceted role of MSC-released protein in reducing cutaneous fibrotic formation. Paracrine action of MSCs delivered by microspheres may thus qualify as a promising strategy to enhance tissue repair and to prevent excessive fibrosis during cutaneous wound healing. Copyright © 2015 International Society for Cellular Therapy. Published by Elsevier Inc. All rights reserved.

  15. Laticifer proteins from Plumeria pudica inhibit the inflammatory and nociceptive responses by decreasing the action of inflammatory mediators and pro-inflammatory cytokines

    Directory of Open Access Journals (Sweden)

    Heliana B. Fernandes

    Full Text Available AbstractSome publications have described the pharmacological properties of latices proteins. Thus, in the present study proteins from Plumeria pudica Jacq., Apocynaceae, latex were evaluated for anti-inflammatory and antinociceptive activities. Obtained data showed that an intraperitoneal administration of different doses of latex was able to reduce the paw edema induced by carrageenan in a dose-dependent manner (better dose 40 mg/kg; 72.7% inhibition at 3rd and 78.7% at 4th hour and the edema induced by dextran (40 mg/kg; 51.5% inhibition at 30 min and 93.0% at 1st hour. Inhibition of edema induced by carrageenan was accompanied by a reduction of myeloperoxidase activity. Pre-treating animals with latex (40 mg/kg also inhibited the paw edema induced by histamine, serotonin, bradykinin, prostaglandin E2, compound 48/80. Additionally, the latex (40 mg/kg reduced the leukocyte peritoneal migration induced by carrageenan and this event was followed by reduction of IL-1β and TNF-α in peritoneal fluid. The latex-treatment (40 mg/kg reduced the animal abdominal constrictions induced by acetic acid and the first phase on paw licking model induced by formalin. When latex was treated with heat (at 100 °C for 30 min, anti-edematogenic and myeloperoxidase activities were significantly reduced, indicating the involvement of heat-sensitive proteins on anti-inflammatory effect. Our results evidence that latex fluids are a source of proteins with pharmacological properties.

  16. Intracellular degradation of microspheres based on cross-linked dextran hydrogels or amphiphilic block copolymers: A comparative Raman microscopy study

    Science.gov (United States)

    van Manen, Henk-Jan; van Apeldoorn, Aart A; Verrijk, Ruud; van Blitterswijk, Clemens A; Otto, Cees

    2007-01-01

    Micro- and nanospheres composed of biodegradable polymers show promise as versatile devices for the controlled delivery of biopharmaceuticals. Whereas important properties such as drug release profiles, biocompatibility, and (bio)degradability have been determined for many types of biodegradable particles, information about particle degradation inside phagocytic cells is usually lacking. Here, we report the use of confocal Raman microscopy to obtain chemical information about cross-linked dextran hydrogel microspheres and amphiphilic poly(ethylene glycol)-terephthalate/poly(butylene terephthalate) (PEGT/PBT) microspheres inside RAW 264.7 macrophage phagosomes. Using quantitative Raman microspectroscopy, we show that the dextran concentration inside phagocytosed dextran microspheres decreases with cell incubation time. In contrast to dextran microspheres, we did not observe PEGT/PBT microsphere degradation after 1 week of internalization by macrophages, confirming previous studies showing that dextran microsphere degradation proceeds faster than PEGT/PBT degradation. Raman microscopy further showed the conversion of macrophages to lipid-laden foam cells upon prolonged incubation with both types of microspheres, suggesting that a cellular inflammatory response is induced by these biomaterials in cell culture. Our results exemplify the power of Raman microscopy to characterize microsphere degradation in cells and offer exciting prospects for this technique as a noninvasive, label-free optical tool in biomaterials histology and tissue engineering. PMID:17722552

  17. Budesonide Inhibits Intracellular Infection with Non-Typeable Haemophilus influenzae Despite Its Anti-Inflammatory Effects in Respiratory Cells and Human Lung Tissue: A Role for p38 MAP Kinase.

    Science.gov (United States)

    Wagner, Christopher; Goldmann, Torsten; Rohmann, Kristina; Rupp, Jan; Marwitz, Sebastian; Rotta Detto Loria, Johannes; Limmer, Stefan; Zabel, Peter; Dalhoff, Klaus; Drömann, Daniel

    2015-01-01

    Inhaled corticosteroids (ICS) are widely used in the treatment of obstructive lung diseases. Recent data suggest a higher pneumonia risk in chronic obstructive pulmonary disease (COPD) patients treated with ICS. Since non-typeable Haemophilus influenzae (NTHi) is the most common pathogen associated with acute exacerbations of COPD, we investigated the effects of budesonide (BUD) on NTHi-induced inflammation and invasive infection. The alveolar epithelial cell line A549 and specimens of human lung tissue (HLT) were used in our experiments. Intracellular infection was determined by a lysis/culture assay of infected cells. Activated p38 mitogen-associated protein kinase (MAPK) was assessed using Western blotting and immunohistochemistry, expression of toll-like receptor 2 (TLR2) was determined by PCR, and CXCL-8 levels were measured using ELISA. Immunohistochemistry was used for detection of CXCL-8, platelet-activating factor receptor (PAF-R) and NTHi. BUD significantly reduced CXCL-8 secretion in A549 cells and lung tissue infected with NTHi. Furthermore, BUD decreased the expression of PAF-R in HLT and A549 cells. In A549 cells and HLT, BUD inhibited intracellular infection and - synergistically with NTHi - increased the expression of TLR2 (in A549 cells). TLR2 stimulation did not influence the intracellular infection of A549 cells, but p38 MAPK inhibition resulted in a significant reduction of infection. The present study adds new insights into the effects of glucocorticoids on pulmonary host defence after NTHi infection. Although the inflammatory response to infection is suppressed by BUD, interestingly, the intracellular infection is also inhibited. This effect seems to depend on the inhibition of p38 MAPK - a key enzyme in many pro-inflammatory pathways - as well as of PAF-R expression. © 2015 S. Karger AG, Basel.

  18. Disparate effects of non-steroidal anti-inflammatory drugs on apoptosis in guinea-pig gastric mucous cells: inhibition of basal apoptosis by diclofenac

    Science.gov (United States)

    Ashton, Miranda; Hanson, Peter J

    2002-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) induce apoptosis in gastrointestinal cancer cell lines. Similar actions on normal gastric epithelial cells could contribute to NSAID gastropathy. The present work therefore compared the actions of diclofenac, ibuprofen, indomethacin, and the cyclo-oxygenase-2 selective inhibitor, NS-398, on a primary culture of guinea-pig gastric mucous epithelial cells. Cell number was assessed by staining with crystal violet. Apoptotic activity was determined by condensation and fragmentation of nuclei and by assay of caspase-3-like activity. Necrosis was evaluated from release of cellular enzymes. Ibuprofen (250 μM for 24 h) promoted cell loss, and apoptosis, under both basal conditions and when apoptosis was increased by 25 μM N-Hexanoyl-D-sphingosine (C6-ceramide). Diclofenac (250 μM for 24 h) reduced the proportion of apoptotic nuclei from 5.2 to 2.1%, and caused inhibition of caspase-3-like activity, without causing necrosis under basal conditions. No such reduction in apoptotic activity was evident in the presence of 25 μM C6-ceramide. The inhibitory effect of diclofenac on basal caspase-3-like activity was also exhibited by the structurally similar mefenamic and flufenamic acids (1–250 μM), but not by niflumic acid. Inhibition of superoxide production by the cells increased caspase-3-like activity, but the inhibitory action of diclofenac on caspase activity remained. Diclofenac did not affect superoxide production. Diclofenac inhibited caspase-3-like activity in cell homogenates and also inhibited human recombinant caspase-3. In conclusion, NSAIDs vary in their effect on apoptotic activity in a primary culture of guinea-pig gastric mucous epithelial cells, and the inhibitory effect of diclofenac on basal apoptosis could involve an action on caspase activity. PMID:11815376

  19. Non-aqueous hybrid supercapacitors fabricated with mesoporous TiO2 microspheres and activated carbon electrodes with superior performance

    Science.gov (United States)

    Cai, Yong; Zhao, Bote; Wang, Jie; Shao, Zongping

    2014-05-01

    Mesoporous TiO2 microspheres, synthesized by a facile template-free solvothermal method and subsequent heat treatment, are exploited as the electrode for hybrid supercapacitors. The effects of the calcination temperature on the phase composition, particulate microstructure and morphology are characterized by XRD, Raman, FE-SEM and N2 adsorption/desorption measurements. Hybrid supercapacitors utilizing the as-prepared TiO2 mesoporous microspheres as the negative electrode and activated carbon (AC) as the positive electrode in a non-aqueous electrolyte are fabricated. The electrochemical performance of these hybrid supercapacitors is studied by galvanostatic charge-discharge and cyclic voltammetry (CV). The hybrid supercapacitor built from TiO2 microspheres calcined at 400 °C shows the best performance, delivering an energy density of 79.3 Wh kg-1 at a power density of 178.1 W kg-1. Even at a power density of 9.45 kW kg-1, an energy density of 31.5 Wh kg-1 is reached. These values are much higher than the AC-AC symmetric supercapacitor. In addition, the hybrid supercapacitor exhibits excellent cycling performance, retaining 98% of the initial energy density after 1000 cycles. Such outstanding electrochemical performance of the hybrid supercapacitor is attributed to the matched reaction kinetics between the two electrodes with different energy storage mechanisms.

  20. Tryptamine-gallic acid hybrid prevents non-steroidal anti-inflammatory drug-induced gastropathy: correction of mitochondrial dysfunction and inhibition of apoptosis in gastric mucosal cells.

    Science.gov (United States)

    Pal, Chinmay; Bindu, Samik; Dey, Sumanta; Alam, Athar; Goyal, Manish; Iqbal, Mohd Shameel; Sarkar, Souvik; Kumar, Rahul; Halder, Kamal Krishna; Debnath, Mita Chatterjee; Adhikari, Susanta; Bandyopadhyay, Uday

    2012-01-27

    We have investigated the gastroprotective effect of SEGA (3a), a newly synthesized tryptamine-gallic acid hybrid molecule against non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy with mechanistic details. SEGA (3a) prevents indomethacin (NSAID)-induced mitochondrial oxidative stress (MOS) and dysfunctions in gastric mucosal cells, which play a pathogenic role in inducing gastropathy. SEGA (3a) offers this mitoprotective effect by scavenging of mitochondrial superoxide anion (O(2)(·-)) and intramitochondrial free iron released as a result of MOS. SEGA (3a) in vivo blocks indomethacin-mediated MOS, as is evident from the inhibition of indomethacin-induced mitochondrial protein carbonyl formation, lipid peroxidation, and thiol depletion. SEGA (3a) corrects indomethacin-mediated mitochondrial dysfunction in vivo by restoring defective electron transport chain function, collapse of transmembrane potential, and loss of dehydrogenase activity. SEGA (3a) not only corrects mitochondrial dysfunction but also inhibits the activation of the mitochondrial pathway of apoptosis by indomethacin. SEGA (3a) inhibits indomethacin-induced down-regulation of bcl-2 and up-regulation of bax genes in gastric mucosa. SEGA (3a) also inhibits indometacin-induced activation of caspase-9 and caspase-3 in gastric mucosa. Besides the gastroprotective effect against NSAID, SEGA (3a) also expedites the healing of already damaged gastric mucosa. Radiolabeled ((99m)Tc-labeled SEGA (3a)) tracer studies confirm that SEGA (3a) enters into mitochondria of gastric mucosal cell in vivo, and it is quite stable in serum. Thus, SEGA (3a) bears an immense potential to be a novel gastroprotective agent against NSAID-induced gastropathy.

  1. P2X7 signaling promotes microsphere embolism-triggered microglia activation by maintaining elevation of Fas ligand

    Directory of Open Access Journals (Sweden)

    Lu Ying-mei

    2012-07-01

    Full Text Available Abstract Background The cerebral microvascular occlusion elicits microvascular injury which mimics the different degrees of stroke severity observed in patients, but the mechanisms underlying these embolic injuries are far from understood. The Fas ligand (FasL-Fas system has been implicated in a number of pathogenic states. Here, we examined the contribution of microglia-derived FasL to brain inflammatory injury, with a focus on the potential to suppress the FasL increase by inhibition of the P2X7-FasL signaling with pharmacological or genetic approaches during ischemia. Methods The cerebral microvascular occlusion was induced by microsphere injection in experimental animals. Morphological changes in microglial cells were studied immunohistochemically. The biochemical analyses were used to examine the intracellular changes of P2X7/FasL signaling. The BV-2 cells and primary microglia from mice genetically deficient in P2X7 were used to further establish a linkage between microglia activation and FasL overproduction. Results The FasL expression was continuously elevated and was spatiotemporally related to microglia activation following microsphere embolism. Notably, P2X7 expression concomitantly increased in microglia and presented a distribution pattern that was similar to that of FasL in ED1-positive cells at pathological process of microsphere embolism. Interestingly, FasL generation in cultured microglia cells subjected to oxygen-glucose deprivation-treated neuron-conditioned medium was prevented by the silencing of P2X7. Furthermore, FasL induced the migration of BV-2 microglia, whereas the neutralization of FasL with a blocking antibody was highly effective in inhibiting ischemia-induced microglial mobility. Similar results were observed in primary microglia from wild-type mice or mice genetically deficient in P2X7. Finally, the degrees of FasL overproduction and neuronal death were consistently reduced in P2X7−/− mice compared with wild

  2. Sargachromenol from Sargassum micracanthum Inhibits the Lipopolysaccharide-Induced Production of Inflammatory Mediators in RAW 264.7 Macrophages

    Directory of Open Access Journals (Sweden)

    Eun-Jin Yang

    2013-01-01

    Full Text Available During our ongoing screening program designed to determine the anti-inflammatory potential of natural compounds, we isolated sargachromenol from Sargassum micracanthum. In the present study, we investigated the anti-inflammatory effects of sargachromenol on lipopolysaccharide (LPS-induced inflammation in murine RAW 264.7 macrophage cells and the underlying mechanisms. Sargachromenol significantly inhibited the LPS-induced production of nitric oxide (NO and prostaglandin E2 (PGE2 in a dose-dependent manner. It also significantly inhibited the protein expression of inducible NO synthase (iNOS and cyclooxygenase-2 (COX-2 in a dose-dependent manner in LPS-stimulated macrophage cells. Further analyses showed that sargachromenol decreased the cytoplasmic loss of inhibitor κBα (IκBα protein. These results suggest that sargachromenol may exert its anti-inflammatory effects on LPS-stimulated macrophage cells by inhibiting the activation of the NF-κB signaling pathway. In conclusion, to our knowledge, this is the first study to show that sargachromenol isolated from S. micracanthum has an effective anti-inflammatory activity. Therefore, sargachromenol might be useful for cosmetic, food, or medical applications requiring anti-inflammatory properties.

  3. Fasitibant chloride, a kinin B2 receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats

    Science.gov (United States)

    Valenti, Claudio; Giuliani, Sandro; Cialdai, Cecilia; Tramontana, Manuela; Maggi, Carlo Alberto

    2012-01-01

    BACKGROUND AND PURPOSE Bradykinin, through the kinin B2 receptor, is involved in inflammatory processes related to arthropathies. B2 receptor antagonists inhibited carrageenan-induced arthritis in rats in synergy with anti-inflammatory steroids. The mechanism(s) underlying this drug interaction was investigated. EXPERIMENTAL APPROACH Drugs inhibiting inflammatory mediators released by carrageenan were injected, alone or in combination, into the knee joint of pentobarbital anaesthetized rats 30 min before intra-articular administration of carrageenan. Their effects on the carrageenan-induced inflammatory responses (joint pain, oedema and neutrophil recruitment) and release of inflammatory mediators (prostaglandins, IL-1β, IL-6 and the chemokine GRO/CINC-1), were assessed after 6 h. KEY RESULTS The combination of fasitibant chloride (MEN16132) and dexamethasone was more effective than each drug administered alone in inhibiting knee joint inflammation and release of inflammatory mediators. Fasitibant chloride, MK571, atenolol, des-Arg9-[Leu8]-bradykinin (B2 receptor, leukotriene, catecholamine and B1 receptor antagonists, respectively) and dexketoprofen (COX inhibitor), reduced joint pain and, except for the latter, also diminished joint oedema. A combination of drugs inhibiting joint pain (fasitibant chloride, des-Arg9-[Leu8]-bradykinin, dexketoprofen, MK571 and atenolol) and oedema (fasitibant chloride, des-Arg9-[Leu8]-bradykinin, MK571 and atenolol) abolished the respective inflammatory response, producing inhibition comparable with that achieved with the combination of fasitibant chloride and dexamethasone. MK571 alone was able to block neutrophil recruitment. CONCLUSIONS AND IMPLICATIONS Bradykinin-mediated inflammatory responses to intra-articular carrageenan were not controlled by steroids, which were not capable of preventing bradykinin effects either by direct activation of the B2 receptor, or through the indirect effects mediated by release of eicosanoids

  4. Metallic coating of microspheres

    International Nuclear Information System (INIS)

    Meyer, S.F.

    1980-01-01

    Extremely smooth, uniform metal coatings of micrometer thicknesses on microscopic glass spheres (microspheres) are often needed as targets for inertial confinement fusion (ICF) experiments. The first part of this paper reviews those methods used successfully to provide metal coated microspheres for ICF targets, including magnetron sputtering, electro- and electroless plating, and chemical vapor pyrolysis. The second part of this paper discusses some of the critical aspects of magnetron sputter coating of microspheres, including substrate requirements, the sticking of microspheres during coating (preventing a uniform coating), and the difficulties in growing the desired dense, smooth, uniform microstructure on continuously moving spherical substrates

  5. Anti-inflammatory activity of Odina wodier Roxb, an Indian folk remedy, through inhibition of toll-like receptor 4 signaling pathway.

    Science.gov (United States)

    Ojha, Durbadal; Mukherjee, Hemanta; Mondal, Supriya; Jena, Aditya; Dwivedi, Ved Prakash; Mondal, Keshab C; Malhotra, Bharti; Samanta, Amalesh; Chattopadhyay, Debprasad

    2014-01-01

    Inflammation is part of self-limiting non-specific immune response, which occurs during bodily injury. In some disorders the inflammatory process becomes continuous, leading to the development of chronic inflammatory diseases including cardiovascular diseases, diabetes, cancer etc. Several Indian tribes used the bark of Odina wodier (OWB) for treating inflammatory disorders. Thus, we have evaluated the immunotherapeutic potential of OWB methanol extract and its major constituent chlorogenic acid (CA), using three popular in vivo antiinflammatory models: Carrageenan- and Dextran-induced paw edema, Cotton pellet granuloma, and Acetic acid-induced vascular permeability. To elucidate the possible anti-inflammatory mechanism of action we determine the level of major inflammatory mediators (NO, iNOS, COX-2-dependent prostaglandin E2 or PGE2), and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and IL-12). Further, we determine the toll-like receptor 4 (TLR4), Myeloid differentiation primary response gene 88 (MyD88), c-Jun N-terminal kinases (JNK), nuclear factor kappa-B cells (NF-κB), and NF-kB inhibitor alpha (IK-Bα) by protein and mRNA expression, and Western blot analysis in drug treated LPS-induced murine macrophage model. Moreover, we determined the acute and sub-acute toxicity of OWB extract in BALB/c mice. Our study demonstrated a significant anti-inflammatory activity of OWB extract and CA along with the inhibition of TNF-α, IL-1β, IL-6 and IL-12 expressions. Further, the expression of TLR4, NF-κBp65, MyD88, iNOS and COX-2 molecules were reduced in drug-treated groups, but not in the LPS-stimulated untreated or control groups, Thus, our results collectively indicated that the OWB extract and CA can efficiently inhibit inflammation through the down regulation of TLR4/MyD88/NF-kB signaling pathway.

  6. Anti-inflammatory activity of Odina wodier Roxb, an Indian folk remedy, through inhibition of toll-like receptor 4 signaling pathway.

    Directory of Open Access Journals (Sweden)

    Durbadal Ojha

    Full Text Available Inflammation is part of self-limiting non-specific immune response, which occurs during bodily injury. In some disorders the inflammatory process becomes continuous, leading to the development of chronic inflammatory diseases including cardiovascular diseases, diabetes, cancer etc. Several Indian tribes used the bark of Odina wodier (OWB for treating inflammatory disorders. Thus, we have evaluated the immunotherapeutic potential of OWB methanol extract and its major constituent chlorogenic acid (CA, using three popular in vivo antiinflammatory models: Carrageenan- and Dextran-induced paw edema, Cotton pellet granuloma, and Acetic acid-induced vascular permeability. To elucidate the possible anti-inflammatory mechanism of action we determine the level of major inflammatory mediators (NO, iNOS, COX-2-dependent prostaglandin E2 or PGE2, and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and IL-12. Further, we determine the toll-like receptor 4 (TLR4, Myeloid differentiation primary response gene 88 (MyD88, c-Jun N-terminal kinases (JNK, nuclear factor kappa-B cells (NF-κB, and NF-kB inhibitor alpha (IK-Bα by protein and mRNA expression, and Western blot analysis in drug treated LPS-induced murine macrophage model. Moreover, we determined the acute and sub-acute toxicity of OWB extract in BALB/c mice. Our study demonstrated a significant anti-inflammatory activity of OWB extract and CA along with the inhibition of TNF-α, IL-1β, IL-6 and IL-12 expressions. Further, the expression of TLR4, NF-κBp65, MyD88, iNOS and COX-2 molecules were reduced in drug-treated groups, but not in the LPS-stimulated untreated or control groups, Thus, our results collectively indicated that the OWB extract and CA can efficiently inhibit inflammation through the down regulation of TLR4/MyD88/NF-kB signaling pathway.

  7. Ethanol Decreases Inflammatory Response in Human Lung Epithelial Cells by Inhibiting the Canonical NF-kB-Pathway

    Directory of Open Access Journals (Sweden)

    Katharina Mörs

    2017-08-01

    Full Text Available Background/Aims: Alcohol (ethanol, EtOH as significant contributor to traumatic injury is linked to suppressed inflammatory response, thereby influencing clinical outcomes. Alcohol-induced immune-suppression during acute inflammation (trauma was linked to nuclear factor-kappaB (NF-ĸB. Here, we analyzed alcohol`s effects and mechanisms underlying its influence on NF-ĸB-signaling during acute inflammation in human lung epithelial cells. Methods: A549-cells were stimulated with interleukin (IL-1β, or sera from trauma patients (TP or healthy volunteers, with positive/negative blood alcohol concentrations (BAC, and subsequently exposed to EtOH (170 Mm, 1h. IL-6-release and neutrophil adhesion to A549 were analyzed. Specific siRNA-NIK mediated downregulation of non-canonical, and IKK-NBD-inhibition of canonical NF-ĸB signaling were performed. Nuclear levels of activated p50 and p52 NF-ĸB-subunits were detected using TransAm ELISA. Results: Both stimuli significantly induced IL-6-release (39.79±4.70 vs. 0.58±0.8 pg/ml and neutrophil adhesion (132.30±8.80 vs. 100% control, p<0.05 to A549-cells. EtOH significantly decreased IL-6-release (22.90±5.40, p<0.05 and neutrophil adherence vs. controls (105.40±14.5%, p<0.05. IL-1β-induced significant activation of canonical/p50 and non-canonical/p52 pathways. EtOH significantly reduced p50 (34.90±23.70 vs. 197.70±36.43, p<0.05 not p52 activation. Inhibition of canonical pathway was further increased by EtOH (less p50-activation, while p52 remained unaltered. Inhibition of non-canonical pathway was unchanged by EtOH. Conclusion: Here, alcohol`s anti-inflammatory effects are mediated via decreasing nuclear levels of activated p50-subunit and canonical NF-ĸB signaling pathway.

  8. Ethanol Decreases Inflammatory Response in Human Lung Epithelial Cells by Inhibiting the Canonical NF-kB-Pathway.

    Science.gov (United States)

    Mörs, Katharina; Hörauf, Jason-Alexander; Kany, Shinwan; Wagner, Nils; Sturm, Ramona; Woschek, Mathias; Perl, Mario; Marzi, Ingo; Relja, Borna

    2017-01-01

    Alcohol (ethanol, EtOH) as significant contributor to traumatic injury is linked to suppressed inflammatory response, thereby influencing clinical outcomes. Alcohol-induced immune-suppression during acute inflammation (trauma) was linked to nuclear factor-kappaB (NF-ĸB). Here, we analyzed alcohol`s effects and mechanisms underlying its influence on NF-ĸB-signaling during acute inflammation in human lung epithelial cells. A549-cells were stimulated with interleukin (IL)-1β, or sera from trauma patients (TP) or healthy volunteers, with positive/negative blood alcohol concentrations (BAC), and subsequently exposed to EtOH (170 Mm, 1h). IL-6-release and neutrophil adhesion to A549 were analyzed. Specific siRNA-NIK mediated downregulation of non-canonical, and IKK-NBD-inhibition of canonical NF-ĸB signaling were performed. Nuclear levels of activated p50 and p52 NF-ĸB-subunits were detected using TransAm ELISA. Both stimuli significantly induced IL-6-release (39.79±4.70 vs. 0.58±0.8 pg/ml) and neutrophil adhesion (132.30±8.80 vs. 100% control, p<0.05) to A549-cells. EtOH significantly decreased IL-6-release (22.90±5.40, p<0.05) and neutrophil adherence vs. controls (105.40±14.5%, p<0.05). IL-1β-induced significant activation of canonical/p50 and non-canonical/p52 pathways. EtOH significantly reduced p50 (34.90±23.70 vs. 197.70±36.43, p<0.05) not p52 activation. Inhibition of canonical pathway was further increased by EtOH (less p50-activation), while p52 remained unaltered. Inhibition of non-canonical pathway was unchanged by EtOH. Here, alcohol`s anti-inflammatory effects are mediated via decreasing nuclear levels of activated p50-subunit and canonical NF-ĸB signaling pathway. © 2017 The Author(s). Published by S. Karger AG, Basel.

  9. Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres

    Directory of Open Access Journals (Sweden)

    Shan L

    2016-01-01

    Full Text Available Lu Shan,1 En-Xue Tao,2 Qing-Hui Meng,3 Wen-Xia Hou,3 Kang Liu,1 Hong-Cai Shang,4 Jin-Bao Tang,1 Wei-Fen Zhang1,4 1School of Pharmacy, Weifang Medical University, 2The Affiliated Hospital of Weifang Medical University, 3School of Nursing, Weifang Medical University, Weifang, 4Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing, Dongzhimen Hospital, Beijing University of Chinese Medicine, Beijing, People’s Republic of China Abstract: Cholinergic neurotransmission loss is the main cause of cognitive impairment in patients with Alzheimer’s disease. Phospholipids (PLs play an essential role in memory and learning abilities. Moreover, PLs act as a source of choline in acetylcholine synthesis. This study aimed to prepare and optimize the formulation of chitosan/phospholipid/β-cyclodextrin (CTS/PL/β-CD microspheres that can improve cognitive impairment. The CTS/PL/β-CD microspheres were prepared by spray drying, and optimized with an orthogonal design. These microspheres were also characterized in terms of morphology, structure, thermostability, drug loading, and encapsulation efficiency. The spatial learning and memory of rats were evaluated using the Morris water maze test, and the neuroprotective effects of the CTS/PL/β-CD microspheres were investigated by immunohistochemistry. Scanning electron microscopic images showed that the CTS/PL/β-CD microspheres were spherical with slightly wrinkled surfaces. Fourier transform infrared spectroscopy and differential scanning calorimetry proved that PLs formed hydrogen bonds with the amide group of CTS and the hydroxyl group of β-CD. The learning and memory abilities of rats in the treated group significantly improved compared with those in the model group. Immunohistochemical analysis revealed that treatment with the CTS/PL/β-CD microspheres attenuated the expression of protein kinase C-δ and inhibited the activation of microglias. These results suggest that the

  10. Non-steroidal anti-inflammatory drugs and cyclooxygenase in Alzheimer's disease

    NARCIS (Netherlands)

    Hoozemans, Jeroen J. M.; Veerhuis, Robert; Rozemuller, Annemieke J. M.; Eikelenboom, Piet

    2003-01-01

    Epidemiological studies indicate that anti-inflammatory drugs, especially the non-steroidal anti-inflammatory drugs (NSAIDs), decrease the risk of developing Alzheimer's disease (AD). Their beneficial effects may be due to interference in the chronic inflammatory reaction, that takes place in AD.

  11. Protection against inflammatory β-cell damage by lysine deacetylase inhibition and microRNA expression?

    DEFF Research Database (Denmark)

    Vestergaard, Anna Lindeløv; Pallesen, Emil Marek Heymans; Novotny, Guy Wayne

    Background and aims: Pro-inflammatory cytokines contribute to pancreatic β-cell apoptosis in type 1 and 2 diabetes mellitus. The detrimental effects resulting from cytokine-induced signaling in the β cell can be reduced by inhibition of class I classical lysine deacetylases (KDACi), especially HDAC...... of oxidative stress proteins responsible for β-cell death. The aim of the study is to identify novel and specific therapeutic targets for β-cell protection by mapping the miR profile of β cells rescued from inflammatory assault by inhibition of lysine deacetylation, thereby identifying miR that repress....... The perspective of this study is to develop novel anti-diabetic drugs targeting HDAC1 and/or associated miR....

  12. "Smart tattoo" glucose biosensors and effect of coencapsulated anti-inflammatory agents.

    Science.gov (United States)

    Srivastava, Rohit; Jayant, Rahul Dev; Chaudhary, Ayesha; McShane, Michael J

    2011-01-01

    Minimally invasive glucose biosensors with increased functional longevity form one of the most promising techniques for continuous glucose monitoring. In the present study, we developed a novel nanoengineered microsphere formulation comprising alginate microsphere glucose sensors and anti-inflammatory-drug-loaded alginate microspheres. The formulation was prepared and characterized for size, shape, in vitro drug release, biocompatibility, and in vivo acceptability. Glucose oxidase (GOx)- and Apo-GOx-based glucose sensors were prepared and characterized. Sensing was performed both in distilled water and simulated interstitial body fluid. Layer-by-layer self-assembly techniques were used for preventing drug and sensing chemistry release. Finally, in vivo studies, involving histopathologic examination of subcutaneous tissue surrounding the implanted sensors using Sprague-Dawley rats, were performed to test the suppression of inflammation and fibrosis associated with glucose sensor implantation. The drug formulation showed 100% drug release with in 30 days with zero-order release kinetics. The GOx-based sensors showed good enzyme retention and enzyme activity over a period of 1 month. Apo-GOx-based visible and near-infrared sensors showed good sensitivity and analytical response range of 0-50 mM glucose, with linear range up to 12 mM glucose concentration. In vitro cell line studies proved biocompatibility of the material used. Finally, both anti-inflammatory drugs were successful in controlling the implant-tissue interface by suppressing inflammation at the implant site. The incorporation of anti-inflammatory drug with glucose biosensors shows promise in improving sensor biocompatibility, thereby suggesting potential application of alginate microspheres as "smart tattoo" glucose sensors with increased functional longevity. © 2010 Diabetes Technology Society.

  13. Non-Steroidal Anti-Inflammatory Drugs, Variation in Inflammatory Genes, and Aggressive Prostate Cancer

    Directory of Open Access Journals (Sweden)

    John S. Witte

    2010-10-01

    Full Text Available Increasing evidence suggests that prostatic inflammation plays a key role in the development of prostate cancer. It remains controversial whether non-steroidal anti-inflammatory drugs (NSAIDs reduce the risk of prostate cancer. Here, we investigate how a previously reported inverse association between NSAID use and the risk of aggressive prostate cancer is modulated by variants in several inflammatory genes. We found that NSAIDs may have differential effects on prostate cancer development, depending on one’s genetic makeup. Further study of these inflammatory pathways may clarify the mechanisms through which NSAIDs impact prostate cancer risk.

  14. Mechanisms underlying the anti-inflammatory effects of Clinacanthus nutans Lindau extracts: inhibition of cytokine production and Toll-like receptor-4 activation

    Directory of Open Access Journals (Sweden)

    Chun Wai eMai

    2016-02-01

    Full Text Available Clinacanthus nutans has had a long history of use in folk medicine in Malaysia and Southeast Asia; mostly in the relief of inflammatory conditions. In this study, we investigated the effects of different extracts of C. nutans upon lipopolysaccharide (LPS induced inflammation in order to identify its mechanism of action. Extracts of leaves and stem bark of C. nutans were prepared using polar and non-polar solvents to produce four extracts, namely polar leaf extract (LP, non-polar leaf extract (LN, polar stem extract (SP and non-polar stem extracts (SN. The extracts were standardized by determining its total phenolic and total flavonoid contents. Its anti-inflammatory effects were assessed on LPS induced nitrite release in RAW264.7 macrophages and Toll-like receptor (TLR-4 activation in TLR-4 transfected human embryonic kidney cells (HEK-BlueTM-hTLR4 cells. The levels of inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-12p40 and IL-17 in treated RAW264.7 macrophages were quantified to verify its anti-inflammatory effects. Western blotting was used to investigate the effect of the most potent extract (LP on TLR-4 related inflammatory proteins (p65, p38, ERK, JNK, IRF3 in RAW264.7 macrophages. All four extracts produced a significant, concentration-dependent reduction in LPS-stimulated nitric oxide, LPS-induced TLR-4 activation in HEK-BlueTM-hTLR4 cells and LPS-stimulated cytokines production in RAW264.7 macrophages. The most potent extract, LP, also inhibited all LPS-induced TLR-4 inflammatory proteins. These results provide a basis for understanding the mechanisms underlying the previously demonstrated anti-inflammatory activity of C. nutans extracts.

  15. Polyphenolics isolated from virgin coconut oil inhibits adjuvant induced arthritis in rats through antioxidant and anti-inflammatory action.

    Science.gov (United States)

    Vysakh, A; Ratheesh, M; Rajmohanan, T P; Pramod, C; Premlal, S; Girish kumar, B; Sibi, P I

    2014-05-01

    We evaluated the protective efficacy of the polyphenolic fraction from virgin coconut oil (PV) against adjuvant induced arthritic rats. Arthritis was induced by intradermal injection of complete Freund's adjuvant. The activities of inflammatory, antioxidant enzymes and lipid peroxidation were estimated. PV showed high percentage of edema inhibition at a dose of 80mg/kg on 21st day of adjuvant arthritis and is non toxic. The expression of inflammatory genes such as COX-2, iNOS, TNF-α and IL-6 and the concentration of thiobarbituric acid reactive substance were decreased by treatment with PV. Antioxidant enzymes were increased and on treatment with PV. The increased level of total WBC count and C-reactive protein in the arthritic animals was reduced in PV treated rats. Synovial cytology showed that inflammatory cells and reactive mesothelial cells were suppressed by PV. Histopathology of paw tissue showed less edema formation and cellular infiltration on supplementation with PV. Thus the results demonstrated the potential beneficiary effect of PV on adjuvant induced arthritis in rats and the mechanism behind this action is due to its antioxidant and anti-inflammatory effects. Copyright © 2014 Elsevier B.V. All rights reserved.

  16. A Novel Anti-Inflammatory Role for Ginkgolide B in Asthma via Inhibition of the ERK/MAPK Signaling Pathway

    Directory of Open Access Journals (Sweden)

    Xiao Chu

    2011-09-01

    Full Text Available Ginkgolide B is an anti-inflammatory extract of Ginkgo biloba and has been used therapeutically. It is a known inhibitor of platelet activating factor (PAF, which is important in the pathogenesis of asthma. Here, a non-infectious mouse model of asthma is used to evaluate the anti-inflammatory capacity of ginkgolide B (GKB and characterize the interaction of GKB with the mitogen activated protein kinase (MAPK pathway. BALB/c mice that were sensitized and challenged to ovalbumin (OVA were treated with GKB (40 mg/kg one hour before they were challenged with OVA. Our study demonstrated that GKB may effectively inhibit the increase of T-helper 2 cytokines, such as interleukin (IL-5 and IL-13 in bronchoalveolar lavage fluid (BALF. Furthermore, the eosinophil count in BALF significantly decreased after treatment of GKB when compared with the OVA-challenged group. Histological studies demonstrated that GKB substantially inhibited OVA-induced eosinophilia in lung tissue and mucus hyper-secretion by goblet cells in the airway. These results suggest that ginkgolide B may be useful for the treatment of asthma and its efficacy is related to suppression of extracellular regulating kinase/MAPK pathway.

  17. Chitosan Microspheres as Radiolabeled Delivery Devices

    International Nuclear Information System (INIS)

    Permtermsin, Chalermsin; Ngamprayad, Tippanan; Phumkhem, Sudkanung; Srinuttrakul, Wannee; Kewsuwan, Prartana

    2007-08-01

    Full text: This study optimized conditions for preparing, characterizing, radiolabeled of chitosan microspheres and the biodistribution of 99mTc-Chitosan microspheres after intravenous administration. Particle size distribution of the microspheres was determined by light scattering. Zeta potential was studied by dynamic light scattering and electrophoresis technique. Biodistribution studies were performed by radiolabeling using 99mTc. The results shown that geometric mean diameter of the microspheres was found to be 77.26?1.96 ?m. Microsphere surface charge of chitosan microspheres was positive charge and zeta potential was 25.80 ? 0.46 mV. The labeling efficiency for this condition was more than 95% and under this condition was stable for at least 6 h. Radioactivity

  18. Synthesis of magnetic polymeric microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Gervald, A Yu; Gritskova, Inessa A; Prokopov, Nikolai I [M.V. Lomonosov Moscow State Academy of Fine Chemical Technology, Moscow (Russian Federation)

    2010-05-13

    The key types of magnetic polymeric microspheres are considered. Methods of synthesis of different types of magnetic nanoparticles and of preparation of stable magnetic fluids on their basis are outlined. The overview of the methods for the manufacture of magnetic polymeric microspheres is presented. The effect of the synthesis conditions on the characteristics of magnetic polymeric microspheres such as the diameter and the particle size distribution and the content of magnetic material is discussed by particular examples. The application fields of magnetic polymeric microspheres are briefly surveyed.

  19. Synthesis of magnetic polymeric microspheres

    International Nuclear Information System (INIS)

    Gervald, A Yu; Gritskova, Inessa A; Prokopov, Nikolai I

    2010-01-01

    The key types of magnetic polymeric microspheres are considered. Methods of synthesis of different types of magnetic nanoparticles and of preparation of stable magnetic fluids on their basis are outlined. The overview of the methods for the manufacture of magnetic polymeric microspheres is presented. The effect of the synthesis conditions on the characteristics of magnetic polymeric microspheres such as the diameter and the particle size distribution and the content of magnetic material is discussed by particular examples. The application fields of magnetic polymeric microspheres are briefly surveyed.

  20. Non-steroidal anti-inflammatory drugs (NSAIDs) for axial spondyloarthritis (ankylosing spondylitis and non-radiographic axial spondyloarthritis)

    NARCIS (Netherlands)

    Kroon, Feline P. B.; van der Burg, Lennart R. A.; Ramiro, Sofia; Landewé, Robert B. M.; Buchbinder, Rachelle; Falzon, Louise; van der Heijde, Désirée

    2015-01-01

    Axial spondyloarthritis (axSpA) comprises ankylosing spondylitis (radiographic axSpA) and non-radiographic (nr-)axSpA and is associated with psoriasis, uveitis and inflammatory bowel disease. Non-steroidal anti-inflammatory drugs (NSAIDs) are recommended as first-line drug treatment. To determine

  1. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2011-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  2. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2010-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  3. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2012-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  4. Preparation and In-vitro Evaluation of Metformin Microspheres Using ...

    African Journals Online (AJOL)

    . Methods: Metformin microspheres were prepared by non-aqueous solvent evaporation method using various polymers, including ethylcellulose (EC), hydroxypropyl methylcellulose (HPMC), carbopol 934P (CA) and chitosan (CH). The effect ...

  5. Retention and subsequent release of radioactivity from the incineration of wastes containing microspheres

    International Nuclear Information System (INIS)

    Emery, R.J.; Watson, J.E. Jr.

    1990-01-01

    Incineration is the preferred method for disposing of animal carcasses containing radioactive microspheres at the authors University. Routine surveys of ash from successive nonradioactive burns revealed significant contamination from previously incinerated microspheres. Past studies on microsphere incineration quantified the amount of activity retained in ash, but did not address any subsequent releases. This topic was not considered in earlier studies because, in most cases, the carcasses were placed in some type of container to facilitate recovery of ash, preventing contamination of the incinerator refractory. In this study, five sets of controlled burns were performed to quantify the subsequent releases of the microsphere radioisotopes 141 Ce, 113 Sn, 102 Ru, 95 Nb, and 46 Sc. Each set consisted of three successive burns. The first burn of each set incinerated a non-radioactive carcass, the second burn, a radioactive carcass, and the third, a non-radioactive carcass. In all of the burns, the carcasses were placed directly on the incinerator refractory floor, which is the standard procedure during normal operations

  6. Investigation of concrete mixtures incorporating hollow plastic microspheres.

    Science.gov (United States)

    1981-01-01

    This study investigated the potential of hollow plastic microspheres, HPM, for providing non-air-entrained portland cement concrete resistance to damage from cycles of freezing and thawing. In the study, a mixture with an air-entraining agent (vinsol...

  7. Non-Steroidal Anti Inflammatory Drugs Usage In Orthopaedics And ...

    African Journals Online (AJOL)

    Background: Non steroidal anti-inflammatory drugs NSAIDs) are a group of heterogeneous compounds with nti inflammatory, analgesic and often times anti pyretic roperties. They are weak organic acids and are the most commonly used drugs in Orthopaedic/Trauma practice. hey provide mild to moderate pain relief.

  8. Tabletted guar gum microspheres of piroxicam for targeted adjuvant therapy for colonic adenocarcinomas.

    Science.gov (United States)

    Vats, Anima; Pathak, Kamla

    2012-11-01

    In recent years, nonsteroidal anti-inflammatory drugs have been found to be cogent as an adjuvant therapeutic agent in mitigating colorectal cancer. Thus, this present investigation was aimed to formulate an oral, targeted tablet of piroxicam microspheres for sustained and targeted adjuvant therapy for colonic adenocarcinomas. Crosslinked guar gum microspheres of piroxicam were directly compressed into matrix tablet and coated with Eudragit S100. The optimized tablet that displayed 0% release in simulated gastric fluid, 15% in simulated intestinal fluid and 97.1% in simulated colonic fluid underwent roentgenographic study in rabbits to check its safe transit to the colon. x-ray images revealed intactness of the tablet until it reached the colon where the tablet matrix eroded. The designed, conceptual formulation emerged as potential carrier for targeted adjuvant therapy of piroxicam.

  9. Non-steroidal anti-inflammatory drug use and the risk of Parkinson's disease

    DEFF Research Database (Denmark)

    Manthripragada, Angelika D; Schernhammer, Eva S; Qiu, Jiaheng

    2011-01-01

    Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD).......Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD)....

  10. Aspirin and its related non-steroidal anti-inflammatory drugs

    African Journals Online (AJOL)

    Aspirin and its related non-steroidal anti-inflammatory drugs. Aspirin or acetylsalicylic acid has been utilised by physicians for hundreds of years as an analgesic, anti-inflammatory and antipyretic (1). Derived from plant sources, such as the willow tree, it has the ability to induce apoptosis in cancer cells and stimulate.

  11. Preparation of open porous polycaprolactone microspheres and their applications as effective cell carriers in hydrogel system

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Qingchun [Key Laboratory for Ultrafine Materials of Ministry of Education, School of Materials Science and Engineering (China); Tan, Ke; Ye, Zhaoyang [State Key Laboratory of Bioreactor Engineering, School of Bioengineering, East China University of Science and Technology, Shanghai, 200237 China (China); Zhang, Yan, E-mail: zhang_yan@ecust.edu.cn [Key Laboratory for Ultrafine Materials of Ministry of Education, School of Materials Science and Engineering (China); Tan, Wensong [State Key Laboratory of Bioreactor Engineering, School of Bioengineering, East China University of Science and Technology, Shanghai, 200237 China (China); Lang, Meidong, E-mail: mdlang@ecust.edu.cn [Key Laboratory for Ultrafine Materials of Ministry of Education, School of Materials Science and Engineering (China)

    2012-12-01

    Common hydrogel, composed of synthetic polymers or natural polysaccharides could not support the adhesion of anchorage-dependent cells due to the lack of cell affinitive interface and high cell constraint. The use of porous polyester microspheres as cell-carriers and introduction of cell-loaded microspheres into the hydrogel system might overcome the problem. However, the preparation of the open porous microsphere especially using polycaprolactone (PCL) has been rarely reported. Here, the open porous PCL microspheres were fabricated via the combined emulsion/solvent evaporation and particle leaching method. The microspheres exhibited porous surface and inter-connective pore structure. Additionally, the pore structure could be easily controlled by adjusting the processing parameters. The surface pore size could be altered from 20 {mu}m to 80 {mu}m and the internal porosities were varied from 30% to 70%. The obtained microspheres were evaluated to delivery mesenchymal stem cells (MSCs) and showed the improved cell adhesion and growth when compared with the non-porous microspheres. Then, the MSCs loaded microspheres were introduced into agarose hydrogel. MSCs remained alive and sustained proliferation in microsphere/agarose composite in 5-day incubation while a decrement of MSCs viabilities was found in agarose hydrogel without microspheres. The results indicated that the microsphere/hydrogel composite had a great potential in cell therapy and injectable system for tissue regeneration. Highlights: Black-Right-Pointing-Pointer The open porous polycaprolactone microspheres were fabricated using paraffin as a porogen. Black-Right-Pointing-Pointer The microspheres exhibited porous surface and inter-connective pore structure. Black-Right-Pointing-Pointer The surface and internal pore size and porosity of microsphere could be controlled. Black-Right-Pointing-Pointer The porous microspheres exhibited an improved cell adhesion and proliferation. Black

  12. Non-intrusive measurements of frictional forces between micro-spheres and flat surfaces

    Science.gov (United States)

    Lin, Wei-Hsun; Daraio, Chiara; Daraio's Group Team

    2014-03-01

    We report a novel, optical pump-probe experimental setup to study micro-friction phenomena between micro-particles and a flat surface. We present a case study of stainless steel microspheres, of diameter near 250 μm, in contact with different surfaces of variable roughness. In these experiments, the contact area between the particles and the substrates is only a few nanometers wide. To excite the particles, we deliver an impulse using a pulsed, high-power laser. The reaction force resulting from the surface ablation induced by the laser imparts a controlled initial velocity to the target particle. This initial velocity can be varied between 10-5 to 1 m/s. We investigate the vibrating and rolling motions of the micro-particles by detecting their velocity and displacement with a laser vibrometer and a high-speed microscope camera. We calculate the effective Hamaker constant from the vibrating motion of a particle, and study its relation to the substrate's surface roughness. We analyze the relation between rolling friction and the minimum momentum required to break surface bonding forces. This non-contact and non-intrusive technique could be employed to study a variety of contact and tribology problems at the microscale.

  13. Inhibition of Group IIA Secretory Phospholipase A2 and its Inflammatory Reactions in Mice by Ethanolic Extract of Andrographis paniculata, a Well-known Medicinal Food

    Science.gov (United States)

    Kishore, V.; Yarla, N. S.; Zameer, F.; Nagendra Prasad, M. N.; Santosh, M. S.; More, S. S.; Rao, D. G.; Dhananjaya, Bhadrapura Lakkappa

    2016-01-01

    Andrographis paniculata Nees is an important medicinal plant found in the tropical regions of the world, which has been traditionally used in Indian and Chinese medicinal systems. It is also used as medicinal food. A. paniculata is found to exhibit anti-inflammatory activities; however, its inhibitory potential on inflammatory Group IIA phospholipases A2 (PLA2) and its associated inflammatory reactions are not clearly understood. The aim of the present study is to evaluate the inhibitory/neutralizing potential of ethanolic extract of A. paniculata on the isolated inflammatory PLA2 (VRV-PL-VIIIa) from Daboii rusellii pulchella (belonging to Group IIA inflammatory secretory PLA2 [sPLA2]) and its associated edema-induced activities in Swiss albino mice. A. paniculata extract dose dependently inhibited the Group IIA sPLA2 enzymatic activity with an IC50 value of 10.3 ± 0.5 μg/ml. Further, the extract dose dependently inhibited the edema formation, when co-injected with enzyme indicating that a strong correlation exists between lipolytic and pro-inflammatory activities of the enzyme. In conclusion, results of this study shows that the ethanolic extract of A. paniculata effectively inhibits Group IIA sPLA2 and its associated inflammatory activities, which substantiate its anti-inflammatory properties. The results of the present study warranted further studies to develop bioactive compound (s) in ethanolic extract of A. paniculata as potent therapeutic agent (s) for inflammatory diseases. SUMMARY This study emphasis the anti-inflammatory effect of A. paniculata by inhibiting the inflammatory Group IIA sPLA2 and its associated inflammatory activities such as edema. It was found that there is a strong correlation between lipolytic activity and pro-inflammatory activity inhibition. Therefore, the study suggests that the extract processes potent anti-inflammatory agents, which could be developed as a potential therapeutic agent against inflammatory and related diseases

  14. Aptamer Based Microsphere Biosensor for Thrombin Detection

    Directory of Open Access Journals (Sweden)

    Xudong Fan

    2006-08-01

    Full Text Available We have developed an optical microsphere resonator biosensor using aptamer asreceptor for the measurement of the important biomolecule thrombin. The sphere surface ismodified with anti-thrombin aptamer, which has excellent binding affinity and selectivityfor thrombin. Binding of the thrombin at the sphere surface is monitored by the spectralposition of the microsphere’s whispering gallery mode resonances. A detection limit on theorder of 1 NIH Unit/mL is demonstrated. Control experiments with non-aptameroligonucleotide and BSA are also carried out to confirm the specific binding betweenaptamer and thrombin. We expect that this demonstration will lead to the development ofhighly sensitive biomarker sensors based on aptamer with lower cost and higher throughputthan current technology.

  15. PLGA/alginate composite microspheres for hydrophilic protein delivery

    International Nuclear Information System (INIS)

    Zhai, Peng; Chen, X.B.; Schreyer, David J.

    2015-01-01

    Poly(lactic-co-glycolic acid) (PLGA) microspheres and PLGA/alginate composite microspheres were prepared by a novel double emulsion and solvent evaporation technique and loaded with bovine serum albumin (BSA) or rabbit anti-laminin antibody protein. The addition of alginate and the use of a surfactant during microsphere preparation increased the encapsulation efficiency and reduced the initial burst release of hydrophilic BSA. Confocal laser scanning microcopy (CLSM) of BSA-loaded PLGA/alginate composite microspheres showed that PLGA, alginate, and BSA were distributed throughout the depths of microspheres; no core/shell structure was observed. Scanning electron microscopy revealed that PLGA microspheres erode and degrade more quickly than PLGA/alginate composite microspheres. When loaded with anti-laminin antibody, the function of released antibody was well preserved in both PLGA and PLGA/alginate composite microspheres. The biocompatibility of PLGA and PLGA/alginate microspheres were examined using four types of cultured cell lines, representing different tissue types. Cell survival was variably affected by the inclusion of alginate in composite microspheres, possibly due to the sensitivity of different cell types to excess calcium that may be released from the calcium cross-linked alginate. - Highlights: • A double emulsion technique is used to prepare protein-loaded PLGA or PLGA/alginate microspheres. • PLGA, alginate and protein are distributed evenly within microsphere structure. • Addition of alginate improves loading efficiency and slows degradation and protein release. • PLGA/alginate microspheres have favorable biocompatibility

  16. PLGA/alginate composite microspheres for hydrophilic protein delivery

    Energy Technology Data Exchange (ETDEWEB)

    Zhai, Peng [Department of Anatomy and Cell Biology, University of Saskatchewan, S7N5E5 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada); Chen, X.B. [Department of Mechanical Engineering, University of Saskatchewan, S7N5A9 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada); Schreyer, David J., E-mail: david.schreyer@usask.ca [Department of Anatomy and Cell Biology, University of Saskatchewan, S7N5E5 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada)

    2015-11-01

    Poly(lactic-co-glycolic acid) (PLGA) microspheres and PLGA/alginate composite microspheres were prepared by a novel double emulsion and solvent evaporation technique and loaded with bovine serum albumin (BSA) or rabbit anti-laminin antibody protein. The addition of alginate and the use of a surfactant during microsphere preparation increased the encapsulation efficiency and reduced the initial burst release of hydrophilic BSA. Confocal laser scanning microcopy (CLSM) of BSA-loaded PLGA/alginate composite microspheres showed that PLGA, alginate, and BSA were distributed throughout the depths of microspheres; no core/shell structure was observed. Scanning electron microscopy revealed that PLGA microspheres erode and degrade more quickly than PLGA/alginate composite microspheres. When loaded with anti-laminin antibody, the function of released antibody was well preserved in both PLGA and PLGA/alginate composite microspheres. The biocompatibility of PLGA and PLGA/alginate microspheres were examined using four types of cultured cell lines, representing different tissue types. Cell survival was variably affected by the inclusion of alginate in composite microspheres, possibly due to the sensitivity of different cell types to excess calcium that may be released from the calcium cross-linked alginate. - Highlights: • A double emulsion technique is used to prepare protein-loaded PLGA or PLGA/alginate microspheres. • PLGA, alginate and protein are distributed evenly within microsphere structure. • Addition of alginate improves loading efficiency and slows degradation and protein release. • PLGA/alginate microspheres have favorable biocompatibility.

  17. One pot synthesis of Ag nanoparticle modified ZnO microspheres in ethylene glycol medium and their enhanced photocatalytic performance

    International Nuclear Information System (INIS)

    Tian Chungui; Li Wei; Pan Kai; Zhang Qi; Tian Guohui; Zhou Wei; Fu Honggang

    2010-01-01

    Ag nanoparticles (NPs) modified ZnO microspheres (Ag/ZnO microspheres) were prepared by a facile one pot strategy in ethylene glycol (EG) medium. The EG played two important roles in the synthesis: it could act as a reaction media for the formation of ZnO and reduce Ag + to Ag 0 . A series of the characterizations indicated the successful combination of Ag NPs with ZnO microspheres. It was shown that Ag modification could greatly enhance the photocatalytic efficiency of ZnO microspheres by taking the photodegradation of Rhodamine B as a model reaction. With appropriate ratio of Ag and ZnO, Ag/ZnO microspheres showed the better photocatalytic performance than commercial Degussa P-25 TiO 2 . Photoluminescence and surface photovoltage spectra demonstrated that Ag modification could effectively inhibit the recombination of the photoinduced electron and holes of ZnO. This is responsible for the higher photocatalytic activity of Ag/ZnO composites. -- Graphical abstract: A 'one-pot' strategy was developed for preparing the Ag/ZnO microspheres in ethylene glycol. The composites exhibited superior photocatalytic performance for photodegradation of Rhodamine B dye in water. Display Omitted

  18. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1994-04-20

    New, high-strength, hollow, glass microspheres filled with pressurized hydrogen exhibit storage densities which make them attractive for bulk hydrogen storage and transport. The hoop stress at failure of our engineered glass microspheres is about 150,000 psi, permitting a three-fold increase in pressure limit and storage capacity above commercial microspheres, which fail at wall stresses of 50,000 psi. For this project, microsphere material and structure will be optimized for storage capacity and charge/discharge kinetics to improve their commercial practicality. Microsphere production scale up will be performed, directed towards large-scale commercial use. Our analysis relating glass microspheres for hydrogen transport with infrastructure and economics` indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as hydride beds, cryocarbons and pressurized tube transports. For microspheres made from advanced materials and processes, analysis will also be performed to identify the appropriate applications of the microspheres considering property variables, and different hydrogen infrastructure, end use, production and market scenarios. This report presents some of the recent modelling results for large beds of glass microspheres in hydrogen storage applications. It includes plans for experiments to identify the properties relevant to large-bed hydrogen transport and storage applications, of the best, currently producible, glass microspheres. This work began in March, 1994. Project successes will be manifest in the matching of cur-rent glass microspheres with a useful application in hydrogen bulk transport and storage, and in developing microsphere materials and processes that increase the storage density and reduce the storage energy requirement.

  19. Temperature influence in crystallinity of polymer microspheres

    International Nuclear Information System (INIS)

    Rezende, Cristiane de P.; Novack, Katia M.

    2011-01-01

    Drug delivery technology is evolving through the creation of new techniques of drug delivery effectively. The new methods used in drugs administration are based in microencapsulation process. Microsphere encapsulation modifies drug delivery bringing benefits and efficiency. In this work has been evaluated the influence of temperature in microspheres preparation. Microspheres were obtained by PMMA-co-PEG (COP) copolymer with indomethacin inserted in polymer matrix. Samples were characterized by SEM, DSC and XRD. SEM micrographs confirmed the formation of different sizes of microspheres and it was verified that higher temperatures make more crystalline microspheres. (author)

  20. Fabrication of Alkoxyamine-Functionalized Magnetic Core-Shell Microspheres via Reflux Precipitation Polymerization for Glycopeptide Enrichment

    Directory of Open Access Journals (Sweden)

    Meng Yu

    2016-03-01

    Full Text Available As a facile method to prepare hydrophilic polymeric microspheres, reflux precipitation polymerization has been widely used for preparation of polymer nanogels. In this article, we synthesized a phthalamide-protected N-aminooxy methyl acrylamide (NAMAm-p for preparation of alkoxyamine-functionalized polymer composite microspheres via reflux precipitation polymerization. The particle size and functional group density of the composite microspheres could be adjusted by copolymerization with the second monomers, N-isopropyl acrylamide, acrylic acid or 2-hydroxyethyl methacrylate. The resultant microspheres have been characterized by TEM, FT-IR, TGA and DLS. The experimental results showed that the alkoxyamine group density of the microspheres could reach as high as 1.49 mmol/g, and these groups showed a great reactivity with ketone/aldehyde compounds. With the aid of magnetic core, the hybrid microspheres could capture and magnetically isolate glycopeptides from the digested mixture of glycopeptides and non-glycopeptides at a 1:100 molar ratio. After that, we applied the composite microspheres to profile the glycol-proteome of a normal human serum sample, 95 unique glycopeptides and 64 glycoproteins were identified with these enrichment substrates in a 5 μL of serum sample.

  1. Dimethyl ester of bilirubin exhibits anti-inflammatory activity through inhibition of secretory phospholipase A2, lipoxygenase and cyclooxygenase.

    Science.gov (United States)

    Joshi, Vikram; Umashankara, M; Ramakrishnan, Chandrasekaran; Nanjaraj Urs, Ankanahalli N; Suvilesh, Kanve Nagaraj; Velmurugan, Devadasan; Rangappa, Kanchugarakoppal S; Vishwanath, Bannikuppe Sannanaik

    2016-05-15

    Overproduction of arachidonic acid (AA) mediated by secretory phospholipase A2 group IIA (sPLA2IIA) is a hallmark of many inflammatory disorders. AA is subsequently converted into pro-inflammatory eicosanoids through 5-lipoxygenase (5-LOX) and cyclooxygenase-1/2 (COX-1/2) activities. Hence, inhibition of sPLA2IIA, 5-LOX and COX-1/2 activities is critical in regulating inflammation. We have previously reported unconjugated bilirubin (UCB), an endogenous antioxidant, as sPLA2IIA inhibitor. However, lipophilic UCB gets conjugated in liver with glucuronic acid into hydrophilic conjugated bilirubin (CB). Since hydrophobicity is pre-requisite for sPLA2IIA inhibition, conjugation reduces the efficacy of UCB. In this regard, UCB was chemically modified and derivatives were evaluated for sPLA2IIA, 5-LOX and COX-1/2 inhibition. Among the derivatives, BD1 (dimethyl ester of bilirubin) exhibited ∼ 3 fold greater inhibitory potency towards sPLA2IIA compared to UCB. Both UCB and BD1 inhibited human 5-LOX and COX-2 activities; however only BD1 inhibited AA induced platelet aggregation. Molecular docking studies demonstrated BD1 as better inhibitor of aforesaid enzymes than UCB and other endogenous antioxidants. These data suggest that BD1 exhibits strong anti-inflammatory activity through inhibition of AA cascade enzymes which is of great therapeutic importance. Copyright © 2016 Elsevier Inc. All rights reserved.

  2. Encapsulation of naproxen in lipid-based matrix microspheres: characterization and release kinetics.

    Science.gov (United States)

    Bhoyar, P K; Morani, D O; Biyani, D M; Umekar, M J; Mahure, J G; Amgaonkar, Y M

    2011-04-01

    The objective of this study was to microencapsulate the anti-inflammatory drug (naproxen) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. Naproxen was microencapsulated with lipid-like carnauba wax, hydrogenated castor oil using modified melt dispersion (modified congealable disperse phase encapsulation) technique. Effect of various formulation and process variables such as drug-lipid ratio, concentration of modifier, concentration of dispersant, stirring speed, stirring time, temperature of external phase, on evaluatory parameters such as size, entrapment efficiency, and in vitro release of naproxen were studied. The microspheres were characterized for particle size, scanning electron microscopy (SEM), FT-IR spectroscopy, drug entrapment efficiency, in vitro release studies, for in vitro release kinetics. The shape of microspheres was found to be spherical by SEM. The drug entrapment efficiency of various batches of microspheres was found to be ranging from 60 to 90 %w/w. In vitro drug release studies were carried out up to 24 h in pH 7.4 phosphate buffer showing 50-65% drug release. In vitro drug release from all the batches showed better fitting with the Korsmeyer-Peppas model, indicating the possible mechanism of drug release to be by diffusion and erosion of the lipid matrix.

  3. Outstanding Anti-inflammatory Potential of Selected Asteraceae Species through the Potent Dual Inhibition of Cyclooxygenase-1 and 5-Lipoxygenase.

    Science.gov (United States)

    Chagas-Paula, Daniela Aparecida; Oliveira, Tiago Branquinho; Faleiro, Danniela Príscylla Vasconcelos; Oliveira, Rejane Barbosa; Costa, Fernando Batista Da

    2015-09-01

    Cyclooxygenase and 5-lipoxygenase are enzymes that catalyze important inflammatory pathways, suggesting that dual cyclooxygenase/lipoxygenase inhibitors should be more efficacious as anti-inflammatory medicines with lower side effects than the currently available nonsteroidal anti-inflammatory drugs. Many plants from the family Asteraceae have anti-inflammatory activities, which could be exerted by inhibiting the cyclooxygenase-1 and 5-lipoxygenase enzymes. Nevertheless, only a small number of compounds from this family have been directly evaluated for their ability to inhibit the enzymes in cell-free assays. Therefore, this study systematically evaluated 57 Asteraceae extracts in vitro in enzyme activity experiments to determine whether any of these extracts exhibit dual inhibition of cyclooxygenase-1 and 5-lipoxygenase. The chemical profiles of the extracts were obtained by the high-performance liquid chromatography-ultraviolet-diode array detector method, and their major constituents were dereplicated. Of the 57 tested extracts, 13 (26.6 %, IC50 range from 0.03-36.2 µg/mL) of them displayed dual inhibition. Extracts from known anti-inflammatory herbs, food plants, and previously uninvestigated species are among the most active. Additionally, the extract action was found to be specific with IC50 values close to or below those of the standard inhibitors. Thus, the active extracts and active substances of these species are potent inhibitors acting through the mechanism of dual inhibition of cyclooxygenase-1 and 5-lipoxygenase. The extracts were prepared for this study using nontoxic extraction solvents (EtOH-H2O), requiring only a small amount of plant material to carry out the bioassays and the phytochemical analyses. In summary, this study demonstrated the potential of the investigated species as dual inhibitors, revealing their potential as pharmaceuticals or nutraceuticals. Georg Thieme Verlag KG Stuttgart · New York.

  4. Neostigmine interactions with non steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Miranda, Hugo F; Sierralta, Fernando; Pinardi, Gianni

    2002-04-01

    1. The common mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs) is the inhibition of the enzyme cyclo-oxygenase (COX), however, this inhibition is not enough to completely account for the efficacy of these agents in several models of acute pain. 2. It has been demonstrated that cholinergic agents can induce antinociception, but the nature of the interaction between these agents and NSAIDs drugs has not been studied. The present work evaluates, by isobolographic analysis, the interactions between the cholinergic indirect agonist neostigmine (NEO) and NSAIDs drugs, using a chemical algesiometric test. 3. Intraperitoneal (i.p.) or intrathecal (i.t.) administration of NEO and of the different NSAIDs produced dose-dependent antinociception in the acetic acid writhing test of the mouse. 4. The i.p. or i.t. co-administration of fixed ratios of ED(50) fractions of NSAIDs and NEO, resulted to be synergistic or supra-additive for the combinations ketoprofen (KETO) and NEO, paracetamol (PARA) and NEO) and diclofenac (DICLO) and NEO administered i.p. However, the same combinations administered i.t. were only additive. In addition, the combinations meloxicam (MELO) and NEO and piroxicam (PIRO) and NEO, administered either i.p. or i.t., were additive. 5. The results suggest that the co-administration of NEO with some NSAIDs (e.g. KETO, PARA or DICLO) resulted in a synergistic interaction, which may provide evidence of supraspinal antinociception modulation by the increased acetylcholine concentration in the synaptic cleft of cholinergic interneurons. The interaction obtained between neostigmine and the NSAIDs could carry important clinical implications.

  5. Processing and Characterization of Sol-Gel Cerium Oxide Microspheres

    Energy Technology Data Exchange (ETDEWEB)

    McClure, Zachary D. [Pacific Northwest National Lab. (PNNL), Richland, WA (United States); Padilla Cintron, Cristina [Pacific Northwest National Lab. (PNNL), Richland, WA (United States)

    2016-09-27

    Of interest to space exploration and power generation, Radioisotope Thermoelectric Generators (RTGs) can provide long-term power to remote electronic systems without the need for refueling or replacement. Plutonium-238 (Pu-238) remains one of the more promising materials for thermoelectric power generation due to its high power density, long half-life, and low gamma emissions. Traditional methods for processing Pu-238 include ball milling irregular precipitated powders before pressing and sintering into a dense pellet. The resulting submicron particulates of Pu-238 quickly accumulate and contaminate glove boxes. An alternative and dust-free method for Pu-238 processing is internal gelation via sol-gel techniques. Sol-gel methodology creates monodisperse and uniform microspheres that can be packed and pressed into a pellet. For this study cerium oxide microspheres were produced as a surrogate to Pu-238. The similar electronic orbitals between cerium and plutonium make cerium an ideal choice for non-radioactive work. Before the microspheres can be sintered and pressed they must be washed to remove the processing oil and any unreacted substituents. An investigation was performed on the washing step to find an appropriate wash solution that reduced waste and flammable risk. Cerium oxide microspheres were processed, washed, and characterized to determine the effectiveness of the new wash solution.

  6. Cephradin-plaga microspheres for sustained delivery to cattle.

    Science.gov (United States)

    Ustariz-Peyret, C; Coudane, J; Vert, M; Kaltsatos, V; Boisramé, B

    1999-01-01

    In the field of controlled drug delivery, most of the reported work is aimed at introducing new systems, or at providing basic information on the critical parameters which affect release profiles in vitro and occasionally in vivo. The situation is totally different when one wants to fulfil the specific requirements imposed by the marketing of a sustained release device to be used in humans or in animals eaten by human beings. The control of the release characteristics is then a difficult challenge. In this work, attempts were made to combine cephradin, a hydrophilic beta-lactam antibiotic, and bioresorbable polymeric matrices of a poly(alpha-hydroxy acid) in the form of microspheres with the aim of delivering the antibiotic to cattle at a dose rate of 4-5 mg/kg/day over a 3-4 days period after i.m. injection. PLAGA aliphatic polyesters were selected because they are already FDA approved as matrices. The solvent evaporation technique using PVA as the emulsion stabilizer was selected because it is efficient and can be extended to an industrial scale. Various experimental conditions were used in order to obtain the highest encapsulation yields compatible with the desired specifications. Decreasing the volume of the aqueous phase and adding a water-miscible organic solvent/non-solvent of cephradin failed. In contrast, microspheres containing up to 30% cephradin were prepared after addition of sodium chloride to the aqueous dispersing phase. The amount of entrapped drug was raised to 40% by decreasing the temperature and the pressure. Preliminary investigations using dogs showed that 20% cephradin microspheres prepared under these conditions extended the presence of cephradin in the blood circulation up to 48 h. Increasing the load led to higher blood concentrations but shorter sustained release. The fact that the microspheres were for cattle limited the volume of the injection and thus the amount of microspheres to be administered. The other limiting factors were

  7. Microsphere-aided optical microscopy and its applications for super-resolution imaging

    Science.gov (United States)

    Upputuri, Paul Kumar; Pramanik, Manojit

    2017-12-01

    The spatial resolution of a standard optical microscope (SOM) is limited by diffraction. In visible spectrum, SOM can provide ∼ 200 nm resolution. To break the diffraction limit several approaches were developed including scanning near field microscopy, metamaterial super-lenses, nanoscale solid immersion lenses, super-oscillatory lenses, confocal fluorescence microscopy, techniques that exploit non-linear response of fluorophores like stimulated emission depletion microscopy, stochastic optical reconstruction microscopy, etc. Recently, photonic nanojet generated by a dielectric microsphere was used to break the diffraction limit. The microsphere-approach is simple, cost-effective and can be implemented under a standard microscope, hence it has gained enormous attention for super-resolution imaging. In this article, we briefly review the microsphere approach and its applications for super-resolution imaging in various optical imaging modalities.

  8. Microspheres for protein delivery prepared from amphiphilic multiblock copolymers. 1. Influence of preparation techniques on particle characteristics and protein delivery.

    Science.gov (United States)

    Bezemer, J M; Radersma, R; Grijpma, D W; Dijkstra, P J; van Blitterswijk, C A; Feijen, J

    2000-07-03

    The entrapment of lysozyme in amphiphilic multiblock copolymer microspheres by emulsification and subsequent solvent removal processes was studied. The copolymers are composed of hydrophilic poly(ethylene glycol) (PEG) blocks and hydrophobic poly(butylene terephthalate) (PBT) blocks. Direct solvent extraction from a water-in-oil (w/o) emulsion in ethanol or methanol did not result in the formation of microspheres, due to massive polymer precipitation caused by rapid solvent extraction in these non-solvents. In a second process, microspheres were first prepared by a water-in-oil-in-water (w/o/w) emulsion system with 4% poly(vinyl alcohol) (PVA) as stabilizer in the external phase, followed by extraction of the remaining solvent. As non-solvents ethanol, methanol and mixtures of methanol and water were employed. However, the use of alcohols in the extraction medium resulted in microspheres which gave an incomplete lysozyme release at a non-constant rate. Complete lysozyme release was obtained from microspheres prepared by an emulsification-solvent evaporation method in PBS containing poly(vinyl pyrrolidone) (PVP) or PVA as stabilizer. PVA was most effective in stabilizing the w/o/w emulsion. Perfectly spherical microspheres were produced, with high protein entrapment efficiencies. These microspheres released lysozyme at an almost constant rate for approximately 28 days. The reproducibility of the w/o/w emulsion process was demonstrated by comparing particle characteristics and release profiles of three batches, prepared under similar conditions.

  9. Vaccinium bracteatum Thunb. Exerts Anti-Inflammatory Activity by Inhibiting NF-κB Activation in BV-2 Microglial Cells.

    Science.gov (United States)

    Kwon, Seung-Hwan; Ma, Shi-Xun; Ko, Yong-Hyun; Seo, Jee-Yeon; Lee, Bo-Ram; Lee, Taek Hwan; Kim, Sun Yeou; Lee, Seok-Yong; Jang, Choon-Gon

    2016-09-01

    This study was designed to evaluate the pharmacological effects of Vaccinium bracteatum Thunb. methanol extract (VBME) on microglial activation and to identify the underlying mechanisms of action of these effects. The anti-inflammatory properties of VBME were studied using lipopolysaccharide (LPS)-stimulated BV-2 microglial cells. We measured the production of nitric oxide (NO), inducible NO synthase (iNOS), cyclooxygenase (COX)-2, prostaglandin E₂ (PGE₂), tumor necrosis factor-alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) as inflammatory parameters. We also examined the effect of VBME on intracellular reactive oxygen species (ROS) production and the activity of nuclear factor-kappa B p65 (NF-κB p65). VBME significantly inhibited LPS-induced production of NO and PGE2 and LPS-mediated upregulation of iNOS and COX-2 expression in a dose-dependent manner; importantly, VBME was not cytotoxic. VBME also significantly reduced the generation of the pro-inflammatory cytokines TNF-α, IL-1β, and IL-6. In addition, VBME significantly dampened intracellular ROS production and suppressed NF-κB p65 translocation by blocking IκB-α phosphorylation and degradation in LPS-stimulated BV2 cells. Our findings indicate that VBME inhibits the production of inflammatory mediators in BV-2 microglial cells by suppressing NF-κB signaling. Thus, VBME may be useful in the treatment of neurodegenerative diseases due to its ability to inhibit inflammatory mediator production in activated BV-2 microglial cells.

  10. A novel route for synthesis and growth formation of metal oxides microspheres: Insights from V_2O_3 microspheres

    International Nuclear Information System (INIS)

    Zhang, Yifu; Huang, Chi; Meng, Changgong; Hu, Tao

    2016-01-01

    Highly polydisperse V_2O_3 solid microspheres with large specific surface area were successfully synthesized via a facile hydrothermal decomposition of VOC_2O_4 solution. The morphology and composition were characterized by scanning electron microscopy (SEM), Energy dispersive spectrometer (EDS), X-ray photoelectron spectroscopy (XPS) and X-ray diffraction (XRD). V_2O_3 microspheres display an obvious Mott phase transition at −128.5 °C (cooling curve) and −114.5 °C (heating curve). Some parameters including the reaction temperature, concentration of VOC_2O_4, reaction time, surfactant, H_2C_2O_4 and precursor were briefly discussed to reveal the formation of V_2O_3 microspheres. It was found that the precursor is crucial for the fabrication of microsphere. A self-assembly growth mechanism was suggested to explain the growth process of microspheres and the autogenic CO and CO_2 gas served as the soft templates. Furthermore, this route was developed to synthesize different metal oxides microspheres, and it was found that AlO(OH), Fe_3O_4, Fe_2O_3, Co_3O_4, Cr_2O_3, MoO_2 and WO_3 microspheres were obtained. All the results showed this process was successfully explored as a methodology to synthesize different metal oxides microspheres using the gas as the templates by this facile hydrothermal route. - Highlights: • Highly uniform V_2O_3 solid microspheres were synthesized. • V_2O_3 microspheres display an obvious Mott phase transition. • The autogenic CO and CO_2 gas served as the soft templates for designed synthesis. • AlO(OH), Fe_3O_4, Fe_2O_3, Co_3O_4, Cr_2O_3, MoO_2 and WO_3 microspheres were obtained. • A methodology to synthesize different metal oxides microspheres was developed.

  11. Fenoterol inhibits LPS-induced AMPK activation and inflammatory cytokine production through β-arrestin-2 in THP-1 cell line

    International Nuclear Information System (INIS)

    Wang, Wei; Zhang, Yuan; Xu, Ming; Zhang, You-Yi; He, Bei

    2015-01-01

    The AMP-activated protein kinase (AMPK) pathway is involved in regulating inflammation in several cell lines. We reported that fenoterol, a β 2 -adrenergic receptor (β 2 -AR) agonist, had anti-inflammatory effects in THP-1 cells, a monocytic cell line. Whether the fenoterol anti-inflammatory effect involves the AMPK pathway is unknown. In this study, we explored the mechanism of β 2 -AR stimulation with fenoterol in a lipopolysaccharide (LPS)-induced inflammatory cytokine secretion in THP-1 cells. We studied whether fenoterol and β-arrestin-2 or AMPKα1 subunit knockdown could affect LPS-induced AMPK activation, nuclear factor-kappa B (NF-κB) activation and inflammatory cytokine secretion. LPS-induced AMPK activation and interleukin 1β (IL-1β) release were reduced with fenoterol pretreatment of THP-1 cells. SiRNA knockdown of β-arrestin-2 abolished the fenoterol inhibition of LPS-induced AMPK activation and interleukin 1β (IL-1β) release, thus β-arrestin-2 mediated the anti-inflammatory effects of fenoterol on LPS-treated THP-1 cells. In addition, siRNA knockdown of AMPKα1 significantly attenuated the LPS-induced NF-κB activation and IL-1β release, so AMPKα1 was a key signaling molecule involved in LPS-induced inflammatory cytokine production. These results suggested the β 2 -AR agonist fenoterol inhibited LPS-induced AMPK activation and IL-1β release via β-arrestin-2 in THP-1 cells. The exploration of these mechanisms may help optimize therapeutic agents targeting these pathways in inflammatory diseases. - Highlights: • β 2 -AR agonist fenoterol exerts its protective effect on LPS-treated THP-1 cells. • Fenoterol inhibits LPS-induced AMPK activation and IL-1β production. • β-arrestin2 mediates fenoterol-inhibited AMPK activation and IL-1β release. • AMPKα1 is involved in LPS-induced NF-κB activation and IL-1β production

  12. Fenoterol inhibits LPS-induced AMPK activation and inflammatory cytokine production through β-arrestin-2 in THP-1 cell line

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Wei [Department of Respiratory Medicine, Peking University Third Hospital, Beijing (China); Department of Infectious Diseases, Peking University Third Hospital, Beijing (China); Zhang, Yuan [Department of Respiratory Medicine, Peking University Third Hospital, Beijing (China); Xu, Ming; Zhang, You-Yi [Department of Institute of Vascular Medicine and Beijing Key Laboratory of Cardiovascular Receptors Research, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides, Peking University Third Hospital, Beijing (China); He, Bei, E-mail: puh3_hb@bjmu.edu.cn [Department of Respiratory Medicine, Peking University Third Hospital, Beijing (China)

    2015-06-26

    The AMP-activated protein kinase (AMPK) pathway is involved in regulating inflammation in several cell lines. We reported that fenoterol, a β{sub 2}-adrenergic receptor (β{sub 2}-AR) agonist, had anti-inflammatory effects in THP-1 cells, a monocytic cell line. Whether the fenoterol anti-inflammatory effect involves the AMPK pathway is unknown. In this study, we explored the mechanism of β{sub 2}-AR stimulation with fenoterol in a lipopolysaccharide (LPS)-induced inflammatory cytokine secretion in THP-1 cells. We studied whether fenoterol and β-arrestin-2 or AMPKα1 subunit knockdown could affect LPS-induced AMPK activation, nuclear factor-kappa B (NF-κB) activation and inflammatory cytokine secretion. LPS-induced AMPK activation and interleukin 1β (IL-1β) release were reduced with fenoterol pretreatment of THP-1 cells. SiRNA knockdown of β-arrestin-2 abolished the fenoterol inhibition of LPS-induced AMPK activation and interleukin 1β (IL-1β) release, thus β-arrestin-2 mediated the anti-inflammatory effects of fenoterol on LPS-treated THP-1 cells. In addition, siRNA knockdown of AMPKα1 significantly attenuated the LPS-induced NF-κB activation and IL-1β release, so AMPKα1 was a key signaling molecule involved in LPS-induced inflammatory cytokine production. These results suggested the β{sub 2}-AR agonist fenoterol inhibited LPS-induced AMPK activation and IL-1β release via β-arrestin-2 in THP-1 cells. The exploration of these mechanisms may help optimize therapeutic agents targeting these pathways in inflammatory diseases. - Highlights: • β{sub 2}-AR agonist fenoterol exerts its protective effect on LPS-treated THP-1 cells. • Fenoterol inhibits LPS-induced AMPK activation and IL-1β production. • β-arrestin2 mediates fenoterol-inhibited AMPK activation and IL-1β release. • AMPKα1 is involved in LPS-induced NF-κB activation and IL-1β production.

  13. Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

    Directory of Open Access Journals (Sweden)

    Marta Szekalska

    2016-01-01

    Full Text Available Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9 with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1 and different sodium alginate concentration (1%, 2%, and 3% were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree. In vitro drug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution. Based on glucose uptake in Saccharomyces cerevisiae cells and α-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluated in vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

  14. Application of magnetic poly(styrene-glycidyl methacrylate) microspheres for immunomagnetic separation of bone marrow cells

    Energy Technology Data Exchange (ETDEWEB)

    Chung, T.-H.; Chang, J.-Y. [Department of Chemical Engineering, National Chung Cheng University, Chiayi 621, Taiwan (China); Lee, W.-C. [Department of Chemical Engineering, National Chung Cheng University, Chiayi 621, Taiwan (China)], E-mail: chmwcl@ccu.edu.tw

    2009-05-15

    Surface-functionalized magnetic poly(styrene-glycidyl methacrylate) (PS-GMA) microspheres were prepared and coupled with Sca-1 antibody for cell selection from murine bone marrow mononuclear cells (MNCs). Biotinylated Sca-1 antibody could be directly coupled to avidin-bound magnetic microspheres. Alternatively, oxidized goat anti-mouse antibody was covalently bound onto the amino group-containing magnetic microspheres in a site-directed manner, and the resultant conjugate was coupled with non-modified Sca-1 antibody. Using the indirect antibody-bound magnetic microspheres, the purity of isolated Sca-1{sup +} cells increased with bead-to-cell ratio. Using a bead-to-cell ratio of 10 beads/cell, a purity of 85% Sca-1{sup +} cells corresponding to a 17-fold enrichment was achieved.

  15. Magnetic susceptibility characterisation of superparamagnetic microspheres

    Science.gov (United States)

    Grob, David Tim; Wise, Naomi; Oduwole, Olayinka; Sheard, Steve

    2018-04-01

    The separation of magnetic materials in microsystems using magnetophoresis has increased in popularity. The wide variety and availability of magnetic beads has fuelled this drive. It is important to know the magnetic characteristics of the microspheres in order to accurately use them in separation processes integrated on a lab-on-a-chip device. To investigate the magnetic susceptibility of magnetic microspheres, the magnetic responsiveness of three types of Dynabeads microspheres were tested using two different approaches. The magnetophoretic mobility of individual microspheres is studied using a particle tracking system and the magnetization of each type of Dynabeads microsphere is measured using SQUID relaxometry. The magnetic beads' susceptibility is obtained at four different applied magnetic fields in the range of 38-70 mT for both the mobility and SQUID measurements. The susceptibility values in both approaches show a consistent magnetic field dependence.

  16. Royal Jelly Inhibits Pseudomonas aeruginosa Adherence and Reduces Excessive Inflammatory Responses in Human Epithelial Cells

    Directory of Open Access Journals (Sweden)

    Heni Susilowati

    2017-01-01

    Full Text Available Pseudomonas aeruginosa is a Gram-negative bacterium and causes respiratory infection especially in elderly patients. Royal jelly has been used worldwide as a traditional remedy and as a nutrient; however, the effect against P. aeruginosa is unclear. The aim of this study was to analyze antibacterial, antiadherent, and anti-inflammatory effects of royal jelly against P. aeruginosa. Wild-type strain PAO1 and clinical isolates of P. aeruginosa were used for antibacterial assay and antiadherent assay to abiotic surface and epithelial cells, which are pharynx (Detroit 562 and lung (NCI-H292 epithelial cells. In anti-inflammatory assay, epithelial cells were pretreated with royal jelly before bacterial exposure to investigate its inhibitory effect on interleukin (IL-8 and macrophage inflammatory protein-3α/CCL20 overproduction. Although royal jelly did not have antibacterial activity at concentration of 50% w/v, antiadherent activity was confirmed on the abiotic surface and epithelial cells under concentration of 25%. Pretreatment with royal jelly significantly inhibited overproduction of IL-8 and CCL20 from both cells. These results demonstrated that royal jelly inhibits P. aeruginosa adherence and protects epithelial cells from excessive inflammatory responses against P. aeruginosa infection. Our findings suggested that royal jelly may be a useful supplement as complementary and alternative medicine for preventing respiratory infection caused by P. aeruginosa.

  17. Method for sizing hollow microspheres

    Science.gov (United States)

    Farnum, E.H.; Fries, R.J.

    1975-10-29

    Hollow Microspheres may be effectively sized by placing them beneath a screen stack completely immersed in an ultrasonic bath containing a liquid having a density at which the microspheres float and ultrasonically agitating the bath.

  18. Sesquiterpene dimmer (DSF-27) inhibits the release of neuroinflammatory mediators from microglia by targeting spleen tyrosine kinase (Syk) and Janus kinase 2 (Jak2): Two major non-receptor tyrosine signaling proteins involved in inflammatory events

    Energy Technology Data Exchange (ETDEWEB)

    Zeng, Ke-Wu [State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191 (China); Wang, Shu [State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191 (China); Department of Medicinal Chemistry and Pharmaceutical Analysis, Logistics College of Chinese People' s Armed Police Forces, Tianjin 300162 (China); Dong, Xin; Jiang, Yong; Jin, Hong-Wei [State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191 (China); Tu, Peng-Fei, E-mail: pengfeitu@vip.163.com [State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191 (China)

    2014-03-15

    Non-receptor protein tyrosine kinases (NRPTKs)-dependent inflammatory signal transduction cascades play key roles in immunoregulation. However, drug intervention through NRPTKs-involved immunoregulation mechanism in microglia (the major immune cells of the central nervous system) has not been widely investigated. A main aim of the present study is to elucidate the contribution of two major NRPTKs (Syk and Jak2) in neuroinflammation suppression by a bioactive sesquiterpene dimmer (DSF-27). We found that LPS-stimulated BV-2 cells activated Syk and further initiated Akt/NF-κB inflammatory pathway. This Syk-dependent Akt/NF-κB inflammatory pathway can be effectively ameliorated by DSF-27. Moreover, Jak2 was activated by LPS, which was followed by transcriptional factor Stat3 activation. The Jak2/Stat3 signal was suppressed by DSF-27 through inhibition of Jak2 and Stat3 phosphorylation, promotion of Jak/Stat3 inhibitory factors PIAS3 expression, and down-regulation of ERK and p38 MAPK phosphorylation. Furthermore, DSF-27 protected cortical and mesencephalic dopaminergic neurons against neuroinflammatory injury. Taken together, our findings indicate NRPTK signaling pathways including Syk/NF-κB and Jak2/Stat3 cascades are potential anti-neuroinflammatory targets in microglia, and may also set the basis for the use of sesquiterpene dimmer as a therapeutic approach for neuroinflammation via interruption of these pathways. - Highlights: • Sesquiterpene dimmer DSF-27 inhibits inflammatory mediators' production in microglia. • Syk-dependent Akt/NF-κB pathway is important for DSF-27's anti-inflammation activity. • Jak2/Stat3 pathway is important for DSF-27's anti-inflammation activity. • Jak2/Stat3 signaling pathway is partly regulated by ERK and p38 MAPKs and PIAS3. • DSF-27 protects neurons against microglia-mediated neuroinflammatory injury.

  19. In vitro evaluation of biodegradable microspheres with surface-bound ligands.

    Science.gov (United States)

    Keegan, Mark E; Royce, Sara M; Fahmy, Tarek; Saltzman, W Mark

    2006-02-21

    Protein ligands were conjugated to the surface of biodegradable microspheres. These microsphere-ligand conjugates were then used in two in vitro model systems to evaluate the effect of conjugated ligands on microsphere behavior. Microsphere retention in agarose columns was increased by ligands on the microsphere surface specific for receptors on the agarose matrix. In another experiment, conjugating the lectin Ulex europaeus agglutinin 1 to the microsphere surface increased microsphere adhesion to Caco-2 monolayers compared to control microspheres. This increase in microsphere adhesion was negated by co-administration of l-fucose, indicating that the increase in adhesion is due to specific interaction of the ligand with carbohydrate receptors on the cell surface. These results demonstrate that the ligands conjugated to the microspheres maintain their receptor binding activity and are present on the microsphere surface at a density sufficient to target the microspheres to both monolayers and three-dimensional matrices bearing complementary receptors.

  20. Non-steroidal anti-inflammatory drugs and benign oesophageal stricture.

    Science.gov (United States)

    Heller, S R; Fellows, I W; Ogilvie, A L; Atkinson, M

    1982-01-01

    Drug histories were obtained from 76 patients at the time of initial Eder-Puestow dilatation for benign oesophageal stricture. Six patients had consumed drugs known to cause oesophageal ulceration (emepronium bromide and potassium preparations). Of the remaining 70 patients, 22 had regularly taken a non-steroidal anti-inflammatory drug before the onset of dysphagia compared with 10 patients in a control group matched for age and sex; this difference was significant (p less than 0.02). Non-steroidal anti-inflammatory drugs may have a causative role in the formation of oesophageal stricture in patients with gastro-oesophageal reflux, in whom they should be prescribed with caution. PMID:6807392

  1. Usnic acid-loaded biocompatible magnetic PLGA-PVA microsphere thin films fabricated by MAPLE with increased resistance to staphylococcal colonization.

    Science.gov (United States)

    Grumezescu, V; Holban, A M; Grumezescu, A M; Socol, G; Ficai, A; Vasile, B S; Truscă, R; Bleotu, C; Lazar, V; Chifiriuc, C M; Mogosanu, G D

    2014-09-01

    Due to their persistence and resistance to the current therapeutic approaches, Staphylococcus aureus biofilm-associated infections represent a major cause of morbidity and mortality in the hospital environment. Since (+)-usnic acid (UA), a secondary lichen metabolite, possesses antimicrobial activity against Gram-positive cocci, including S. aureus, the aim of this study was to load magnetic polylactic-co-glycolic acid-polyvinyl alcohol (PLGA-PVA) microspheres with UA, then to obtain thin coatings using matrix-assisted pulsed laser evaporation and to quantitatively assess the capacity of the bio-nano-active modified surface to control biofilm formation by S. aureus, using a culture-based assay. The UA-loaded microspheres inhibited both the initial attachment of S. aureus to the coated surfaces, as well as the development of mature biofilms. In vitro bioevalution tests performed on the fabricated thin films revealed great biocompatibility, which may endorse them as competitive candidates for the development of improved non-toxic surfaces resistant to S. aureus colonization and as scaffolds for stem cell cultivation and tissue engineering.

  2. Usnic acid-loaded biocompatible magnetic PLGA-PVA microsphere thin films fabricated by MAPLE with increased resistance to staphylococcal colonization

    International Nuclear Information System (INIS)

    Grumezescu, V; Grumezescu, A M; Ficai, A; Vasile, B S; Holban, A M; Lazar, V; Chifiriuc, C M; Socol, G; Truscă, R; Bleotu, C; Mogosanu, G D

    2014-01-01

    Due to their persistence and resistance to the current therapeutic approaches, Staphylococcus aureus biofilm-associated infections represent a major cause of morbidity and mortality in the hospital environment. Since (+)-usnic acid (UA), a secondary lichen metabolite, possesses antimicrobial activity against Gram-positive cocci, including S. aureus, the aim of this study was to load magnetic polylactic-co-glycolic acid-polyvinyl alcohol (PLGA-PVA) microspheres with UA, then to obtain thin coatings using matrix-assisted pulsed laser evaporation and to quantitatively assess the capacity of the bio-nano-active modified surface to control biofilm formation by S. aureus, using a culture-based assay. The UA-loaded microspheres inhibited both the initial attachment of S. aureus to the coated surfaces, as well as the development of mature biofilms. In vitro bioevalution tests performed on the fabricated thin films revealed great biocompatibility, which may endorse them as competitive candidates for the development of improved non-toxic surfaces resistant to S. aureus colonization and as scaffolds for stem cell cultivation and tissue engineering. (paper)

  3. Usnic acid-loaded biocompatible magnetic PLGA-PVA microsphere thin films fabricated by MAPLE with increased resistance to staphylococcal colonization

    Energy Technology Data Exchange (ETDEWEB)

    Grumezescu, V; Grumezescu, A M; Ficai, A; Vasile, B S [Department of Science and Engineering of Oxide Materials and Nanomaterials, Faculty of Applied Chemistry and Materials Science, University Politehnica of Bucharest, Polizu Street no 1-7, 011061 Bucharest (Romania); Holban, A M; Lazar, V; Chifiriuc, C M [Microbiology Immunology Department, Faculty of Biology, University of Bucharest, Aleea Portocalelor 1-3, Sector 5, 77206-Bucharest (Romania); Socol, G [Lasers Department, Plasma and Radiation Physics, National Institute for Lasers, PO Box MG-36, Bucharest-Magurele (Romania); Truscă, R [Metav SA - CD SA, 31 Rosetti Str., 020015 Bucharest (Romania); Bleotu, C [Stefan S Nicolau Institute of Virology, Bucharest (Romania); Mogosanu, G D, E-mail: grumezescu@yahoo.com [Department of Pharmacognosy and Phytotherapy, Faculty of Pharmacy, University of Medicine and Pharmacy of Craiova, 2 PetruRareş Street, 200349 Craiova (Romania)

    2014-09-01

    Due to their persistence and resistance to the current therapeutic approaches, Staphylococcus aureus biofilm-associated infections represent a major cause of morbidity and mortality in the hospital environment. Since (+)-usnic acid (UA), a secondary lichen metabolite, possesses antimicrobial activity against Gram-positive cocci, including S. aureus, the aim of this study was to load magnetic polylactic-co-glycolic acid-polyvinyl alcohol (PLGA-PVA) microspheres with UA, then to obtain thin coatings using matrix-assisted pulsed laser evaporation and to quantitatively assess the capacity of the bio-nano-active modified surface to control biofilm formation by S. aureus, using a culture-based assay. The UA-loaded microspheres inhibited both the initial attachment of S. aureus to the coated surfaces, as well as the development of mature biofilms. In vitro bioevalution tests performed on the fabricated thin films revealed great biocompatibility, which may endorse them as competitive candidates for the development of improved non-toxic surfaces resistant to S. aureus colonization and as scaffolds for stem cell cultivation and tissue engineering. (paper)

  4. Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.

    Science.gov (United States)

    Canning, Peter; Ruan, Qui; Schwerd, Tobias; Hrdinka, Matous; Maki, Jenny L; Saleh, Danish; Suebsuwong, Chalada; Ray, Soumya; Brennan, Paul E; Cuny, Gregory D; Uhlig, Holm H; Gyrd-Hansen, Mads; Degterev, Alexei; Bullock, Alex N

    2015-09-17

    RIPK2 mediates pro-inflammatory signaling from the bacterial sensors NOD1 and NOD2, and is an emerging therapeutic target in autoimmune and inflammatory diseases. We observed that cellular RIPK2 can be potently inhibited by type II inhibitors that displace the kinase activation segment, whereas ATP-competitive type I inhibition was only poorly effective. The most potent RIPK2 inhibitors were the US Food and Drug Administration-approved drugs ponatinib and regorafenib. Their mechanism of action was independent of NOD2 interaction and involved loss of downstream kinase activation as evidenced by lack of RIPK2 autophosphorylation. Notably, these molecules also blocked RIPK2 ubiquitination and, consequently, inflammatory nuclear factor κB signaling. In monocytes, the inhibitors selectively blocked NOD-dependent tumor necrosis factor production without affecting lipopolysaccharide-dependent pathways. We also determined the first crystal structure of RIPK2 bound to ponatinib, and identified an allosteric site for inhibitor development. These results highlight the potential for type II inhibitors to treat indications of RIPK2 activation as well as inflammation-associated cancers. Copyright © 2015 The Authors. Published by Elsevier Ltd.. All rights reserved.

  5. Atractylenolide I restores HO-1 expression and inhibits Ox-LDL-induced VSMCs proliferation, migration and inflammatory responses in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Li, Weifeng, E-mail: liwf@mail.xjtu.edu.cn; Zhi, Wenbing; Liu, Fang; He, Zehong; Wang, Xiuei; Niu, Xiaofeng, E-mail: niuxf@mail.xjtu.edu.cn

    2017-04-01

    Pathogenesis of atherosclerosis is characterized by the proliferation and migration of vascular smooth muscle cells (VSMCs) and inflammatory lesions. The aim of this study is to elucidate the effect of atractylenolide I (AO-I) on smooth muscle cell inflammation, proliferation and migration induced by oxidized modified low density lipoprotein (Ox-LDL). Here, We found that atractylenolide I inhibited Ox-LDL-induced VSMCs proliferation and migration in a dose-dependent manner, and decreased the production of inflammatory cytokines and the expression of monocyte chemoattractant protein-1 (MCP-1) in VSMCs. The study also identified that AO-I prominently inhibited p38-MAPK and NF-κB activation. More importantly, the specific heme oxygenase-1 (HO-1) inhibitor zinc protoporphyrin (ZnPP) IX partially abolished the beneficial effects of atractylenolide I on Ox-LDL-induced VSMCs. Furthermore, atractylenolide I blocked the foam cell formation in macrophages induced by Ox-LDL. In summary, inhibitory roles of AO-I in VSMCs proliferation and migration, lipid peroxidation and subsequent inflammatory responses might contribute to the anti-atherosclerotic property of AO-I. - Highlights: • AO-I inhibited Ox-LDL-induced VSMCs proliferation and migration. • AO-I alleviated inflammatory response via inhibiting TNF-α, IL-6 and NO production. • AO-I restored HO-1 expression and down-regulated PCNA expression. • MCP-1 overexpression is potentially regulated by NF-κB and p38 MAPK pathway. • AO-I possesses strong anti-lipid peroxidation effect.

  6. Review: microspheres for radioembolization therapy

    International Nuclear Information System (INIS)

    Zhao Mingqiang; Xu Shuhe

    2007-12-01

    Radioembolization of liver cancer has been proven to be an effective therapy in nuclear medicine. The yttrium-90 glass microspheres has been used to treat both primary and metastatic liver tumors in clinic which shown encouraging results. The preparation, stability, degradation and application for medical purpose of radioactive microspheres are reviewed. At first, the theory of radioem- bolization treating cancer is discussed; and then three major radiolabled micro- sphere materials are expounded: viz. glass, resin-based and polymer-based; Future improvements in the preparation and use of radioactive microspheres are prospected at last. (authors)

  7. Review: microspheres for radioembolization therapy

    Energy Technology Data Exchange (ETDEWEB)

    Mingqiang, Zhao; Shuhe, Xu [China Inst. of Atomic Energy, Beijing (China)

    2007-12-15

    Radioembolization of liver cancer has been proven to be an effective therapy in nuclear medicine. The yttrium-90 glass microspheres has been used to treat both primary and metastatic liver tumors in clinic which shown encouraging results. The preparation, stability, degradation and application for medical purpose of radioactive microspheres are reviewed. At first, the theory of radioem- bolization treating cancer is discussed; and then three major radiolabled micro- sphere materials are expounded: viz. glass, resin-based and polymer-based; Future improvements in the preparation and use of radioactive microspheres are prospected at last. (authors)

  8. Intestinal absorption of PLAGA microspheres in the rat.

    Science.gov (United States)

    Damgé, C; Aprahamian, M; Marchais, H; Benoit, J P; Pinget, M

    1996-12-01

    Rhodamine B-labelled poly (DL-lactide-co-glycolide) (PLAGA) microspheres of 2 different sizes, 1-5 microns and 5-10 microns, were administered as a single dose (1.44 x 10(9) and 1.83 x 10(8) particles, respectively) into the ileal lumen of adult rats. The content of rhodamine in the mesenteric vein and ileal lumen was analysed periodically from 10 min to 48 h as well as the distribution of microspheres in the intestinal mucosa and various other tissues. The concentration of rhodamine decreased progressively in the intestinal lumen and was negligible after 24 h. The number of microspheres in the mesenteric vein increased rapidly and reached a maximum after 4 h whatever the size of the particles. It then decreased progressively, but more rapidly with microspheres > 5 microns than with microspheres PLAGA microspheres mainly crossed the intestinal mucosa at the site of Peyer's patches where microspheres of 5 microns were retained in the ileal lumen. A few small microspheres were occasionally observed in the epithelial cells. Only the smallest particles were recovered in the liver, lymph nodes and spleen while basement membranes were always labelled. It is concluded that PLAGA microspheres could be useful for the oral delivery of antigens if their size is between 1 and 5 microns.

  9. Gastroretentive Floating Microspheres of Silymarin: Preparation and ...

    African Journals Online (AJOL)

    Methods: Cellulose microspheres – formulated with hydroxylpropyl methylcellulose (HPMC) and ethyl cellulose (EC) – and Eudragit microspheres – formulated with Eudragit® S 100 (ES) and Eudragit® RL (ERL) - were prepared by an emulsion-solvent evaporation method. The floating microspheres were evaluated for flow ...

  10. Fabrication of Cerium Oxide and Uranium Oxide Microspheres for Space Nuclear Power Applications

    Energy Technology Data Exchange (ETDEWEB)

    Jeffrey A. Katalenich; Michael R. Hartman; Robert C. O' Brien

    2013-02-01

    Cerium oxide and uranium oxide microspheres are being produced via an internal gelation sol-gel method to investigate alternative fabrication routes for space nuclear fuels. Depleted uranium and non-radioactive cerium are being utilized as surrogates for plutonium-238 (Pu-238) used in radioisotope thermoelectric generators and for enriched uranium required by nuclear thermal rockets. While current methods used to produce Pu-238 fuels at Los Alamos National Laboratory (LANL) involve the generation of fine powders that pose a respiratory hazard and have a propensity to contaminate glove boxes, the sol-gel route allows for the generation of oxide microsphere fuels through an aqueous route. The sol-gel method does not generate fine powders and may require fewer processing steps than the LANL method with less operator handling. High-quality cerium dioxide microspheres have been fabricated in the desired size range and equipment is being prepared to establish a uranium dioxide microsphere production capability.

  11. 2-hydroxy arachidonic acid: a new non-steroidal anti-inflammatory drug.

    Directory of Open Access Journals (Sweden)

    Daniel H Lopez

    Full Text Available BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs are a family of COX1 and COX2 inhibitors used to reduce the synthesis of pro-inflammatory mediators. In addition, inflammation often leads to a harmful generation of nitric oxide. Efforts are being done in discovering safer NSAIDs molecules capable of inhibiting the synthesis of pro-inflammatory lipid mediators and nitric oxide to reduce the side effects associated with long term therapies. METHODOLOGY/PRINCIPAL FINDINGS: The analogue of arachidonic acid (AA, 2-hydroxy-arachidonic acid (2OAA, was designed to inhibit the activities of COX1 and COX2 and it was predicted to have similar binding energies as AA for the catalytic sites of COX1 and COX2. The interaction of AA and 2OAA with COX1 and COX2 was investigated calculating the free energy of binding and the Fukui function. Toxicity was determined in mouse microglial BV-2 cells. COX1 and COX2 (PGH2 production activities were measured in vitro. COX1 and COX2 expression in human macrophage-like U937 cells were carried out by Western blot, immunocytochemistry and RT-PCR analysis. NO production (Griess method and iNOS (Western blot were determined in mouse microglial BV-2 cells. The comparative efficacy of 2OAA, ibuprofen and cortisone in lowering TNF-α serum levels was determined in C57BL6/J mice challenged with LPS. We show that the presence of the -OH group reduces the likelihood of 2OAA being subjected to H* abstraction in COX, without altering significantly the free energy of binding. The 2OAA inhibited COX1 and COX2 activities and the expression of COX2 in human U937 derived macrophages challenged with LPS. In addition, 2OAA inhibited iNOS expression and the production of NO in BV-2 microglial cells. Finally, oral administration of 2OAA decreased the plasma TNF-α levels in vivo. CONCLUSION/SIGNIFICANCE: These findings demonstrate the potential of 2OAA as a NSAID.

  12. Co-culture with human synovium-derived mesenchymal stem cells inhibits inflammatory activity and increases cell proliferation of sodium nitroprusside-stimulated chondrocytes

    International Nuclear Information System (INIS)

    Ryu, Jae-Sung; Jung, Yeon-Hwa; Cho, Mi-Young; Yeo, Jee Eun; Choi, Yun-Jin; Kim, Yong Il; Koh, Yong-Gon

    2014-01-01

    Highlights: • Co-culture of hSDMSCs with SNP-stimulated chondrocytes improves anti-inflammation. • Co-culture system produces IGF-1. • Co-culture system suppresses inflammatory genes expression. • Co-culture system improves cell proliferation. • Exogenous IGF-1 inhibits inflammatory activity in SNP-stimulated chondrocytes. - Abstract: Rheumatoid arthritis (RA) and osteoarthritis (OA) are primarily chronic inflammatory diseases. Mesenchymal stem cells (MSCs) have the ability to differentiate into cells of the mesodermal lineage, and to regulate immunomodulatory activity. Specifically, MSCs have been shown to secrete insulin-like growth factor 1 (IGF-1). The purpose of the present study was to examine the inhibitory effects on inflammatory activity from a co-culture of human synovium-derived mesenchymal stem cells (hSDMSCs) and sodium nitroprusside (SNP)-stimulated chondrocytes. First, chondrocytes were treated with SNP to generate an in vitro model of RA or OA. Next, the co-culture of hSDMSCs with SNP-stimulated chondrocytes reduced inflammatory cytokine secretion, inhibited expression of inflammation activity-related genes, generated IGF-1 secretion, and increased the chondrocyte proliferation rate. To evaluate the effect of IGF-1 on inhibition of inflammation, chondrocytes pre-treated with IGF-1 were treated with SNP, and then the production of inflammatory cytokines was analyzed. Treatment with IGF-1 was shown to significantly reduce inflammatory cytokine secretion in SNP-stimulated chondrocytes. Our results suggest that hSDMSCs offer a new strategy to promote cell-based cartilage regeneration in RA or OA

  13. Co-culture with human synovium-derived mesenchymal stem cells inhibits inflammatory activity and increases cell proliferation of sodium nitroprusside-stimulated chondrocytes

    Energy Technology Data Exchange (ETDEWEB)

    Ryu, Jae-Sung; Jung, Yeon-Hwa; Cho, Mi-Young; Yeo, Jee Eun; Choi, Yun-Jin; Kim, Yong Il; Koh, Yong-Gon, E-mail: yonseranglab@daum.net

    2014-05-16

    Highlights: • Co-culture of hSDMSCs with SNP-stimulated chondrocytes improves anti-inflammation. • Co-culture system produces IGF-1. • Co-culture system suppresses inflammatory genes expression. • Co-culture system improves cell proliferation. • Exogenous IGF-1 inhibits inflammatory activity in SNP-stimulated chondrocytes. - Abstract: Rheumatoid arthritis (RA) and osteoarthritis (OA) are primarily chronic inflammatory diseases. Mesenchymal stem cells (MSCs) have the ability to differentiate into cells of the mesodermal lineage, and to regulate immunomodulatory activity. Specifically, MSCs have been shown to secrete insulin-like growth factor 1 (IGF-1). The purpose of the present study was to examine the inhibitory effects on inflammatory activity from a co-culture of human synovium-derived mesenchymal stem cells (hSDMSCs) and sodium nitroprusside (SNP)-stimulated chondrocytes. First, chondrocytes were treated with SNP to generate an in vitro model of RA or OA. Next, the co-culture of hSDMSCs with SNP-stimulated chondrocytes reduced inflammatory cytokine secretion, inhibited expression of inflammation activity-related genes, generated IGF-1 secretion, and increased the chondrocyte proliferation rate. To evaluate the effect of IGF-1 on inhibition of inflammation, chondrocytes pre-treated with IGF-1 were treated with SNP, and then the production of inflammatory cytokines was analyzed. Treatment with IGF-1 was shown to significantly reduce inflammatory cytokine secretion in SNP-stimulated chondrocytes. Our results suggest that hSDMSCs offer a new strategy to promote cell-based cartilage regeneration in RA or OA.

  14. Inhibition of release of inflammatory mediators in primary and cultured cells by a Chinese herbal medicine formula for allergic rhinitis

    Directory of Open Access Journals (Sweden)

    McPhee Sarah

    2007-02-01

    Full Text Available Abstract Background We demonstrated that a Chinese herbal formula, which we refer to as RCM-101, developed from a traditional Chinese medicine formula, reduced nasal and non-nasal symptoms of seasonal allergic rhinitis (SAR. The present study in primary and cultured cells was undertaken to investigate the effects of RCM-101 on the production/release of inflammatory mediators known to be involved in SAR. Methods Compound 48/80-induced histamine release was studied in rat peritoneal mast cells. Production of leukotriene B4 induced by the calcium ionophore A23187 was studied in porcine neutrophils using an HPLC assay and lipopolysaccharide-stimulated prostaglandin E2 production was studied in murine macrophage (Raw 264.7 cells by immune-enzyme assay. Expression of cyclooxygenase-1 (COX-1 and cyclooxygenase-2 (COX-2 was determined in Raw 264.7 cells, using western blotting techniques. Results RCM-101 (1–100 μg/mL produced concentration-dependent inhibition of compound 48/80-induced histamine release from rat peritoneal mast cells and of lipopolysaccharide-stimulated prostaglandin E2 release from Raw 264.7 cells. Over the range 1 – 10 μg/mL, it inhibited A23187-induced leukotriene B4 production in porcine neutrophils. In addition, RCM-101 (100 μg/mL inhibited the expression of COX-2 protein but did not affect that of COX-1. Conclusion The findings indicate that RCM-101 inhibits the release and/or synthesis of histamine, leukotriene B4 and prostaglandin E2 in cultured cells. These interactions of RCM-101 with multiple inflammatory mediators are likely to be related to its ability to reduce symptoms of allergic rhinitis.

  15. Tryptamine-Gallic Acid Hybrid Prevents Non-steroidal Anti-inflammatory Drug-induced Gastropathy

    Science.gov (United States)

    Pal, Chinmay; Bindu, Samik; Dey, Sumanta; Alam, Athar; Goyal, Manish; Iqbal, Mohd. Shameel; Sarkar, Souvik; Kumar, Rahul; Halder, Kamal Krishna; Debnath, Mita Chatterjee; Adhikari, Susanta; Bandyopadhyay, Uday

    2012-01-01

    We have investigated the gastroprotective effect of SEGA (3a), a newly synthesized tryptamine-gallic acid hybrid molecule against non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy with mechanistic details. SEGA (3a) prevents indomethacin (NSAID)-induced mitochondrial oxidative stress (MOS) and dysfunctions in gastric mucosal cells, which play a pathogenic role in inducing gastropathy. SEGA (3a) offers this mitoprotective effect by scavenging of mitochondrial superoxide anion (O2˙̄) and intramitochondrial free iron released as a result of MOS. SEGA (3a) in vivo blocks indomethacin-mediated MOS, as is evident from the inhibition of indomethacin-induced mitochondrial protein carbonyl formation, lipid peroxidation, and thiol depletion. SEGA (3a) corrects indomethacin-mediated mitochondrial dysfunction in vivo by restoring defective electron transport chain function, collapse of transmembrane potential, and loss of dehydrogenase activity. SEGA (3a) not only corrects mitochondrial dysfunction but also inhibits the activation of the mitochondrial pathway of apoptosis by indomethacin. SEGA (3a) inhibits indomethacin-induced down-regulation of bcl-2 and up-regulation of bax genes in gastric mucosa. SEGA (3a) also inhibits indometacin-induced activation of caspase-9 and caspase-3 in gastric mucosa. Besides the gastroprotective effect against NSAID, SEGA (3a) also expedites the healing of already damaged gastric mucosa. Radiolabeled (99mTc-labeled SEGA (3a)) tracer studies confirm that SEGA (3a) enters into mitochondria of gastric mucosal cell in vivo, and it is quite stable in serum. Thus, SEGA (3a) bears an immense potential to be a novel gastroprotective agent against NSAID-induced gastropathy. PMID:22157011

  16. Microencapsulation of Clostridium acetobutylicum ATCC 824 spores in gellan gum microspheres for the production of biobutanol.

    Science.gov (United States)

    Rathore, Sweta; Wan Sia Heng, Paul; Chan, Lai Wah

    2015-01-01

    The purpose of the present study was to provide further insights on the applicability of microencapsulation using emulsification method, to immobilise Clostridium acetobutylicum ATCC 824 spores, for biobutanol production. The encapsulated spores were revived using heat shock treatment and the fermentation efficiency of the resultant encapsulated cells was compared with that of the free (non-encapsulated) cells. The microspheres were easily recovered from the fermentation medium by filtration and reused up to five cycles of fermentation. In contrast, the free (non-encapsulated) cells could be reused for two cycles only. The microspheres remained intact throughout repeated use. Although significant cell leakage was observed during the course of fermentation, the microspheres could be reused with relatively high butanol yield, demonstrating their role as microbial cell nurseries. Both encapsulated and liberated cells contributed to butanol production.

  17. MiR-125b Inhibits LPS-Induced Inflammatory Injury via Targeting MIP-1α in Chondrogenic Cell ATDC5

    Directory of Open Access Journals (Sweden)

    Jinling Jia

    2018-03-01

    Full Text Available Background/Aims: Chondrocyte apoptosis is largely responsible for cartilage degeneration in osteoarthritis (OA. MicroRNAs (miRNAs play an important role in chondrogenesis and cartilage remodeling. This study explored the effect of miR-125b on inflammatory injury in chondrogenic cells. Methods: LPS was used to simulate inflammatory injury in murine chondrogenic ATDC5 cell lines. Targeting effect of miR-125b on MIP-1α 3’UTR was assessed by dual luciferase activity assay. Regulatory effect of miR-125b on MIP-1α expression and the potential regulatory mechanism on inflammatory injury were assessed by Western blot. Results: miR-125b expression was decreased in LPS-induced ATDC5 cells and overexpression of miR-125b inhibited LPS-induced cell viability decline, the rise of apoptosis and inflammatory factors’ productions. MIP-1α expression was negatively related to miR-125b, and miR-125b directly targeted with 3’UTR of MIP-1α. Knockdown of miR-125b promoted LPS-induced inflammatory response via upregulation of MIP-1α. miR-125b expression in LPS-induced ATDC5 cells was negatively related with activations of NF-κB and JNK signaling pathways. Overexpression of miR-125b inhibited LPS-induced inflammation injury via suppressing MIP-1α expression and inhibiting activations of NF-κB and JNK signaling pathways. Conclusion: miR-125b could play an important role in inflammatory injury of chondrogenic cells and miR-125b affected inflammatory injury of ATDC5 cells via regulating expression of MIP-1α and regulating NF-κB and JNK signaling pathways.

  18. Preparation and in vitro evaluation of xanthan gum facilitated superabsorbent polymeric microspheres.

    Science.gov (United States)

    Bhattacharya, Shiv Sankar; Mazahir, Farhan; Banerjee, Subham; Verma, Anurag; Ghosh, Amitava

    2013-10-15

    Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superabsorbent polymer (SAP) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for sustained release of ciprofloxacin hydrochloride (CIPRO). The microspheres were prepared with various ratios of hydrolyzed SAP to PVA and extent of crosslinking density. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acidic and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results, this study suggest that CIPRO loaded IPN microspheres were suitable for sustained release application. Copyright © 2013 Elsevier Ltd. All rights reserved.

  19. Sulindac, a nonsteroidal anti-inflammatory drug, selectively inhibits interferon-γ-induced expression of the chemokine CXCL9 gene in mouse macrophages

    International Nuclear Information System (INIS)

    Sakaeda, Yoshiichi; Hiroi, Miki; Shimojima, Takahiro; Iguchi, Mayumi; Kanegae, Haruhide; Ohmori, Yoshihiro

    2006-01-01

    Sulindac, a non-steroidal anti-inflammatory drug, has been shown to exert an anti-tumor effect on several types of cancer. To determine the effect of sulindac on intracellular signaling pathways in host immune cells such as macrophages, we investigated the effect of the drug on interferon gamma (IFNγ)-induced expression of signal transducer and activator of transcription 1 (STAT1) and other genes in mouse macrophage-like cell line RAW264.7 cells. Sulindac, but not aspirin or sodium salicylate, inhibited IFNγ-induced expression of the CXC ligand 9 (CXCL9) mRNA, a chemokine for activated T cells, whereas the interferon-induced expression of CXCL10 or IFN regulatory factor-1 was not affected by sulindac. Luciferase reporter assay demonstrated that sulindac inhibited IFNγ-induced promoter activity of the CXCL9 gene. Surprisingly, sulindac had no inhibitory effect on IFNγ-induced STAT1 activation; however, constitutive nuclear factor κB activity was suppressed by the drug. These results indicate that sulindac selectively inhibited IFNγ-inducible gene expression without inhibiting STAT1 activation

  20. In vitro evaluation and intra-articular administration of biodegradable microspheres containing naproxen sodium.

    Science.gov (United States)

    Bozdağ, S; Caliş, S; Kaş, H S; Ercan, M T; Peksoy, I; Hincal, A A

    2001-01-01

    The dispersion of non-steroidal antiinflammatory drugs (NSAIDs) into biodegradable polymeric matrices have been accepted as a good approach for obtaining a therapeutic effect in a predetermined period of time meanwhile minimizing the side effects of NSAIDs. In the present study, it was aimed to prepare Naproxen Sodium (NS), (a NSAID) loaded microsphere formulation using natural Bovine Serum Albumin (BSA) and synthetic biodegradable polymers such as poly(lactide-co-glycolic acid) (PLGA) (50:50 MW 34,000 and 88,000 Da) for intra-articular administration, and to study the retention of the drug at the site of injection in the knee joint. NS incorporated microspheres were evaluated in vitro for particle size (the mean particle size; for BSA microspheres, 10.0 +/- 0.3 microm, for PLGA microspheres, 9.0 +/- 0.2 and 5.0 +/- 0.1 microm for MW 34,000 and 88,000 Da, respectively), yield value, drug loading, surface morphology and drug release. For in vivo studies, monoarticular arthritis was induced in the left knee joints of rabbits by using ovalbumin and Freund's Complete Adjuvant as antigen and adjuvant. A certain time (4 days) is allowed for the formation of arthritis in the knee joints, then the NS loaded microspheres were injected directly into the articular cavity. At specific time points, gamma scintigrams were obtained to determine the residence time of the microspheres in knee joints, in order to determine the most suitable formulation. This study indicated that PLGA, a synthetic polymer, is more promising than the natural type BSA microspheres for an effective cure of mono-articular arthritis in rabbits.

  1. Histamine-imprinted microspheres: Comparison between conventional and raft-mediated polymerization techniques

    International Nuclear Information System (INIS)

    Romano, Edwin F. Jr.; So, Regina C.; Holdsworth, Clovia I.

    2015-01-01

    Molecularly imprinted microspheres (MIM) were synthesized via conventional free radical polymerization (CTP) and RAFT-mediated controlled radical polymerization (CRP) method using histamine as the template molecule. Optimal polymerization conditions were achieved using 4%(w/w) monomer feed concentration with 80=90% EGDMA as crosslinker, and histamine: MAA ratio of 1:4 in acetonitrile at 60°C for 24 hours. The size of CTP-M90 and CTP-M80 imprinted microspheres are comparable with that of RAFT polymer CRP-M80 at 264.5 ±12 nm in the swollen (DLS-DMSO) and collapsed state (SEM). For the CTP method, the presence of the template allows for a bigger particle size compared to the non-imprinted counterpart (NIM). Further, controlled growth was observed for the CRP technique, where the size of the imprinted microsphere, CRP-M80, is comparable to CRP-N80. The binding studies of CTP and CRP microspheres toward histamine were studied at concentrations well below biding with buffer concentration of 25mM at pH7. Results showed that the binding isotherms were found to conform to the Freundlich model. Moreover, results revealed that the difference in binding capacity (N) between MIM and NIM imparted by the imprinting process is significantly higher in CTP-80 (26 μmol/g) than both CTP-90 and CRP-80 (9 μmol/g). Non-competitive and competitive binding assays with L-histidine, imidazole, and tryptamine using CTP-80 and CRP-80 were also carried out. MIMs were shown to exhibit binding preference towards the template. (author)

  2. Celastrol ameliorates HIV-1 Tat-induced inflammatory responses via NF-kappaB and AP-1 inhibition and heme oxygenase-1 induction in astrocytes

    International Nuclear Information System (INIS)

    Youn, Gi Soo; Kwon, Dong-Joo; Ju, Sung Mi; Rhim, Hyangshuk; Bae, Yong Soo; Choi, Soo Young; Park, Jinseu

    2014-01-01

    HIV-1 Tat causes extensive neuroinflammation that may progress to AIDS-related encephalitis and dementia. Celastrol possesses various biological activities such as anti-oxidant, anti-tumor, and anti-inflammatory activities. In this study, we investigated the modulatory effects of celastrol on HIV-1 Tat-induced inflammatory responses and the molecular mechanisms underlying its action in astrocytes. Pre-treatment of CRT-MG human astroglioma cells with celastrol significantly inhibited HIV-1 Tat-induced expression of ICAM-1/VCAM-1 and subsequent monocyte adhesiveness in CRT-MG cells. In addition, celastrol suppressed HIV-1 Tat-induced expression of pro-inflammatory chemokines, such as CXCL10, IL-8, and MCP-1. Celastrol decreased HIV-1 Tat-induced activation of JNK MAPK, AP-1, and NF-κB. Furthermore, celastrol induced mRNA and protein expression of HO-1 as well as Nrf2 activation. Blockage of HO-1 expression using siRNA reversed the inhibitory effect of celastrol on HIV-1 Tat-induced inflammatory responses. These results suggest that celastrol has regulatory effects on HIV-1 Tat-induced inflammatory responses by blocking the JNK MAPK-AP-1/NF-κB signaling pathways and inducing HO-1 expression in astrocytes. - Highlights: • Celastrol suppressed HIV-1 Tat-induced expression of pro-inflammatory genes. • Celastrol inhibited HIV-1 Tat -induced activation of JNK MAPK. • Celastrol inhibited HIV-1 Tat-induced activation of both NF-κB and AP-1. • Celastrol inhibited HIV-1 Tat-induced inflammatory responses via HO-1 induction

  3. Celastrol ameliorates HIV-1 Tat-induced inflammatory responses via NF-kappaB and AP-1 inhibition and heme oxygenase-1 induction in astrocytes

    Energy Technology Data Exchange (ETDEWEB)

    Youn, Gi Soo; Kwon, Dong-Joo; Ju, Sung Mi [Department of Biomedical Science and Research Institute for Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Rhim, Hyangshuk [Department of Biomedical Sciences, Department of Medical Life Sciences, College of Medicine, the Catholic University of Korea, Seoul 137-701 (Korea, Republic of); Bae, Yong Soo [Department of Biological Science, College of Natural Sciences, Sungkyunkwan University, Suwon 440-746 (Korea, Republic of); Choi, Soo Young [Department of Biomedical Science and Research Institute for Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Park, Jinseu, E-mail: jinpark@hallym.ac.kr [Department of Biomedical Science and Research Institute for Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of)

    2014-10-01

    HIV-1 Tat causes extensive neuroinflammation that may progress to AIDS-related encephalitis and dementia. Celastrol possesses various biological activities such as anti-oxidant, anti-tumor, and anti-inflammatory activities. In this study, we investigated the modulatory effects of celastrol on HIV-1 Tat-induced inflammatory responses and the molecular mechanisms underlying its action in astrocytes. Pre-treatment of CRT-MG human astroglioma cells with celastrol significantly inhibited HIV-1 Tat-induced expression of ICAM-1/VCAM-1 and subsequent monocyte adhesiveness in CRT-MG cells. In addition, celastrol suppressed HIV-1 Tat-induced expression of pro-inflammatory chemokines, such as CXCL10, IL-8, and MCP-1. Celastrol decreased HIV-1 Tat-induced activation of JNK MAPK, AP-1, and NF-κB. Furthermore, celastrol induced mRNA and protein expression of HO-1 as well as Nrf2 activation. Blockage of HO-1 expression using siRNA reversed the inhibitory effect of celastrol on HIV-1 Tat-induced inflammatory responses. These results suggest that celastrol has regulatory effects on HIV-1 Tat-induced inflammatory responses by blocking the JNK MAPK-AP-1/NF-κB signaling pathways and inducing HO-1 expression in astrocytes. - Highlights: • Celastrol suppressed HIV-1 Tat-induced expression of pro-inflammatory genes. • Celastrol inhibited HIV-1 Tat -induced activation of JNK MAPK. • Celastrol inhibited HIV-1 Tat-induced activation of both NF-κB and AP-1. • Celastrol inhibited HIV-1 Tat-induced inflammatory responses via HO-1 induction.

  4. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1995-02-28

    New, high strength glass microspheres filled with pressurized hydrogen exhibit densities which make them attractive for bulk hydrogen storage and transport. The membrane tensile stress at failure for engineered glass microspheres is about 150,000 psi, permitting a three-fold increase in pressure limit and storage capacity above commercial microspheres, which have been studied a decade ago and have been shown to fail at membrane stresses of 50,000 psi. This analysis relating glass microspheres for hydrogen transport with infrastructure and economics, indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as pressurized tube transports and liquid hydrogen trailers. This paper will describe the matching of current glass microspheres with the useful application in commercial hydrogen bulk transport and storage.

  5. The anti-inflammatory activity of standard aqueous stem bark extract of Mangifera indica L. as evident in inhibition of Group IA sPLA2.

    Science.gov (United States)

    Dhananjaya, Bhadrapura Lakkappa; Shivalingaiah, Sudharshan

    2016-03-01

    The standard aqueous stem bark extract is consumed as herbal drink and used in the pharmaceutical formulations to treat patients suffering from various disease conditions in Cuba. This study was carried out to evaluate the modulatory effect of standard aqueous bark extract of M. indica on Group IA sPLA2. M. indica extract, dose dependently inhibited the GIA sPLA2 (NN-XIa-PLA2) activity with an IC50 value 8.1 µg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ~40 µg/ml concentration and at various concentrations (0-50 µg/ml), it dose dependently inhibited the edema formation. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect on the GIA sPLA2. Furthermore, the inhibition was irreversible as evidenced from binding studies. It is observed that the aqueous extract ofM. indica effectively inhibits sPLA2 and it is associated inflammatory activities, which substantiate their anti-inflammatory properties. The mode of inhibition could be due to direct interaction of components present in the extract, with sPLA2 enzyme. Further studies on understanding the principal constituents, responsible for the anti-inflammatory activity would be interesting to develop this into potent anti-inflammatory agent.

  6. Innovative hydrogen storage in hollow glass-microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Keding, M.; Schmid, G.; Tajmar, M. [Austrian Research Centers, Vienna (Austria)

    2009-07-01

    Hydrogen storage technologies are becoming increasingly important for a number of future applications. The Austrian Research Centers (ARC) are developing a unique hydrogen storage system that combines the advantages of both hollow glass microsphere and chemical compound hydrogen storage, but eliminates their respective drawbacks. Water is utilized as a functional liquid to carry the hollow glass microspheres that are loaded with up to 700 bar of hydrogen gas. Sodium borohydride (NaBH{sub 4}) is then injected together with the glass microspheres into a reaction chamber where the water reacts catalytically with the NaBH{sub 4} producing hydrogen and heat. The heat is then utilized to release the hydrogen from the hollow glass microspheres providing a double hydrogen generation process without any external energy or heat during storage or gas release. The paper described this hydrogen storage system with particular reference to microspheres, the coating process, the experimental facility and NaBH{sub 4} test results. It was concluded that hydrogen storage and production on demand is possible with microspheres and sodium borohydride solution. 9 refs., 16 figs.

  7. Cheongsangbangpung-tang ameliorated the acute inflammatory response via the inhibition of NF-κB activation and MAPK phosphorylation.

    Science.gov (United States)

    Kim, Seon Young; Park, Sang Mi; Hwangbo, Min; Lee, Jong Rok; Byun, Sung Hui; Ku, Sae Kwang; Cho, Il Je; Kim, Sang Chan; Jee, Seon Young; Park, Sook Jahr

    2017-01-13

    Cheongsangbangpung-tang (CBT) is a traditional herbal formula used in Eastern Asia to treat heat-related diseases and swellings in the skin. The present study was conducted to evaluate the anti-inflammatory effects of cheongsangbangpung-tang extract (CBTE) both in vitro and in vivo. The in vitro effects of CBTE on the lipopolysaccharide (LPS)-induced production of inflammation-related proteins were examined in RAW 264.7 cells. The levels of nitric oxide (NO) were measured with the Griess reagent. Inflammatory cytokines and prostaglandin E 2 (PGE 2 ) were detected using the enzyme-linked immunosorbent assay (ELISA) method. Inflammation-related proteins were detected by Western blot. The effect of CBTE on acute inflammation in vivo was evaluated using carrageenan (CA)-induced paw oedema. To evaluate the anti-inflammatory effect, paw oedema volume, thickness of the dorsum and ventrum pedis skin, number of infiltrated inflammatory cells, and number of COX-2-, iNOS-immunoreactive cells were measured. In an in vitro study, CBTE inhibited the production of NO and PGE 2 and also decreased the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) activity, interleukin (IL)-1β, IL-6 and tumuor necrosis factor-α. In LPS-activated macrophages, nuclear factor-kappaB (NF-κB) and mitogen-activated protein kinase (MAPK) signalling is a pivotal pathway in the inflammatory process. These plausible molecular mechanisms increased the phosphorylation of I-κBα, while the activation of NF-κB and the phosphorylation of MAPK by LPS were blocked by CBTE treatment. In our in vivo study, a CA-induced acute oedematous paw inflammation rat model was used to evaluate the anti-inflammatory effect of CBTE. CBTE significantly reduced the increases in paw swelling, skin thicknesses, infiltrated inflammatory cells and iNOS-, COX-2 positive cells induced by CA injection. Based on these results, CBTE should favourably inhibit the acute inflammatory response through

  8. 20(S-Protopanaxatriol inhibits release of inflammatory mediators in immunoglobulin E-mediated mast cell activation

    Directory of Open Access Journals (Sweden)

    Dae Yong Kim

    2015-07-01

    Conclusion: PPT reduces the release of inflammatory mediators via inhibiting multiple cellular signaling pathways comprising the Ca2+ influx, protein kinase C, and PLA2, which are propagated by Syk activation upon allergic stimulation of mast cells.

  9. Toxicity of Doxorubicin on Pig Liver After Chemoembolization with Doxorubicin-loaded Microspheres: A Pilot DNA-microarrays and Histology Study

    Energy Technology Data Exchange (ETDEWEB)

    Verret, Valentin, E-mail: valentin.verret@archimmed.com; Namur, Julien; Ghegediban, Saieda Homayra [ArchimMed (France); Wassef, Michel [University of Paris 7-Denis Diderot, Department of Pathology, Faculty of Medicine, AP-HP Hopital Lariboisiere (France); Moine, Laurence [Universite Paris Sud, Faculte de Pharmacie, UMR CNRS 8612, IFR 141-ITFM (France); Bonneau, Michel [AP-HP/INRA, Centre de Recherche En Imagerie Interventionnelle (France); Pelage, Jean-Pierre [AP-HP Hopital Ambroise Pare, Department of Interventional Radiology (France); Laurent, Alexandre [AP-HP/INRA, Centre de Recherche En Imagerie Interventionnelle (France)

    2013-02-15

    The potential mechanisms accounting for the hepatotoxicity of doxorubicin-loaded microspheres in chemoembolization were examined by combining histology and DNA-microarray techniques.The left hepatic arteries of two pigs were embolized with 1 mL of doxorubicin-loaded (25 mg; (DoxMS)) or non-loaded (BlandMS) microspheres. The histopathological effects of the embolization were analyzed at 1 week. RNAs extracted from both the embolized and control liver areas were hybridized onto Agilent porcine microarrays. Genes showing significantly different expression (p < 0.01; fold-change > 2) between two groups were classified by biological process. At 1 week after embolization, DoxMS caused arterial and parenchymal necrosis in 51 and 38 % of embolized vessels, respectively. By contrast, BlandMS did not cause any tissue damage. Up-regulated genes following embolization with DoxMS (vs. BlandMS, n = 353) were mainly involved in cell death, apoptosis, and metabolism of doxorubicin. Down-regulated genes (n = 120) were mainly related to hepatic functions, including enzymes of lipid and carbohydrate metabolisms. Up-regulated genes included genes related to cell proliferation (growth factors and transcription factors), tissue remodeling (MMPs and several collagen types), inflammatory reaction (interleukins and chemokines), and angiogenesis (angiogenic factors and HIF1a pathway), all of which play an important role in liver healing and regeneration. DoxMS caused lesions to the liver, provoked cell death, and disturbed liver metabolism. An inflammatory repair process with cell proliferation, tissue remodeling, and angiogenesis was rapidly initiated during the first week after chemoembolization. This pilot study provides a comprehensive method to compare different types of DoxMS in healthy animals or tumor models.

  10. Microsphere estimates of blood flow: Methodological considerations

    International Nuclear Information System (INIS)

    von Ritter, C.; Hinder, R.A.; Womack, W.; Bauerfeind, P.; Fimmel, C.J.; Kvietys, P.R.; Granger, D.N.; Blum, A.L.

    1988-01-01

    The microsphere technique is a standard method for measuring blood flow in experimental animals. Sporadic reports have appeared outlining the limitations of this method. In this study the authors have systematically assessed the effect of blood withdrawals for reference sampling, microsphere numbers, and anesthesia on blood flow estimates using radioactive microspheres in dogs. Experiments were performed on 18 conscious and 12 anesthetized dogs. Four blood flow estimates were performed over 120 min using 1 x 10 6 microspheres each time. The effects of excessive numbers of microspheres pentobarbital sodium anesthesia, and replacement of volume loss for reference samples with dextran 70 were assessed. In both conscious and anesthetized dogs a progressive decrease in gastric mucosal blood flow and cardiac output was observed over 120 min. This was also observed in the pancreas in conscious dogs. The major factor responsible for these changes was the volume loss due to the reference sample withdrawals. Replacement of the withdrawn blood with dextran 70 led to stable blood flows to all organs. The injection of excessive numbers of microspheres did not modify hemodynamics to a greater extent than did the injection of 4 million microspheres. Anesthesia exerted no influence on blood flow other than raising coronary flow. The authors conclude that although blood flow to the gastric mucosa and the pancreas is sensitive to the minor hemodynamic changes associated with the microsphere technique, replacement of volume loss for reference samples ensures stable blood flow to all organs over a 120-min period

  11. Microsphere based improved sunscreen formulation of ethylhexyl methoxycinnamate.

    Science.gov (United States)

    Gogna, Deepak; Jain, Sunil K; Yadav, Awesh K; Agrawal, G P

    2007-04-01

    Polymethylmethacrylate (PMMA) microspheres of ethylhexyl methoxycinnamate (EHM) were prepared by emulsion solvent evaporation method to improve its photostability and effectiveness as sunscreening agent. Process parameters like stirring speed and aqueous polyvinyl alcohol (PVA) concentration were analyzed in order to optimize the formulations. Shape and surface morphology of the microspheres were examined using scanning electron microscopy. Particle size of the microspheres was determined using laser diffraction particle size analyzer. The PMMA microspheres of EHM were incorporated in water-removable cream base. The in vitro drug release of EHM in pH 7.4 was performed using dialysis membrane. Thin layer chromatography was performed to determine photostability of EHM inside the microspheres. The formulations were evaluated for sun protection factor (SPF) and minimum erythema dose (MED) in albino rats. Cream base formulation containing microspheres prepared using EHM:PMMA in ratio of 1:3 (C(3)) showed slowest drug (EHM) release and those prepared with EHM: PMMA in ratio of 1:1 showed fastest release. The cream base formulations containing EHM loaded microspheres had shown better SPF (more than 16.0) as compared to formulation C(d) that contained 3% free EHM as sunscreen agent and showed SPF 4.66. These studies revealed that the incorporation of EHM loaded PMMA microspheres into cream base had greatly increased the efficacy of sunscreen formulation approximately four times. Further, photostability was also shown to be improved in PMMA microspheres.

  12. Long non-coding RNA TUG1 inhibits apoptosis and inflammatory response in LPS-treated H9c2 cells by down-regulation of miR-29b.

    Science.gov (United States)

    Zhang, Haifang; Li, Hui; Ge, Ang; Guo, Enyu; Liu, Shuxia; Zhang, Lijuan

    2018-05-01

    Myocarditis is an important cause for cardiovascular morbidity and mortality in children and adults. The lncRNA taurine up-regulated gene 1 (TUG1) plays important roles in cell apoptosis and inflammation in tumor and liver injury. The present study aimed to investigate the role of TUG1 in LPS-injured H9c2 cells and explore the underlying molecular mechanism. H9c2 cells were stimulated with LPS to induce inflammatory injury. The expression of TUG1 was altered by transient transfections. Cell viability and apoptotic cell rates were detected by CCK-8 assay and flow cytometry assay, respectively. Inflammatory response was determined by detecting levels of inflammatory cytokines using qRT-PCR and ELISA. Furthermore, western blot analysis was conducted to assess the expression levels of core factors related with apoptosis and activations of NF-κB and JAK/STAT signaling pathways. LPS exposure reduced cell viability but enhanced cell apoptosis and inflammation in H9c2 cells. Moreover, TUG1 expression was down-regulated in LPS-injured H9c2 cells. TUG1 overexpression attenuated LPS-induced injuries in H9c2 cells, evidenced by augmented cell viability, declined apoptotic cell rates and decreased levels of pro-apoptotic factors and inflammatory cytokines. Inversely, TUG1 inhibition exerted the opposite effects. More importantly, TUG1 negatively modulated the expression of miR-29b and miR-29b mimic blocked the effect of TUG1 overexpression on cell viability, apoptosis, inflammation and inactivation of NF-κB and JAK/STAT signaling pathways in LPS-stimulated H9c2 cells. This study demonstrated that TUG1 played the anti-apoptotic and anti-inflammatory roles in LPS-injured H9c2 cells via down-regulating miR-29b and inhibiting NF-κB and JAK/STAT pathways. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  13. Preparation and Characterization of Sugar Cane Wax Microspheres ...

    African Journals Online (AJOL)

    ... and characterize indomethacin (IM) microspheres prepared with sugar cane wax microsperes. Methods: Microspheres were prepared by melt-emulsified dispersion and cooling-induced solidification method. The microspheres were characterized by scanning electron microscopy (SEM) and differntial scanning calorimetry ...

  14. Preparation of mesoporous zirconia microspheres as inert matrix

    Energy Technology Data Exchange (ETDEWEB)

    Guo, Ting [State Key Laboratory of New Ceramics and Fine Processing, Institute of Nuclear and New Energy Technology, Tsinghua University, Beijing, 100084 (China); Wang, Chen; Lv, Jinlong [Beijing Key Laboratory of Fine Ceramics, Institute of Nuclear and New Energy Technology, Tsinghua University, Beijing, 100084 (China); Liang, Tongxiang, E-mail: txliang@tsinghua.edu.cn [State Key Laboratory of New Ceramics and Fine Processing, Institute of Nuclear and New Energy Technology, Tsinghua University, Beijing, 100084 (China)

    2016-12-01

    Mesoporous zirconia microspheres, with a diameter of 900 μm, were prepared as an inert accelerator driven system (ADS) transmutation element matrix by the sol-gel method. The purpose of mesopores is to improve the adsorption capacity of inert matrix fuel (IMF) for minor actinides. The study indicated that the mesoporous zirconia performance was improved after the microspheres were hydrothermally treated at 150 °C, the specific surface area increased from 28.29 m{sup 2}/g to 61.28 m{sup 2}/g, and hydrothermal treatment avoided the cracking of the microspheres. Pre-decomposition of the organics during the hydrothermal process stabilized the mesoporous structure. The average pore diameter of mesoporous microsphere was 14.3 nm. - Highlights: • Mesoporous zirconia microspheres with a diameter of 900 μm were prepared as ADS transmutation element inert matrix. • The mesoporous performance was improved after the microspheres were hydrothermally treated at 150 °C. • The specific surface area increased from 28.29 m{sup 2}/g to 61.28 m{sup 2}/g. • The hydrothermal treatment could avoid the cracking of the microspheres. • The specific surface area of mesoporous microsphere was 61.28 m{sup 2}/g and the average pore diameter was 14.3 nm.

  15. Insulin delivery through nasal route using thiolated microspheres.

    Science.gov (United States)

    Nema, Tarang; Jain, Ashish; Jain, Aviral; Shilpi, Satish; Gulbake, Arvind; Hurkat, Pooja; Jain, Sanjay K

    2013-01-01

    The aim of the present study was to investigate the potential of developed thiolated microspheres for insulin delivery through nasal route. In the present study, cysteine was immobilized on carbopol using EDAC. A total of 269.93 µmol free thiol groups per gram polymer were determined. The prepared nonthiolated and thiolated microspheres were studied for particle shape, size, drug content, swellability, mucoadhesion and in vitro insulin release. The thiolated microspheres exhibited higher mucoadhesion due to formation of covalent bonds via disulfide bridges with the mucus gel layer. Drug permeation through goat nasal mucosa of nonthiolated and thiolated microspheres were found as 52.62 ± 2.4% and 78.85 ± 3.1% in 6 h, respectively. Thiolated microspheres bearing insulin showed better reduction in blood glucose level (BGL) in comparison to nonthiolated microspheres as 31.23 ± 2.12% and 75.25 ± 0.93% blood glucose of initial BGL were observed at 6 h after nasal delivery of thiolated and nonthiolated microspheres in streptozotocin-induced diabetic rabbits.

  16. K88 Fimbrial Adhesin Targeting of Microspheres Containing Gentamicin Made with Albumin Glycated with Lactose

    Directory of Open Access Journals (Sweden)

    Andre-i Sarabia-Sainz

    2015-09-01

    Full Text Available The formulation and characterization of gentamicin-loaded microspheres as a delivery system targeting enterotoxigenic Escherichia coli K88 (E. coli K88 was investigated. Glycated albumin with lactose (BSA-glucose-β (4-1 galactose was used as the microsphere matrix (MS-Lac and gentamicin included as the transported antibiotic. The proposed target strategy was that exposed galactoses of MS-Lac could be specifically recognized by E. coli K88 adhesins, and the delivery of gentamicin would inhibit bacterial growth. Lactosylated microspheres (MS-Lac1, MS-Lac2 and MS-Lac3 were obtained using a water-in-oil emulsion, containing gentamicin, followed by crosslinking with different concentrations of glutaraldehyde. Electron microscopy displayed spherical particles with a mean size of 10–17 µm. In vitro release of gentamicin from MS-Lac was best fitted to a first order model, and the antibacterial activity of encapsulated and free gentamicin was comparable. MS-Lac treatments were recognized by plant galactose-specific lectins from Ricinus communis and Sophora japonica and by E. coli K88 adhesins. Results indicate MS-Lac1, produced with 4.2 mg/mL of crosslinker, as the best treatment and that lactosylated microsphere are promising platforms to obtain an active, targeted system against E. coli K88 infections.

  17. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1995-04-18

    New, high strength glass microspheres filled with pressurized hydrogen exhibit densities which make them attractive for bulk hydrogen storage and transport. The membrane tensile stress at failure for our engineered glass microspheres is about 150,000 psi, permitting a threefold increase in pressure limit and storage capacity above commercial microspheres, which have been studied a decade ago and have been shown to fail at membrane stresses of 50,000 psi. Our analysis relating glass microspheres for hydrogen transport with infrastructure and economics, indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as pressurized tube transports and liquid hydrogen trailers.

  18. Evaluation of radiolabelled microspheres as digesta markers

    International Nuclear Information System (INIS)

    Young, B.A.; Turner, B.V.; Dixon, A.E.; Exley, D.M.; Young, S.B.; Abidin, Z.

    1991-01-01

    The suitability of microspheres as markers for measuring digesta kinetics in sheep was examined. Microspheres offer advantages of uniformity of size and density, and stability during passage through the gastrointestinal tract. They are commercially available labelled with the choice of one of eleven different radionuclides and can be easily measured in digesta and faecal material. Tests comparing several types of digesta markers gave different measures of kinetic parameters when the measurements were made concurrently in the same sheep. However, concurrent measurements derived from use of microspheres were consistent. Microspheres offer a new alternative for digestive studies. (author). 19 refs, 4 tabs

  19. Ketoprofen-loaded Eudragit RSPO microspheres: an influence of sodium carbonate on in vitro drug release and surface topology.

    Science.gov (United States)

    Pandit, Sachin S; Hase, Dinesh P; Bankar, Manish M; Patil, Arun T; Gaikwad, Naresh J

    2009-05-01

    Eudragit RSPO microspheres containing ketoprofen as model drug, prepared by solvent evaporation technique using acetone-liquid paraffin (heavy) solvent system were examined. Depending upon polymer concentration in the internal phase, microspheres of particle mean diameter (122.8, 213.6 and 309.5 μm) were obtained. The influence of surface washing of microspheres with n-hexane, i.e. untreated microspheres (UM) on the drug content, drug release and surface topology of microspheres were compared to those of microspheres washed with sodium carbonate, i.e. treated microspheres (TM) in order to make the non-encapsulated surface drug soluble. The significant reduction in encapsulation efficiency (p < 0.001) and drug content (p < 0.001) after treatment, in combination with the small crystalline peaks observed during XRD testing and lack of melting endotherm observed in DSC testing, suggests that the washing process actually removes a significant amount of drug (p < 0.001) from the surface and encapsulated near to the surface of the microsphere polymer matrix. Scanning electron microscopy (SEM) examination revealed that the removal of surface drug did not affect the size of microspheres but the topology of treated smallest microspheres was modified. The ketoprofen release profiles were examined in phosphate buffer pH 7.4, using USPXXIII paddle type dissolution apparatus. In general both UM and TM result in biphasic release patterns, but the initial burst effect (first release phase) of TM was lower than that of UM. The second release phase did not change for the bigger size but increased for the smallest microspheres, probably owing to the modification of matrix porosity.

  20. Novel microspheres reduce the formation of deep venous thrombosis and repair the vascular wall in a rat model.

    Science.gov (United States)

    Dai, Bingyang; Li, Lan; Li, Qiangqiang; Song, Xiaoxiao; Chen, Dongyang; Dai, Jin; Yao, Yao; Yan, Wenjin; Teng, Huajian; Yang, Fang; Xu, Zhihong; Jiang, Qing

    2017-07-01

    : L-Arginine (L-arg), widely known as a substrate for endogenous nitric oxide synthesis, can improve endothelial function associated with the vasculature, inhibit platelet aggregation, and alter the activity of vascular smooth muscle cells. P-selectin is a membrane component of the platelet alpha-granule and the endothelial cell-specific Wiebel-Palade body that plays a central role in mediating interactions between platelets and both leukocytes and the endothelium. The experiment was designed to evaluate the effect of novel microspheres with L-arg targeting P-selectin on the formation of deep vein thrombosis and repair of vascular wall in a rat model. Thrombosis of the inferior vena cava was induced by applying a piece of filter paper (5 mm × 10 mm) saturated with 10% FeCl3 solution for 5 min. Targeted microspheres with L-arg, targeted microspheres with water, and saline were injected into the tail veins of the rats after 30 min of applying the filter paper saturated with 10% FeCl3 solution. The dry weight and length of the thrombus isolated from the inferior vena cava were significantly decreased in the group with L-arg in microsphere after 24 h. No significant differences in prothrombin time, activated partial thromboplastin time, thrombin time, and fibrinogen among the groups were indicated. Images revealed that apoptosis in the vascular wall was less in the group injected with targeted microspheres with L-arg than in the other two groups at 1 and 8 d postsurgery. Meanwhile, cell proliferation was considerably excessive in the group injected with L-arg wrapped in targeted microspheres. Therefore, these novel microspheres could decrease the formation of thrombus in the early stages and in the subsequent periods of thrombosis. The microspheres can also enhance the vitality of impaired endothelial cells and reduce cell apoptosis.

  1. Versatile microsphere attachment of GFP-labeled motors and other tagged proteins with preserved functionality

    Directory of Open Access Journals (Sweden)

    Michael Bugiel

    2015-11-01

    Full Text Available Microspheres are often used as handles for protein purification or force spectroscopy. For example, optical tweezers apply forces on trapped particles to which motor proteins are attached. However, even though many attachment strategies exist, procedures are often limited to a particular biomolecule and prone to non-specific protein or surface attachment. Such interactions may lead to loss of protein functionality or microsphere clustering. Here, we describe a versatile coupling procedure for GFP-tagged proteins via a polyethylene glycol linker preserving the functionality of the coupled proteins. The procedure combines well-established protocols, is highly reproducible, reliable, and can be used for a large variety of proteins. The coupling is efficient and can be tuned to the desired microsphere-to-protein ratio. Moreover, microspheres hardly cluster or adhere to surfaces. Furthermore, the procedure can be adapted to different tags providing flexibility and a promising attachment strategy for any tagged protein.

  2. Glass microspheres for brachytherapy

    International Nuclear Information System (INIS)

    Prado, Miguel O.; Prastalo, Simon; Blaumann, Herman; Longhino, Juan M.; Repetto Llamazares, A.H.V.

    2007-01-01

    We developed the capacity to produce glass microspheres containing in their structure one or more radioactive isotopes useful for brachytherapy. We studied the various facts related with their production: (Rare earth) alumino silicate glass making, glass characterization, microspheres production, nuclear activation through (n,γ) nuclear reactions, mechanical characterization before and after irradiation. Corrosion tests in simulated human plasma and mechanical properties characterization were done before and after irradiation. (author) [es

  3. Antioxidants inhibit SAA formation and pro-inflammatory cytokine release in a human cell model of alkaptonuria.

    Science.gov (United States)

    Spreafico, Adriano; Millucci, Lia; Ghezzi, Lorenzo; Geminiani, Michela; Braconi, Daniela; Amato, Loredana; Chellini, Federico; Frediani, Bruno; Moretti, Elena; Collodel, Giulia; Bernardini, Giulia; Santucci, Annalisa

    2013-09-01

    Alkaptonuria (AKU) is an ultra-rare autosomal recessive disease that currently lacks an appropriate therapy. Recently we provided experimental evidence that AKU is a secondary serum amyloid A (SAA)-based amyloidosis. The aim of the present work was to evaluate the use of antioxidants to inhibit SAA amyloid and pro-inflammatory cytokine release in AKU. We adopted a human chondrocytic cell AKU model to evaluate the anti-amyloid capacity of a set of antioxidants that had previously been shown to counteract ochronosis in a serum AKU model. Amyloid presence was evaluated by Congo red staining. Homogentisic acid-induced SAA production and pro-inflammatory cytokine release (overexpressed in AKU patients) were evaluated by ELISA and multiplex systems, respectively. Lipid peroxidation was evaluated by means of a fluorescence-based assay. Our AKU model allowed us to prove the efficacy of ascorbic acid combined with N-acetylcysteine, taurine, phytic acid and lipoic acid in significantly inhibiting SAA production, pro-inflammatory cytokine release and membrane lipid peroxidation. All the tested antioxidant compounds were able to reduce the production of amyloid and may be the basis for establishing new therapies for AKU amyloidosis.

  4. The role of non-CRF inhibition in contour detection

    NARCIS (Netherlands)

    Grigorescu, C.; Petkov, N.; Westenberg, M.A.

    2003-01-01

    We propose a biologically motivated computational step, called non-classical receptive field (non-CRF) inhibition, to improve the performance of contour detectors. Non-CRF inhibition is exhibited by 80% of the orientation selective neurons in the primary visual cortex of macaque monkeys and has been

  5. Preparation of polystyrene microsphere with emulsion microencapsulation method

    International Nuclear Information System (INIS)

    Li Bo Zhang Lin; Zhang Zhganwen; You Dan; Wei Yun; Wang Chaoyang; Lin Bo; Shi Tao; Chu Qiaomei

    2003-01-01

    The preparation of hollow polystyrene microspheres that are used as inner shell of multi-shell plastic microspheres in the ICF experiments is focused on. The effects of surfactants, water-soluble polymer and electrolyte on the properties of resultant microspheres are studied. Based on these experiments, a fabricating procedure was established with which hollow microspheres were prepared with diameter about 150-3000 μm, wall thickness 0.8-15 μm and toughness Ra less than 4 nm. (authors)

  6. [Exploring a non-inflammatory clinical breast mass: Clinical practice guidelines].

    Science.gov (United States)

    Legendre, G; Guilhen, N; Nadeau, C; Brossard, A; Fauvet, R

    2015-12-01

    The aim of the study was to assess the diagnostic value of physical examination, radiologic explorations and percutaneous procedures of the breast in the exploration of a non-inflammatory palpable mass, in order to propose guidelines. A systematic literature review was conducted in the Medline and Cochrane library databases. International guidelines in French and English language were also consulted until April 30th 2015. Physical examination of a non-inflammatory palpable breast mass is not sufficient to eliminate a breast cancer (LE2). Mammography alone has a sensitivity between 70 and 95% for the diagnosis of breast cancer (LE3). Echography alone has a sensitivity of 98 to 100% for the diagnosis of breast cancer (LE2). The core needle biopsy has a better sensitivity and specificity than the fine-needle aspiration for breast cancer diagnosis (LE2). The association of mammography and 2D echography presents excellent sensitivity and negative predictive value (close to 100 %) to exclude a breast cancer (LE3). A double evaluation using mammography and echography is recommended in the exploration of a non-inflammatory palpable breast mass (grade B). Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  7. Preparation of alumina microspheres

    International Nuclear Information System (INIS)

    Santos, W.R. dos; Abrao, A.

    1980-01-01

    Inorganic exchangers are widely used for adsorption and column partition chromatography. The main difficulty of using commercial alumina (in powder) for column chromatography is related to its packing, and the operations through the column become diffcult and time-consuming; also it turns to be virtually impossible to use large dimension columns. In order to eliminate these problems, a process for the preparation of alumina micro-spheres was developed as an adaptation of a similar process used to prepare nuclear fuel microspheres (UO 2 , ThO 2 ). The flowsheet of this process is presented together with the analytical results of sphericity after calcination, granulometry, density and characterization by X-ray diffractometry. Solubility tests showed that the so-prepared microspheres are well resistant to strong acids and bases; retention tests showed their efficiency, mainly to copper. (C.L.B.) [pt

  8. Controlling silk fibroin microspheres via molecular weight distribution

    International Nuclear Information System (INIS)

    Zeng, Dong-Mei; Pan, Jue-Jing; Wang, Qun; Liu, Xin-Fang; Wang, Hui; Zhang, Ke-Qin

    2015-01-01

    Silk fibroin (SF) microspheres were produced by salting out SF solution via the addition of potassium phosphate buffer solution (K 2 HPO 4 –KH 2 PO 4 ). The morphology, size and polydispersity of SF microspheres were adjusted by changing the molecular weight (MW) distribution and concentration of SF, as well as the ionic strength and pH of the buffer solution. Changing the conditions under which the SF fiber dissolved in the Lithium Boride (LiBr) solution resulted in altering the MW distribution of SF solution. Under optimal salting-out conditions (ionic strength > 0.7 M and pH > 7) and using a smaller and narrower SF MW distribution, SF microspheres with smoother shapes and more uniform sizes were produced. Meanwhile, the size and polydispersity of the microspheres increased when the SF concentration was increased from 0.25 mg/mL to 20 mg/mL. The improved SF microspheres, obtained by altering the distribution of molecular weight, have potential in drug and gene delivery applications. - Highlights: • MW distribution was changed by applying different dissolving methods of SF fiber. • Smaller and narrower MW distribution improves the quality of SF microspheres. • Size and polydispersity of microspheres increase as SF concentration increases. • Improved SF microspheres have potential in drug and gene delivery applications

  9. Controlling silk fibroin microspheres via molecular weight distribution

    Energy Technology Data Exchange (ETDEWEB)

    Zeng, Dong-Mei; Pan, Jue-Jing; Wang, Qun; Liu, Xin-Fang; Wang, Hui [National Engineering Laboratory for Modern Silk, College for Textile and Clothing Engineering, Soochow University, Suzhou, Jiangsu 215123 (China); Zhang, Ke-Qin, E-mail: kqzhang@suda.edu.cn [National Engineering Laboratory for Modern Silk, College for Textile and Clothing Engineering, Soochow University, Suzhou, Jiangsu 215123 (China); Research Center of Cooperative Innovation for Functional Organic/Polymer Material Micro/Nanofabrication, Soochow University, Suzhou, Jiangsu 215123 (China)

    2015-05-01

    Silk fibroin (SF) microspheres were produced by salting out SF solution via the addition of potassium phosphate buffer solution (K{sub 2}HPO{sub 4}–KH{sub 2}PO{sub 4}). The morphology, size and polydispersity of SF microspheres were adjusted by changing the molecular weight (MW) distribution and concentration of SF, as well as the ionic strength and pH of the buffer solution. Changing the conditions under which the SF fiber dissolved in the Lithium Boride (LiBr) solution resulted in altering the MW distribution of SF solution. Under optimal salting-out conditions (ionic strength > 0.7 M and pH > 7) and using a smaller and narrower SF MW distribution, SF microspheres with smoother shapes and more uniform sizes were produced. Meanwhile, the size and polydispersity of the microspheres increased when the SF concentration was increased from 0.25 mg/mL to 20 mg/mL. The improved SF microspheres, obtained by altering the distribution of molecular weight, have potential in drug and gene delivery applications. - Highlights: • MW distribution was changed by applying different dissolving methods of SF fiber. • Smaller and narrower MW distribution improves the quality of SF microspheres. • Size and polydispersity of microspheres increase as SF concentration increases. • Improved SF microspheres have potential in drug and gene delivery applications.

  10. Antibacterial activity of ciprofloxacin-loaded zein microsphere films

    International Nuclear Information System (INIS)

    Fu Jianxi; Wang Huajie; Zhou Yanqing; Wang Jinye

    2009-01-01

    Our aim was to produce an antibiotic-emitting coating composed of zein microspheres for the prevention of bacterial infection on implanted devices. Ciprofloxacin-loaded zein microspheres were prepared using a phase separation procedure, with particle sizes between 0.5 and 2 μm. Drug encapsulation and drug loading varied with the amount of both zein and ciprofloxacin, and the highest encapsulation efficiency was 8.27% (2 mg/ml ciprofloxacin and 20 mg/ml zein; n = 3). A ciprofloxacin-loaded zein microsphere film (CF-MS film) was generated via solvent evaporation. Continuous drug release from a trypsin-degraded microsphere film was observed for up to 28 days. The liberation of ciprofloxacin from the trypsin-degraded film and the biodegradation of the microsphere film were highly correlated. Proliferation assay of the growth of human umbilical vein endothelial cells (HUVECs) by the MTT method showed that the microsphere film had no toxicity when compared with cells grown on Corning culture plates alone and plates with a zein film alone. Quantification of bacteria adhesion showed that adhesion on the microsphere film is significantly suppressed. In addition, according to the results of bacterial growth tests, ciprofloxacin-loaded microsphere films maintained antibacterial activity for more than 6 days. In contrast, a control medium containing a zein film allowed constant bacterial growth. These results indicate that CF-MS films might be useful as antibacterial films on implanted devices.

  11. Antibacterial activity of ciprofloxacin-loaded zein microsphere films

    Energy Technology Data Exchange (ETDEWEB)

    Fu Jianxi [Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032 (China); Henan Normal University, 46 East Construction Road, Xinxiang, Henan 453007 (China); Wang Huajie [College of Life Science and Biotechnology, Shanghai Jiao Tong University, 1954 Huashan Road, Shanghai 200030 (China); Zhou Yanqing [Henan Normal University, 46 East Construction Road, Xinxiang, Henan 453007 (China); Wang Jinye, E-mail: jywang@mail.sioc.ac.cn [Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032 (China); College of Life Science and Biotechnology, Shanghai Jiao Tong University, 1954 Huashan Road, Shanghai 200030 (China)

    2009-05-05

    Our aim was to produce an antibiotic-emitting coating composed of zein microspheres for the prevention of bacterial infection on implanted devices. Ciprofloxacin-loaded zein microspheres were prepared using a phase separation procedure, with particle sizes between 0.5 and 2 {mu}m. Drug encapsulation and drug loading varied with the amount of both zein and ciprofloxacin, and the highest encapsulation efficiency was 8.27% (2 mg/ml ciprofloxacin and 20 mg/ml zein; n = 3). A ciprofloxacin-loaded zein microsphere film (CF-MS film) was generated via solvent evaporation. Continuous drug release from a trypsin-degraded microsphere film was observed for up to 28 days. The liberation of ciprofloxacin from the trypsin-degraded film and the biodegradation of the microsphere film were highly correlated. Proliferation assay of the growth of human umbilical vein endothelial cells (HUVECs) by the MTT method showed that the microsphere film had no toxicity when compared with cells grown on Corning culture plates alone and plates with a zein film alone. Quantification of bacteria adhesion showed that adhesion on the microsphere film is significantly suppressed. In addition, according to the results of bacterial growth tests, ciprofloxacin-loaded microsphere films maintained antibacterial activity for more than 6 days. In contrast, a control medium containing a zein film allowed constant bacterial growth. These results indicate that CF-MS films might be useful as antibacterial films on implanted devices.

  12. U3O8 microspheres sintering kinetics

    International Nuclear Information System (INIS)

    Godoy, A.L.E.

    1986-01-01

    U 3 O 8 microspheres sintering kinetics was determined using a hot-stage optical microscopy apparatus, able to reach temperature up to 1350 0 C in controlled atmospheres. The sintered material had its microstructure analysed by optical and electron microscopy. The microspheres were characterized initialy utilizing X-ray diffractometry and thermogravimetry. The equation which describes the microspheres shrinkage in function of the time was obtained using finite difference analysis X-ray diffractometry indicated hexagonal structure for the microspheres main starting material, ammonium diuranate thermogravimetric analysis showed reduction of this material to U 3 O 8 at 600 0 C. Ceramography results showed 5 hours sintered microspheres grain sizes G vary with the temperature. Sintered U 3 O 8 micrographs compared with published results for UO 2 , indicate similar homogeneity microstructural characteristics and suggest the processed micorspheres to be potentially useful as nuclear fuels. (Author) [pt

  13. Synchrotron radiation-based Fourier-transform infrared spectromicroscopy for characterization of the protein/peptide distribution in single microspheres

    Directory of Open Access Journals (Sweden)

    Manli Wang

    2015-05-01

    Full Text Available The present study establishes a visualization method for the measurement of the distribution and localization of protein/peptide constituents within a single poly-lactide-co-glycolide (PLGA microsphere using synchrotron radiation–based Fourier-transform infrared spectromicroscopy (SR-FTIR. The representative infrared wavenumbers specific for protein/peptide (Exenatide and excipient (PLGA were identified and chemical maps at the single microsphere level were generated by measuring and plotting the intensity of these specific bands. For quantitative analysis of the distribution within microspheres, Matlab software was used to transform the map file into a 3D matrix and the matrix values specific for the drug and excipient were extracted. Comparison of the normalized SR-FTIR maps of PLGA and Exenatide indicated that PLGA was uniformly distributed, while Exenatide was relatively non-uniformly distributed in the microspheres. In conclusion, SR-FTIR is a rapid, nondestructive and sensitive detection technology to provide the distribution of chemical constituents and functional groups in microparticles and microspheres.

  14. Synthesis and characterization of emamectin-benzoate slow-release microspheres with different surfactants.

    Science.gov (United States)

    Wang, Yan; Wang, Anqi; Wang, Chunxin; Cui, Bo; Sun, Changjiao; Zhao, Xiang; Zeng, Zhanghua; Shen, Yue; Gao, Fei; Liu, Guoqiang; Cui, Haixin

    2017-10-06

    Pesticide slow-release formulations provide a way to increase the efficiency of active components by reducing the amount of pesticide that needs to be applied. Slow-release formulations also increase the stability and prolong the control effect of photosensitive pesticides. Surfactants are an indispensable part of pesticide formulations, and the choice of surfactant can strongly affect formulation performance. In this study, emamectin-benzoate (EMB) slow-release microspheres were prepared by the microemulsion polymerization method. We explored the effect of different surfactants on the particle size and dispersity of EMB in slow-release microspheres. The results indicated that the samples had uniform spherical shapes with an average diameter of 320.5 ±5.24 nm and good dispersity in the optimal formulation with the polymeric stabilizer polyvinyl alcohol (PVA) and composite non-ionic surfactant polyoxyethylene castor oil (EL-40). The optimal EMB pesticide slow-release microspheres had excellent anti-photolysis performance, stability, controlled release properties, and good leaf distribution. These results demonstrated that EMB slow-release microspheres are an attractive candidate for improving pesticide efficacy and prolonging the control effect of EMB in the environment.

  15. Reducing inappropriate non-steroidal anti-inflammatory prescription in primary care patients with chronic kidney disease.

    Science.gov (United States)

    Keohane, David M; Dennehy, Thomas; Keohane, Kenneth P; Shanahan, Eamonn

    2017-08-14

    Purpose The purpose of this paper is to reduce inappropriate non-steroidal anti-inflammatory prescribing in primary care patients with chronic kidney disease (CKD). Once diagnosed, CKD management involves delaying progression to end stage renal failure and preventing complications. It is well established that non-steroidal anti-inflammatories have a negative effect on kidney function and consequently, all nephrology consensus groups suggest avoiding this drug class in CKD. Design/methodology/approach The sampling criteria included all practice patients with a known CKD risk factor. This group was refined to include those with an estimated glomerular filtration rate (eGFR)<60 ml/min per 1.73m2 (stage 3 CKD or greater). Phase one analysed how many prescriptions had occurred in this group over the preceding three months. The intervention involved creating an automated alert on at risk patient records if non-steroidal anti-inflammatories were prescribed and discussing the rationale with practice staff. The re-audit phase occurred three months' post intervention. Findings The study revealed 728/7,500 (9.7 per cent) patients at risk from CKD and 158 (2.1 per cent) who were subsequently found to have an eGFR<60 ml/min, indicating=stage 3 CKD. In phase one, 10.2 per cent of at risk patients had received a non-steroidal anti-inflammatory prescription in the preceding three months. Additionally, 6.2 per cent had received non-steroidal anti-inflammatories on repeat prescription. Phase two post intervention revealed a significant 75 per cent reduction in the total non-steroidal anti-inflammatories prescribed and a 90 per cent reduction in repeat non-steroidal anti-inflammatory prescriptions in those with CKD. Originality/value The study significantly reduced non-steroidal anti-inflammatory prescription in those with CKD in primary care settings. It also created a CKD register within the practice and an enduring medication alert system for individuals that risk nephrotoxic

  16. Tat-CBR1 inhibits inflammatory responses through the suppressions of NF-κB and MAPK activation in macrophages and TPA-induced ear edema in mice

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Young Nam [Department of Biomedical Science and Research Institute of Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Kim, Dae Won [Department of Biochemistry and Molecular Biology, Research Institute of Oral Sciences, College of Dentistry, Kangnung-Wonju National University, Kangneung 210-702 (Korea, Republic of); Jo, Hyo Sang; Shin, Min Jea; Ahn, Eun Hee; Ryu, Eun Ji; Yong, Ji In; Cha, Hyun Ju; Kim, Sang Jin; Yeo, Hyeon Ji; Youn, Jong Kyu; Hwang, Jae Hyeok [Department of Biomedical Science and Research Institute of Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Jeong, Ji-Heon; Kim, Duk-Soo [Department of Anatomy, College of Medicine, Soonchunhyang University, Cheonan-Si 330-090 (Korea, Republic of); Cho, Sung-Woo [Department of Biochemistry and Molecular Biology, University of Ulsan College of Medicine, Seoul 138-736 (Korea, Republic of); Park, Jinseu [Department of Biomedical Science and Research Institute of Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Eum, Won Sik, E-mail: wseum@hallym.ac.kr [Department of Biomedical Science and Research Institute of Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of); Choi, Soo Young, E-mail: sychoi@hallym.ac.kr [Department of Biomedical Science and Research Institute of Bioscience and Biotechnology, Hallym University, Chunchon 200-702 (Korea, Republic of)

    2015-07-15

    Human carbonyl reductase 1 (CBR1) plays a crucial role in cell survival and protects against oxidative stress response. However, its anti-inflammatory effects are not yet clearly understood. In this study, we examined whether CBR1 protects against inflammatory responses in macrophages and mice using a Tat-CBR1 protein which is able to penetrate into cells. The results revealed that purified Tat-CBR1 protein efficiently transduced into Raw 264.7 cells and inhibited lipopolysaccharide (LPS)-induced cyclooxygenase-2 (COX-2), nitric oxide (NO) and prostaglandin E{sub 2} (PGE{sub 2}) expression levels. In addition, Tat-CBR1 protein leads to decreased pro-inflammatory cytokine expression through suppression of nuclear transcription factor-kappaB (NF-κB) and mitogen activated protein kinase (MAPK) activation. Furthermore, Tat-CBR1 protein inhibited inflammatory responses in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin inflammation when applied topically. These findings indicate that Tat-CBR1 protein has anti-inflammatory properties in vitro and in vivo through inhibition of NF-κB and MAPK activation, suggesting that Tat-CBR1 protein may have potential as a therapeutic agent against inflammatory diseases. - Highlights: • Transduced Tat-CBR1 reduces LPS-induced inflammatory mediators and cytokines. • Tat-CBR1 inhibits MAPK and NF-κB activation. • Tat-CBR1 ameliorates inflammation response in vitro and in vivo. • Tat-CBR1 may be useful as potential therapeutic agent for inflammation.

  17. Preparation and drug controlled release of porous octyl-dextran microspheres.

    Science.gov (United States)

    Hou, Xin; Liu, Yanfei

    2015-01-01

    In this work, porous octyl-dextran microspheres with excellent properties were prepared by two steps. Firstly, dextran microspheres were synthesized by reversed-phase suspension polymerization. Secondly, octyl-dextran microspheres were prepared by the reaction between dextran microspheres and ethylhexyl glycidyl ether and freezing-drying method. Porous structure of microspheres was formed through the interaction between octyl groups and organic solvents. The structure, morphology, dry density, porosity and equilibrium water content of porous octyl-dextran microspheres were systematically investigated. The octyl content affected the properties of microspheres. The results showed that the dry density of microspheres decreased from 2.35 to 1.21 g/ml, porosity increased from 80.68 to 95.05% with the octyl content increasing from 0.49 to 2.28 mmol/g. Meanwhile, the equilibrium water content presented a peak value (90.18%) when the octyl content was 2.25 mmol/g. Octyl-dextran microspheres showed high capacity. Naturally drug carriers play an important role in drug-delivery systems for their biodegradability, wide raw materials sources and nontoxicity. Doxorubicin (DOX) was used as a drug model to examine the drug-loading capacity of porous octyl-dextran microspheres. The drug-loading efficiency increased with the increase in microspheres/drug ratio, while the encapsulation efficiency decreased. When microspheres/drug mass ratio was 4/1, the drug-loading efficiency and encapsulation efficiency were 10.20 and 51.00%, respectively. The release rate of DOX increased as drug content and porosity increased. In conclusion, porous octyl-dextran microspheres were synthesized successfully and have the potential to serve as an effective delivery system in drug controlled release.

  18. Baicalein inhibits IL-1β- and TNF-α-induced inflammatory cytokine production from human mast cells via regulation of the NF-κB pathway

    Directory of Open Access Journals (Sweden)

    Krishnaswamy Guha

    2007-11-01

    Full Text Available Abstract Background Human mast cells are multifunctional cells capable of a wide variety of inflammatory responses. Baicalein (BAI, isolated from the traditional Chinese herbal medicine Huangqin (Scutellaria baicalensis Georgi, has been shown to have anti-inflammatory effects. We examined its effects and mechanisms on the expression of inflammatory cytokines in an IL-1β- and TNF-α-activated human mast cell line, HMC-1. Methods HMC-1 cells were stimulated either with IL-1β (10 ng/ml or TNF-α (100 U/ml in the presence or absence of BAI. We assessed the expression of IL-6, IL-8, and MCP-1 by ELISA and RT-PCR, NF-κB activation by electrophoretic mobility shift assay (EMSA, and IκBα activation by Western blot. Results BAI (1.8 to 30 μM significantly inhibited production of IL-6, IL-8, and MCP-1 in a dose-dependent manner in IL-1β-activated HMC-1. BAI (30 μM also significantly inhibited production of IL-6, IL-8, and MCP-1 in TNF-α-activated HMC-1. Inhibitory effects appear to involve the NF-κB pathway. BAI inhibited NF-κB activation in IL-1β- and TNF-α-activated HMC-1. Furthermore, BAI increased cytoplasmic IκBα proteins in IL-1β- and TNF-α-activated HMC-1. Conclusion Our results showed that BAI inhibited the production of inflammatory cytokines through inhibition of NF-κB activation and IκBα phosphorylation and degradation in human mast cells. This inhibitory effect of BAI on the expression of inflammatory cytokines suggests its usefulness in the development of novel anti-inflammatory therapies.

  19. Poly(ADP-ribose) polymerase inhibition reduces tumor necrosis factor-induced inflammatory response in rheumatoid synovial fibroblasts

    NARCIS (Netherlands)

    García, S.; Bodaño, A.; Pablos, J. L.; Gómez-Reino, J. J.; Conde, C.

    2008-01-01

    To investigate the effect of poly(ADP-ribose) polymerase (PARP) inhibition on the production of inflammatory mediators and proliferation in tumour necrosis factor (TNF)-stimulated fibroblast-like synoviocytes (FLS) from patients with rheumatoid arthritis (RA). Cultured FLS from patients with RA were

  20. Full factorial design optimization of anti-inflammatory drug release by PCL–PEG–PCL microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Azouz, L' Hachemi, E-mail: azouz.chimie@gmail.com [Laboratoire des Matériaux Organiques (LMO), Faculté des Sciences Exactes, Département de Chimie, Université de Bejaia, 06000 Bejaia Algérie (Algeria); Dahmoune, Farid, E-mail: farid.dahmoune@yahoo.fr [Laboratoire de Biomathématiques, Biophysique, Biochimie et Scientométrie (L3BS-Bejaia), Faculté des Sciences de la Nature et de la Vie et des Sciences de la Terre, Université de Bouira 10000 Bouira (Algeria); Rezgui, Farouk, E-mail: rezgui-farouk@netcourrier.com [Laboratoire des Matériaux Organiques (LMO), Faculté de Technologie, Département de Génie des Procédés, Université de Bejaia, 06000 Bejaia (Algeria); G' Sell, Christian, E-mail: gsell.christian@univ-lorraine.fr [Université de Lorraine, Pôle scientifique M4, Institut Jean Lamour - UMR CNRS-UL 7198, Département SI2M, 54000 Nancy (France)

    2016-01-01

    A biodegradable triblock poly(ε-caprolactone)–poly(ethylene glycol)–poly(ε-caprolactone) copolymer was successfully synthesized by ring-opening polymerization of ε-caprolactone, and was characterized by intrinsic viscosimetry, {sup 1}H nuclear magnetic resonance, infrared spectroscopy and X-ray diffraction. Copolymer microparticles loaded with ibuprofen were prepared by an oil-in-water (o/w) emulsion solvent evaporation process. They were carefully weighted and characterized through their zeta potential. In this work, 4 selected process parameters (shaking speed X{sub 1}, time of contact X{sub 2}, poly(vinyl alcohol) concentration X{sub 3}, and ibuprofen concentration X{sub 4}) were adjusted at 2 different values. For each of the 16 experimental conditions, repeated twice, the drug encapsulation efficiency of the microspheres was determined, according to the following definition: EE (X{sub 1}, X{sub 2}, X{sub 3}, X{sub 4}) = mass of encapsulated ibuprofen / total weight of ibuprofen. A “full factorial design method” was applied to analyze the results statistically according to a polynomial fit and to determine the optimal conditions for the microencapsulation of the ibuprofen through an accurate statistical protocol. The microparticles obtained exhibit a spherical shape as shown by electron microscopy. - Highlights: • PCEC copolymer was synthesized by ring-opening polymerization of ε-caprolactone. • 2{sup 4} experimental design was used to optimize the IBF encapsulation efficiency (EE). • 88.86% of ibuprofen (IBF) was encapsulated in PCEC microspheres. • EE significantly decreases with increasing shaking speed (antagonist effect). • EE significantly increases with increasing IBF concentration (synergetic effect).

  1. Full factorial design optimization of anti-inflammatory drug release by PCL–PEG–PCL microspheres

    International Nuclear Information System (INIS)

    Azouz, L'Hachemi; Dahmoune, Farid; Rezgui, Farouk; G'Sell, Christian

    2016-01-01

    A biodegradable triblock poly(ε-caprolactone)–poly(ethylene glycol)–poly(ε-caprolactone) copolymer was successfully synthesized by ring-opening polymerization of ε-caprolactone, and was characterized by intrinsic viscosimetry, 1 H nuclear magnetic resonance, infrared spectroscopy and X-ray diffraction. Copolymer microparticles loaded with ibuprofen were prepared by an oil-in-water (o/w) emulsion solvent evaporation process. They were carefully weighted and characterized through their zeta potential. In this work, 4 selected process parameters (shaking speed X 1 , time of contact X 2 , poly(vinyl alcohol) concentration X 3 , and ibuprofen concentration X 4 ) were adjusted at 2 different values. For each of the 16 experimental conditions, repeated twice, the drug encapsulation efficiency of the microspheres was determined, according to the following definition: EE (X 1 , X 2 , X 3 , X 4 ) = mass of encapsulated ibuprofen / total weight of ibuprofen. A “full factorial design method” was applied to analyze the results statistically according to a polynomial fit and to determine the optimal conditions for the microencapsulation of the ibuprofen through an accurate statistical protocol. The microparticles obtained exhibit a spherical shape as shown by electron microscopy. - Highlights: • PCEC copolymer was synthesized by ring-opening polymerization of ε-caprolactone. • 2 4 experimental design was used to optimize the IBF encapsulation efficiency (EE). • 88.86% of ibuprofen (IBF) was encapsulated in PCEC microspheres. • EE significantly decreases with increasing shaking speed (antagonist effect). • EE significantly increases with increasing IBF concentration (synergetic effect).

  2. Low pressure gas filling of laser fusion microspheres

    International Nuclear Information System (INIS)

    Koo, J.C.; Dressler, J.L.; Hendricks, C.D.

    1979-01-01

    In our laser fusion microsphere production, large, thin gel-microspheres are formed before the chemicals are fused into glass. In this transient stage,, the gel-microspheres are found to be highly permeable to argon and many other inert gases. When the gel transforms to glass, the argon gas, for example, is trapped within to form argon filled, fusion target quality, glass microspheres. On the average, the partial pressure of the argon fills attained in this process is around 2 x 10 4 Pa at room temperature

  3. Hollow porous-wall glass microspheres for hydrogen storage

    Science.gov (United States)

    Heung, Leung K.; Schumacher, Ray F.; Wicks, George G.

    2010-02-23

    A porous wall hollow glass microsphere is provided having a diameter range of between 1 to 200 microns, a density of between 1.0 to 2.0 gm/cc, a porous-wall structure having wall openings defining an average pore size of between 10 to 1000 angstroms, and which contains therein a hydrogen storage material. The porous-wall structure facilitates the introduction of a hydrogen storage material into the interior of the porous wall hollow glass microsphere. In this manner, the resulting hollow glass microsphere can provide a membrane for the selective transport of hydrogen through the porous walls of the microsphere, the small pore size preventing gaseous or liquid contaminants from entering the interior of the hollow glass microsphere.

  4. Paeoniflorin Attenuates Inflammatory Pain by Inhibiting Microglial Activation and Akt-NF-κB Signaling in the Central Nervous System

    Directory of Open Access Journals (Sweden)

    Bo Hu

    2018-05-01

    Full Text Available Background/Aims: Paeoniflorin (PF is known to have anti-inflammatory and paregoric effects, but the mechanism underlying its analgesic effect remains unclear. The aim of this study was to clarify the effect of PF on Freund’s complete adjuvant (CFA-induced inflammatory pain and explore the underlying molecular mechanism. Methods: An inflammatory pain model was established by intraplantar injection of CFA in C57BL/6J mice. After intrathecal injection of PF daily for 8 consecutive days, thermal and mechanical withdrawal thresholds, the levels of inflammatory factors TNF-α, IL-1β and IL-6, microglial activity, and the expression of Akt-NF-κB signaling pathway in the spinal cord tissue were detected by animal ethological test, cell culture, enzyme-linked immunosorbent assay, immunofluorescence histochemistry, and western blot. Results: PF inhibited the spinal microglial activation in the CFA-induced pain model. The production of proinflammatory cytokines was decreased in the central nervous system after PF treatment both in vivo and in vitro. PF further displayed a remarkable effect on inhibiting the activation of Akt-NF-κB signaling pathway in vivo and in vitro. Conclusion: These results suggest that PF is a potential therapeutic agent for inflammatory pain and merits further investigation.

  5. Encapsulated PDMS microspheres with reactive handles

    DEFF Research Database (Denmark)

    Gonzalez, Lidia; Ma, Baoguang; Li, Li

    2014-01-01

    , cured PDMS microspheres are coated with poly(methyl methacrylate) using a chemical process (solvent evaporation technique). Three solvents are used in three different experiments: dichloromethane, tetrahydrofuran, and acetone. The composition and morphology of the cured PDMS microspheres and PMMA coated...

  6. Microencapsulation and microspheres for food applications

    NARCIS (Netherlands)

    Sagis, L.M.C.

    2015-01-01

    This book provides an update on the latest developments, challenges, and opportunities in the highly expanding field of microencapsulation and microspheres for food applications, examining the various types of microspheres and microcapsules essential to those who need to develop stable and

  7. Inhibition of inflammatory and proliferative responses of human keratinocytes exposed to the sesquiterpene lactones dehydrocostuslactone and costunolide.

    Directory of Open Access Journals (Sweden)

    Claudia Scarponi

    Full Text Available The imbalance of the intracellular redox state and, in particular, of the glutathione (GSH/GSH disulfide couple homeostasis, is involved in the pathogenesis of a number of diseases. In many skin diseases, including psoriasis, oxidative stress plays an important role, as demonstrated by the observation that treatments leading to increase of the local levels of oxidant species ameliorate the disease. Recently, dehydrocostuslactone (DCE and costunolide (CS, two terpenes naturally occurring in many plants, have been found to exert various anti-inflammatory and pro-apoptotic effects on different human cell types. These compounds decrease the level of the intracellular GSH by direct interaction with it, and, therefore, can alter cellular redox state. DCE and CS can trigger S-glutathionylation of various substrates, including the transcription factor STAT3 and JAK1/2 proteins. In the present study, we investigated on the potential role of DCE and CS in regulating inflammatory and proliferative responses of human keratinocytes to cytokines. We demonstrated that DCE and CS decreased intracellular GSH levels in human keratinocytes, as well as inhibited STAT3 and STAT1 phosphorylation and activation triggered by IL-22 or IFN-γ, respectively. Consequently, DCE and CS decreased the IL-22- and IFN-γ-induced expression of inflammatory and regulatory genes in keratinocytes, including CCL2, CXCL10, ICAM-1 and SOCS3. DCE and CS also inhibited proliferation and cell-cycle progression-related gene expression, as well as they promoted cell cycle arrest and apoptosis. In parallel, DCE and CS activated the anti-inflammatory EGFR and ERK1/2 molecules in keratinocytes, and, thus, wound healing in an in vitro injury model. In light of our findings, we can hypothesize that the employment of DCE and CS in psoriasis could efficiently counteract the pro-inflammatory effects of IFN-γ and IL-22 on keratinocytes, revert the apoptosis-resistant phenotype, as well as inhibit

  8. Radioisotope diagnosis of pneumonia with the help of labelled microspheres of the blood serum albumin of man (experimental study)

    International Nuclear Information System (INIS)

    Khachirov, Dzh.G.; Petriev, V.M.

    1978-01-01

    The level of accumulation of albumin- 131 I microspheres in the lungs of intact animals reaches 90 per cent of the activity of the introduced preparation. In experimental pneumonia the inclusion of the preparation comprises 81.1+-6.23 per cent. The elimination of the labelled preparation from the lungs in experimental pneumonia occurs two times as slow than that in the control. The labelled microspheres of albumin make it possible to visualize the focus of inflammation, its spreading, conduct observations in dynamics. The peculiarities of accumulation and elimination from the lungs of the mentioned preparation make it possible with its help to differentiate pathological conditions of the lungs: inflammatory process, malignant neoformations and experimental embolism of the pulmonary artery

  9. A reproducible accelerated in vitro release testing method for PLGA microspheres.

    Science.gov (United States)

    Shen, Jie; Lee, Kyulim; Choi, Stephanie; Qu, Wen; Wang, Yan; Burgess, Diane J

    2016-02-10

    The objective of the present study was to develop a discriminatory and reproducible accelerated in vitro release method for long-acting PLGA microspheres with inner structure/porosity differences. Risperidone was chosen as a model drug. Qualitatively and quantitatively equivalent PLGA microspheres with different inner structure/porosity were obtained using different manufacturing processes. Physicochemical properties as well as degradation profiles of the prepared microspheres were investigated. Furthermore, in vitro release testing of the prepared risperidone microspheres was performed using the most common in vitro release methods (i.e., sample-and-separate and flow through) for this type of product. The obtained compositionally equivalent risperidone microspheres had similar drug loading but different inner structure/porosity. When microsphere particle size appeared similar, porous risperidone microspheres showed faster microsphere degradation and drug release compared with less porous microspheres. Both in vitro release methods investigated were able to differentiate risperidone microsphere formulations with differences in porosity under real-time (37 °C) and accelerated (45 °C) testing conditions. Notably, only the accelerated USP apparatus 4 method showed good reproducibility for highly porous risperidone microspheres. These results indicated that the accelerated USP apparatus 4 method is an appropriate fast quality control tool for long-acting PLGA microspheres (even with porous structures). Copyright © 2015 Elsevier B.V. All rights reserved.

  10. Morphology-dependent resonances of a microsphere-optical fiber system

    Science.gov (United States)

    Griffel, Giora; Arnold, Stephen; Taskent, Dogan; Serpengüzel, Ali; Connolly, John; Morris, Nancy

    1996-05-01

    Morphology-dependent resonances of microspheres sitting upon an index-matched single-mode fiber half-coupler are excited by a tunable 753-nm distributed-feedback laser. Resonance peaks in the scattering spectra and associated dips in the transmission spectra for the TE and TM modes are observed. We present a new model that describes this interaction in terms of the fiber-sphere coupling coefficient and the microsphere's intrinsic quality factor Q0 . This model enables us to obtain expressions for the finesse and the Q factor of the composite particle-fiber system, the resonance width, and the depth of the dips measured in the transmission spectra. Our model shows that index matching improves the coupling efficiency by more than a factor of 2 compared with that of a non-index-matched system.

  11. Magnetic poly(glycidyl methacrylate) microspheres for protein capture.

    Science.gov (United States)

    Koubková, Jana; Müller, Petr; Hlídková, Helena; Plichta, Zdeněk; Proks, Vladimír; Vojtěšek, Bořivoj; Horák, Daniel

    2014-09-25

    The efficient isolation and concentration of protein antigens from complex biological samples is a critical step in several analytical methods, such as mass spectrometry, flow cytometry and immunochemistry. These techniques take advantage of magnetic microspheres as immunosorbents. The focus of this study was on the development of new superparamagnetic polymer microspheres for the specific isolation of the tumor suppressor protein p53. Monodisperse macroporous poly(glycidyl methacrylate) (PGMA) microspheres measuring approximately 5 μm and containing carboxyl groups were prepared by multistep swelling polymerization of glycidyl methacrylate (GMA), 2-[(methoxycarbonyl)methoxy]ethyl methacrylate (MCMEMA) and ethylene dimethylacrylate (EDMA) as a crosslinker in the presence of cyclohexyl acetate as a porogen. To render the microspheres magnetic, iron oxide was precipitated within their pores; the Fe content in the particles received ∼18 wt%. Nonspecific interactions between the magnetic particles and biological media were minimized by coating the microspheres with poly(ethylene glycol) (PEG) terminated by carboxyl groups. The carboxyl groups of the magnetic PGMA microspheres were conjugated with primary amino groups of mouse monoclonal DO-1 antibody using conventional carbodiimide chemistry. The efficiency of protein p53 capture and the degree of nonspecific adsorption on neat and PEG-coated magnetic microspheres were determined by western blot analysis. Copyright © 2014 Elsevier B.V. All rights reserved.

  12. An electromechanically coupled micro-sphere framework: application to the finite element analysis of electrostrictive polymers

    International Nuclear Information System (INIS)

    Thylander, Sara; Menzel, Andreas; Ristinmaa, Matti

    2012-01-01

    The number of industrial applications of electroactive polymers (EAPs) is increasing and, consequently, the need for reliable modelling frameworks for such materials as well as related robust simulation techniques continuously increases. In this context, we combine the modelling of non-linear electroelasticity with a computational micro-sphere formulation in order to simulate the behaviour of EAPs. The micro-sphere approach in general enables the use of physics-based constitutive models like, for instance, the so-called worm-like chain model. By means of the micro-sphere formulation, scalar-valued micromechanical constitutive relations can conveniently be extended to a three-dimensional continuum setting. We discuss several electromechanically coupled numerical examples and make use of the finite element method to solve inhomogeneous boundary value problems. The incorporated material parameters are referred to experimental data for an electrostrictive polymer. The numerical examples show that the coupled micro-sphere formulation combined with the finite element method results in physically sound simulations that mimic the behaviour of an electrostrictive polymer. (paper)

  13. Core/shell cellulose-based microspheres for oral administration of Ketoprofen Lysinate.

    Science.gov (United States)

    Guarino, Vincenzo; Caputo, Tania; Calcagnile, Paola; Altobelli, Rosaria; Demitri, Christian; Ambrosio, Luigi

    2018-01-26

    Herein, we propose the fabrication of a new carrier with core/shell structure-inner core of cellulose acetate (CA) coated by a micrometric layer of chitosan (CS)-fabricated through an integrated process, which combines Electro Dynamic Atomization (EDA) and layer-by-layer (LbL) technique. We demonstrate that CA based microspheres possess a unique capability to relevantly retain the drugs-that is, Ketoprofen Lysinate (KL)-along the gastric tract, while providing a massive release along the intestine. CS shell slightly influences the morphology and water retention under different pH conditions, improving drug encapsulation without compromising drug release kinetics. In vitro studies in simulated gastric and intestine fluids (SGF, SIF) with physiological enzymes, show a moderate release of LSK during the first 2 h (ca. 20% at pH 2), followed by a sustained release during the next 6 h (ca. 80% at pH 7). The obtained results demonstrate that CA-based microspheres hold strong potential to be used as carriers for a delayed oral administration of anti-inflammatory drugs. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2018. © 2018 Wiley Periodicals, Inc.

  14. Albumin microspheres labeled with Ga-67 by chelation: concise communication

    International Nuclear Information System (INIS)

    Hnatowich, D.J.; Schlegel, P.

    1981-01-01

    Albumin microspheres have been synthesized with EDTA and DTPA chelating groups covalently bound to their surface. The microspheres may be labeled with Ga-67 at high yield (97 +- 2%) by transcomplexation from a 0.1 M Ga-67 acetate solution. With EDTA microspheres the resulting label dissociates only slightly after 24 hr in 50% plasma at 37 0 C, whereas with DTPA microspheres the label shows no detectable dissociation over this period. By contrast, microspheres without chelating groups lose their label virtually completely under these conditions. Following intravenous administration of sized Ga-67 DTPA microspheres in mice, about (84 +- 16)% of the activity localizes in the lungs at 5 min, with (60 +- 7)% remaining after 2 h. Since labeling is by chelation, the microspheres may also be tagged with other metallic radionuclides

  15. Momordica charantia Inhibits Inflammatory Responses in Murine Macrophages via Suppression of TAK1.

    Science.gov (United States)

    Yang, Woo Seok; Yang, Eunju; Kim, Min-Jeong; Jeong, Deok; Yoon, Deok Hyo; Sung, Gi-Ho; Lee, Seungihm; Yoo, Byong Chul; Yeo, Seung-Gu; Cho, Jae Youl

    2018-01-01

    Momordica charantia known as bitter melon is a representative medicinal plant reported to exhibit numerous pharmacological activities such as antibacterial, antidiabetic, anti-inflammatory, anti-oxidant, antitumor, and hypoglycemic actions. Although this plant has high ethnopharmacological value for treating inflammatory diseases, the molecular mechanisms by which it inhibits the inflammatory response are not fully understood. In this study, we aim to identify the anti-inflammatory mechanism of this plant. To this end, we studied the effects of its methanol extract (Mc-ME) on lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Specifically, we evaluated nitric oxide (NO) production, mRNA expression of inflammatory genes, luciferase reporter gene activity, and putative molecular targets. Mc-ME blocked NO production in a dose-dependent manner in RAW264.7 cells; importantly, no cytotoxicity was observed. Moreover, the mRNA expression levels of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 were decreased by Mc-ME treatment in a dose-dependent manner. Luciferase assays and nuclear lysate immunoblotting analyses strongly indicated that Mc-ME decreases the levels of p65 [a nuclear factor (NF)-[Formula: see text]B subunit] and c-Fos [an activator protein (AP)-1 subunit]. Whole lysate immunoblotting assays, luciferase assays, and overexpression experiments suggested that transforming growth factor [Formula: see text]-activated kinase 1 (TAK1) is targeted by Mc-ME, thereby suppressing NF-[Formula: see text]B and AP-1 activity via downregulation of extracellular signal-regulated kinases (ERKs) and AKT. These results strongly suggest that Mc-ME exerts its anti-inflammatory activity by reducing the action of TAK1, which also affects the activation of NF-[Formula: see text]B and AP-1.

  16. Fermented non-digestible fraction from combined nixtamalized corn (Zea mays L.)/cooked common bean (Phaseolus vulgaris L.) chips modulate anti-inflammatory markers on RAW 264.7 macrophages.

    Science.gov (United States)

    Luzardo-Ocampo, I; Campos-Vega, R; Cuellar-Nuñez, M L; Vázquez-Landaverde, P A; Mojica, L; Acosta-Gallegos, J A; Loarca-Piña, G

    2018-09-01

    Chronic non-communicable diseases (NCDs) are low-level inflammation processes affected by several factors including diet. It has been reported that mixed whole grain and legume consumption, e.g. corn and common bean, might be a beneficial combination due to its content of bioactive compounds. A considerable amount would be retained in the non-digestible fraction (NDF), reaching the colon, where microbiota produce short-chain fatty acids (SCFAs) and phenolic compounds (PC) with known anti-inflammatory effect. The aim of this study was to estimate the anti-inflammatory potential of fermented-NDF of corn-bean chips (FNDFC) in RAW 264.7 macrophages. After 24 h, FNDFC produced SCFAs (0.156-0.222 mmol/l), inhibited nitric oxide production > 80% and H 2 O 2  > 30%, up-regulated anti-inflammatory cytokines (I-TAC, TIMP-1) > 2-fold, and produced angiostatic and protective factors against vascular/tissue damage, and amelioration of tumor necrosis factor signalling and inflammatory bowel disease. These results confirm the anti-inflammatory potential derived from healthy corn-bean chips. Copyright © 2018. Published by Elsevier Ltd.

  17. Photoluminescence and lasing in whispering gallery mode glass microspherical resonators

    Energy Technology Data Exchange (ETDEWEB)

    Ristić, D. [Ruđer Bošković Institute, Division of Materials Physics, Laboratory for Molecular Physics, Bijenička c. 54, Zagreb (Croatia); Center of Excellence for Advanced Materials and Sensing Devices, Research unit New Functional Materials, Bijenička c. 54, Zagreb (Croatia); Berneschi, S.; Camerini, M. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Farnesi, D.; Pelli, S. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy); Trono, C. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Chiappini, A.; Chiasera, A.; Ferrari, M. [CSMFO Group, Istituto di Fotonica e Nanotecnologie, IFN-CNR, Via alla Cascata 56/C, 38050 Povo-Trento (Italy); Lukowiak, A. [Institute of Low Temperature and Structure Research, PAS, ul. Okolna 2, Wroclaw 50-950 (Poland); Dumeige, Y.; Féron, P. [Laboratoire d' Optronique, (CNRS-UMR 6082-Foton), ENSSAT, 6 rue de Kérampont, 22300 Lannion (France); Righini, G.C. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy); Soria, S., E-mail: s.soria@ifac.cnr.it [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Conti, G. Nunzi [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy)

    2016-02-15

    We report experimental results regarding the development of Er{sup 3+}-doped glass microspherical cavities for the fabrication of compact sources at 1.55 μm. We investigate several different approaches in order to fabricate the microspheres including direct melting of Er{sup 3+}-doped glass powders, synthesis of Er{sup 3+}-doped monolithic microspheres by drawing Er{sup 3+}-doped glass, and coating of silica microspheres with an Er{sup 3+}-doped sol–gel layer. Details of the different fabrication processes are presented together with the photoluminescence characterization in free space configuration of the microspheres and of the glass precursor. We have analyzed the photoluminescence spectra of the whispering gallery modes of the microspheres excited using evanescent coupling and we demonstrate tunable laser action in a wide range of wavelengths around 1.55 μm. As much as 90 μW of laser output power was measured in Er{sup 3+}-doped glass microspheres. - Highlights: • Different approaches in microsphere fabrication and various types of post-processing. • Trimming of photorefractive glass microsphere lasers with UV light. • Peak power record of 90 μW by pumping at 1480 nm.

  18. Curcumin in inflammatory diseases.

    Science.gov (United States)

    Shehzad, Adeeb; Rehman, Gauhar; Lee, Young Sup

    2013-01-01

    Curcumin (diferuloylmethane), a yellow coloring agent extracted from turmeric is also used as a remedy for the treatment and prevention of inflammatory diseases. Acute and chronic inflammation is a major factor in the progression of obesity, type II diabetes, arthritis, pancreatitis, cardiovascular, neurodegenerative and metabolic diseases, as well as certain types of cancer. Turmeric has a long history of use in Ayurvedic medicine for the treatment of inflammatory disorders. Recent studies on the efficacy and therapeutic applicability of turmeric have suggested that the active ingredient of tumeric is curcumin. Further, compelling evidence has shown that curcumin has the ability to inhibit inflammatory cell proliferation, invasion, and angiogenesis through multiple molecular targets and mechanisms of action. Curcumin is safe, non-toxic, and mediates its anti-inflammatory effects through the down-regulation of inflammatory transcription factors, cytokines, redox status, protein kinases, and enzymes that all promote inflammation. In addition, curcumin induces apoptosis through mitochondrial and receptor-mediated pathways, as well as activation of caspase cascades. In the current study, the anti-inflammatory effects of curcumin were evaluated relative to various chronic inflammatory diseases. Based on the available pharmacological data obtained from in vitro and in vivo research, as well as clinical trials, an opportunity exists to translate curcumin into clinics for the prevention of inflammatory diseases in the near future. Copyright © 2012 International Union of Biochemistry and Molecular Biology, Inc.

  19. Optically Levitated Microspheres as a Probe for New Interactions

    Science.gov (United States)

    Rider, Alexander; Moore, David; Blakemore, Charles; Lu, Marie; Gratta, Giorgio

    2016-03-01

    We are developing novel techniques to probe new interactions at micron distances using optically levitated dielectric microspheres. Levitated microspheres are an ideal probe for short-range interactions because they are suspended using the radiation pressure at the focus of a laser beam, which means that the microspheres can be precisely manipulated and isolated from the surrounding environment at high vacuum. We have performed a search for unknown charged particles bound within the bulk of the microspheres. Currently, we are searching for the presence of a Chameleon field postulated to explain the presence of dark energy in the universe. In the future we plan to use optically levitated microspheres to search for micron length-scale gravity like interactions that could couple between a microsphere and another mass. We will present resent results from these experiments and plans for future searches for new interactions.

  20. Silicon Microspheres Photonics

    International Nuclear Information System (INIS)

    Serpenguzel, A.

    2008-01-01

    Electrophotonic integrated circuits (EPICs), or alternatively, optoelectronic integrated circuit (OEICs) are the natural evolution of the microelectronic integrated circuit (IC) with the addition of photonic capabilities. Traditionally, the IC industry has been based on group IV silicon, whereas the photonics industry on group III-V semiconductors. However, silicon based photonic microdevices have been making strands in siliconizing photonics. Silicon microspheres with their high quality factor whispering gallery modes (WGMs), are ideal candidates for wavelength division multiplexing (WDM) applications in the standard near-infrared communication bands. In this work, we will discuss the possibility of using silicon microspheres for photonics applications in the near-infrared

  1. Randomized trial of switching from prescribed non-selective non-steroidal anti-inflammatory drugs to prescribed celecoxib

    DEFF Research Database (Denmark)

    Macdonald, Thomas M; Hawkey, Chris J; Ford, Ian

    2017-01-01

    BACKGROUND: Selective cyclooxygenase-2 inhibitors and conventional non-selective non-steroidal anti-inflammatory drugs (nsNSAIDs) have been associated with adverse cardiovascular (CV) effects. We compared the CV safety of switching to celecoxib vs. continuing nsNSAID therapy in a European setting...

  2. Preparation of UN microspheres by internal gelation process

    Energy Technology Data Exchange (ETDEWEB)

    Shirasu, Yoshiro; Yamagishi, Shigeru [Japan Atomic Energy Research Inst., Tokai, Ibaraki (Japan). Tokai Research Establishment

    1997-07-01

    UN microspheres were prepared from (UO{sub 3}+C) microspheres internally gelled in a hot silicone oil column. The gel microspheres were calcined at 480degC in nitrogen, after washing and drying. The calcined ones were carbothermically nitrided at 1400-1800degC in a nitrogen-based atmosphere in two ways: one in N{sub 2} followed by N{sub 2}-8%H{sub 2}, and the other in N{sub 2}-8%H{sub 2} only. In both cases, highly pure UN microspheres around 500 ppm of both oxygen and carbon impurities were obtained, although their densities were still low. (author)

  3. A template-free method for stable CuO hollow microspheres fabricated from a metal organic framework (HKUST-1).

    Science.gov (United States)

    Zhang, Suoying; Liu, Hong; Liu, Pengfei; Yang, Zhuhong; Feng, Xin; Huo, Fengwei; Lu, Xiaohua

    2015-06-07

    Uniform CuO hollow microspheres were successfully achieved from a non-uniform metal organic framework by using a template-free method. The process mechanism has been revealed to be spherical aggregation and Ostwald ripening. When tested in CO oxidation and heat treatment, these assembled microspheres exhibited an excellent catalytic performance and show a much better stability than the inherited hollow structure from MOFs.

  4. Microsphere-based super-resolution scanning optical microscope.

    Science.gov (United States)

    Huszka, Gergely; Yang, Hui; Gijs, Martin A M

    2017-06-26

    High-refractive index dielectric microspheres positioned within the field of view of a microscope objective in a dielectric medium can focus the light into a so-called photonic nanojet. A sample placed in such nanojet can be imaged by the objective with super-resolution, i.e. with a resolution beyond the classical diffraction limit. However, when imaging nanostructures on a substrate, the propagation distance of a light wave in the dielectric medium in between the substrate and the microsphere must be small enough to reveal the sample's nanometric features. Therefore, only the central part of an image obtained through a microsphere shows super-resolution details, which are typically ∼100 nm using white light (peak at λ = 600 nm). We have performed finite element simulations of the role of this critical distance in the super-resolution effect. Super-resolution imaging of a sample placed beneath the microsphere is only possible within a very restricted central area of ∼10 μm 2 , where the separation distance between the substrate and the microsphere surface is very small (∼1 μm). To generate super-resolution images over larger areas of the sample, we have fixed a microsphere on a frame attached to the microscope objective, which is automatically scanned over the sample in a step-by-step fashion. This generates a set of image tiles, which are subsequently stitched into a single super-resolution image (with resolution of λ/4-λ/5) of a sample area of up to ∼10 4 μm 2 . Scanning a standard optical microscope objective with microsphere therefore enables super-resolution microscopy over the complete field-of-view of the objective.

  5. Optimization of sustained release aceclofenac microspheres using response surface methodology

    Energy Technology Data Exchange (ETDEWEB)

    Deshmukh, Rameshwar K.; Naik, Jitendra B., E-mail: jitunaik@gmail.com

    2015-03-01

    Polymeric microspheres containing aceclofenac were prepared by single emulsion (oil-in-water) solvent evaporation method using response surface methodology (RSM). Microspheres were prepared by changing formulation variables such as the amount of Eudragit® RS100 and the amount of polyvinyl alcohol (PVA) by statistical experimental design in order to enhance the encapsulation efficiency (E.E.) of the microspheres. The resultant microspheres were evaluated for their size, morphology, E.E., and in vitro drug release. The amount of Eudragit® RS100 and the amount of PVA were found to be significant factors respectively for determining the E.E. of the microspheres. A linear mathematical model equation fitted to the data was used to predict the E.E. in the optimal region. Optimized formulation of microspheres was prepared using optimal process variables setting in order to evaluate the optimization capability of the models generated according to IV-optimal design. The microspheres showed high E.E. (74.14 ± 0.015% to 85.34 ± 0.011%) and suitably sustained drug release (minimum; 40% to 60%; maximum) over a period of 12 h. The optimized microspheres formulation showed E.E. of 84.87 ± 0.005 with small error value (1.39). The low magnitudes of error and the significant value of R{sup 2} in the present investigation prove the high prognostic ability of the design. The absence of interactions between drug and polymers was confirmed by Fourier transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRPD) revealed the dispersion of drug within microspheres formulation. The microspheres were found to be discrete, spherical with smooth surface. The results demonstrate that these microspheres could be promising delivery system to sustain the drug release and improve the E.E. thus prolong drug action and achieve the highest healing effect with minimal gastrointestinal side effects. - Highlights: • Aceclofenac microspheres

  6. Preparation of polymer microspheres by radiation-induced polymerization

    International Nuclear Information System (INIS)

    Naka, Y.; Yamamoto, Y.; Yoshida, Y.; Tagawa, S.

    1995-01-01

    Cross-liking monomer, diethylene glycol dimethacrylate gives microspheres from organic solution by radiation-induced polymerization. /One of the remarkable result is that the number of the microspheres is not changing during the polymerization. Ethyl methacrylate, maleic anhydride, styrene and acrylamide are used as comonomers. These comonomers give the microspheres in the range of 0 to 0.4 as mol fractions. (author)

  7. Thioredoxin ameliorates cutaneous inflammation by regulating the epithelial production and release of pro-Inflammatory cytokines

    Directory of Open Access Journals (Sweden)

    Hai eTian

    2013-09-01

    Full Text Available Human thioredoxin-1 (TRX is a 12-kDa protein with redox-active dithiol in the active site -Cys-Gly-Pro-Cys-. It has been demonstrated that systemic administration and transgenic overexpression of TRX ameliorate inflammation in various animal models, but its anti-inflammatory mechanism is not well characterized. We investigated the anti-inflammatory effects of topically applied recombinant human TRX (rhTRX in a murine irritant contact dermatitis (ICD induced by croton oil. Topically applied rhTRX was distributed only in the skin tissues under both non-inflammatory and inflammatory conditions, and significantly suppressed the inflammatory response by inhibiting the production of cytokines and chemokines, such as TNF-α, Il-1β, IL-6, CXCL-1, and MCP-1. In an in vitro study, rhTRX also significantly inhibited the formation of cytokines and chemokines produced by keratinocytes after exposure to croton oil and phorbol 12-myristate 13-acetate. These results indicate that TRX prevents skin inflammation via the inhibition of local formation of inflammatory cytokines and chemokines. As a promising new approach, local application of TRX may be useful for the treatment of various skin and mucosal inflammatory disorders.

  8. An antisense peptide nucleic acid against Pseudomonas aeruginosa inhibiting bacterial-induced inflammatory responses in the cystic fibrosis IB3-1 cellular model system

    DEFF Research Database (Denmark)

    Montagner, Giulia; Bezzerri, Valentino; Cabrini, Giulio

    2017-01-01

    of the essential acpP gene of P. aeruginosa, and previously shown to inhibit bacterial growth, concomitantly also strongly inhibits induced up-regulation of the pro-inflammatory markers IL-8, IL-6, G-CSF, IFN-γ, IP-10, MCP-1 and TNF-α in IB3-1 cystic fibrosis cells infected by P. aeruginosa PAO1. Remarkably...... are significant considering the key role of this protein in the cystic fibrosis inflammatory process exacerbated by P. aeruginosa infection....

  9. Cardiovascular safety of non-steroidal anti-inflammatory drugs: network meta-analysis.

    Science.gov (United States)

    Trelle, Sven; Reichenbach, Stephan; Wandel, Simon; Hildebrand, Pius; Tschannen, Beatrice; Villiger, Peter M; Egger, Matthias; Jüni, Peter

    2011-01-11

    To analyse the available evidence on cardiovascular safety of non-steroidal anti-inflammatory drugs. Network meta-analysis. Bibliographic databases, conference proceedings, study registers, the Food and Drug Administration website, reference lists of relevant articles, and reports citing relevant articles through the Science Citation Index (last update July 2009). Manufacturers of celecoxib and lumiracoxib provided additional data. All large scale randomised controlled trials comparing any non-steroidal anti-inflammatory drug with other non-steroidal anti-inflammatory drugs or placebo. Two investigators independently assessed eligibility. The primary outcome was myocardial infarction. Secondary outcomes included stroke, death from cardiovascular disease, and death from any cause. Two investigators independently extracted data. 31 trials in 116 429 patients with more than 115 000 patient years of follow-up were included. Patients were allocated to naproxen, ibuprofen, diclofenac, celecoxib, etoricoxib, rofecoxib, lumiracoxib, or placebo. Compared with placebo, rofecoxib was associated with the highest risk of myocardial infarction (rate ratio 2.12, 95% credibility interval 1.26 to 3.56), followed by lumiracoxib (2.00, 0.71 to 6.21). Ibuprofen was associated with the highest risk of stroke (3.36, 1.00 to 11.6), followed by diclofenac (2.86, 1.09 to 8.36). Etoricoxib (4.07, 1.23 to 15.7) and diclofenac (3.98, 1.48 to 12.7) were associated with the highest risk of cardiovascular death. Although uncertainty remains, little evidence exists to suggest that any of the investigated drugs are safe in cardiovascular terms. Naproxen seemed least harmful. Cardiovascular risk needs to be taken into account when prescribing any non-steroidal anti-inflammatory drug.

  10. Preparation of nano-hydroxyapatite/poly(l-lactide) biocomposite microspheres

    International Nuclear Information System (INIS)

    Qiu Xueyu; Han Yadong; Zhuang Xiuli; Chen Xuesi; Li Yuesheng; Jing Xiabin

    2007-01-01

    Nano-hydroxyapatite (HA)/poly(l-lactide) (PLLA) composite microspheres with relatively uniform size distribution were prepared by a solid-in-oil-in-water (s/o/w) emusion solvent evaporation method. The encapsulation of the HA nanopaticles in microshperes was significantly improved by grafting PLLA on the surface of the HA nanoparticles (p-HA) during emulsion process. This procedure gave a possibility to obtain p-HA/PLLA composite microspheres with uniform morphology and the encapsulated p-HA nanoparticle loading reached up to 40 wt% (33 wt% of pure HA) in the p-HA/PLLA composite microspheres. The microstructure of composite microspheres from core-shell to single phase changed with the variation of p-HA to PLLA ratios. p-HA/PLLA composite microspheres with the diameter range of 2-3 μm were obtained. The entrapment efficiency of p-HA in microspheres could high up to 90 wt% and that of HA was only 13 wt%. Surface and bulk characterizations of the composite microspheres were performed by measurements such as wide angle X-ray diffraction (WAXD), thermal gravimetric analysis (TGA), environmental scanning electron microscope (ESEM) and transmission electron microscopy (TEM)

  11. PREPARATION AND CHARACTERIZATION OF POROUS WALLED HOLLOW GLASS MICROSPHERES

    Energy Technology Data Exchange (ETDEWEB)

    Raszewski, F; Erich Hansen, E; Ray Schumacher, R; David Peeler, D

    2008-04-21

    Porous-walled hollow glass microspheres (PWHGMs) of a modified alkali borosilicate composition have been successfully fabricated by combining the technology of producing hollow glass microspheres (HGMs) with the knowledge associated with porous glasses. HGMs are first formed by a powder glass--flame process, which are then transformed to PWHGMs by heat treatment and subsequent treatment in acid. Pore diameter and pore volume are most influenced by heat treatment temperature. Pore diameter is increased by a factor of 10 when samples are heat treated prior to acid leaching; 100 {angstrom} in non-heat treated samples to 1000 {angstrom} in samples heat treated at 600 C for 8 hours. As heat treatment time is increased from 8 hours to 24 hours there is a slight shift increase in pore diameter and little or no change in pore volume.

  12. Hypersensitivity to non-steroidal anti-inflammatory drugs (NSAIDs)

    DEFF Research Database (Denmark)

    Nissen, Christoffer V; Bindslev-Jensen, Carsten; Mørtz, Charlotte G

    2015-01-01

    BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are reported to be the second most common cause of drug hypersensitivity. In 2011, experts from the EAACI/ENDA group and GA(2)LEN proposed a new classification system for NSAID hypersensitivity. The aim of this study was to classify...... responders reacted to non-pyrazolone drugs. Only one patient could not be classified according to the EAACI/ENDA system. An overlap between respiratory and cutaneous symptoms was found in 15/39 (38%) of patients. CONCLUSIONS: All but one of our patients could be classified according to the EAACI...

  13. Prolonged pharmacological inhibition of cathepsin C results in elimination of neutrophil serine proteases

    DEFF Research Database (Denmark)

    Guarino, Carla; Hamon, Yveline; Croix, Cécile

    2017-01-01

    cyclopropyl nitrile CatC inhibitor almost totally lack elastase. We confirmed the elimination of neutrophil elastase-like proteases by prolonged inhibition of CatC in a non-human primate. We also showed that neutrophils lacking elastase-like protease activities were still recruited to inflammatory sites....... These preclinical results demonstrate that the disappearance of neutrophil elastase-like proteases as observed in PLS patients can be achieved by pharmacological inhibition of bone marrow CatC. Such a transitory inhibition of CatC might thus help to rebalance the protease load during chronic inflammatory diseases...

  14. Dexmedetomidine Inhibits Inflammatory Reaction in Lung Tissues of Septic Rats by Suppressing TLR4/NF-κB Pathway

    Directory of Open Access Journals (Sweden)

    Yuqing Wu

    2013-01-01

    and 20 μg/kg significantly decreased mortality and pulmonary inflammation of septic rats, as well as suppressed CLP-induced elevation of TNF-α and IL-6 and inhibited TLR4/MyD88 expression and NF-κB activation. These results suggest that dexmedetomidine may decrease mortality and inhibit inflammatory reaction in lung tissues of septic rats by suppressing TLR4/MyD88/NF-κB pathway.

  15. Thermal analysis of iron hydroxide microspheres

    International Nuclear Information System (INIS)

    Turcanu, C.N.; Cornescu, M.

    1979-03-01

    The thermal treatment is an important step in the preparative technology of the iron oxids microspheres with well established mechanical, physical and chemical characteristics. The first indications on the heating procedure have been obtained from the thermal analysis on iron hydroxide microspheres prepared by the support precipitation and internal gelification methods. (author)

  16. Active spice-derived components can inhibit inflammatory responses of adipose tissue in obesity by suppressing inflammatory actions of macrophages and release of monocyte chemoattractant protein-1 from adipocytes.

    Science.gov (United States)

    Woo, Hae-Mi; Kang, Ji-Hye; Kawada, Teruo; Yoo, Hoon; Sung, Mi-Kyung; Yu, Rina

    2007-02-13

    Inflammation plays a key role in obesity-related pathologies such as cardiovascular disease, type II diabetes, and several types of cancer. Obesity-induced inflammation entails the enhancement of the recruitment of macrophages into adipose tissue and the release of various proinflammatory proteins from fat tissue. Therefore, the modulation of inflammatory responses in obesity may be useful for preventing or ameliorating obesity-related pathologies. Some spice-derived components, which are naturally occurring phytochemicals, elicit antiobesity and antiinflammatory properties. In this study, we investigated whether active spice-derived components can be applied to the suppression of obesity-induced inflammatory responses. Mesenteric adipose tissue was isolated from obese mice fed a high-fat diet and cultured to prepare an adipose tissue-conditioned medium. Raw 264.7 macrophages were treated with the adipose tissue-conditioned medium with or without active spice-derived components (i.e., diallyl disulfide, allyl isothiocyanate, piperine, zingerone and curcumin). Chemotaxis assay was performed to measure the degree of macrophage migration. Macrophage activation was estimated by measuring tumor necrosis factor-alpha (TNF-alpha), nitric oxide, and monocyte chemoattractant protein-1 (MCP-1) concentrations. The active spice-derived components markedly suppressed the migration of macrophages induced by the mesenteric adipose tissue-conditioned medium in a dose-dependent manner. Among the active spice-derived components studied, allyl isothiocyanate, zingerone, and curcumin significantly inhibited the cellular production of proinflammatory mediators such as TNF-alpha and nitric oxide, and significantly inhibited the release of MCP-1 from 3T3-L1 adipocytes. Our findings suggest that the spice-derived components can suppress obesity-induced inflammatory responses by suppressing adipose tissue macrophage accumulation or activation and inhibiting MCP-1 release from adipocytes

  17. Nanomechanics of biocompatible hollow thin-shell polymer microspheres.

    Science.gov (United States)

    Glynos, Emmanouil; Koutsos, Vasileios; McDicken, W Norman; Moran, Carmel M; Pye, Stephen D; Ross, James A; Sboros, Vassilis

    2009-07-07

    The nanomechanical properties of biocompatible thin-shell hollow polymer microspheres with approximately constant ratio of shell thickness to microsphere diameter were measured by nanocompression tests in aqueous conditions. These microspheres encapsulate an inert gas and are used as ultrasound contrast agents by releasing free microbubbles in the presence of an ultrasound field as a result of free gas leakage from the shell. The tests were performed using an atomic force microscope (AFM) employing the force-distance curve technique. An optical microscope, on which the AFM was mounted, was used to guide the positioning of tipless cantilevers on top of individual microspheres. We performed a systematic study using several cantilevers with spring constants varying from 0.08 to 2.3 N/m on a population of microspheres with diameters from about 2 to 6 microm. The use of several cantilevers with various spring constants allowed a systematic study of the mechanical properties of the microsphere thin shell at different regimes of force and deformation. Using thin-shell mechanics theory for small deformations, the Young's modulus of the thin wall material was estimated and was shown to exhibit a strong size effect: it increased as the shell became thinner. The Young's modulus of thicker microsphere shells converged to the expected value for the macroscopic bulk material. For high applied forces, the force-deformation profiles showed a reversible and/or irreversible nonlinear behavior including "steps" and "jumps" which were attributed to mechanical instabilities such as buckling events.

  18. N-Acetylcysteine enhances the action of anti-inflammatory drugs as suppressors of prostaglandin production in monocytes

    Directory of Open Access Journals (Sweden)

    Erica Hoffer

    2002-01-01

    Full Text Available The anti-inflammatory effect of non-steroidal anti-inflammatory drugs (NSAIDs is associated with inhibition of cyclooxygenase (COX, the rate-limiting enzyme responsible for the synthesis of prostaglandins. Since oxygen free radicals can act as second cellular messengers, especially to modulate the metabolism of arachidonic acid and the prostaglandin tract, it seems plausible that antioxidants might affect the production of prostaglandin by activated cells. This research is focused on the effect of the antioxidant N-acetylcysteine (NAC on the inhibition of prostaglandin E2 formation in activated monocytes by specific and non-specific COX inhibitors. We found that lipopolysaccharide-induced prostaglandin E2 formation was significantly reduced by rofecoxib and by diclofenac, two NSAIDs. Addition of NAC to each of these drugs enhanced the effect of the NSAIDs. These results suggest that one might expect either a potentiation of the anti-inflammatory effect of COX inhibitors by their simultaneous administration with NAC, or obtaining the same anti-inflammatory at lower drug levels.

  19. Anti-metastatic Action of Non-steroidal Anti-inflammatory Drugs

    Directory of Open Access Journals (Sweden)

    Wen-Chun Hung

    2008-08-01

    Full Text Available Epidemiological studies suggest that nonsteroidal anti-inflammatory drugs (NSAIDs reduce the incidence and mortality of several types of human cancer. However, the molecular mechanisms by which NSAIDs exert their chemopreventive and anticancer effects are not fully understood. Cyclooxygenase 1 (COX-1 and COX-2 are the main targets for NSAIDs. Recent studies demonstrate that COX-2 is overexpressed in many human cancers and may promote tumorigenesis via: (1 stimulation of cancer cell proliferation; (2 increase of tumor angiogenesis; (3 prevention of cancer cell apoptosis; (4 modulation of immunoregulatory reactions; and (5 enhancement of tumor metastasis. NSAIDs may target the signaling molecules (from upstream activators to downstream effectors involved in these mechanisms to attenuate the development and progression of cancer. In this review, we discuss the recent findings with regard to the mechanisms by which NSAIDs inhibit tumorigenesis and will specifically focus on the elucidation of NSAID-induced inhibition of tumor metastasis.

  20. Inhibition of Pro-inflammatory and Anti-apoptotic Biomarkers during Experimental Oral Cancer Chemoprevention by Dietary Black Raspberries

    Directory of Open Access Journals (Sweden)

    Steve Oghumu

    2017-10-01

    Full Text Available Oral cancer continues to be a significant public health problem worldwide. Recently conducted clinical trials demonstrate the ability of black raspberries (BRBs to modulate biomarkers of molecular efficacy that supports a chemopreventive strategy against oral cancer. However, it is essential that a preclinical animal model of black raspberry (BRB chemoprevention which recapitulates human oral carcinogenesis be developed, so that we can validate biomarkers and evaluate potential mechanisms of action. We therefore established the ability of BRBs to inhibit oral lesion formation in a carcinogen-induced rat oral cancer model and examined potential mechanisms. F344 rats were administered 4-nitroquinoline 1-oxide (4NQO (20 µg/ml in drinking water for 14 weeks followed by regular drinking water for 6 weeks. At week 14, rats were fed a diet containing either 5 or 10% BRB, or 0.4% ellagic acid (EA, a BRB phytochemical. Dietary administration of 5 and 10% BRB reduced oral lesion incidence and multiplicity by 39.3 and 28.6%, respectively. Histopathological analyses demonstrate the ability of BRBs and, to a lesser extent EA, to inhibit the progression of oral cancer. Oral lesion inhibition by BRBs was associated with a reduction in the mRNA expression of pro-inflammatory biomarkers Cxcl1, Mif, and Nfe2l2 as well as the anti-apoptotic and cell cycle associated markers Birc5, Aurka, Ccna1, and Ccna2. Cellular proliferation (Ki-67 staining in tongue lesions was inhibited by BRBs and EA. Our study demonstrates that, in the rat 4NQO oral cancer model, dietary administration of BRBs inhibits oral carcinogenesis via inhibition of pro-inflammatory and anti-apoptotic pathways.

  1. Anti-Inflammatory Effect of Malva sylvestris, Sida cordifolia, and Pelargonium graveolens Is Related to Inhibition of Prostanoid Production.

    Science.gov (United States)

    Martins, Cleverson Antonio Ferreira; Campos, Michel Leandro; Irioda, Ana Carolina; Stremel, Dile Pontarolo; Trindade, Angela Cristina Leal Badaró; Pontarolo, Roberto

    2017-11-03

    The ability of plant extracts and preparations to reduce inflammation has been proven by different means in experimental models. Since inflammation enhances the release of specific mediators, inhibition of their production can be used to investigate the anti-inflammatory effect of plants widely used in folk medicine for this purpose. The study was performed for leaves and flowers of Malva sylvestris , and leaves of Sida cordifolia and Pelargonium graveolens . These are three plant species known in Brazil as Malva. The anti-inflammatory activity of extracts and fractions (hexane, chloroform, ethyl acetate, and residual) was evaluated by quantitation of prostaglandins (PG) PGE₂, PGD₂, PGF 2α , and thromboxane B₂ (the stable nonenzymatic product of TXA₂) concentration in the supernatant of lipopolysaccharide (LPS)- induced RAW 264.7 cells. Inhibition of anti-inflammatory mediator release was observed for plants mainly in the crude extract, ethyl acetate fraction, and residual fraction. The results suggest superior activity of S. cordifolia , leading to significantly lower values of all mediators after treatment with its residual fraction, even at the lower concentration tested (10 μg/mL). M. sylvestris and P. graveolens showed similar results, such as the reduction of all mediators after treatment, with leaf crude extracts (50 μg/mL). These results suggest that the three species known as Malva have anti-inflammatory properties, S. cordifolia being the most potent.

  2. A novel synthetic derivative of melatonin, 5-hydroxy-2’-isobutyl-streptochlorin (HIS), inhibits inflammatory responses via regulation of TRIF-dependent signaling and inflammasome activation

    International Nuclear Information System (INIS)

    Shim, Do-Wan; Shin, Hee Jae; Han, Ji-Won; Ji, Young-Eun; Jang, Cheol-Hun; Koppula, Sushruta; Kang, Tae-Bong; Lee, Kwang-Ho

    2015-01-01

    Melatonin is substantially reported to possess anti-inflammatory properties. In the present study, we synthesized a novel melatonin derivative, 5-hydroxy-2′-isobutyl-streptochlorin (HIS), which displayed superior anti-inflammatory properties to its parent compound. Further, we explored its underlying mechanisms in cellular and experimental animal models. Lipopolysaccharide was used to induce in vitro inflammatory responses in RAW 264.7 macrophages. LPS-primed macrophages were pulsed with biologically unrelated toxic molecules to evaluate the role of HIS on inflammasome activation. In vivo verifications were carried out using acute lung injury (ALI) and Escherichia coli-induced septic shock mouse models. HIS inhibited the production of proinflammatory mediators and cytokines such as nitric oxide, cyclooxygenase 2, IL-1β, IL-6 and TNF-α in LPS-stimulated RAW 264.7 macrophages. HIS suppressed the infiltration of immune cells into the lung and the production of pro-inflammatory cytokines such as IL-6 and TNF-α in broncho-alveolar lavage fluid in the ALI mouse model. Mechanistic studies revealed that the inhibitory effects of HIS were mediated through the regulation of the TIR domain-containing, adaptor-inducing, interferon-β (TRIF)-dependent signaling pathway from toll-like receptors. Further, HIS attenuated IL-1β secretion via the inhibition of NLRP3 inflammasome activation independent of mitochondrial ROS production. Furthermore, HIS suppressed IL-1β, IL-6 and interferon-β production in peritoneal lavage in the Escherichia coli-induced sepsis mouse model. In conclusion, HIS exerted potent anti-inflammatory effects via the regulation of TRIF-dependent signaling and inflammasome activation. Notably, the superior anti-inflammatory properties of this derivative compared with its parent compound could be a promising lead for treating various inflammatory-mediated diseases. - Highlights: • Νovel compound, 5-hydroxy-2′-isobutyl-streptochlorin (HIS) was

  3. A novel synthetic derivative of melatonin, 5-hydroxy-2’-isobutyl-streptochlorin (HIS), inhibits inflammatory responses via regulation of TRIF-dependent signaling and inflammasome activation

    Energy Technology Data Exchange (ETDEWEB)

    Shim, Do-Wan [Department of Biotechnology, Research Institute of Inflammatory Disease, Konkuk University, Chungju (Korea, Republic of); Shin, Hee Jae [Marine Natural Products Chemistry Laboratory, Korea Institute of Ocean Science & Technology, Ansan (Korea, Republic of); Han, Ji-Won; Ji, Young-Eun; Jang, Cheol-Hun; Koppula, Sushruta; Kang, Tae-Bong [Department of Biotechnology, Research Institute of Inflammatory Disease, Konkuk University, Chungju (Korea, Republic of); Lee, Kwang-Ho, E-mail: kwangho@kku.ac.kr [Department of Biotechnology, Research Institute of Inflammatory Disease, Konkuk University, Chungju (Korea, Republic of)

    2015-04-15

    Melatonin is substantially reported to possess anti-inflammatory properties. In the present study, we synthesized a novel melatonin derivative, 5-hydroxy-2′-isobutyl-streptochlorin (HIS), which displayed superior anti-inflammatory properties to its parent compound. Further, we explored its underlying mechanisms in cellular and experimental animal models. Lipopolysaccharide was used to induce in vitro inflammatory responses in RAW 264.7 macrophages. LPS-primed macrophages were pulsed with biologically unrelated toxic molecules to evaluate the role of HIS on inflammasome activation. In vivo verifications were carried out using acute lung injury (ALI) and Escherichia coli-induced septic shock mouse models. HIS inhibited the production of proinflammatory mediators and cytokines such as nitric oxide, cyclooxygenase 2, IL-1β, IL-6 and TNF-α in LPS-stimulated RAW 264.7 macrophages. HIS suppressed the infiltration of immune cells into the lung and the production of pro-inflammatory cytokines such as IL-6 and TNF-α in broncho-alveolar lavage fluid in the ALI mouse model. Mechanistic studies revealed that the inhibitory effects of HIS were mediated through the regulation of the TIR domain-containing, adaptor-inducing, interferon-β (TRIF)-dependent signaling pathway from toll-like receptors. Further, HIS attenuated IL-1β secretion via the inhibition of NLRP3 inflammasome activation independent of mitochondrial ROS production. Furthermore, HIS suppressed IL-1β, IL-6 and interferon-β production in peritoneal lavage in the Escherichia coli-induced sepsis mouse model. In conclusion, HIS exerted potent anti-inflammatory effects via the regulation of TRIF-dependent signaling and inflammasome activation. Notably, the superior anti-inflammatory properties of this derivative compared with its parent compound could be a promising lead for treating various inflammatory-mediated diseases. - Highlights: • Νovel compound, 5-hydroxy-2′-isobutyl-streptochlorin (HIS) was

  4. Preparing microspheres of actinide nitrides from carbon containing oxide sols

    International Nuclear Information System (INIS)

    Triggiani, L.V.

    1975-01-01

    A process is given for preparing uranium nitride, uranium oxynitride, and uranium carboxynitride microspheres and the microspheres as compositions of matter. The microspheres are prepared from carbide sols by reduction and nitriding steps. (Official Gazette)

  5. Chitosan microspheres loaded with holmium-165 produced by spray dryer for liver cancer therapy: preliminary experiments

    International Nuclear Information System (INIS)

    Miyamoto, Douglas Massao; Pires, Geovanna; Lira, Raphael A. de; Melo, Vitor H.S.; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de; Osso Junior, Joao Alberto

    2011-01-01

    Chitosan is a biopolymer of 2-deoxy-2-amino-D-glucose that is obtained by deacetylation of chitin. It's biocompatible, biodegradable, non toxic and has antitumor activity. Chitosan has many applications, such as their microparticles that can be used to treat prostate cancer, rheumatoid arthritis, and for liver tumor brachytherapy treatment. Our group is developing different biodegradable polymer-based microspheres loaded with holmium-165 for this purpose. The Chitosan microspheres were produced loaded with holmium (III) chloride, and not loaded with it, by Mini Spray Dryer procedure. The microspheres were evaluated by scanning electron microscopy, energy dispersive spectroscopy (EDS), confocal laser scanning microscopy, thermogravimetric analysis, particle size, and X-ray diffraction. The EDS analysis confirmed the holmium chloride presence into the prepared chitosan microparticles. (author)

  6. Chitosan microspheres loaded with holmium-165 produced by spray dryer for liver cancer therapy: preliminary experiments

    Energy Technology Data Exchange (ETDEWEB)

    Miyamoto, Douglas Massao; Pires, Geovanna; Lira, Raphael A. de; Melo, Vitor H.S.; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de, E-mail: douglas.miyamoto@usp.b [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil); Osso Junior, Joao Alberto [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Radiofarmacia

    2011-07-01

    Chitosan is a biopolymer of 2-deoxy-2-amino-D-glucose that is obtained by deacetylation of chitin. It's biocompatible, biodegradable, non toxic and has antitumor activity. Chitosan has many applications, such as their microparticles that can be used to treat prostate cancer, rheumatoid arthritis, and for liver tumor brachytherapy treatment. Our group is developing different biodegradable polymer-based microspheres loaded with holmium-165 for this purpose. The Chitosan microspheres were produced loaded with holmium (III) chloride, and not loaded with it, by Mini Spray Dryer procedure. The microspheres were evaluated by scanning electron microscopy, energy dispersive spectroscopy (EDS), confocal laser scanning microscopy, thermogravimetric analysis, particle size, and X-ray diffraction. The EDS analysis confirmed the holmium chloride presence into the prepared chitosan microparticles. (author)

  7. Mesoporous metal oxide microsphere electrode compositions and their methods of making

    Science.gov (United States)

    Parans Paranthaman, Mariappan; Bi, Zhonghe; Bridges, Craig A.; Brown, Gilbert M.

    2017-04-11

    Compositions and methods of making are provided for treated mesoporous metal oxide microspheres electrodes. The compositions include microspheres with an average diameter between about 200 nanometers and about 10 micrometers and mesopores on the surface and interior of the microspheres. The methods of making include forming a mesoporous metal oxide microsphere composition and treating the mesoporous metal oxide microspheres by at least annealing in a reducing atmosphere, doping with an aliovalent element, and coating with a coating composition.

  8. Accumulation of 111In-neutrophils in rabbit skin in allergic and non-allergic inflammatory reactions in vivo. Inhibition by neutrophil pretreatment in vitro with a monoclonal antibody recognizing the CD18 antigen

    International Nuclear Information System (INIS)

    Nourshargh, S.; Rampart, M.; Hellewell, P.G.; Jose, P.J.; Harlan, J.M.; Edwards, A.J.; Williams, T.J.

    1989-01-01

    The mAb 60.3 recognizes the neutrophil CD18 Ag. We have investigated the effect of in vitro pretreatment of radiolabeled neutrophils with mAb 60.3 on their accumulation in vivo. Further, we have compared the in vivo effects of mAb 60.3 with its effects on neutrophil adherence in vitro. Neutrophil accumulation in vivo was measured in response to: (1) exogenous mediators FMLP, C5a des Arg, LTB4 and IL-1; (2) endogenous mediators generated in a non-allergic inflammatory reaction induced by zymosan; and (3) endogenous mediators generated in two allergic inflammatory reactions, a passive cutaneous anaphylactic reaction and a reversed passive Arthus reaction in rabbit skin. Pretreatment of neutrophils with mAb 60.3 inhibited their accumulation in all the responses. The results demonstrate that there is a common mechanism mediating neutrophil accumulation in these inflammatory reactions. Neutrophils pretreated with mAb 60.3 were also unresponsive to chemoattractants in in vitro adherence assays. However, the antibody-treated neutrophils responded normally to FMLP and C5a with respect to granular enzyme release. These results suggest that the basal expression of CD18 Ag is important for the adherence of neutrophils to microvascular endothelial cells stimulated by the local generation, or administration, of chemical mediators in vivo. Despite the fact that mediators such as FMLP can increase CD18 expression in vitro, it appears more likely that such mediators act in vivo by inducing a conformational change in the basally expressed neutrophil adhesive molecules

  9. In vitro Evaluation of Nateglinide-Loaded Microspheres Formulated ...

    African Journals Online (AJOL)

    Keywords: Nateglinide, Microspheres, Micromeritics, Drug release, Ionic ... Oral drug delivery systems (DDS) are commonly divided into immediate release and modified release systems. ..... Albumin Microspheres for Potential Intramuscular.

  10. Inhibition of human polimorfonuclear leucocyte migration by clofazimine: a new pro-oxidative anti-inflammatory agent

    International Nuclear Information System (INIS)

    Jansen van Rensburg, C.E.

    1986-10-01

    Preliminary studies on the in vitro and in vivo effects of clofazimine on the function of polymorphonuclear leucocytes (PMNL) from normal individuals and patients with lepromatous leprosy showed that clofazimine caused a progressive dose-dependent inhibition of both random mortality of PMNL as well as migration of PMNL induced by the leucoattractant endotoxin-activated serum (EAS). The drug also increased chemiluminescence as well as hexose monophosphate shunt (HMS). These studies on clofazimine include the use of radiolabelling with 14 C, 125 I and 3 H. Clofazimine-mediated inhibition of PMNL migration is dependent on intact membrane-associated oxidative metabolism. Clofazimine is therefore a pro-oxidative anti-inflammatory agent

  11. Study on the Degradation of Polylactide Microsphere In Vitro

    Institute of Scientific and Technical Information of China (English)

    HeYing; WeiShuli

    2001-01-01

    This report concentrated on the rules and mechanism of the degradation of polylactide and the microspheres. The rate of degradation was assessed with five methods: observation of microsphere surface morphology by SEM, determination of the weight loss of the microspheres, determination of the molecular mass of the polymers by GPC, determination of pH and determination of the contents of lactic acid by UV spectrophotometry. The degradation of polylactide microspheres showed two-phase characteristics. At the early stage of the degradation, the high molecular mass polymers were cleaved into lower molecular mass fractions and at the late stage, there was a period of erosion and weight loss of the microspheres. The degradation was much slower for polymers with a higher molecular mass. The polylactide degradation showed good regularity.

  12. Preparation and Characterization of Fluorescent SiO2 Microspheres

    Science.gov (United States)

    Xu, Cui; Zhang, Hao; Guan, Ruifang

    2018-01-01

    Fluorescent compound without typical fluorophores was synthesized with citric acid (CA) and aminopropyltriethoxysilane (APTS) firstly, and then it was grafted to the surface of the prepared SiO2 microspheres by chemical reaction. The fluorescent SiO2 microspheres with good fluorescent properties were obtained by optimizing the reaction conditions. And the morphology and structure of the fluorescent SiO2 microspheres have been characterized by scanning electron microscopy (SEM) and fourier transform infrared (FTIR) spectroscopy. The results showed that the preparation of fluorescent SiO2 microspheres have good monodispersity and narrow particle size distribution. Moreover, the fluorescent SiO2 microspheres can be applied to detect Fe3+ in aqueous solution, prepare fluorescent SiO2 rubber, and have potential to be applied in the fluorescent labeling and fingerprint appearing technique fields.

  13. Use of non-steroidal anti-inflammatory drugs and nutritional ...

    African Journals Online (AJOL)

    Background. The use of medications by football players in many populations is known to be high. Data on African players are scarce. Objective. To determine the magnitude of use of non-steroidal anti-inflammatory drugs (NSAIDs) and nutritional supplements by Zimbabwean football players. Methods. We conducted a ...

  14. PEGylation controls attachment and engulfment of monodisperse magnetic poly(2-hydroxyethyl methacrylate) microspheres by murine J774.2 macrophages

    Science.gov (United States)

    Horák, Daniel; Hlidková, Helena; Klyuchivska, Olga; Grytsyna, Iryna; Stoika, Rostyslav

    2017-12-01

    The first objective of this work was to prepare biocompatible magnetic polymer microspheres with reactive functional groups that could withstand nonspecific protein adsorption from biological media. Carboxyl group-containing magnetic poly(2-hydroxyethyl methacrylate) (mgt.PHEMA) microspheres ∼4 μm in size were prepared by multistage swelling polymerization, precipitation of iron oxide inside their pores, and coating with an α-methoxy-ω-amino poly(ethylene glycol) (CH3O-PEG750-NH2 or CH3O-PEG5,000-NH2)/α-amino-ω-t-Boc-amino poly(ethylene glycol) (H2N-PEG5,000-NH-t-Boc) mixture. The mgt.PHEMA@PEG microspheres contained ∼10 μmol COOH per g. Biocompatibility of the particles was evaluated by their treatment with human embryonic kidney cells of the HEK293 line. The microspheres did not interfere with the growth of these cells, suggesting that the particles can be considered non-toxic. A second goal of this study was to address on the interaction of the developed microspheres with macrophages that commonly eliminate foreign microbodies appearing in organisms. Murine J774.2 macrophages (J774.2) were cultured in the presence of the neat and PEGylated microspheres for 2 h. Mgt.PHEMA@PEG5,000 microspheres significantly adhered to the surface of J774.2 macrophages but were minimally engulfed. Due to these properties, the mgt.PHEMA@PEG microspheres might be useful for application in drug delivery systems and monitoring of the efficiency of phagocytosis.

  15. Robust platforms for creating organic-inorganic nanocomposite microspheres: decorating polymer microspheres containing mussel-inspired adhesion layers with inorganic nanoparticles.

    Science.gov (United States)

    Satoh, H; Saito, Y; Yabu, H

    2014-12-07

    We describe a method for creating robust and stable core-shell polymer microspheres decorated with inorganic (IO) nanoparticles (NPs) by a self-organization process and heterocoagulation using a mussel-inspired polymer adhesive layer between the IO NPs and the microspheres.

  16. Non-specific Inflammatory Disease Showed Abnormal FDG Uptake in Lower Extremities

    International Nuclear Information System (INIS)

    Chun, Kyung Ah; Kong, Eun Jung; Cho, Ihn Ho; Hong, Young Hoon; Lee, Choong Ki

    2008-01-01

    Including malignancy, various disease can show abnormal uptake in bone marrow. 1,2) We report a case of non-specific inflammatory FDG uptake in bone marrow mimicking malignancy. A 35-year old woman with fever of unknown origin (FUO) underwent 18 F-FDG PET/CT to find out fever focus and unknown malignancy. 18 F-FDG was injected and imaged 1hr after injection with Discovery ST (GE, USA). 18 F-FDG PET/CT whole body image showed abnormal uptake in lower extremities. MRI and biopsy was also done in the sites of abnormal uptake. PET and MRI suspect malignancy, but biopsy result was non-specific inflammatory process. The patient was improved her clinical condition after antibiotics therapy

  17. PET/MRI of Hepatic 90Y Microsphere Deposition Determines Individual Tumor Response

    Energy Technology Data Exchange (ETDEWEB)

    Fowler, Kathryn J. [Washington University, Department of Radiology (United States); Maughan, Nichole M. [Washington University, Department of Biomedical Engineering (United States); Laforest, Richard [Washington University, Department of Nuclear Medicine (United States); Saad, Nael E. [Washington University, Department of Radiology (United States); Sharma, Akash [Washington University, Department of Nuclear Medicine (United States); Olsen, Jeffrey; Speirs, Christina K.; Parikh, Parag J., E-mail: parikh@wustl.edu [Washington University, Department of Radiation Oncology (United States)

    2016-06-15

    PurposeThe purpose of our study is to determine if there is a relationship between dose deposition measured by PET/MRI and individual lesion response to yttrium-90 ({sup 90}Y) microsphere radioembolization.Materials and Methods26 patients undergoing lobar treatment with {sup 90}Y microspheres underwent PET/MRI within 66 h of treatment and had follow-up imaging available. Adequate visualization of tumor was available in 24 patients, and contours were drawn on simultaneously acquired PET/MRI data. Dose volume histograms (DVHs) were extracted from dose maps, which were generated using a voxelized dose kernel. Similar contours to capture dimensional and volumetric change of tumors were drawn on follow-up imaging. Response was analyzed using both RECIST and volumetric RECIST (vRECIST) criteria.ResultsA total of 8 hepatocellular carcinoma (HCC), 4 neuroendocrine tumor (NET), 9 colorectal metastases (CRC) patients, and 3 patients with other metastatic disease met inclusion criteria. Average dose was useful in predicting response between responders and non-responders for all lesion types and for CRC lesions alone using both response criteria (p < 0.05). D70 (minimum dose to 70 % of volume) was also useful in predicting response when using vRECIST. No significant trend was seen in the other tumor types. For CRC lesions, an average dose of 29.8 Gy offered 76.9 % sensitivity and 75.9 % specificity for response.ConclusionsPET/MRI of {sup 90}Y microsphere distribution showed significantly higher DVH values for responders than non-responders in patients with CRC. DVH analysis of {sup 90}Y microsphere distribution following treatment may be an important predictor of response and could be used to guide future adaptive therapy trials.

  18. Conductive hearing loss with an intact tympanic membrane due to non-inflammatory causes.

    Science.gov (United States)

    Choi, Jin Hyuk; Lee, Min Young; Park, Ji Hye; Lee, Kyu-Yup; Lee, Sang Heun; Jang, Jeong Hun

    2016-04-01

    We analyzed audiologic and surgical findings in patients with conductive hearing loss (CHL) with an intact tympanic membrane (TM) that was of a non-inflammatory origin. We reviewed data from patients who underwent exploratory tympanotomy for CHL with intact TM from January 1995 to November 2012. Patients with diseases of non-inflammatory origin were enrolled (69 patients; 79 ears). Patients were categorized into two groups: non-trauma (50 ears) and trauma (29 ears). Demographic data, intraoperative findings, and audiologic results were obtained and analyzed. Overall, the second decade was the most common age of diagnosis in both the non-trauma and trauma groups. Operative findings showed that ossicular dislocation was more prevalent than ossicular fixation; all trauma group subjects had ossicular dislocation. Short columellization or partial ossicular replacement was the most frequently adopted surgical procedures in both groups. Overall, audiologically, air-conduction thresholds (ACs) and air-bone gaps were significantly improved over the short- and long-term period in both groups. However, the non-trauma group had significantly higher preoperative ACs than the trauma group, especially at low frequencies. This study provides clinicians with useful information regarding the clinical characteristics of CHL with intact TM of non-inflammatory origin. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

  19. 5-Fluorouracil:carnauba wax microspheres for chemoembolization: an in vitro evaluation.

    Science.gov (United States)

    Benita, S; Zouai, O; Benoit, J P

    1986-09-01

    5-Fluorouracil:carnauba wax microspheres were prepared using a meltable dispersion process with the aid of a surfactant as a wetting agent. It was noted that only hydrophilic surfactants were able to wet the 5-fluorouracil and substantially increased its content in the microspheres. No marked effect was observed in the particle size distribution of the solid microspheres as a function of the nature of the surfactant. Increasing the stirring rate in the preparation process decreased, first, the mean droplet size of the emulsified melted dispersion in the vehicle during the heating process, and, consequently, the mean particle size of the solidified microspheres during the cooling process. 5-Fluorouracil cumulative release from the microspheres followed first-order kinetics, as shown by nonlinear regression analysis. Although the kinetic results were not indicative of the true release mechanism from a single microsphere, it was believed that 5-fluorouracil release from the microspheres was probably governed by a dissolution process, rather than by a leaching process through the carnauba wax microspheres.

  20. Prevention of polydimethylsiloxane microsphere migration using a mussel-inspired polydopamine coating for potential application in injection therapy.

    Directory of Open Access Journals (Sweden)

    Eun-Jae Chung

    Full Text Available The use of injectable bulking agents is a feasible alternative procedure for conventional surgical therapy. In this study, poly(dimethylsiloxane (PDMS microspheres coated with polydopamine (PDA were developed as a potential injection agent to prevent migration in vocal fold. Uniform PDMS microspheres are fabricated using a simple fluidic device and then coated with PDA. Cell attachment test reveals that the PDA-coated PDMS (PDA-PDMS substrate favors cell adhesion and attachment. The injected PDA-PDMS microspheres persist without migration on reconstructed axial CT images, whereas, pristine PDMS locally migrates over a period of 12 weeks. The gross appearance of the implants retrieved at 4, 8, 12 and 34 weeks indicates that the PDA-PDMS group maintained their original position without significant migration until 34 weeks after injection. By contrast, there is diffuse local migration of the pristine PDMS group from 4 weeks after injection. The PDA-coated PDMS microspheres can potentially be used as easily injectable, non-absorbable filler without migration.

  1. A novel imidazopyridine derivative, X22, attenuates sepsis-induced lung and liver injury by inhibiting the inflammatory response in vitro and in vivo.

    Science.gov (United States)

    Ge, Xiangting; Feng, Zhiguo; Xu, Tingting; Wu, Beibei; Chen, Hongjin; Xu, Fengli; Fu, Lili; Shan, Xiaoou; Dai, Yuanrong; Zhang, Yali; Liang, Guang

    2016-01-01

    Sepsis remains a leading cause of death worldwide. Despite years of extensive research, effective drugs to treat sepsis in the clinic are lacking. In this study, we found a novel imidazopyridine derivative, X22, which has powerful anti-inflammatory activity. X22 dose-dependently inhibited lipopolysaccharide (LPS)-induced proinflammatory cytokine production in mouse primary peritoneal macrophages and RAW 264.7 macrophages. X22 also downregulated the LPS-induced proinflammatory gene expression in vitro. In vivo, X22 exhibited a significant protection against LPS-induced death. Pretreatment or treatment with X22 attenuated the sepsis-induced lung and liver injury by inhibiting the inflammatory response. In addition, X22 showed protection against LPS-induced acute lung injury. We additionally found that pretreatment with X22 reduced the inflammatory pain in the acetic acid and formalin models and reduced the dimethylbenzene-induced ear swelling and acetic acid-increased vascular permeability. Together, these data confirmed that X22 has multiple anti-inflammatory effects and may be a potential therapeutic option in the treatment of inflammatory diseases.

  2. Src Is a Prime Target Inhibited by Celtis choseniana Methanol Extract in Its Anti-Inflammatory Action

    Directory of Open Access Journals (Sweden)

    Han Gyung Kim

    2018-01-01

    Full Text Available Celtis choseniana is the traditional plant used at Korea as a herbal medicine to ameliorate inflammatory responses. Although Celtis choseniana has been traditionally used as a herbal medicine at Korea, no systemic research has been conducted on its anti-inflammatory activity. Therefore, the present study explored an anti-inflammatory effect and its underlying molecular mechanism using Celtis choseniana methanol extract (Cc-ME in macrophage-mediated inflammatory responses. In vitro anti-inflammatory activity of Cc-ME was evaluated using RAW264.7 cells and peritoneal macrophages stimulated by lipopolysaccharide (LPS, pam3CSK4 (Pam3, or poly(I:C. In vivo anti-inflammatory activity of Cc-ME was investigated using acute inflammatory disease mouse models, such as LPS-induced peritonitis and HCl/EtOH-induced gastritis. The molecular mechanism of Cc-ME-mediated anti-inflammatory activity was examined by Western blot analysis and immunoprecipitation using whole cell and nuclear fraction prepared from the LPS-stimulated RAW264.7 cells and HEK293 cells. Cc-ME inhibited NO production and mRNA expression of inducible nitric oxide synthase (iNOS, cyclooxygenase (COX-2, and tumor necrosis factor-alpha (TNF-α in the RAW264.7 cells and peritoneal macrophages induced by LPS, pam3, or poly(I:C without cytotoxicity. High-performance liquid chromatography (HPLC analysis showed that Cc-ME contained anti-inflammatory flavonoids quercetin, luteolin, and kaempferol. Among those, the content of luteolin, which showed an inhibitory effect on NO production, was highest. Cc-ME suppressed the NF-κB signaling pathway by targeting Src and interrupting molecular interactions between Src and p85, its downstream kinase. Moreover, Cc-ME ameliorated the morphological finding of peritonitis and gastritis in the mouse disease models. Therefore, these results suggest that Cc-ME exerted in vitro and in vivo anti-inflammatory activity in LPS-stimulated macrophages and mouse models of

  3. Assessment Of Pattern Of Non-steroidal Anti-Inflammatory Drugs ...

    African Journals Online (AJOL)

    Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used in the treatment of pains. Self-medication is a common practice all over the world. Unwanted effects from use of this class of medication could pose health challenges. This study evaluated the prevalence and pattern of inappropriate use of NSAIDs among ...

  4. Preparation of porous zirconia microspheres by internal gelation method

    International Nuclear Information System (INIS)

    Pathak, Sachin S.; Pius, I.C.; Bhanushali, R.D.; Rao, T.V. Vittal; Mukerjee, S.K.

    2008-01-01

    A modified internal gelation process for the preparation of porous zirconia microspheres has been developed. The conventional method has been modified by adding a surfactant in the feed broth. The effects of variation of surfactant concentration, washing techniques and temperature of calcination on the pore volume and the surface area of the microspheres have been studied. The conditions were optimized to obtain porous stable microspheres suitable for various applications. The microspheres were characterized by surface area analysis, pore volume analysis, thermogravimetric analysis and X-ray diffraction. The ion exchange behavior was studied using pH titration

  5. NF-κB/AP-1-Targeted Inhibition of Macrophage-Mediated Inflammatory Responses by Depigmenting Compound AP736 Derived from Natural 1,3-Diphenylpropane Skeleton

    Directory of Open Access Journals (Sweden)

    Van Thai Ha

    2014-01-01

    Full Text Available AP736 was identified as an antimelanogenic drug that can be used for the prevention of melasma, freckles, and dark spots in skin by acting as a suppressor of melanin synthesis and tyrosinase expression. Since macrophage-mediated inflammatory responses are critical for skin health, here we investigated the potential anti-inflammatory activity of AP736. The effects of AP736 on various inflammatory events such as nitric oxide (NO/prostaglandin (PG E2 production, inflammatory gene expression, phagocytic uptake, and morphological changes were examined in RAW264.7 cells. AP736 was found to strongly inhibit the production of both NO and PGE2 in lipopolysaccharide- (LPS- treated RAW264.7 cells. In addition, AP736 strongly inhibited both LPS-induced morphological changes and FITC-dextran-induced phagocytic uptake. Furthermore, AP736 also downregulated the expression of multiple inflammatory genes, such as inducible NO synthase (iNOS, cyclooxygenase- (COX- 2, and interleukin- (IL- 1β in LPS-treated RAW264.7 cells. Transcription factor analysis, including upstream signalling events, revealed that both NF-κB and AP-1 were targeted by AP736 via inhibition of the IKK/IκBα and IRAK1/TAK1 pathways. Therefore, our results strongly suggest that AP736 is a potential anti-inflammatory drug due to its suppression of NF-κB-IKK/IκBα and AP-1-IRAK1/TAK1 signalling, which may make AP736 useful for the treatment of macrophage-mediated skin inflammation.

  6. Effect of various polymers concentrations on physicochemical properties of floating microspheres.

    Science.gov (United States)

    Jagtap, Y M; Bhujbal, R K; Ranade, A N; Ranpise, N S

    2012-11-01

    Floating microspheres have emerged as a potential candidate for gastroretentive drug delivery system. For developing a desired intragastric floatation system employing these microspheres, it is necessary to select an appropriate balance between buoyancy and drug releasing rate. These properties mainly depend on the polymers used in the formulation of the microspheres. Hence it is necessory to study the effect of these polymer concentrations on the various physicochemical properties of the microspheres. Floating microspheres were prepared by emulsion solvent evaporation technique utilising different polymers such as ethyl cellulose, Eudragit(®) RS and Eudragit(®) RL by dissolving them in a mixture of dichloromethane and methanol. Release modifiers studied were hydroxypropyl methylcellulose K4M, hydroxypropyl methylcellulose E50 LV and Eudragit(®) EPO. Prepared microspheres were analysed for particle size, surface morphology, entrapment efficiency, buoyancy, differential scanning calorimetry and in-vitro drug release. Ethyl cellulose and Eudragit(®) EPO resulted microspheres with high percentage yield, excellent spherical shape but had very less buoyancies with a high cumulative drug release. Ethyl cellulose microspheres prepared using hydroxypropyl methylcellulose K4M showed more sustained drug release and high buoyancies than that of the microspheres formulated with the hydroxypropyl methylcellulose E50 LV. Amongst these hydroxypropyl methylcellulose E50 LV showed good balance between buoyancy and the drug release.

  7. Screening and identification of dietary oils and unsaturated fatty acids in inhibiting inflammatory prostaglandin E2 signaling in fat stromal cells

    Directory of Open Access Journals (Sweden)

    Ruan Diana

    2012-08-01

    Full Text Available Abstract Background The molecular mechanisms of dietary oils (such as fish oil and unsaturated fatty acids, which are widely used by the public for anti-inflammation and vascular protection, have not been settled yet. In this study, prostaglandin E2 (PGE2-mediated calcium signaling was used to screen dietary oils and eight unsaturated fatty acids for identification of their anti-inflammatory mechanisms. Isolated fat/stromal cells expressing endogenous PGE2 receptors and an HEK293 cell line specifically expressing the recombinant human PGE2 receptor subtype-1 (EP1 were cultured and used in live cell calcium signaling assays. The different dietary oils and unsaturated fatty acids were used to affect cell signaling under the specific stimulation of a pathological amount of inflammatory PGE2. Results It was identified that fish oil best inhibited the PGE2 signaling in the primary cultured stromal cells. Second, docosahexaenoic acid (DHA, found in abundance in fish oil, was identified as a key factor of inhibition of PGE2 signaling. Eicosapentaenoic acid (EPA, another major fatty acid found in fish oil and tested in this study was found to have small effect on EP1 signaling. The study suggested one of the four PGE2 subtype receptors, EP1 as the key target for the fish oil and DHA target. These findings were further confirmed by using the recombinant EP1 expressed in HEK293 cells as a target. Conclusion This study demonstrated the new mechanism behind the positive effects of dietary fish oils in inhibiting inflammation originates from the rich concentration of DHA, which can directly inhibit the inflammatory EP1-mediated PGE2 receptor signaling, and that the inflammatory response stimulated by PGE2 in the fat stromal cells, which directly related to metabolic diseases, could be down regulated by fish oil and DHA. These findings also provided direct evidence to support the use of dietary oils and unsaturated fatty acids for protection against heart

  8. Biocompatibility of Polyhydroxybutyrate Microspheres: in vitro and in vivo Evaluation

    OpenAIRE

    Shishatskaya, Ekaterina I.; Voinova, Olga N.; Goreva, Anastasya V.; Mogilnaya, Olga A.; Volova, Tatiana G.

    2008-01-01

    Microspheres have been prepared from the resorbable linear polyester of β-hydroxybutyric acid (polyhydroxybutyrate, PHB) by the solvent evaporation technique and investigated in vitro and in vivo. Biocompatibility of the microspheres has been proved in tests in the culture of mouse fibroblast cell line NIH 3Т3 and in experiments on intramuscular implantation of the microspheres to Wistar rats for 3 months. Tissue response to the implantation of polymeric microspheres has been found to consist...

  9. Development of Risperidone PLGA Microspheres

    Directory of Open Access Journals (Sweden)

    Susan D’Souza

    2014-01-01

    Full Text Available The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25 were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.

  10. AZD5363 inhibits inflammatory synergy between interleukin-17 and insulin/insulin-like growth factor 1

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    Chong eChen

    2014-12-01

    Full Text Available In the United States, one third of population is affected by obesity and almost 29 million people are suffering from type 2 diabetes. Obese people have elevated serum levels of insulin, insulin-like growth factor 1 (IGF1 and interleukin-17 (IL-17. Insulin and IGF1 are known to enhance IL-17-induced expression of inflammatory cytokines and chemokines, which may contribute to the chronic inflammatory status observed in obese people. We have previously demonstrated that insulin/IGF1 signaling pathway crosstalks with IL-17-activated nuclear factor-kappa B (NF-κB pathway through inhibiting glycogen synthase kinase 3β (GSK3β activity. However, it is unclear whether GSK3α also plays a role and whether this crosstalk can be manipulated by AZD5363, a novel pan-Akt inhibitor that has been shown to increase GSK3 activity through reducing phosphorylation of GSK3α and GSK3β. In this study, we investigated IL-17-induced expression of C-X-C motif ligand 1 (Cxcl1, C-C motif ligand 20 (Ccl20 and interleukin-6 (Il-6 in wild-type, GSK3α-/-, and GSK3β-/- mouse embryonic fibroblast (MEF cells as well as in mouse prostate tissues by real-time quantitative PCR. We examined the proteins involved in the signaling pathways by Western blot analysis. We found that insulin and IGF1 enhanced IL-17- induced expression of Cxcl1, Ccl20 and Il-6, which was associated with increased phosphorylation of GSK3α and GSK3β in the presence of insulin and IGF1. AZD5363 inhibited the synergy between IL-17 and insulin/IGF1 through reducing phosphorylation of GSK3α and GSK3β by inhibiting Akt function. These findings imply that the cooperative crosstalk of IL-17 and insulin/IGF1 in initiating inflammatory responses may be alleviated by AZD5363.

  11. Scalable and sustainable synthesis of carbon microspheres via a purification-free strategy for sodium-ion capacitors

    Science.gov (United States)

    Wang, Shijie; Wang, Rutao; Zhang, Yabin; Jin, Dongdong; Zhang, Li

    2018-03-01

    Sodium-based energy storage receives a great deal of interest due to the virtually inexhaustible sodium reserve, while the scalable and sustainable strategies to synthesize carbon-based materials with suitable interlayer spaces and large sodium storage capacities are yet to be fully investigated. Carbon microspheres, with regular geometry, non-graphitic characteristic, and stable nature are promising candidates, yet the synthetic methods are usually complex and energy consuming. In this regard, we report a scalable purification-free strategy to synthesize carbon microspheres directly from 5 species of fresh juice. As-synthesized carbon microspheres exhibit dilated interlayer distance of 0.375 nm and facilitate Na+ uptake and release. For example, such carbon microsphere anodes have a specific capacity of 183.9 mAh g-1 at 50 mA g-1 and exhibit ultra-stability (99.0% capacity retention) after 10000 cycles. Moreover, via facile activation, highly porous carbon microsphere cathodes are fabricated and show much higher energy density at high rate than commercial activated carbon. Coupling the compelling anodes and cathodes above, novel sodium-ion capacitors show the high working potential up to 4.0 V, deliver a maximum energy density of 52.2 Wh kg-1, and exhibit an acceptable capacity retention of 85.7% after 2000 cycles.

  12. Measurement of thermal diffusivity of depleted uranium metal microspheres

    Science.gov (United States)

    Humrickhouse-Helmreich, Carissa J.; Corbin, Rob; McDeavitt, Sean M.

    2014-03-01

    The high void space of nuclear fuels composed of homogeneous uranium metal microspheres may allow them to achieve ultra-high burnup by accommodating fuel swelling and reducing fuel/cladding interactions; however, the relatively low thermal conductivity of microsphere nuclear fuels may limit their application. To support the development of microsphere nuclear fuels, an apparatus was designed in a glovebox and used to measure the apparent thermal diffusivity of a packed bed of depleted uranium (DU) microspheres with argon fill in the void spaces. The developed Crucible Heater Test Assembly (CHTA) recorded radial temperature changes due to an initial heat pulse from a central thin-diameter cartridge heater. Using thermocouple positions and time-temperature data, the apparent thermal diffusivity was calculated. The thermal conductivity of the DU microspheres was calculated based on the thermal diffusivity from the CHTA, known material densities and specific heat capacities, and an assumed 70% packing density based on prior measurements. Results indicate that DU metal microspheres have very low thermal conductivity, relative to solid uranium metal, and rapidly form an oxidation layer even in a low oxygen environment. At 500 °C, the thermal conductivity of the DU metal microsphere bed was 0.431 ± 0.0560 W/m-K compared to the literature value of approximately 32 W/m-K for solid uranium metal.

  13. Measurement of thermal diffusivity of depleted uranium metal microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Humrickhouse-Helmreich, Carissa J., E-mail: carissahelmreich@tamu.edu [Texas A and M University, Department of Nuclear Engineering, 337 Zachry Engineering Center, 3133 TAMU, College Station, TX 77843 (United States); Corbin, Rob, E-mail: rcorbin@terrapower.com [TerraPower, LLC, 330 120th Ave NE, Suite 100, Bellevue, WA 98005 (United States); McDeavitt, Sean M., E-mail: mcdeavitt@tamu.edu [Texas A and M University, Department of Nuclear Engineering, 337 Zachry Engineering Center, 3133 TAMU, College Station, TX 77843 (United States)

    2014-03-15

    The high void space of nuclear fuels composed of homogeneous uranium metal microspheres may allow them to achieve ultra-high burnup by accommodating fuel swelling and reducing fuel/cladding interactions; however, the relatively low thermal conductivity of microsphere nuclear fuels may limit their application. To support the development of microsphere nuclear fuels, an apparatus was designed in a glovebox and used to measure the apparent thermal diffusivity of a packed bed of depleted uranium (DU) microspheres with argon fill in the void spaces. The developed Crucible Heater Test Assembly (CHTA) recorded radial temperature changes due to an initial heat pulse from a central thin-diameter cartridge heater. Using thermocouple positions and time–temperature data, the apparent thermal diffusivity was calculated. The thermal conductivity of the DU microspheres was calculated based on the thermal diffusivity from the CHTA, known material densities and specific heat capacities, and an assumed 70% packing density based on prior measurements. Results indicate that DU metal microspheres have very low thermal conductivity, relative to solid uranium metal, and rapidly form an oxidation layer even in a low oxygen environment. At 500 °C, the thermal conductivity of the DU metal microsphere bed was 0.431 ± 0.0560 W/m-K compared to the literature value of approximately 32 W/m-K for solid uranium metal.

  14. Measurement of thermal diffusivity of depleted uranium metal microspheres

    International Nuclear Information System (INIS)

    Humrickhouse-Helmreich, Carissa J.; Corbin, Rob; McDeavitt, Sean M.

    2014-01-01

    The high void space of nuclear fuels composed of homogeneous uranium metal microspheres may allow them to achieve ultra-high burnup by accommodating fuel swelling and reducing fuel/cladding interactions; however, the relatively low thermal conductivity of microsphere nuclear fuels may limit their application. To support the development of microsphere nuclear fuels, an apparatus was designed in a glovebox and used to measure the apparent thermal diffusivity of a packed bed of depleted uranium (DU) microspheres with argon fill in the void spaces. The developed Crucible Heater Test Assembly (CHTA) recorded radial temperature changes due to an initial heat pulse from a central thin-diameter cartridge heater. Using thermocouple positions and time–temperature data, the apparent thermal diffusivity was calculated. The thermal conductivity of the DU microspheres was calculated based on the thermal diffusivity from the CHTA, known material densities and specific heat capacities, and an assumed 70% packing density based on prior measurements. Results indicate that DU metal microspheres have very low thermal conductivity, relative to solid uranium metal, and rapidly form an oxidation layer even in a low oxygen environment. At 500 °C, the thermal conductivity of the DU metal microsphere bed was 0.431 ± 0.0560 W/m-K compared to the literature value of approximately 32 W/m-K for solid uranium metal

  15. A review on target drug delivery: magnetic microspheres

    Directory of Open Access Journals (Sweden)

    Amit Chandna

    2013-01-01

    Magnetic microsphere is newer approach in pharmaceutical field. Magnetic microspheres as an alternative to traditional radiation methods which use highly penetrating radiation that is absorbed throughout the body. Its use is limited by toxicity and side effects. The aim of the specific targeting is to enhance the efficiency of drug delivery & at the same time to reduce the toxicity & side effects. This kind of delivery system is very much important which localises the drug to the disease site. In this larger amount of freely circulating drug can be replaced by smaller amount of magnetically targeted drug. Magnetic carriers receive magnetic responses to a magnetic field from incorporated materials that are used for magnetic microspheres are chitosan, dextran etc. magnetic microspheres can be prepared from a variety of carrier material. One of the most utilized is serum albumin from human or other appropriate species. Drug release from albumin microspheres can be sustained or controlled by various stabilization procedures generally involving heat or chemical cross-linking of the protein carrier matrix.

  16. Non-inflammatory causes of emergency consultation in patients with multiple sclerosis.

    Science.gov (United States)

    Rodríguez de Antonio, L A; García Castañón, I; Aguilar-Amat Prior, M J; Puertas, I; González Suárez, I; Oreja Guevara, C

    2018-05-26

    To describe non-relapse-related emergency consultations of patients with multiple sclerosis (MS): causes, difficulties in the diagnosis, clinical characteristics, and treatments administered. We performed a retrospective study of patients who attended a multiple sclerosis day hospital due to suspected relapse and received an alternative diagnosis, over a 2-year period. Demographic data, clinical characteristics, final diagnosis, and treatments administered were evaluated. Patients who were initially diagnosed with pseudo-relapse and ultimately diagnosed with true relapse were evaluated specifically. As an exploratory analysis, patients who consulted with non-inflammatory causes were compared with a randomly selected cohort of patients with true relapses who attended the centre in the same period. The study included 50 patients (33 were women; mean age 41.4±11.7years). Four patients (8%) were initially diagnosed with pseudo-relapse and later diagnosed as having a true relapse. Fever and vertigo were the main confounding factors. The non-inflammatory causes of emergency consultation were: neurological, 43.5% (20 patients); infectious, 15.2% (7); psychiatric, 10.9% (5); vertigo, 8.6% (4); trauma, 10.9% (5); and miscellaneous, 10.9% (5). MS-related symptoms constituted the most frequent cause of non-inflammatory emergency consultations. Close follow-up of relapse and pseudo-relapse is necessary to detect incorrect initial diagnoses, avoid unnecessary treatments, and relieve patients' symptoms. Copyright © 2018 Sociedad Española de Neurología. Publicado por Elsevier España, S.L.U. All rights reserved.

  17. Novel chloroacetamido compound CWR-J02 is an anti-inflammatory glutaredoxin-1 inhibitor.

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    Olga Gorelenkova Miller

    Full Text Available Glutaredoxin (Grx1 is a ubiquitously expressed thiol-disulfide oxidoreductase that specifically catalyzes reduction of S-glutathionylated substrates. Grx1 is known to be a key regulator of pro-inflammatory signaling, and Grx1 silencing inhibits inflammation in inflammatory disease models. Therefore, we anticipate that inhibition of Grx1 could be an anti-inflammatory therapeutic strategy. We used a rapid screening approach to test 504 novel electrophilic compounds for inhibition of Grx1, which has a highly reactive active-site cysteine residue (pKa 3.5. From this chemical library a chloroacetamido compound, CWR-J02, was identified as a potential lead compound to be characterized. CWR-J02 inhibited isolated Grx1 with an IC50 value of 32 μM in the presence of 1 mM glutathione. Mass spectrometric analysis documented preferential adduction of CWR-J02 to the active site Cys-22 of Grx1, and molecular dynamics simulation identified a potential non-covalent binding site. Treatment of the BV2 microglial cell line with CWR-J02 led to inhibition of intracellular Grx1 activity with an IC50 value (37 μM. CWR-J02 treatment decreased lipopolysaccharide-induced inflammatory gene transcription in the microglial cells in a parallel concentration-dependent manner, documenting the anti-inflammatory potential of CWR-J02. Exploiting the alkyne moiety of CWR-J02, we used click chemistry to link biotin azide to CWR-J02-adducted proteins, isolating them with streptavidin beads. Tandem mass spectrometric analysis identified many CWR-J02-reactive proteins, including Grx1 and several mediators of inflammatory activation. Taken together, these data identify CWR-J02 as an intracellularly effective Grx1 inhibitor that may elicit its anti-inflammatory action in a synergistic manner by also disabling other pro-inflammatory mediators. The CWR-J02 molecule provides a starting point for developing more selective Grx1 inhibitors and anti-inflammatory agents for therapeutic

  18. Photonic nanojet super-resolution in immersed ordered assembly of dielectric microspheres

    International Nuclear Information System (INIS)

    Geints, Y.E.; Zemlyanov, A.A.

    2017-01-01

    Highlights: • Ordered microassemblies of dielectric microspheres immersed in a transparent matrix exposed to a light wave produce an array of the “photonic nanojets” coupled through the field interference. • “Photonic nanojet” parameters depend on the inter-sphere gap and immersion depth. • Sphere microassembly can produce the jets with the sub-diffraction spatial resolution if the particles are loosely packed and semi-immersed. - Abstract: Specific spatially-localized optical field structure, which is often referred to as a photonic nanojet (PNJ), is formed in the near-field scattering area of non-absorbing dielectric micron-sized particle exposed to an optical radiation. By virtue of the finite-difference time-domain technique we numerically simulate the two-dimensional array of PNJs created by an ordered single-layer microassembly of glass microspheres immersed in a transparent polymer matrix. The behavior of the main PNJ parameters (length, diameter, and intensity) is analyzed subject to the immersion depth of the microparticles and cooperative interference effects of the neighboring microspheres. We show that depending on microassembly configuration, the PNJ quality can be significantly improved; in particular, the PNJ spatial resolution better than λ/5 can be achieved.

  19. Silicon microspheres for near-IR communication applications

    International Nuclear Information System (INIS)

    Serpengüzel, Ali; Demir, Abdullah

    2008-01-01

    We have performed transverse electric and transverse magnetic polarized elastic light scattering calculations at 90° and 0° in the o-band at 1.3 µm for a 15 µm radius silicon microsphere with a refractive index of 3.5. The quality factors are on the order of 10 7 and the mode/channel spacing is 7 nm, which correlate well with the refractive index and the optical size of the microsphere. The 90° elastic light scattering can be used to monitor a dropped channel (drop port), whereas the 0° elastic scattering can be used to monitor the transmission channel (through port). The optical resonances of the silicon microspheres provide the necessary narrow linewidths that are needed for high-resolution optical communication applications. Potential telecommunication applications include filters, modulators, switches, wavelength converters, detectors, amplifiers and light sources. Silicon microspheres show promise as potential building blocks for silicon-based electrophotonic integration

  20. Neuro-immune interactions via the cholinergic anti-inflammatory pathway

    Science.gov (United States)

    Gallowitsch-Puerta, Margot; Pavlov, Valentin A.

    2010-01-01

    The overproduction of TNF and other cytokines can cause the pathophysiology of numerous diseases. Controlling cytokine synthesis and release is critical for preventing unrestrained inflammation and maintaining health. Recent studies identified an efferent vagus nerve-based mechanism termed “the cholinergic anti-inflammatory pathway” that controls cytokine production and inflammation. Here we review current advances related to the role of this pathway in neuro-immune interactions that prevent excessive inflammation. Experimental evidence indicates that vagus nerve cholinergic anti-inflammatory signaling requires alpha7 nicotinic acetylcholine receptors expressed on non-neuronal cytokine producing cells. Alpha7 nicotinic acetylcholine receptor agonists inhibit cytokine release and protect animals in a variety of experimental lethal inflammatory models. Knowledge related to the cholinergic anti-inflammatory pathway can be exploited in therapeutic approaches directed towards counteracting abnormal chronic and hyper-activated inflammatory responses. PMID:17289087

  1. [Evaluation of anti-inflammatory activity of extracts from Siberian plants].

    Science.gov (United States)

    Nesterova, Iu V; Povet'eva, T N; Aksinenko, S G; Suslov, N I; Gaĭdamovich, N N; Nagorniak, Iu G; Popova, E V; Kravtsova, S S; Andreeva, T I

    2009-01-01

    Experimental investigations have shown that water-alcohol extracts from plants containing alkaloids (Aconitum baikalense, Aconitum septentrionale, Delphinium elatum L., Conium maculatum) and salicylic acid (Filipendula ulmaria, Salix viminalis, Fragaria vesca, Rubus idaeus) inhibited the development of main symptoms of inflammation, viz. exudation, pain, fever, to the same extent as non-steroidal anti-inflammatory agents. The substances studied in this work may be used to develop new efficient pharmacological preparations for the treatment of different inflammatory conditions associated with severe pain syndrome.

  2. Microwave Irradiation Assisted Preparation of Chitosan Composite Microsphere for Dye Adsorption

    Directory of Open Access Journals (Sweden)

    Xiaoyu Chen

    2017-01-01

    Full Text Available Chitosan-activated carbon composite microspheres were prepared by emulsion cross-linking method and its adsorption properties for methyl orange were studied. Chitosan solution was mixed with activated carbon powder and then chitosan was cross-linked by epichlorohydrin under microwave irradiation. SEM photos show that the composite microspheres have diameters of 200–400 μm and activated carbon powder dispersed on the surface of composite microsphere. FTIR spectrum indicates chitosan is successfully cross-linked. Microwave irradiation can effectively shorten the cross-linking time. Composite microspheres have enhanced dye adsorption capacity for methyl orange compared to chitosan microspheres. Kinetic studies showed that the adsorption followed a pseudo-second-order model. Isotherm studies show that the isotherm adsorption equilibrium is better described by Freundlich isotherm. Regeneration results show that adsorption capacity of composite microsphere decreased about 5.51% after being reused for three times. These results indicated that chitosan-activated carbon composite microsphere has potential application in the removal of dye from wastewaters.

  3. Development and Evaluation of Isoniazid Loaded Silk Fibroin Microsphere

    Directory of Open Access Journals (Sweden)

    Narinder Singh

    Full Text Available Aim: Current experimental investigation is dedicated to prepare microspheres with small size and good sphericity by Phase Separation method using Isoniazid (INH as model drug. Silk fibroin has unique intrinsic qualities like biodegradability, biocompatibility or release properties and their tunable drug loading capacity. The delivery loading proficiency of the drug molecules in silk spheres be contingent on their charge, and hydrophobicity or subsequent in altered drug release profiles. Methods: In the present work Isoniazid loaded silk fibroin microsphere was prepared by using phase separation method. Microsphere was evaluated for Ultraviolet-visible spectroscopy, Fourier Transform infrared spectroscopy, Entrapment efficiency, Scanning electron microscopy Studies. Results: Scanning electron microscopy studies revealed that Isoniazid Loaded Silk Fibroin Microspheres were spherical. Entrapment Efficiency of Isoniazid loaded Microspheres of different Formulation from F1 to F5 was in range of 53 to 68 %. F3 showed 68.47 % entrapment Efficiency and the optimized formulation drug release was 93.56 % at 24 hours. Conclusion: Experimental report disclosed a new aqueous based formulation method for silk spheres with controllable shape or size and sphere. Isoniazid loaded silk microspheres may act as ideal nano formulation with elaborated studies.

  4. Synthesis and characterization of Supeparamagnetics Microspheres (PMMA via suspension polymerization

    Directory of Open Access Journals (Sweden)

    Paulo Emilio Feuser

    2014-02-01

    Full Text Available Magnetics nanoparticles (NPMs has found many applications in biomedical and technological areas. The objective of this work is the preparation and characterization of PMMA microspheres containing NPMs coated with oleic acid (NPMs-AO. For the preparation of MNPs-AO was used the coprecipitation method in an aqueous medium. For the preparation of the superparamagnetic microspheres used in suspension polymerization technique. The microspheres showed a size distribution particles of approximately 150um and a spherical morphology. From the analysis of gel permeation chromatography (GPC determined the number average molecular weight (Mw of the magnetics microspheres and there was a variation in the Mw depending on the concentration of MNPs-AO in this reaction. To analyze the magnetic properties used the vibrating sample magnetometer (MAV. The microspheres showed superparamagnetic properties and a value of saturation magnetization (Ms of about 8 emu/g MNPs. Therefore you can conclude that it is possible to obtain superparamagnetics microspheres for a particular application, either, biomedical or technological.

  5. Low-Dose Tramadol and Non-Steroidal Anti-Inflammatory Drug Combination Therapy Prevents the Transition to Chronic Low Back Pain.

    Science.gov (United States)

    Inage, Kazuhide; Orita, Sumihisa; Yamauchi, Kazuyo; Suzuki, Takane; Suzuki, Miyako; Sakuma, Yoshihiro; Kubota, Go; Oikawa, Yasuhiro; Sainoh, Takeshi; Sato, Jun; Fujimoto, Kazuki; Shiga, Yasuhiro; Abe, Koki; Kanamoto, Hirohito; Inoue, Masahiro; Kinoshita, Hideyuki; Takahashi, Kazuhisa; Ohtori, Seiji

    2016-08-01

    Retrospective study. To determine whether low-dose tramadol plus non-steroidal anti-inflammatory drug combination therapy could prevent the transition of acute low back pain to chronic low back pain. Inadequately treated early low back pain transitions to chronic low back pain occur in approximately 30% of affected individuals. The administration of non-steroidal anti-inflammatory drugs is effective for treatment of low back pain in the early stages. However, the treatment of low back pain that is resistant to non-steroidal anti-inflammatory drugs is challenging. Patients who presented with acute low back pain at our hospital were considered for inclusion in this study. After the diagnosis of acute low back pain, non-steroidal anti-inflammatory drug administration was started. Forty patients with a visual analog scale score of >5 for low back pain 1 month after treatment were finally enrolled. The first 20 patients were included in a non-steroidal anti-inflammatory drug group, and they continued non-steroidal anti-inflammatory drug therapy for 1 month. The next 20 patients were included in a combination group, and they received low-dose tramadol plus non-steroidal anti-inflammatory drug combination therapy for 1 month. The incidence of adverse events and the improvement in the visual analog scale score at 2 months after the start of treatment were analyzed. No adverse events were observed in the non-steroidal anti-inflammatory drug group. In the combination group, administration was discontinued in 2 patients (10%) due to adverse events immediately following the start of tramadol administration. At 2 months, the improvement in the visual analog scale score was greater in the combination group than in the non-steroidal anti-inflammatory drug group (ppain to chronic low back pain.

  6. Synthetic secoisolariciresinol diglucoside (LGM2605) inhibits myeloperoxidase activity in inflammatory cells.

    Science.gov (United States)

    Mishra, Om P; Popov, Anatoliy V; Pietrofesa, Ralph A; Nakamaru-Ogiso, Eiko; Andrake, Mark; Christofidou-Solomidou, Melpo

    2018-06-01

    Myeloperoxidase (MPO) generates hypochlorous acid (HOCl) during inflammation and infection. We showed that secoisolariciresinol diglucoside (SDG) scavenges radiation-induced HOCl in physiological solutions. However, the action of SDG and its synthetic version, LGM2605, on MPO-catalyzed generation of HOCl is unknown. The present study evaluated the effect of LGM2605 on human MPO, and murine MPO from macrophages and neutrophils. MPO activity was determined fluorometrically using hypochlorite-specific 3'-(p-aminophenyl) fluorescein (APF). The effect of LGM2605 on (a) the peroxidase cycle of MPO was determined using Amplex Red while the effect on (b) the chlorination cycle was determined using a taurine chloramine assay. Using electron paramagnetic resonance (EPR) spectroscopy we determined the effect of LGM2605 on the EPR signals of MPO. Finally, computational docking of SDG was used to identify energetically favorable docking poses to enzyme's active site. LGM2605 inhibited human and murine MPO activity. MPO inhibition was observed in the absence and presence of Cl - . EPR confirmed that LGM2605 suppressed the formation of Compound I, an oxoiron (IV) intermediate [Fe(IV)O] containing a porphyrin π-radical of MPO's catalytic cycle. Computational docking revealed that SDG can act as an inhibitor by binding to the enzyme's active site. We conclude that LGM2605 inhibits MPO activity by suppressing both the peroxidase and chlorination cycles. EPR analysis demonstrated that LGM2605 inhibits MPO by decreasing the formation of the highly oxidative Compound I. This study identifies a novel mechanism of LGM2605 action as an inhibitor of MPO and indicates that LGM2605 may be a promising attenuator of oxidant-dependent inflammatory tissue damage. Copyright © 2018 Elsevier B.V. All rights reserved.

  7. Treatment for non-inflammatory pain in a rheumatologist's practice

    Directory of Open Access Journals (Sweden)

    Natalia Vladimirovna Chichasova

    2013-01-01

    Full Text Available The paper presents data on different approaches to analgesia in relation to the mechanism of pain. Pregabalin (lyrica has demonstrated a rapid development of an analgesic effect in different types of non-inflammatory pain: neuropathic pain, pain in fibromyalgia syndrome. The dose-dependent effect of pregabalin and its satisfactory tolerance are noted.

  8. Mobilization of microspheres from a fractured soil during intermittent infiltration events

    Science.gov (United States)

    Mohanty, Sanjay; Bulicek, Mark; Metge, David W.; Harvey, Ronald W.; Ryan, Joseph N.; Boehm, Alexandria B.

    2015-01-01

    Pathogens or biocolloids mobilized in the vadose zone may consequently contaminate groundwater. We found that microspheres were mobilized from a fractured soil during intermittent rainfall and the mobilization was greater when the microsphere size was larger and when the soil had greater water permeability.The vadose zone filters pathogenic microbes from infiltrating water and consequently protects the groundwater from possible contamination. In some cases, however, the deposited microbes may be mobilized during rainfall and migrate into the groundwater. We examined the mobilization of microspheres, surrogates for microbes, in an intact core of a fractured soil by intermittent simulated rainfall. Fluorescent polystyrene microspheres of two sizes (0.5 and 1.8 mm) and Br− were first applied to the core to deposit the microspheres, and then the core was subjected to three intermittent infiltration events to mobilize the deposited microspheres. Collecting effluent samples through a 19-port sampler at the base of the core, we found that water flowed through only five ports, and the flow rates varied among the ports by a factor of 12. These results suggest that flow paths leading to the ports had different permeabilities, partly due to macropores. Although 40 to 69% of injected microspheres were retained in the core during their application, 12 to 30% of the retained microspheres were mobilized during three intermittent infiltration events. The extent of microsphere mobilization was greater in flow paths with greater permeability, which indicates that macropores could enhance colloid mobilization during intermittent infiltration events. In all ports, the 1.8-mm microspheres were mobilized to a greater extent than the 0.5-mm microspheres, suggesting that larger colloids are more likely to mobilize. These results are useful in assessing the potential of pathogen mobilization and colloid-facilitated transport of contaminants in the subsurface under natural infiltration

  9. (−-Epigallocatechin gallate inhibits endotoxin-induced expression of inflammatory cytokines in human cerebral microvascular endothelial cells

    Directory of Open Access Journals (Sweden)

    Li Jieliang

    2012-07-01

    Full Text Available Abstract Background (−-Epigallocatechin gallate (EGCG is a major polyphenol component of green tea that has antioxidant activities. Lipopolysaccharide (LPS induces inflammatory cytokine production and impairs blood–brain barrier (BBB integrity. We examined the effect of EGCG on LPS-induced expression of the inflammatory cytokines in human cerebral microvascular endothelial cells (hCMECs and BBB permeability. Methods The expression of TNF-α, IL-1β and monocyte chemotactic protein-1 (MCP-1/CCL2 was determined by quantitative real time PCR (qRT-PCR and ELISA. Intercellular adhesion molecule 1 (ICAM-1 and vascular cell adhesion molecule (VCAM in hCMECs were examined by qRT-PCR and Western blotting. Monocytes that adhered to LPS-stimulated endothelial cells were measured by monocyte adhesion assay. Tight junctional factors were detected by qRT-PCR (Claudin 5 and Occludin and immunofluorescence staining (Claudin 5 and ZO-1. The permeability of the hCMEC monolayer was determined by fluorescence spectrophotometry of transmembrane fluorescin and transendothelial electrical resistance (TEER. NF-kB activation was measured by luciferase assay. Results EGCG significantly suppressed the LPS-induced expression of IL-1β and TNF-α in hCMECs. EGCG also inhibited the expression of MCP-1/CCL2, VCAM-1 and ICAM-1. Functional analysis showed that EGCG induced the expression of tight junction proteins (Occludin and Claudin-5 in hCMECs. Investigation of the mechanism showed that EGCG had the ability to inhibit LPS-mediated NF-κB activation. In addition, 67-kD laminin receptor was involved in the anti-inflammatory effect of EGCG. Conclusions Our results demonstrated that LPS induced inflammatory cytokine production in hCMECs, which could be attenuated by EGCG. These data indicate that EGCG has a therapeutic potential for endotoxin-mediated endothelial inflammation.

  10. Progress in Preparation of Monodisperse Polymer Microspheres

    Science.gov (United States)

    Zhang, Hongyan

    2017-12-01

    The monodisperse crosslinked polymer microspheres have attracted much attention because of their superior thermal and solvent resistance, mechanical strength, surface activity and adsorption properties. They are of wide prospects for using in many fields such as biomedicine, electronic science, information technology, analytical chemistry, standard measurement and environment protection etc. Functional polymer microspheres prepared by different methods have the outstanding surface property, quantum size effect and good potential future in applications with its designable structure, controlled size and large ratio of surface to volume. Scholars of all over the world have focused on this hot topic. The preparation method and research progress in functional polymer microspheres are addressed in the paper.

  11. In vitro anti-inflammatory effects of arctigenin, a lignan from Arctium lappa L., through inhibition on iNOS pathway.

    Science.gov (United States)

    Zhao, Feng; Wang, Lu; Liu, Ke

    2009-04-21

    Arctigenin, a bioactive constituent from dried seeds of Arctium lappa L. (Compositae) which has been widely used as a Traditional Chinese Medicine for dispelling wind and heat included in Chinese Pharmacophere, was found to exhibit anti-inflammatory activities but its molecular mechanism remains unknown yet. To investigate the anti-inflammatory mechanism of arctigenin. Cultured macrophage RAW 264.7 cells and THP-1 cells were used for the experiments. Griess assay was used to evaluate the inhibitory effect of arctigenin on the overproduction of nitric oxide (NO). ELISA was used to determine the level of pro-inflammatory cytokines including tumor necrosis factor alpha (TNF-alpha) and interleukin-6 (IL-6). The inhibitory effect on the enzymatic activity of cyclooxygenase-2 (COX-2) was tested by colorimetric method. Western blot was used to detect the expression of inducible nitric oxide synthase (iNOS) and COX-2. Arctigenin suppressed lipopolysaccharide (LPS)-stimulated NO production and pro-inflammatory cytokines secretion, including TNF-alpha and IL-6 in a dose-dependent manner. Arctigenin also strongly inhibited the expression of iNOS and iNOS enzymatic activity, whereas the expression of COX-2 and COX-2 enzymatic activity were not affected by arctigenin. These results indicated that potent inhibition on NO, TNF-alpha and IL-6, but not COX-2 expression and COX-2 activity, might constitute the anti-inflammatory mechanism of arctigenin. Arctigenin suppressed the overproduction of NO through down-regulation of iNOS expression and iNOS enzymatic activity in LPS-stimulated macrophage.

  12. Controlled Inhibition of the Mesenchymal Stromal Cell Pro-inflammatory Secretome via Microparticle Engineering

    Directory of Open Access Journals (Sweden)

    Sudhir H. Ranganath

    2016-06-01

    Full Text Available Mesenchymal stromal cells (MSCs are promising therapeutic candidates given their potent immunomodulatory and anti-inflammatory secretome. However, controlling the MSC secretome post-transplantation is considered a major challenge that hinders their clinical efficacy. To address this, we used a microparticle-based engineering approach to non-genetically modulate pro-inflammatory pathways in human MSCs (hMSCs under simulated inflammatory conditions. Here we show that microparticles loaded with TPCA-1, a small-molecule NF-κB inhibitor, when delivered to hMSCs can attenuate secretion of pro-inflammatory factors for at least 6 days in vitro. Conditioned medium (CM derived from TPCA-1-loaded hMSCs also showed reduced ability to attract human monocytes and prevented differentiation of human cardiac fibroblasts to myofibroblasts, compared with CM from untreated or TPCA-1-preconditioned hMSCs. Thus, we provide a broadly applicable bioengineering solution to facilitate intracellular sustained release of agents that modulate signaling. We propose that this approach could be harnessed to improve control over MSC secretome post-transplantation, especially to prevent adverse remodeling post-myocardial infarction.

  13. Screening of traditional Chinese medicines with therapeutic potential on chronic obstructive pulmonary disease through inhibiting oxidative stress and inflammatory response.

    Science.gov (United States)

    Zhou, Ming-Xing; Wei, Xuan; Li, Ai-Ling; Wang, Ai-Min; Lu, Ling-Zi; Yang, Yue; Ren, Dong-Mei; Wang, Xiao-Ning; Wen, Xue-Sen; Lou, Hong-Xiang; Shen, Tao

    2016-09-13

    Chronic obstructive pulmonary disease (COPD) is a major public health problem and gives arise to severe chronic morbidity and mortality in the world. Inflammatory response and oxidative stress play dominant roles in the pathological mechanism of COPD, and have been regarded to be two important targets for the COPD therapy. Traditional Chinese medicines (TCMs) possess satisfying curative effects on COPD under guidance of the TCM theory in China, and merit in-depth investigations as a resource of lead compounds. One hundred ninety-six of TCMs were collected, and extracted to establish a TCM extract library, and then further evaluated for their potency on inhibitions of oxidative stress and inflammatory response using NADP(H):quinone oxidoreductase (QR) assay and nitric oxide (NO) production assay, respectively. Our investigation observed that 38 of the tested TCM extracts induced QR activity in hepa 1c1c7 murine hepatoma cells, and 55 of them inhibited NO production in RAW 264.7 murine macrophages at the tested concentrations. Noteworthily, 20 of TCM extracts simultaneously inhibited oxidative stress and inflammatory responses. The observed bioactive TCMs, particularly these 20 TCMs with dual inhibitory effects, might be useful for the treatment of COPD. More importantly, the results of the present research afford us an opportunity to discover new lead molecules as COPD therapeutic agents from these active TCMs.

  14. Microsphere formation in droplets using antisolvent vapour precipitation technique

    OpenAIRE

    Chew, Sean Jun Liang

    2017-01-01

    In previous studies, the antisolvent vapour precipitation method has been proven to produce uniformly sized lactose microspheres (1.0 µm) from a single droplet (1.2 mm diameter) at atmospheric pressure. These types of particles have potential applications in the pharmaceutical industry, especially due to their high dissolution rate. This project looked into the possibility of using antisolvent vapour precipitation to produce microspheres from finely atomised droplets. Microspheres in the sub-...

  15. Negative effect of non-steroidal anti-inflammatory drugs on the ...

    African Journals Online (AJOL)

    Ciprofloxacin, a second generation fluoroquinolone is often co-administered with non-steroidal anti-inflammatory drugs (NSAIDs) in life threatening situations in which Staphylococcus aureus infections are accompanied with pain and inflammation. This study was carried out to investigate possible in vitro interactions in co ...

  16. Simulation Model of Microsphere Distribution for Selective Internal Radiation Therapy Agrees With Observations

    Energy Technology Data Exchange (ETDEWEB)

    Högberg, Jonas, E-mail: jonas.hogberg@radfys.gu.se [Department of Radiation Physics, Sahlgrenska Academy, University of Gothenburg, Gothenburg (Sweden); Rizell, Magnus [Department of Surgery, Sahlgrenska University Hospital, Gothenburg (Sweden); Hultborn, Ragnar; Svensson, Johanna [Department of Oncology, Sahlgrenska University Hospital, Gothenburg (Sweden); Henrikson, Olof [Department of Radiology, Sahlgrenska University Hospital, Gothenburg (Sweden); Mölne, Johan [Department of Pathology, Sahlgrenska University Hospital, Gothenburg (Sweden); Gjertsson, Peter [Department of Clinical Physiology, Sahlgrenska University Hospital, Gothenburg (Sweden); Bernhardt, Peter [Department of Radiation Physics, Sahlgrenska Academy, University of Gothenburg, Gothenburg (Sweden); Department of Medical Physics and Biomedical Engineering, Sahlgrenska University Hospital, Gothenburg (Sweden)

    2016-10-01

    Purpose: To perform a detailed analysis of microsphere distribution in biopsy material from a patient treated with {sup 90}Y-labeled resin spheres and characterize microsphere distribution in the hepatic artery tree, and to construct a novel dichotomous bifurcation model for microsphere deposits and evaluate its accuracy in simulating the observed microsphere deposits. Methods and Materials: Our virtual model consisted of arteries that successively branched into 2 new generations of arteries at 20 nodes. The artery diameter exponentially decreased from the lowest generation to the highest generation. Three variable parameters were optimized to obtain concordance between simulations and measure microsphere distributions: an artery coefficient of variation (ACV) for the diameter of all artery generations and the microsphere flow distribution at the nodes; a hepatic tree distribution volume (HDV) for the artery tree; and an artery diameter reduction (ADR) parameter. The model was tested against previously measured activity concentrations in 84 biopsies from the liver of 1 patient. In 16 of 84 biopsies, the microsphere distribution regarding cluster size and localization in the artery tree was determined via light microscopy of 30-μm sections (mean concentration, 14 microspheres/mg; distributions divided into 3 groups with mean microsphere concentrations of 4.6, 14, and 28 microspheres/mg). Results: Single spheres and small clusters were observed in terminal arterioles, whereas large clusters, up to 450 microspheres, were observed in larger arterioles. For 14 microspheres/mg, the optimized parameter values were ACV=0.35, HDV = 50 cm{sup 3}, and ADR=6 μm. For 4.6 microspheres/mg, ACV and ADR decreased to 0.26 and 0 μm, respectively, whereas HDV increased to 130 cm{sup 3}. The opposite trend was observed for 28 microspheres/mg: ACV = 0.49, HDV = 20 cm{sup 3}, and ADR = 8 μm. Conclusion: Simulations and measurements reveal that microsphere clusters are

  17. XPS analysis of aluminosilicate microspheres bioactivity tested in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Todea, M.; Vanea, E. [Faculty of Physics and Institute of Interdisciplinary Research on Bio-Nano-Sciences, Babes Bolyai University, Cluj-Napoca 400084 (Romania); Bran, S. [University of Medicine and Pharmacy “Iuliu Haţieganu”, Department of Cranio-Maxillofacial Surgery, 400029 Cluj-Napoca (Romania); Berce, P. [Technical University of Cluj-Napoca, Faculty of Machine Building and National Centre of Rapid Prototyping, 400641 Cluj-Napoca (Romania); Simon, S., E-mail: simons@phys.ubbcluj.ro [Faculty of Physics and Institute of Interdisciplinary Research on Bio-Nano-Sciences, Babes Bolyai University, Cluj-Napoca 400084 (Romania)

    2013-04-01

    The study aims to characterize surface properties of aluminosilicate microspheres incorporating yttrium, with potential biomedical applications. Micrometric particles of spherical shape were obtained by spray drying method. The behavior of aluminosilicate microspheres without yttrium and with yttrium was investigated under in vitro conditions, by seven days incubation in simulated body fluid (SBF). The surface elemental composition and the atomic environments on outermost layer of the microspheres, prior to and after incubation in SBF were evaluated by X-ray photoelectron spectroscopy (XPS) in order to investigate their bioactivity. The results were analyzed to underline the effect of yttrium addition on surface properties of the aluminosilicate microspheres and implicitly on the behavior of the samples in simulated body environments.

  18. Liver cancer cells: targeting and prolonged-release drug carriers consisting of mesoporous silica nanoparticles and alginate microspheres.

    Science.gov (United States)

    Liao, Yu-Te; Liu, Chia-Hung; Yu, Jiashing; Wu, Kevin C-W

    2014-01-01

    A new microsphere consisting of inorganic mesoporous silica nanoparticles (MSNs) and organic alginate (denoted as MSN@Alg) was successfully synthesized by air-dynamic atomization and applied to the intracellular drug delivery systems (DDS) of liver cancer cells with sustained release and specific targeting properties. MSN@Alg microspheres have the advantages of MSN and alginate, where MSN provides a large surface area for high drug loading and alginate provides excellent biocompatibility and COOH functionality for specific targeting. Rhodamine 6G was used as a model drug, and the sustained release behavior of the rhodamine 6G-loaded MSN@Alg microspheres can be prolonged up to 20 days. For targeting therapy, the anticancer drug doxorubicin was loaded into MSN@Alg microspheres, and the (lysine)4-tyrosine-arginine-glycine-aspartic acid (K4YRGD) peptide was functionalized onto the surface of MSN@Alg for targeting liver cancer cells, hepatocellular carcinoma (HepG2). The results of the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay and confocal laser scanning microscopy indicate that the MSN@Alg microspheres were successfully uptaken by HepG2 without apparent cytotoxicity. In addition, the intracellular drug delivery efficiency was greatly enhanced (ie, 3.5-fold) for the arginine-glycine-aspartic acid (RGD)-labeled, doxorubicin-loaded MSN@Alg drug delivery system compared with the non-RGD case. The synthesized MSN@Alg microspheres show great potential as drug vehicles with high biocompatibility, sustained release, and targeting features for future intracellular DDS.

  19. Microspheres with an ultra high holmium content for brachytherapy of malignancies

    International Nuclear Information System (INIS)

    Lira, Raphael A.; Myamoto, Douglas M.; Souza, Jaime R.; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de; Osso Junior, Joao A.; Martinelli, Jose R.

    2011-01-01

    The overall objective of this work is to develop biodegradable microspheres intended for internal radiation therapy which provides an improved treatment for hepatic carcinomas. The most studied brachytherapy system employing microspheres made of holmium-biopolymer system is composed by poly(L-lactic acid) (PLLA) and holmium acetylacetonate (HoAcAc). The importance of the holmium high content in the microspheres can be interpreted as follow from a therapeutic standpoint, to achieve an effective use of microspheres loaded with HoAcAc, a high content of holmium is required to yield enough radioactivity with a relatively low amount of microspheres.The usual amounts of holmium that are incorporated in the microspheres composed by poly(L-lactic acid) and HoAcAc are 17.0 ± 0.5% (w/w) of holmium, which corresponds to a loading of about 50% of HoAcAc. Different approaches have been investigated to increase that value. One updated approach towards this direction is the production of microspheres with ultrahigh holmium as matrix using HoAcAc crystals as the sole starting material without the use of biopolymer. Likewise, in the search of microspheres with increased holmium content , it has been demonstrated that by changing the HoAcAc crystal structure by its recrystallization from crystal phase to the amorphous there is lost of acetylacetonate and water molecules causing the increasing of the holmium content. Microspheres were prepared by solvent evaporation, using holmium acetylacetonate (HoAcAc) crystals as the sole ingredient. Microspheres were characterized by using light and scanning electron microscopy, infrared and Raman spectroscopy, differential scanning calorimetry, X-rays diffraction, and confocal laser scanning microscopy. (author)

  20. Microspheres with an ultra high holmium content for brachytherapy of malignancies

    Energy Technology Data Exchange (ETDEWEB)

    Lira, Raphael A.; Myamoto, Douglas M.; Souza, Jaime R.; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Biotecnologia; Osso Junior, Joao A. [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Radiofarmacia; Martinelli, Jose R. [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Ciencias e Tecnologia de Materiais

    2011-07-01

    The overall objective of this work is to develop biodegradable microspheres intended for internal radiation therapy which provides an improved treatment for hepatic carcinomas. The most studied brachytherapy system employing microspheres made of holmium-biopolymer system is composed by poly(L-lactic acid) (PLLA) and holmium acetylacetonate (HoAcAc). The importance of the holmium high content in the microspheres can be interpreted as follow from a therapeutic standpoint, to achieve an effective use of microspheres loaded with HoAcAc, a high content of holmium is required to yield enough radioactivity with a relatively low amount of microspheres.The usual amounts of holmium that are incorporated in the microspheres composed by poly(L-lactic acid) and HoAcAc are 17.0 {+-} 0.5% (w/w) of holmium, which corresponds to a loading of about 50% of HoAcAc. Different approaches have been investigated to increase that value. One updated approach towards this direction is the production of microspheres with ultrahigh holmium as matrix using HoAcAc crystals as the sole starting material without the use of biopolymer. Likewise, in the search of microspheres with increased holmium content , it has been demonstrated that by changing the HoAcAc crystal structure by its recrystallization from crystal phase to the amorphous there is lost of acetylacetonate and water molecules causing the increasing of the holmium content. Microspheres were prepared by solvent evaporation, using holmium acetylacetonate (HoAcAc) crystals as the sole ingredient. Microspheres were characterized by using light and scanning electron microscopy, infrared and Raman spectroscopy, differential scanning calorimetry, X-rays diffraction, and confocal laser scanning microscopy. (author)

  1. New insights into the use of currently available non-steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Brune K

    2015-02-01

    Full Text Available Kay Brune,1 Paola Patrignani2 1Department of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander University Erlangen-Nuremberg, Erlangen, Germany; 2Department of Neuroscience, Imaging and Clinical Sciences, Center of Excellence on Aging, G d’Annunzio University, Chieti, Italy Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs, which act via inhibition of the cyclooxygenase (COX isozymes, were discovered more than 100 years ago. They remain a key component of the pharmacological management of acute and chronic pain. The COX-1 and COX-2 isozymes have different biological functions; analgesic activity is primarily (although not exclusively associated with inhibition of COX-2, while different side effects result from the inhibition of COX-1 and COX-2. All available NSAIDs, including acetaminophen and aspirin, are associated with potential side effects, particularly gastrointestinal and cardiovascular effects, related to their relative selectivity for COX-1 and COX-2. Since all NSAIDs exert their therapeutic activity through inhibition of the COX isozymes, strategies are needed to reduce the risks associated with NSAIDs while achieving sufficient pain relief. A better understanding of the inhibitory activity and COX-1/COX-2 selectivity of an NSAID at therapeutic doses, based on pharmacokinetic and pharmacodynamic properties (eg, inhibitory dose, absorption, plasma versus tissue distribution, and elimination, and the impact on drug tolerability and safety can guide the selection of appropriate NSAIDs for pain management. For example, many NSAIDs with moderate to high selectivity for COX-2 versus COX-1 can be administered at doses that maximize efficacy (~80% inhibition of COX-2 while minimizing COX-1 inhibition and associated side effects, such as gastrointestinal toxicity. Acidic NSAIDs with favorable tissue distribution and short plasma half-lives can additionally be dosed to provide near-constant analgesia while

  2. Surface modification of imprinted polymer microspheres with ultrathin hydrophilic shells to improve selective recognition of glutathione in aqueous media

    Energy Technology Data Exchange (ETDEWEB)

    Song, Renyuan, E-mail: songrenyuan0726@163.com; Hu, Xiaoling; Guan, Ping; Li, Ji; Du, Chunbao; Qian, Liwei; Wang, Chaoli

    2016-03-01

    A universal, effective approach addressing the classical limitations of hydrophobic molecularly imprinted polymer (MIP) microspheres was described. Two water-compatible MIP microspheres with ultrathin hydrophilic shells were synthesized by controllable surface-graft polymerization using a charged monomer (methacrylic acid) and uncharged monomer (N-isopropylacrylamide) as the hydrophilic functional monomers for the recognition of glutathione in the aqueous medium. The morphological and chemical characteristics of the as-prepared water-compatible MIP microspheres were investigated by scanning electron microscopy, Fourier transform infrared spectroscopy and contact angle measurements. Their selective recognition properties were investigated by static binding tests and compared with those of the ungrafted MIP microspheres. The results of this study showed that the both as-prepared water-compatible MIP microspheres effectively decreased non-specific binding and enhanced the imprinting factor significantly, and the water-compatible MIP microspheres prepared using N-isopropylacrylamide as monomer exhibited a more remarkable recognition property. In addition, the thickness of surface-grafted hydrophilic layer was well controlled by adjusting the irradiation time to obtain the excellent recognition property. Finally, the applicability of the as-prepared water-compatible MIP microspheres as solid-phase extraction materials was investigated by competitive binding tests using a mixture of glutathione and its analogs. - Highlights: • Ultrathin hydrophilic shell was synthesized by controllable SIP approach. • Low nonspecific binding, high imprinting factor and selectivity were achieved. • Value of imprinting factor was controlled by adjusting irradiation time. • Selective solid-phase extraction of glutathione from a mixed solution of peptides.

  3. Preparation and Comparative Bioavailability Studies of Indomethacin-Loaded Cetyl Alcohol Microspheres

    Directory of Open Access Journals (Sweden)

    N. Vishal Gupta

    2013-01-01

    Full Text Available The purpose of the present study was to compare the in vitro release and to find out whether the bioavailability of a 75 mg indomethacin capsule (Microcid SR was equivalent to optimized formulation (indomethacin-loaded cetyl alcohol microspheres. Indomethacin-loaded cetyl alcohol microspheres were prepared by meltable emulsified cooling-induced technique. Surface morphology of microspheres has been evaluated using scanning electron microscopy. A single dose, randomized, complete cross over study of IM microspheres was carried out on 10 healthy male and female Albino sheep’s under fasting conditions. The plasma was separated and the concentrations of the drug were determined by HPLC-UV method. Plasma indomethacin concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The SEM images revealed the spherical shape of fat microspheres, and more than 98.0% of the isolated microspheres were in the size range 12–32 μm. DSC, FTIR spectroscopy and stability studies indicated that the drug after encapsulation with fat microspheres was stable and compatible. Both formulations were found to be bioequivalent as evidenced by in vivo studies. Based on this study, it can be concluded that cetyl alcohol microspheres and Microcid SR capsule are bioequivalent in terms of the rate and extent of absorption.

  4. Application of superparamagnetic microspheres for affinity adsorption and purification of glutathione

    International Nuclear Information System (INIS)

    Wang Qiang; Guan Yueping; Yang Mingzhu

    2012-01-01

    The superparamagnetic poly-(MA–DVB) microspheres with micron size were synthesized by the modified suspension polymerization method. Adsorption of glutathione by magnetic poly-(MA–DVB) microspheres with IDA-copper was investigated. The effect of solution pH value, affinity adsorption and desorption of glutathione was studied. The results showed that the optimum pH value for glutathione adsorption was found at pH=3.5, the maximum capacity for glutathione of magnetic poly-(MA–DVB) microspheres was estimated at 42.4 mg/g by fitting the experimental data to the Langmuir equation. The adsorption equilibrium of glutathione was obtained in about 10 min and the adsorbed glutathione was desorbed from the magnetic microspheres in about 30 min using NaCl buffer solution. The magnetic microspheres could be repeatedly utilized for the affinity adsorption of glutathione. - Highlights: ► The magnetic microsphere with surface IDA–Cu groups was synthesized. ► The magnetic microspheres were applied for adsorption of GSH. ► The adsorption–desorption of glutathione was investigated. ► The maximum adsorption capacity of GSH was fitted at 42.4 mg/g.

  5. Effects of Intermediates between Vitamins K2 and K3 on Mammalian DNA Polymerase Inhibition and Anti-Inflammatory Activity

    Directory of Open Access Journals (Sweden)

    Takeshi Azuma

    2011-02-01

    Full Text Available Previously, we reported that vitamin K3 (VK3, but not VK1 or VK2 (=MK-4, inhibits the activity of human DNA polymerase γ (pol γ. In this study, we chemically synthesized three intermediate compounds between VK2 and VK3, namely MK-3, MK-2 and MK-1, and investigated the inhibitory effects of all five compounds on the activity of mammalian pols. Among these compounds, MK-2 was the strongest inhibitor of mammalian pols α, κ and λ, which belong to the B, Y and X families of pols, respectively; whereas VK3 was the strongest inhibitor of human pol γ, an A-family pol. MK-2 potently inhibited the activity of all animal species of pol tested, and its inhibitory effect on pol λ activity was the strongest with an IC50 value of 24.6 μM. However, MK-2 did not affect the activity of plant or prokaryotic pols, or that of other DNA metabolic enzymes such as primase of pol α, RNA polymerase, polynucleotide kinase or deoxyribonuclease I. Because we previously found a positive relationship between pol λ inhibition and anti-inflammatory action, we examined whether these compounds could inhibit inflammatory responses. Among the five compounds tested, MK-2 caused the greatest reduction in 12-O-tetradecanoylphorbol-13-acetate (TPA-induced acute inflammation in mouse ear. In addition, in a cell culture system using mouse macrophages, MK-2 displayed the strongest suppression of the production of tumor necrosis factor (TNF-α induced by lipopolysaccharide (LPS. Moreover, MK-2 was found to inhibit the action of nuclear factor (NF-κB. In an in vivo mouse model of LPS-evoked acute inflammation, intraperitoneal injection of MK-2 in mice led to suppression of TNF-α production in serum. In conclusion, this study has identified VK2 and VK3 intermediates, such as MK-2, that are promising anti-inflammatory candidates.

  6. Surface modification of cyclomatrix polyphosphazene microsphere by thiol-ene chemistry and lectin recognition

    International Nuclear Information System (INIS)

    Chen, Chen; Zhu, Xue-yan; Gao, Qiao-ling; Fang, Fei; Huang, Xiao-jun

    2016-01-01

    Graphical abstract: A new synthetic route leading to polyphosphazene cyclomatrix microsphere with various functional groups has achieved via thiol-ene click modification. Herein, hexacholorocyclophosphazene (HCCP) crosslinked with bisphenol-S and 4,4′-diallyl bisphenol-S to generate broadly dispersed microspheres. Thiol-ene modification under UV irradiation not only presented high efficiency and flexibility for post-functionalization, but also imposed no harm on global morphology and crosslinked skeleton of such microspheres. - Highlights: • Functional polyphosphazene microspheres with high chemical flexibility were synthesized by thiol-ene modification. • Polyphosphazene microspheres possessed high thermal stability. • Glycosylated polyphosphazene microspheres showed affinity to lectin Con-A, which inferred potential application in biomedicine. - Abstract: A new synthetic route leading to functional polyphosphazene cyclomatrix microsphere has been developed via thiol-ene click modification. Hexacholorocyclophosphazene (HCCP) was crosslinked with both bisphenol-S and 4,4′-diallyl bisphenol-S to obtain vinyl polyphosphazene microspheres (VPZM) in order to ensure high crosslinking degree and introduce vinyl moieties. Compared to the microspheres obtained by HCCP and bisphenol-S, the size of VPZM was broadly dispersed from 400 nm to 1.40 μm. Thiol-ene click reactions were carried out to attach functional groups, such as glucosyl, carboxyl, ester and dodecyl groups onto polyphosphazene microspheres, which demonstrated no change in morphology and size after modification. Solid state NMR (SSNMR) and Fourier transform infrared spectoscopy (FT-IR) results showed that the vinyl moieties were introduced in the period of crosslinking and functionalization was also successful via click reactions. Moreover, the microspheres presented a little difference in thermal properties after modification. Concanavalin A (Con-A) fluorescent adsorption was also observed for

  7. Surface modification of cyclomatrix polyphosphazene microsphere by thiol-ene chemistry and lectin recognition

    Energy Technology Data Exchange (ETDEWEB)

    Chen, Chen; Zhu, Xue-yan; Gao, Qiao-ling; Fang, Fei; Huang, Xiao-jun, E-mail: hxjzxh@zju.edu.cn

    2016-11-30

    Graphical abstract: A new synthetic route leading to polyphosphazene cyclomatrix microsphere with various functional groups has achieved via thiol-ene click modification. Herein, hexacholorocyclophosphazene (HCCP) crosslinked with bisphenol-S and 4,4′-diallyl bisphenol-S to generate broadly dispersed microspheres. Thiol-ene modification under UV irradiation not only presented high efficiency and flexibility for post-functionalization, but also imposed no harm on global morphology and crosslinked skeleton of such microspheres. - Highlights: • Functional polyphosphazene microspheres with high chemical flexibility were synthesized by thiol-ene modification. • Polyphosphazene microspheres possessed high thermal stability. • Glycosylated polyphosphazene microspheres showed affinity to lectin Con-A, which inferred potential application in biomedicine. - Abstract: A new synthetic route leading to functional polyphosphazene cyclomatrix microsphere has been developed via thiol-ene click modification. Hexacholorocyclophosphazene (HCCP) was crosslinked with both bisphenol-S and 4,4′-diallyl bisphenol-S to obtain vinyl polyphosphazene microspheres (VPZM) in order to ensure high crosslinking degree and introduce vinyl moieties. Compared to the microspheres obtained by HCCP and bisphenol-S, the size of VPZM was broadly dispersed from 400 nm to 1.40 μm. Thiol-ene click reactions were carried out to attach functional groups, such as glucosyl, carboxyl, ester and dodecyl groups onto polyphosphazene microspheres, which demonstrated no change in morphology and size after modification. Solid state NMR (SSNMR) and Fourier transform infrared spectoscopy (FT-IR) results showed that the vinyl moieties were introduced in the period of crosslinking and functionalization was also successful via click reactions. Moreover, the microspheres presented a little difference in thermal properties after modification. Concanavalin A (Con-A) fluorescent adsorption was also observed for

  8. Low-Intensity Ultrasound-Induced Anti-inflammatory Effects Are Mediated by Several New Mechanisms Including Gene Induction, Immunosuppressor Cell Promotion, and Enhancement of Exosome Biogenesis and Docking

    Directory of Open Access Journals (Sweden)

    Qian Yang

    2017-10-01

    Full Text Available Background: Low-intensity ultrasound (LIUS was shown to be beneficial in mitigating inflammation and facilitating tissue repair in various pathologies. Determination of the molecular mechanisms underlying the anti-inflammatory effects of LIUS allows to optimize this technique as a therapy for the treatment of malignancies and aseptic inflammatory disorders.Methods: We conducted cutting-edge database mining approaches to determine the anti-inflammatory mechanisms exerted by LIUS.Results: Our data revealed following interesting findings: (1 LIUS anti-inflammatory effects are mediated by upregulating anti-inflammatory gene expression; (2 LIUS induces the upregulation of the markers and master regulators of immunosuppressor cells including MDSCs (myeloid-derived suppressor cells, MSCs (mesenchymal stem cells, B1-B cells and Treg (regulatory T cells; (3 LIUS not only can be used as a therapeutic approach to deliver drugs packed in various structures such as nanobeads, nanospheres, polymer microspheres, and lipidosomes, but also can make use of natural membrane vesicles as small as exosomes derived from immunosuppressor cells as a novel mechanism to fulfill its anti-inflammatory effects; (4 LIUS upregulates the expression of extracellular vesicle/exosome biogenesis mediators and docking mediators; (5 Exosome-carried anti-inflammatory cytokines and anti-inflammatory microRNAs inhibit inflammation of target cells via multiple shared and specific pathways, suggesting exosome-mediated anti-inflammatory effect of LIUS feasible; and (6 LIUS-mediated physical effects on tissues may activate specific cellular sensors that activate downstream transcription factors and signaling pathways.Conclusions: Our results have provided novel insights into the mechanisms underlying anti-inflammatory effects of LIUS, and have provided guidance for the development of future novel therapeutic LIUS for cancers, inflammatory disorders, tissue regeneration and tissue repair.

  9. Development and Evaluation of Floating Microspheres of Curcumin ...

    African Journals Online (AJOL)

    Purpose: To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence time and increased drug bioavailability. Methods: Floating microsphere were prepared by emulsion solvent diffusion method, using hydroxylpropyl methylcellulose (HPMC), ethyl cellulose (EC), Eudragit S 100 polymer in ...

  10. Microspheres of poly(ε-caprolactone) loaded Holmium-165: morphology and thermal degradation behavior

    International Nuclear Information System (INIS)

    Geraldes, Adriana Napoleao; Miyamoto, Douglas Massao; Lira, Raphael Arivar de; Osso Junior, Joao Alberto; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de

    2011-01-01

    Polycaprolactone (PCL), being one of the most important biocompatible and biodegradable aliphatic polyester, provides many potential biomedical. The preparation of biodegradable materials, polymer-based microspheres, is being developed by our group and the goal is to prepare and label with Ho-165 different polymer-based microspheres. The use of radionuclide-loaded microspheres is a promising treatment of liver malignancies. PCL microspheres can be loaded with holmium acetylacetonate (HoAcAc). PCL and PCL/HoAcAc microspheres were prepared by an emulsion solvent extraction/evaporation technique. The PCL/ HoAcAc microspheres were irradiated in a nuclear reactor IEA-R1 at IPEN/CNEN-SP to radionuclide activation. Gamma irradiation was performed at 25 and 50 kGy doses. The microspheres were evaluated by differential scanning calorimetry analysis (DSC), thermogravimetric analysis (TG), Fourier transformed infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and con focal laser scanning microscopy (CLSM). In the CLSM images were observed emission in 488 nm characteristic of holmium. The SEM surface image of PCL/HoAcAc microspheres showed more roughness than PCL microspheres. TG of PCL/HoAcAc microspheres showed a substantial weight loss above 200 degree C, indicating decomposition of HoAcAc. The residual weight indicates the presence of Ho 2 O 3 . Gamma irradiation at 25 and 50 kGy doses had no effect on the PCL/HoAcAc microspheres, which indicates that the chemical composition of the microspheres had not change. (author)

  11. Microspheres of poly({epsilon}-caprolactone) loaded Holmium-165: morphology and thermal degradation behavior

    Energy Technology Data Exchange (ETDEWEB)

    Geraldes, Adriana Napoleao; Miyamoto, Douglas Massao; Lira, Raphael Arivar de; Osso Junior, Joao Alberto; Nascimento, Nanci; Azevedo, Mariangela de Burgos M. de [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil)

    2011-07-01

    Polycaprolactone (PCL), being one of the most important biocompatible and biodegradable aliphatic polyester, provides many potential biomedical. The preparation of biodegradable materials, polymer-based microspheres, is being developed by our group and the goal is to prepare and label with Ho-165 different polymer-based microspheres. The use of radionuclide-loaded microspheres is a promising treatment of liver malignancies. PCL microspheres can be loaded with holmium acetylacetonate (HoAcAc). PCL and PCL/HoAcAc microspheres were prepared by an emulsion solvent extraction/evaporation technique. The PCL/ HoAcAc microspheres were irradiated in a nuclear reactor IEA-R1 at IPEN/CNEN-SP to radionuclide activation. Gamma irradiation was performed at 25 and 50 kGy doses. The microspheres were evaluated by differential scanning calorimetry analysis (DSC), thermogravimetric analysis (TG), Fourier transformed infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and con focal laser scanning microscopy (CLSM). In the CLSM images were observed emission in 488 nm characteristic of holmium. The SEM surface image of PCL/HoAcAc microspheres showed more roughness than PCL microspheres. TG of PCL/HoAcAc microspheres showed a substantial weight loss above 200 degree C, indicating decomposition of HoAcAc. The residual weight indicates the presence of Ho{sub 2}O{sub 3}. Gamma irradiation at 25 and 50 kGy doses had no effect on the PCL/HoAcAc microspheres, which indicates that the chemical composition of the microspheres had not change. (author)

  12. Effect of Fabrication Process Parameters on the Size of Gelatin/Nanohydroxyapatite Microspheres

    Directory of Open Access Journals (Sweden)

    S. Bagheri-Khoulenjani

    2009-12-01

    Full Text Available Nano-hydroxyapatite/gelatin (nHA/Ge microspheres are currently used in bone tissue engineering as bone filler. In this  study, the effect of fabrication process parameters on the particle size of nano-hydroxyapatite/gelatinmicrospheres was investigated. The nHA/Ge microspheres were fabricated using water in oil emulsion. In order to design an experimental design, a surface response model with 2 factors including the rate of shaking and water to oil volume ratio in 3 levels was applied. Particle size was evaluated by using an optical microscope. The morphology of microspheres and distribution of nano-particles within the microspheres were studied by using scanning electron microscope and Ca elemental map obtained from energy dispersive X-ray analysis (EDX, respectively. Statistical analysis of the results obtained from particle size measurements revealed that the rate of shaking has stronger influence on the particle size of microspheres. Morphological studies showed that the fabricated microspheres were spherical with smooth surface. Ca elemental map of the microspheres showed that nano-hydroxyapatite particles distributed uniformly within the microspheres.

  13. Gastroduodenal mucosal defence mechanisms and the action of non-steroidal anti-inflammatory agents.

    Science.gov (United States)

    Garner, A; Allen, A; Rowe, P H

    1987-01-01

    This review summarises gastroduodenal protective mechanisms, the actions of non-steroidal anti-inflammatory (NSAI) agents on mucus and HCO3 secretions, and the basis of gastric mucosal injury induced by acetylsalicylic and salicylic acids (ASA and SA). Resistance to autodigestion by acid and pepsin present in gastric juice is multifactorial involving pre-epithelial (mucus-bicarbonate barrier) and post-epithelial (blood flow, acid-base balance) factors in addition to properties of the surface cell layer per se. The latter includes mucosal re-epithelialisation, a property which appears particularly important with respect to recovery from acute injury. A range of NSAI agents (ASA, fenclofenac, ibuprofen and indomethacin) inhibit gastric HCO3 transport in isolated mucosal preparations. Inhibition of duodenal HCO3 transport has been demonstrated in response to indomethacin in vitro and in vivo. These effects on secretion can be antagonised by exogenous prostaglandins of the E series. The layer of secreted mucus gel overlying the epithelial surface is not affected by NSAI drugs in the short term. However a number of these agents have been shown to inhibit glycoprotein biosynthesis by the epithelial cells. Thus loss of this protective coat could be anticipated during chronic drug exposure since erosion of adherent mucus by luminal shear and proteolysis would not be compensated by continued secretion. Detailed analysis of the gastric mucosal injury induced by salicylates both in vitro and in vivo reveals that much of the damage previously attributed to ASA is in fact due to the metabolic product SA. In this respect it is concluded that mucosal injury caused by ASA is due to a combination of two factors.(ABSTRACT TRUNCATED AT 250 WORDS)

  14. TIPE2 Inhibits the Expression of Asthma-Related Inflammatory Factors in Hyperstretched Bronchial Epithelial Cells Through the Wnt/β-Catenin Pathway.

    Science.gov (United States)

    Sun, Xinrong; Chen, Lu; Yan, Wen

    2017-06-01

    Childhood asthma, an airway inflammatory disease, is a serious threat to the child's quality of life. Recently, TIPE2 expression was reported to be decreased in children with asthma. Therefore, additional studies focusing on TIPE2 might provide an approach for treating childhood asthma. In this study, we found that TIPE2 was poorly expressed in hyperstretched human bronchial epithelial cells (BEAS-2B). TIPE2 overexpression also significantly suppressed the stretch-induced secretion of asthma-related inflammatory factors (TNF-α, TSLP, MMP-9, and VEGF). In contrast, TIPE2 inhibition significantly promoted the secretion of TNF-α, TSLP, MMP-9, and VEGF. Furthermore, overexpression of TIPE2 remarkably inhibited the activation of Wnt/β-catenin in hyperstretched BEAS-2B cells, while siTIPE2 activated Wnt/β-catenin in hyperstretched BEAS-2B cells. Further analysis showed that the Wnt/β-catenin signal inhibitor Dkk-1 could further enhance the TIPE2-induced suppression of Wnt/β-catenin signaling, which also suppressed the siTIPE2-induced secretion of TNF-α, TSLP, MMP-9, and VEGF in hyperstretched BEAS-2B cells. Dkk-1 reversed the effects of siRNA-TIPE2 on Wnt/β-catenin signaling and inflammatory cytokines. In summary, we have exhibited that TIPE2 inhibited the expression of asthma-related inflammatory factors in hyperstretched BEAS-2B cells by suppressing the Wnt/β-catenin signaling pathway. TIPE2 may be involved in airway inflammation during asthma attack, and it may be used as a potential therapeutic target for bronchial epithelial inflammation in childhood asthma.

  15. Evaluation of nonradioactive, colored microspheres for measurement of regional myocardial blood flow in dogs

    International Nuclear Information System (INIS)

    Hale, S.L.; Alker, K.J.; Kloner, R.A.

    1988-01-01

    Measurement of regional myocardial blood flow (RMBF) is crucial in experimental studies of myocardial ischemia and reperfusion in dogs. The standard measurement technique uses radioactive microspheres; however, not all institutions are able to dispose of radioactive waste and therefore cannot make use of this method. We tested a new, nonradioactive microsphere, labeled with colors instead of nuclides. Simultaneous blood flow measurements with two nuclide-labeled and two colored microspheres were performed after coronary occlusion in dogs. Both techniques show a within-method correlation of r greater than 0.98. Duplicate variability for paired RMBF values in 80 samples was 8.7 +/- 0.1% when computed with radioactive microspheres and 13.2 +/- 1.8% when computed with colored microspheres. There was a good correlation in the measurement of RMBF between the radioactive- and colored-microsphere methods (r = 0.98). The best-fitting linear regression line was expressed by the formula: Colored-microsphere RMBF = 1.11 (radioactive-microsphere RMBF)-0.02. When measured by colored microspheres, RMBF was approximately 8% higher than when computed with radioactive microspheres for blood flow values of 0-2 ml/min/g. When blood flow was increased pharmacologically to levels of 2-7.5 ml/min/g, colored microspheres yielded blood flow values 39% higher than the values computed by radioactive microspheres. We conclude that the nonradioactive, colored-microsphere method correlates with the radioactive technique, but at high flows, it yields values greater than those obtained with radioactive microspheres

  16. Assessment of topical non-steroidal anti-inflammatory drugs in animal models.

    Science.gov (United States)

    Hiramatsu, Y; Akita, S; Salamin, P A; Maier, R

    1990-10-01

    Four commercial gel preparations of topical anti-inflammatory agents have been assessed in six animal models commonly used to determine the biological activity of non-steroidal anti-inflammatory agents for systemic administration. Only UV-induced erythema of the skin, adjuvant induced arthritis and the measurement of vascular permeability proved suitable for differentiation of the potency of the four topical agents. Carrageenin-induced paw oedema, the cotton pellet test and the assessment of the pain threshold according to Randall and Selitto were of little value. The effects of the gel preparation of diclofenac (CAS 15307-86-5) diethylammonium (Voltaren Emulgel) were comparable to two preparations containing 1% and 5% active ingredient, respectively. Gel 4 showed low overall activity. The experiments demonstrated that some of the models used for the assessment of anti-inflammatory agent for systemic administration proved suitable for the testing of topical preparations and that percutaneous absorption was insufficient to elicit anti-inflammatory effect in the animals at sites remote from the site of application.

  17. Toxic effects of non-steroidal anti-inflammatory agents in rats ...

    African Journals Online (AJOL)

    The toxicosis of some non-steroidal anti-inflammatory drugs, piroxicam, indomethacin, phenylbutazone, and aspirin, which occasionally are locally used in Nigeria as rodenticides have been evaluated in rats using changes in the serum biochemical and haematological parameters as indices of toxicity. In the study, no ...

  18. Non-steroidal anti-inflammatory drugs and risk of pulmonary embolism

    NARCIS (Netherlands)

    Biere-Rafi, Sara; Di Nisio, Marcello; Gerdes, Victor; Porreca, Ettore; Souverein, Patrick; de Boer, Anthonius; Büller, Harry; Kamphuisen, Pieter

    2011-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with an increased risk of arterial thrombosis, but their effect on venous thrombotic events is less well established. The study aimed to assess the risk of symptomatic pulmonary embolism (PE) in patients using NSAIDs and to evaluate

  19. Non-steroidal anti-inflammatory drugs for chronic low back pain

    NARCIS (Netherlands)

    W.T.M. Enthoven (Wendy); P.D.D.M. Roelofs (Pepijn); R.A. Deyo (Richard); M.W. van Tulder (Maurits); B.W. Koes (Bart)

    2016-01-01

    textabstractBackground: Chronic back pain is an important health problem. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat people with low back pain, especially people with acute back pain. Short term NSAID use is also recommended for pain relief in people with chronic back

  20. Novel local drug delivery system using thermoreversible gel in combination with polymeric microspheres or liposomes.

    Science.gov (United States)

    Arai, Takao; Benny, Ofra; Joki, Tatsuhiro; Menon, Lata G; Machluf, Marcelle; Abe, Toshiaki; Carroll, Rona S; Black, Peter M

    2010-04-01

    The purpose of our study was to evaluate the application of thermoreversible gelation polymer (TGP) as a local drug delivery system for malignant glioma. Polymeric microspheres or liposomes loaded with doxorubicin (sphere-dox or lipo-dox) were combined with TGP to provide continuous drug delivery of doxorubicin (dox) for kinetic release studies and cell viability assays on glioma cell lines in vitro. For in vivo studies, TGP loaded with dox alone (TGP-dox) was combined with sphere-dox or lipo-dox. Their antitumor effects on subcutaneous human glioma xenografts were evaluated in nude mice. In vitro, TGP combined with sphere-dox or lipo-dox released dox for up to 30 days. In vivo, TGP-dox combined with sphere-dox or lipo-dox inhibited subcutaneous glioma tumor growth until day 32 and day 38, respectively. TGP in combination with microspheres or liposomes successfully prolonged the release of dox and its antitumor effects.

  1. The synthesis and photocatalytic activity of ZnSe microspheres

    International Nuclear Information System (INIS)

    Cao Huaqiang; Xiao Yujiang; Zhang Sichun

    2011-01-01

    This paper reports the synthesis of semiconductor ZnSe microspheres composed of nanoparticles via a solvothermal route between the organic molecule selenophene (C 4 H 4 Se) and ZnCl 2 without adding any surfactant. The ZnSe microspheres were characterized by x-ray diffraction (XRD), Raman spectroscopy, scanning electron microscopy (SEM), field emission scanning electron microscopy (FE-SEM), transmission electron microscopy (TEM), high resolution transmission electron microscopy (HRTEM), specific surface area measurement, and photoluminescence (PL) spectra. A strong and broad blue PL emission at 443 nm in wavelength (∼2.79 eV in photon energy) is attributed to the near-band-edge (NBE) emission of ZnSe, while the 530 nm peak is a defect-related (DL) emission. The photocatalytic activity of the as-prepared ZnSe microspheres was evaluated by photodegradation of methyl orange (MO) dye under ultraviolet (UV) light and visible light irradiation. The degradations of MO reach 94% or 95.1%, close to 100%, in the presence of the as-synthesized ZnSe microspheres or commercial ZnSe powder after 7 or 10 h under UV irradiation, respectively. Meanwhile the degradations of MO reach 94.3% or 60.6% in the presence of the as-synthesized ZnSe microspheres or commercial ZnSe powder after 12 h, respectively. The degradation rate of ZnSe microspheres is twice that of ZnSe commercial powder under UV light irradiation, and three times under visible light irradiation. The degradation process of MO dye on ZnSe microspheres under UV or visible light is also discussed.

  2. Role of glycogen synthase kinase-3 beta in the inflammatory response caused by bacterial pathogens.

    Science.gov (United States)

    Cortés-Vieyra, Ricarda; Bravo-Patiño, Alejandro; Valdez-Alarcón, Juan J; Juárez, Marcos Cajero; Finlay, B Brett; Baizabal-Aguirre, Víctor M

    2012-06-12

    Glycogen synthase kinase 3β (GSK3β) plays a fundamental role during the inflammatory response induced by bacteria. Depending on the pathogen and its virulence factors, the type of cell and probably the context in which the interaction between host cells and bacteria takes place, GSK3β may promote or inhibit inflammation. The goal of this review is to discuss recent findings on the role of the inhibition or activation of GSK3β and its modulation of the inflammatory signaling in monocytes/macrophages and epithelial cells at the transcriptional level, mainly through the regulation of nuclear factor-kappaB (NF-κB) activity. Also included is a brief overview on the importance of GSK3 in non-inflammatory processes during bacterial infection.

  3. Nonsteroidal Anti-inflammatory Drugs (NSAIDS) Inhibit the Growth and Reproduction of Chaetomium globosum and Other Fungi Associated with Water-Damaged Buildings.

    Science.gov (United States)

    Dalmont, Kelsey; Biles, Charles L; Konsure, Heather; Dahal, Sujita; Rowsey, Tyler; Broge, Matthew; Poudyal, Shubhra; Gurung, Tara; Shrestha, Sabina; Biles, Caleb L; Cluck, Terry; Howard, Alisha

    2017-12-01

    Indoor mold due to water damage causes serious human respiratory disorders, and the remediation to homes, schools, and businesses is a major expense. Prevention of mold infestation of building materials would reduce health problems and building remediation costs. Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit yeasts and a limited number of filamentous fungi. The purpose of this research was to determine the possible inhibitory activity of nonsteroidal anti-inflammatory drugs (NSAIDs) on germination, fungal growth, and reproduction of Chaetomium globosum and other important filamentous fungi that occur in water-damaged buildings. Several NSAIDs were found to inhibit C. globosum germination, growth, and reproduction. The most effective NSAIDs inhibiting C. globosum were ibuprofen, diflunisal, and diclofenac. Fusarium oxysporum, Fusarium solani, Aspergillus niger, and Stachybotrys atra were also tested on the various media with similar results obtained. However, F. oxysporum and A. niger exhibited a higher level of resistance to aspirin and NaSAL when compared to the C. globosum isolates. The inhibition exhibited by NSAIDs was variable depending on growth media and stage of fungal development. These compounds have a great potential of inhibiting fungal growth on building materials such as gypsum board. Formulations of sprays or building materials with NSAID-like chemical treatments may hold promise in reducing mold in homes and buildings.

  4. [Preparation of citrulline microspheres by spray drying technique for colonic targeting].

    Science.gov (United States)

    Bahri, S; Zerrouk, N; Lassoued, M-A; Tsapis, N; Chaumeil, J-C; Sfar, S

    2014-03-01

    Citrulline is an amino acid that becomes essential in situations of intestinal insufficiency such as short bowel syndrome. It is therefore interesting to provide the patients with dosage forms for routing citrulline to the colon. The aim of this work is to formulate microspheres of citrulline for colonic targeting by the technique of spray drying. Eudragit(®) FS 30D was selected as polymer to encapsulate citrulline using the spray drying technique. Citrulline and Eudragit(®) FS 30D were dissolved in water and ethanol, respectively. The aqueous and the ethanolic solutions were then mixed in 1:2 (v/v) ratio. Microspheres were obtained by nebulizing the citrulline-Eudragit(®) FS 30D solution using a Mini spray dryer equipped with a 0.7mm nozzle. The microspheres have been formulated using citrulline and Eudragit(®) FS 30D. The size distribution of microspheres was determined by light diffraction. The morphology of the microspheres was studied by electron microscopy. Manufacturing yields, encapsulation rate and dissolution profiles were also studied. The microspheres obtained had a spherical shape with a smooth surface and a homogeneous size except for the microspheres containing the highest concentration of polymer (90 %). The formulation showed that the size and morphology of the microspheres are influenced by the polymer concentration. Manufacturing yields were about 51 % but encapsulation rate were always very high (above 90 %). The in vitro dissolution study showed that the use of the Eudragit(®) FS 30D under these conditions is not appropriate to change the dissolution profile of the citrulline. This technique has led to the formulation of microspheres with good physical properties in terms of morphology and size. The compression of the microspheres should help to control citrulline release for colonic targeting. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  5. Investigation of the strontium (Sr(II)) adsorption of an alginate microsphere as a low-cost adsorbent for removal and recovery from seawater.

    Science.gov (United States)

    Hong, Hye-Jin; Ryu, Jungho; Park, In-Su; Ryu, Taegong; Chung, Kang-Sup; Kim, Byuong-Gyu

    2016-01-01

    In this paper, we investigated alginate microspheres as a low-cost adsorbent for strontium (Sr(II)) removal and recovery from seawater. Alginate microspheres have demonstrated a superior adsorption capacity for Sr(II) ions (≈110 mg/g). A Freundlich isotherm model fits well with the Sr(II) adsorption of an alginate microsphere. The mechanism of Sr(II) adsorption is inferred as an ion exchange reaction with Ca(II) ions. The effects of the solution pH and co-existing ions in seawater are also investigated. Except for a pH of 1-2, Sr(II) adsorption capacity is not affected by pH. However, increasing the seawater concentration of metal cations seriously decreases Sr(II) uptake. In particular, highly concentrated (15,000 mg/L) Na(I) ions significantly interfere with Sr(II) adsorption. Sr(II) desorption was performed using 0.1 M HCl and CaCl2. Both regenerants show an excellent desorption efficiency, but the FTIR spectrum reveals that the chemical structure of the microsphere is destroyed after repeated use of HCl. Conversely, CaCl2 successfully desorbed Sr(II) without damage, and the Sr(II) adsorption capacity does not decrease after three repeated uses. The alginate microsphere was also applied to the adsorption of Sr(II) in a real seawater medium. Because of inhibition by co-existing ions, the Sr(II) adsorption capacity was decreased and the adsorption rate was retarded compared with D.I. water. Although the Sr(II) adsorption capacity was decreased, the alginate microsphere still exhibited 17.8 mg/g of Sr(II) uptake in the seawater medium. Considering its excellent Sr(II) uptake in seawater and its reusability, an alginate microsphere is an appropriate cost-effective adsorbent for the removal and recovery of Sr(II) from seawater. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Facile preparation of hierarchically porous polymer microspheres for superhydrophobic coating

    Science.gov (United States)

    Gao, Jiefeng; Wong, Julia Shuk-Ping; Hu, Mingjun; Li, Wan; Li, Robert. K. Y.

    2013-12-01

    A facile method, i.e., nonsolvent assisted electrospraying, is proposed to fabricate hierarchically porous microspheres. The pore size on the microsphere surface ranges from a few tens to several hundred nanometers. Thermally and nonsolvent induced phase separation as well as breath figure is responsible for the formation of the hierarchical structures with different nano-sized pores. The nonsolvent could not only induce phase separation, but also stabilize the interface between the droplet and air, which can prevent the droplet from strong deformation, and is therefore beneficial to the formation of regular and uniform microspheres. On the other hand, solvent evaporation, polymer diffusion and Coulomb fission during electrospraying influence the morphology of finally obtained products. In this paper, the influence of polymer concentration, the weight ratio between nonsolvent and polymer and the flowing rate on the morphology of the porous microsphere is carefully studied. The hierarchically porous microsphere significantly increases the surface roughness and thus the hydrophobicity, and the contact angle can reach as high as 152.2 +/- 1.2°. This nonsolvent assisted electrospraying opens a new way to fabricate superhydrophobic coating materials.A facile method, i.e., nonsolvent assisted electrospraying, is proposed to fabricate hierarchically porous microspheres. The pore size on the microsphere surface ranges from a few tens to several hundred nanometers. Thermally and nonsolvent induced phase separation as well as breath figure is responsible for the formation of the hierarchical structures with different nano-sized pores. The nonsolvent could not only induce phase separation, but also stabilize the interface between the droplet and air, which can prevent the droplet from strong deformation, and is therefore beneficial to the formation of regular and uniform microspheres. On the other hand, solvent evaporation, polymer diffusion and Coulomb fission during

  7. Gelatin-based microspheres crosslinked with glutaraldehyde and rutin oriented to cosmetics

    Directory of Open Access Journals (Sweden)

    Fabiana Graziola

    Full Text Available ABSTRACT Glutaraldehyde (GTA has been extensively used as a gelatin crosslinking agent, however, new natural ones have been suggested as more biocompatible. Polyphenols are possible candidates and the flavonols, such as rutin (RUT, also exhibit potential synergism with sunscreens and antioxidant agents used in cosmetics. In this work, gelatin microspheres (M0 were obtained and crosslinked with GTA 10 mM (MG or RUT 10 mM (MR, dissolved in acetone:NaOH 0,01M (70:30 v/v. MG exhibited crosslinking extent of 54.4%. Gelatin, M0, MG and MR did not elicit any signs of skin damage, regarding the formation of erythema, the barrier function disruption and negative interference in the stratum corneum hydration. Oily dispersions containing M0, MG or MR, isolated or combined with benzophenone-3 or octyl methoxycinnamate, suggested that the microspheres, at a 5.0% w/w, had no additional chemical or physical photoprotective effect in vitro. Crosslinking with RUT had occurred, but in a lower degree than GTA. Microspheres had not improved sun protection parameters, although, non-treated gelatin interfered positively with the SPF for both UV filters. The in vivo studies demonstrated that these materials had very good skin compatibility.

  8. Magnetic propulsion of microspheres at liquid-glass interfaces

    Science.gov (United States)

    Helgesen, Geir

    2018-02-01

    Bio-coated, magnetic microspheres have many applications in biotechnology and medical technology as a tool to separate and extract cells or molecules in a water solution by applying external strong magnetic field gradients. However, magnetic microspheres with or without attached cargo can also be separated in the liquid solution if they are exposed to alternating or rotating, relatively weak magnetic fields. Microspheres that have a higher density than the liquid will approach the bottom surface of the sample cell, and then a combination of viscous and surface frictional forces can propel the magnetic microspheres along the surface in a direction perpendicular to the axis of field rotation. Experiments demonstrating this type of magnetic propulsion are shown, and the forces active in the process are discussed. The motion of particles inside sample cells that were tilted relative to the horizontal direction was studied, and the variation of propulsion velocity as a function of tilt angle was used to find the values of different viscous and mechanical parameters of motion. Propulsion speeds of up to 5 μm/s were observed and were found to be caused by a partly rolling and partly slipping motion of rotating microspheres with a slipping coefficient near 0.6.

  9. PAMs ameliorates the imiquimod-induced psoriasis-like skin disease in mice by inhibition of translocation of NF-κB and production of inflammatory cytokines.

    Directory of Open Access Journals (Sweden)

    Rongkun Dou

    Full Text Available Psoriasis is a chronic and persistent inflammatory skin disease seriously affecting the quality of human life. In this study, we reported an ancient formula of Chinese folk medicine, the natural plant antimicrobial solution (PAMs for its anti-inflammatory effects and proposed the primary mechanisms on inhibiting the inflammatory response in TNF-α/IFN-γ-induced HaCaT cells and imiquimod-induced psoriasis-like skin disease mouse model. Two main functional components of hydroxysafflor Yellow A and allantoin in PAMs were quantified by HPLC to be 94.2±2.2 and 262.9±12.5 μg/mL respectively. PAMs could significantly reduce the gene expression and inflammatory cytokines production of Macrophage-Derived Chemokine (MDC, IL-8 and IL-6 in TNF-α/IFN-γ-induced HaCaT cells. PAMs also significantly ameliorates the psoriatic-like symptoms in a mouse model with the evaluation scores for both the single (scales, thickness, erythema and cumulative features were in the order of blank control < Dexamethasone < PAMs < 50% ethanol < model groups. The results were further confirmed by hematoxylin-eosin staining, RT-qPCR and immunohistochemistry. The down-regulated gene expression of IL-8, TNF-α, ICAM-1 and IL-23 in mouse tissues was consistent with the results from those of the HaCaT cells. The inhibition of psoriasis-like skin inflammation by PAMs was correlated with the inactivation of the translocation of P65 protein into cellular nucleus, indicating the inhibition of the inflammatory NF-κB signaling pathway. Taken together, these findings suggest that PAMs may be a promising drug candidate for the treatment of inflammatory skin disorders, such as psoriasis.

  10. Study on Magnetic Responsibility of Rare Earth Ferrite/Polyacrylamide Magnetic Microsphere

    Institute of Scientific and Technical Information of China (English)

    Zhang Ming; Wang Zhifeng; Zhang Hong; Dai Shaojun; Qiu Guanming; Okamoto Hiroshi

    2005-01-01

    In inverse microemulsion, rare earth ferrite/polyacrylamide magnetic microsphere were prepared and their magnetic responsibility were studied by magnetic balance. Results indicate that the magnetic responsibility of microsphere relates to magnetic moment of rare earth ion, and it can be improved by the addition of dysprosium ion of high magnetic moment. Dysprosium content has an effect on magnetic responsibility of dysprosium ferrite/polyacrylamide magnetic microsphere. The microsphere displays strong magnetic responsibility when the molar ratio of Dy3+/iron is 0.20.

  11. Targeted adenovirus mediated inhibition of NF-kappa B-dependent inflammatory gene expression in endothelial cells in vitro and in vivo

    NARCIS (Netherlands)

    Kuldo, J. M.; Asgeirsdottir, S. A.; Zwiers, P. J.; Bellu, A. R.; Rots, M. G.; Schalk, J. A. C.; Ogawara, K. I.; Trautwein, C.; Banas, B.; Haisma, H. J.; Molema, G.; Kamps, J. A. A. M.

    2013-01-01

    In chronic inflammatory diseases the endothelium expresses mediators responsible for harmful leukocyte infiltration. We investigated whether targeted delivery of a therapeutic transgene that inhibits nuclear factor kappa B signal transduction could silence the proinflammatory activation status of

  12. Targeted adenovirus mediated inhibition of NF-κB-dependent inflammatory gene expression in endothelial cells in vitro and in vivo.

    Science.gov (United States)

    Kułdo, J M; Ásgeirsdóttir, S A; Zwiers, P J; Bellu, A R; Rots, M G; Schalk, J A C; Ogawara, K I; Trautwein, C; Banas, B; Haisma, H J; Molema, G; Kamps, J A A M

    2013-02-28

    In chronic inflammatory diseases the endothelium expresses mediators responsible for harmful leukocyte infiltration. We investigated whether targeted delivery of a therapeutic transgene that inhibits nuclear factor κB signal transduction could silence the proinflammatory activation status of endothelial cells. For this, an adenovirus encoding dominant-negative IκB (dnIκB) as a therapeutic transgene was employed. Selectivity for the endothelial cells was achieved by introduction of antibodies specific for inflammatory endothelial adhesion molecules E-selectin or VCAM-1 chemically linked to the virus via polyethylene glycol. In vitro, the retargeted adenoviruses selectively infected cytokine-activated endothelial cells to express functional transgene. The comparison of transductional capacity of both retargeted viruses revealed that E-selectin based transgene delivery exerted superior pharmacological effects. Targeted delivery mediated dnIκB transgene expression in endothelial cells inhibited the induced expression of several inflammatory genes, including adhesion molecules, cytokines, and chemokines. In vivo, in mice suffering from glomerulonephritis, E-selectin-retargeted adenovirus selectively homed in the kidney to microvascular glomerular endothelium. Subsequent downregulation of endothelial adhesion molecule expression 2 days after induction of inflammation demonstrated the pharmacological potential of this gene therapy approach. The data justify further studies towards therapeutic virus design and optimization of treatment schedules to investigate their capacity to interfere with inflammatory disease progression. Copyright © 2012 Elsevier B.V. All rights reserved.

  13. Preparation of chitosan/nano hydroxyapatite organic-inorganic hybrid microspheres for bone repair.

    Science.gov (United States)

    Chen, Jingdi; Pan, Panpan; Zhang, Yujue; Zhong, Shengnan; Zhang, Qiqing

    2015-10-01

    In this work, we encapsulated icariin (ICA) into chitosan (CS)/nano hydroxyapatite (nHAP) composite microspheres to form organic-inorganic hybrid microspheres for drug delivery carrier. The composition and morphology of composite microspheres were characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and differential scanning calorimetry- thermogravimetric analysis (DSC-TGA). Moreover, we further studied the performance of swelling properties, degradation properties and drug release behavior of the microspheres. ICA, the extract of traditional Chinese medicine-epimedium, was combined to study drug release properties of the microspheres. ICA loaded microspheres take on a sustained release behavior, which can be not only ascribed to electrostatic interaction between reactive negative hydroxyl (OH) of ICA and positive amine groups (NH₂) of CS, but also depended on the homogeneous dispersion of HAP nanoparticles inside CS organic matrix. In addition, the adhesion and morphology of osteoblasts were detected by inverted fluorescence microscopy. The biocompatibility of CS/nHAP/ICA microspheres was evaluated by the MTT cytotoxicity assay, Hoechst 33258 and PI fluorescence staining. These studies demonstrate that composite microspheres provide a suitable microenvironment for osteoblast attachment and proliferation. It can be speculated that the ICA loaded CS-based organic-inorganic hybrid microspheres might have potential applications in drug delivery systems. Copyright © 2015 Elsevier B.V. All rights reserved.

  14. Recent advances in polymeric microspheres for parenteral drug delivery--part 1.

    Science.gov (United States)

    Mao, Shirui; Guo, Chunqiang; Shi, Yi; Li, Luk Chiu

    2012-09-01

    Polymeric microspheres have been established as a valuable parenteral drug delivery system for sustained release of therapeutic agents via subcutaneous or intramuscular injection. Biodegradable polymers which are either synthetic or from natural sources are reviewed with respect to recent advances in exploring their applications for microsphere fabrications. New information on the impact of formulation variables on the properties of microspheres formed by an emulsion method was also presented. The characterization of microspheres using advanced physical analytical techniques was also reviewed and the utilization of the information in assessing in vivo performance of the product was also highlighted. The broad clinical use of microspheres for delivery of therapeutic agents in particular biologics such as proteins has not been realized commercially. The limited availability of biodegradable polymers with a long history of regulatory approval and the challenges in gaining regulatory approval of a new polymer have hindered the development of microspheres for parenteral drug delivery.

  15. Formulation and characterization of ketoprofen embedded polycaprolactone microspheres using solvent evaporation method

    Directory of Open Access Journals (Sweden)

    Pankaj Wagh

    2015-07-01

    Full Text Available The purpose of this study was to prepare polymeric microspheres containing Ketoprofen (KFN by single emulsion [oil-in-water (o/w] solvent evaporation method. Polycaprolactone (PCL, biocompatible polymer, was used for the preparation of sustained released microspheres of KFN. A Plackett–Burman design was employed by using the Design-Expert® software (Version- 9.0.3.1, Stat-Ease Inc., Minneapolis, MN. Eleven factors out of six processing factors were investigated in order to enhance the encapsulation efficiency (EE of the microspheres. The resultant microspheres were characterized for their size, morphology, EE, and drug release. Imaging of particles was performed by field emission scanning electron microscopy. Interaction between the drug and polymers were investigated by Fourier transform infrared (FTIR spectroscopy, X-ray powder diffractometry (XRPD and Differential Scanning Calorimetry (DSC. Graphical and mathematical analyses of the design showed that concentration of factor PCL (B and varying speed (F, revolution per minute, rpm were significant negative effect on the EE and identified as the significant factor determining the EE of the microspheres. The microspheres showed high % EE (31.18 % to 96.81 %. The microspheres were found to be discrete, oval with porous surface. The FTIR analysis confirmed no interaction of KFN with the polymer. The XRPD revealed the dispersion of drug within microspheres formulation. Sustained drug release profile over 12 h was achieved by PCL polymer. In conclusion, polymeric microspheres containing KFN can be successfully prepared using the technique of experimental design, and these results helped in finding the optimum formulation variables for EE of microspheres.

  16. Formulation and Evaluation of Microspheres Based on Gelatin ...

    African Journals Online (AJOL)

    Formulation and Evaluation of Microspheres Based on Gelatin-Mucin Admixtures for the Rectal Delivery of Cefuroxime Sodium. K C Ofokansi, M U Adikwu. Abstract. Purpose: Swellable microspheres based on polymers or their admixtures are frequently employed as drug delivery systems to achieve a controlled release ...

  17. Ulex europaeus 1 lectin targets microspheres to mouse Peyer's patch M-cells in vivo.

    Science.gov (United States)

    Foster, N; Clark, M A; Jepson, M A; Hirst, B H

    1998-03-01

    The interaction of latex microspheres with mouse Peyer's patch membranous M-cells was studied in a mouse gut loop model after the microspheres were coated with a variety of agents. Carboxylated microspheres (diameter 0.5 micron) were covalently coated with lectins Ulex europaeus 1, Concanavalin A, Euonymus europaeus and Bandeiraea simplicifolia 1 isolectin-B4, human immunoglobulin A or bovine serum albumin. Of the treatments examined, only Ulex europaeus (UEA1) resulted in significant selective binding of microspheres to M-cells. UEA1-coated microspheres bound to M-cells at a level 100-fold greater than BSA-coated microspheres, but binding to enterocytes was unaffected. Incubation of UEA1-coated microspheres with alpha-L-fucose reduced M-cell binding to a level comparable with BSA-coated microspheres. This indicated that targeting by UEA1 was via a carbohydrate receptor on the M-cell surface. Adherence of UEA1-coated microspheres to M-cells occurred within 10 min of inoculation into mouse gut loops and UEA1-coated microspheres were transported to 10 microns below the apical surface of M-cells within 60 min of inoculation. UEA1-coated microspheres also targeted mouse Peyer's patch M-cells after intragastric administration. These results demonstrated that altering the surface chemistry of carboxylated polystyrene microspheres increased M-cell targeting, suggesting a strategy to enhance delivery of vaccine antigens to the mucosal immune system.

  18. Ursolic acid isolated from guava leaves inhibits inflammatory mediators and reactive oxygen species in LPS-stimulated macrophages.

    Science.gov (United States)

    Kim, Min-Hye; Kim, Jin Nam; Han, Sung Nim; Kim, Hye-Kyeong

    2015-06-01

    Psidium guajava (guava) leaves have been frequently used for the treatment of rheumatism, fever, arthritis and other inflammatory conditions. The purpose of this study was to identify major anti-inflammatory compounds from guava leaf extract. The methanol extract and its hexane-, dichloromethane-, ethylacetate-, n-butanol- and water-soluble phases derived from guava leaves were evaluated to determine their inhibitory activity on nitric oxide (NO) production by RAW 264.7 cells stimulated with lipopolysaccharide (LPS). The methanol extract decreased NO production in a dose-dependent manner without cytotoxicity at a concentration range of 0-100 μg/mL. The n-butanol soluble phase was the most potent among the five soluble phases. Four compounds were isolated by reversed-phase HPLC from the n-butanol soluble phase and identified to be avicularin, guaijaverin, leucocyanidin and ursolic acid by their NMR spectra. Among these compounds, ursolic acid inhibited LPS-induced NO production in a dose-dependent manner without cytotoxity at a concentration range of 1-10 µM, but the other three compounds had no effect. Ursolic acid also inhibited LPS-induced prostaglandin E2 production. A western blot analysis showed that ursolic acid decreased the LPS-stimulated inducible nitric oxide synthase and cyclooxygenase protein levels. In addition, ursolic acid suppressed the production of intracellular reactive oxygen species in LPS-stimulated RAW 264.7 cells, as measured by flow cytometry. Taken together, these results identified ursolic acid as a major anti-inflammatory compound in guava leaves.

  19. Ankle sprain: the effects of non-steroidal anti-inflammatory drugs

    NARCIS (Netherlands)

    Struijs, Peter A. A.; Kerkhoffs, Gino M. M. J.

    2015-01-01

    Injury of the lateral ligament complex of the ankle joint occurs in about one in 10,000 people per day, accounting for a quarter of all sports injuries. We conducted a systematic overview, aiming to answer the following clinical question: What are the effects of non-steroidal anti-inflammatory drugs

  20. Investigation of defects on PAMS microspheres fabricated with microencapsulation method

    International Nuclear Information System (INIS)

    Chen Sufen; Li Bo; Liu Yiyang; Zhang Zhanwen; Qi Xiaobo

    2012-01-01

    Poly-(α-methylstyrene) (PAMS) microspheres were fabricated with W1/O/W2 double emulsion microencapsulation method, and the effects of polyvinylalcohol (PVA) and CaCl 2 weight concentrations and the O/W2 phase ratio on the percentages of defected PAMS microspheres were studied. The weight concentrations of PVA and CaCl 2 and the O/W2 phase ratio in the fabrication process of PAMS microspheres were optimized. The results show that, for the three parameters being 1.0%, 1.5%, and 0.01, respectively, the percentage of the defect-free PAMS microspheres without vacuoles in the shell wall can be up to 60%. (authors)

  1. Preparation and characterization of composite microspheres for brachytherapy and hyperthermia treatment of cancer

    International Nuclear Information System (INIS)

    Zhao Di; Huang Wenhai; Rahaman, Mohamed N.; Day, Delbert E.; Wang Deping; Gu Yifei

    2012-01-01

    Composite microspheres were prepared by coating yttrium–aluminum–silicate (YAS) glass microspheres (20–30 μm) with a layer of Fe 3 O 4 nanoparticles and evaluated for potential use in brachytherapy and hyperthermia treatment of cancer. After neutron activation to form the β-emitting 90 Y radionuclide, the composite microspheres can be injected into a patient to destroy cancerous tumors; at the same time, the composite microspheres can generate heat upon application of a magnetic field to also destroy the tumors. The results showed that the composite microspheres were chemically durable when immersed in a simulated body fluid (SBF), with ∼ 0.25% weight loss and ∼ 3.2% yttrium dissolved into the SBF after 30 days at 37 °C. The composite microspheres also showed ferromagnetic properties as a result of the Fe 3 O 4 coating; when immersed in water at 20 °C (20 mg in 1 mL of water), the application of an alternating magnetic field produced a temperature increase from 20 °C to 38−46 °C depending on the thickness of the Fe 3 O 4 coating. The results indicate that these composite microspheres have promising potential in combined brachytherapy and hyperthermia treatment of cancerous tumors. - Highlights: ► Composite microspheres for brachytherapy and hyperthermia treatment of cancer. ► Fe 3 O 4 nanoparticles coated on the yttrium–aluminum–silicate glass microspheres. ► Microspheres are chemically stable in SBF. ► Microspheres can generate heat for hyperthermia under an alternating magnetic field. ► Microspheres can emit β-rays for brachytherapy after neutron activation.

  2. Inhibition of the transcription factor c-Jun by the MAPK family, and not the NF-κB pathway, suggests that peanut extract has anti-inflammatory properties.

    Science.gov (United States)

    Catalán, Úrsula; Fernández-Castillejo, Sara; Anglès, Neus; Morelló, Jose Ramón; Yebras, Martí; Solà, Rosa

    2012-10-01

    Tumor necrosis factor-α (TNF-α) is involved in inflammatory responses in atherosclerosis. We propose an in vitro cellular assay to evaluate the anti-inflammatory mechanisms of potential modifiers such as food extracts. In the current model we assessed an anti-inflammatory effect of polyphenol-rich peanut extract in lipopolysaccharide (LPS)-induced THP-1 monocytes. THP-1 monocytes were incubated with peanut extract (5, 25, 50 and 100 μg/mL) consisting of 39% flavonols, 37% flavanols and 24% phenolic acid (or BAY 11-7082 (5 μM) as experiment control) for 1 h and then stimulated with LPS (500 ng/mL) for 4 h. Cytotoxicity was measured as lactate dehydrogenase (LDH) activity release. NF-κB and MAPK family were determined by TransAm kit while TNF-α mRNA levels and its mRNA stability by RT-PCR. Intra- and extracellular TNF-α protein was measured by ELISA, and TNF-α converting enzyme (TACE) activity by a fluorimetric assay. Peanut extract inhibited the maximal LPS-induced extracellular TNF-α protein secretion by 18%, 29% and 47% at 25, 50 and 100 μg/mL, respectively (P<0.05). LPS stimulation revealed that 85% of TNF-α was released extracellularly while 15% remained intracellular. Peanut extract did not modify NF-κB but, instead, reduced c-Jun transcription factor activity (P<0.05), decreased TNF-α mRNA (albeit non-significantly) and had no effect on mRNA stability and TACE activity. Polyphenol-rich peanut extract reduces extracellular TNF-α protein by inhibiting c-Jun transcription factor from MAPK family, suggesting an anti-inflammatory effect. The proposed THP-1 monocyte model could be used to assess food extract impact (site and size effects) on the inflammation pathway. Copyright © 2012 Elsevier Ltd. All rights reserved.

  3. Piperine Inhibits the Activities of Platelet Cytosolic Phospholipase A2 and Thromboxane A2 Synthase without Affecting Cyclooxygenase-1 Activity: Different Mechanisms of Action Are Involved in the Inhibition of Platelet Aggregation and Macrophage Inflammatory Response

    Directory of Open Access Journals (Sweden)

    Dong Ju Son

    2014-08-01

    Full Text Available PURPOSE: Piperine, a major alkaloid of black pepper (Piper nigrum and long pepper (Piper longum, was shown to have anti-inflammatory activity through the suppression of cyclooxygenase (COX-2 gene expression and enzyme activity. It is also reported to exhibit anti-platelet activity, but the mechanism underlying this action remains unknown. In this study, we investigated a putative anti-platelet aggregation mechanism involving arachidonic acid (AA metabolism and how this compares with the mechanism by which it inhibits macrophage inflammatory responses; METHODS: Rabbit platelets and murine macrophage RAW264.7 cells were treated with piperine, and the effect of piperine on the activity of AA-metabolizing enzymes, including cytosolic phospholipase A2 (cPLA2, COX-1, COX-2, and thromboxane A2 (TXA2 synthase, as well as its effect on AA liberation from the plasma membrane components, were assessed using isotopic labeling methods and enzyme immunoassay kit; RESULTS: Piperine significantly suppressed AA liberation by attenuating cPLA2 activity in collagen-stimulated platelets. It also significantly inhibited the activity of TXA2 synthase, but not of COX-1, in platelets. These results suggest that piperine inhibits platelet aggregation by attenuating cPLA2 and TXA2 synthase activities, rather than through the inhibition of COX-1 activity. On the other hand, piperine significantly inhibited lipopolysaccharide-induced generation of prostaglandin (PGE2 and PGD2 in RAW264.7 cells by suppressing the activity of COX-2, without effect on cPLA2; CONCLUSION: Our findings indicate that piperine inhibits platelet aggregation and macrophage inflammatory response by different mechanisms.

  4. Wu-Tou Decoction Inhibits Chronic Inflammatory Pain in Mice: Participation of TRPV1 and TRPA1 Ion Channels

    Directory of Open Access Journals (Sweden)

    Chao Wang

    2015-01-01

    Full Text Available Wu-tou decoction (WTD is a classic traditional Chinese medicine formula and has been used effectively to treat joint diseases clinically. Previous reports indicated that WTD possesses anti-inflammatory activity; however, its actions on pain have not been clarified. Here, we investigated the antinociceptive activity of WTD in CFA-induced mice, and its possible mechanism of the action associated with transient receptor potential (TRP ion channels was also explored. Our results showed that 1.58, 3.15, and 6.30 g/kg WTD significantly attenuated mechanical, cold, and heat hypersensitivities. Moreover, WTD effectively inhibited spontaneous nociceptive responses to intraplantar injections of capsaicin and cinnamaldehyde, respectively. WTD also effectively suppressed jumping and wet-dog-shake behaviors to intraperitoneal injection of icilin. Additionally, WTD significantly reduced protein expression of TRPV1 and TRPA1 in dorsal root ganglia and skins of injured paw. Collectively, our data demonstrate firstly that WTD exerts antinociceptive activity in inflammatory conditions by attenuating mechanical, cold, and heat hypersensitivities. This antinociceptive effect may result in part from inhibiting the activities of TRPV1, TRPA1, and TRPM8, and the suppression of TRPV1 and TRPA1 protein by WTD was also highly effective. These findings suggest that WTD might be an attractive and suitable therapeutic agent for the management of chronic inflammatory pain.

  5. Polydimethylsiloxane microspheres with poly(methyl methacrylate) coating: Modelling, preparation, and characterization

    DEFF Research Database (Denmark)

    Ma, Baoguang; Hansen, Jens Henrik; Hvilsted, Søren

    2015-01-01

    functional PDMS microspheres were coated with poly(methyl methacrylate) (PMMA) by spin coating with different concentrations of PMMA solutions. The quality of the resulting PMMA shell is investigated using rheological measurements at 50 8C with a timesweep procedure. The results strongly suggest that PMMA-coated...... PDMS microspheres react around 20 times slower than the uncoated ones, and that the PMMA shell significantly hinders the reaction between the PDMS microsphere and cross-linker. Thus the thin PMMA shells are very efficient in protecting the reactive PDMS microspheres, since the PMMA shell forms...

  6. FEMIC (Fibromes Embolises aux MICrospheres calibrees): Uterine Fibroid Embolization using Tris-acryl Microspheres. A French Multicenter Study

    International Nuclear Information System (INIS)

    Joffre, Francis; Tubiana, Jean-Michel; Pelage, Jean-Pierre

    2004-01-01

    Purpose: A French multicenter registry was set up to confirm the safety and efficacy of large calibrated tris-acryl gelatin microspheres for embolization of symptomatic fibroids. Methods: Technical recommendations included embolization using large microspheres (>500 μm) with no secondary embolization agent. Postprocedural pain, clinical improvement and adverse events were prospectively evaluated during a follow-up period of at least 6 months.Results: Eighty-five women complaining of fibroid-related symptoms entered the study. In seven women, a secondary embolization agent was used in addition to microspheres. Complete resolution of menorrhagia was achieved in 84% of women at 24 months and significant uterine and fibroid volume reductions were noted after 6 months (37% and 73%, respectively). Three women experienced definitive amenorrhea (4%) and two women required hysteroscopic resection of a fibroid. Eight women were treated by hysterectomy because of treatment failure. In seven of these women, treatment failure was explained by an additional cause of symptoms including diffuse adenomyosis, endometrial hyperplasia or ovarian artery supply to the fibroids.Conclusion: Limited uterine artery embolization using large microspheres has good clinical success rate with low postprocedural pain and complications. Women can expect excellent midterm results with a high level of symptom control and significant fibroid volume reduction. Confidence in the end-point recommended here may require the experience of several cases

  7. Diet Restriction Inhibits Apoptosis and HMGB1 Oxidation and Promotes Inflammatory Cell Recruitment during Acetaminophen Hepatotoxicity

    Science.gov (United States)

    Antoine, Daniel James; Williams, Dominic P; Kipar, Anja; Laverty, Hugh; Park, B Kevin

    2010-01-01

    Acetaminophen (APAP) overdose is a major cause of acute liver failure and serves as a paradigm to elucidate mechanisms, predisposing factors and therapeutic interventions. The roles of apoptosis and inflammation during APAP hepatotoxicity remain controversial. We investigated whether fasting of mice for 24 h can inhibit APAP-induced caspase activation and apoptosis through the depletion of basal ATP. We also investigated in fasted mice the critical role played by inhibition of caspase-dependent cysteine 106 oxidation within high mobility group box-1 protein (HMGB1) released by ATP depletion in dying cells as a mechanism of immune activation. In fed mice treated with APAP, necrosis was the dominant form of hepatocyte death. However, apoptosis was also observed, indicated by K18 cleavage, DNA laddering and procaspase-3 processing. In fasted mice treated with APAP, only necrosis was observed. Inflammatory cell recruitment as a consequence of hepatocyte death was observed only in fasted mice treated with APAP or fed mice cotreated with a caspase inhibitor. Hepatic inflammation was also associated with loss in detection of serum oxidized-HMGB1. A significant role of HMGB1 in the induction of inflammation was confirmed with an HMGB1-neutralizing antibody. The differential response between fasted and fed mice was a consequence of a significant reduction in basal hepatic ATP, which prevented caspase processing, rather than glutathione depletion or altered APAP metabolism. Thus, the inhibition of caspase-driven apoptosis and HMGB1 oxidation by ATP depletion from fasting promotes an inflammatory response during drug-induced hepatotoxicity/liver pathology. PMID:20811657

  8. Controllable growth and photocatalytic activity of Cu{sub 2}O solid microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Gao, Hong; Zhang, Junying, E-mail: zjy@buaa.edu.cn; Wang, Mei

    2013-09-01

    Graphical abstract: - Highlights: • 3 μm uniform Cu{sub 2}O solid microspheres with abundant nanopores are achieved. • NH{sub 2}OH·HCl and SDS are main factors that manipulate morphologies of Cu{sub 2}O particles. • Surface features of microspheres influenced the photocatalytic activity of Cu{sub 2}O. • Microspheres are transforming to polyhedrons with extended holding time. - Abstract: A series of Cu{sub 2}O solid microspheres with different surface features were prepared and their photocatalytic activities were studied. The experiment conditions were investigated and the formation mechanism was explored systematically. It was found that varying the amounts of NH{sub 2}OH·HCl reductant in alkaline solutions changed the reaction process and thus altered the surface features of Cu{sub 2}O microspheres. Sodium dodecyl sulfate (SDS) surfactant, introduced as a morphology directing agent, caused the nuclei aggregation and growth process of Cu{sub 2}O solid microspheres by precisely realizing the opposite charges’ directional attraction. This SDS-mediated method can be readily extended to synthesizing solid microspheres of other metal oxides. Meanwhile, it was found that Cu{sub 2}O solid microspheres with abundant nanopores on the surface showed much higher efficient catalytic activity for decoloring methyl orange (MO) aqueous solution than with other surface features under visible light irradiation. Furthermore, we found that prolonging the holding time made Cu{sub 2}O microspheres transform to polyhedrons.

  9. Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon.

    Science.gov (United States)

    Rai, Gopal; Yadav, Awesh K; Jain, Narendra K; Agrawal, Govind P

    2015-01-01

    Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.

  10. A Comparative Study of Production of Glass Microspheres by using Thermal Process

    Science.gov (United States)

    Lee, May Yan; Tan, Jully; Heng, Jerry YY; Cheeseman, Christopher

    2017-06-01

    Microspheres are spherical particles that can be distinguished into two categories; solid or hollow. Microspheres typical ranges from 1 to 200 μm in diameter. Microsphere are made from glass, ceramic, carbon or plastic depending on applications. Solid glass microsphere is manufactured by direct burning of glass powders while hollow glass microspheres is produced by adding blowing agent to glass powder. This paper presented the production of glass microspheres by using the vertical thermal flame (VTF) process. Pre-treated soda lime glass powder with particle sized range from 90 to 125μm was used in this work. The results showed that glass microspheres produced by two passes through the flame have a more spherical shape as compared with the single pass. Under the Scanning Electron Microscope (SEM), it is observed that there is a morphology changed from uneven surface of glass powders to smooth spherical surface particles. Qualitative analysis for density of the pre-burned and burned particles was performed. Burned particles floats in water while pre-burned particles sank indicated the change of density of the particles. Further improvements of the VTF process in terms of the VTF set-up are required to increase the transformation of glass powders to glass microspheres.

  11. Apparatus for manufacturing ceramics microspheres for cementing applications

    NARCIS (Netherlands)

    2012-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The micro spheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about Illbs/g. The resultant cement slurry may then be

  12. DEGRADATION AND INTRAHEPATIC COMPATIBILITY OF ALBUMIN-HEPARIN CONJUGATE MICROSPHERES

    NARCIS (Netherlands)

    CREMERS, HFM; WOLF, RFE; BLAAUW, EH; SCHAKENRAAD, JM; LAM, KH; NIEUWENHUIS, P; VERRIJK, R; KWON, G; BAE, YH; KIM, SW; FEIJEN, J

    The in vitro degradation properties of glutaraldehyde cross-linked albumin and albumin-heparin conjugate microspheres (AMS and AHCMS respectively) were evaluated using light microscopy, turbidity measurements and heparin release determinations, showing that the microspheres are degraded by

  13. Anti-inflammatory effects of ursodeoxycholic acid by lipopolysaccharide-stimulated inflammatory responses in RAW 264.7 macrophages.

    Directory of Open Access Journals (Sweden)

    Wan-Kyu Ko

    Full Text Available The aim of this study was to investigate the anti-inflammatory effects of Ursodeoxycholic acid (UDCA in lipopolysaccharide (LPS-stimulated RAW 264.7 macrophages.We induced an inflammatory process in RAW 264.7 macrophages using LPS. The anti-inflammatory effects of UDCA on LPS-stimulated RAW 264.7 macrophages were analyzed using nitric oxide (NO. Pro-inflammatory and anti-inflammatory cytokines were analyzed by quantitative real time polymerase chain reaction (qRT-PCR and enzyme-linked immunosorbent assay (ELISA. The phosphorylations of extracellular signal-regulated kinase (ERK, c-Jun N-terminal kinase (JNK, and p38 in mitogen-activated protein kinase (MAPK signaling pathways and nuclear factor kappa-light polypeptide gene enhancer in B-cells inhibitor, alpha (IκBα signaling pathways were evaluated by western blot assays.UDCA decreased the LPS-stimulated release of the inflammatory mediator NO. UDCA also decreased the pro-inflammatory cytokines tumor necrosis factor-α (TNF-α, interleukin 1-α (IL-1α, interleukin 1-β (IL-1β, and interleukin 6 (IL-6 in mRNA and protein levels. In addition, UDCA increased an anti-inflammatory cytokine interleukin 10 (IL-10 in the LPS-stimulated RAW 264.7 macrophages. UDCA inhibited the expression of inflammatory transcription factor nuclear factor kappa B (NF-κB in LPS-stimulated RAW 264.7 macrophages. Furthermore, UDCA suppressed the phosphorylation of ERK, JNK, and p38 signals related to inflammatory pathways. In addition, the phosphorylation of IκBα, the inhibitor of NF-κB, also inhibited by UDCA.UDCA inhibits the pro-inflammatory responses by LPS in RAW 264.7 macrophages. UDCA also suppresses the phosphorylation by LPS on ERK, JNK, and p38 in MAPKs and NF-κB pathway. These results suggest that UDCA can serve as a useful anti-inflammatory drug.

  14. Structure of Agaricus spp. fucogalactans and their anti-inflammatory and antinociceptive properties.

    Science.gov (United States)

    Komura, Dirce L; Carbonero, Elaine R; Gracher, Ana Helena P; Baggio, Cristiane H; Freitas, Cristina S; Marcon, Rodrigo; Santos, Adair R S; Gorin, Philip A J; Iacomini, Marcello

    2010-08-01

    Fucogalactans from Agaricus brasiliensis (EPF-Ab) and A. bisporus var. hortensis (EPF-Ah) were prepared via by aqueous extraction and a purification procedure. EPF-Ab had M(w) 19.4 x 10(3)g/mol and EPF-Ah M(w) 31.1 x 10(3)g/mol. EPF-Ab had a (1-->6)-linked alpha-D-Galp main-chain partially substituted in O-2 by non-reducing end-units of alpha-L-Fucp. EPF-Ah had a similar main-chain with O-2 substitution, but was partially methylated at HO-3, as well as having 2.5% non-reducing end-units of beta-D-Gal. In mice, EPF-Ab gave 39% antinociceptive inhibition (ID(50)>100mg/kg) and no anti-inflammatory activity. EPF-Ah also gave an inhibition of 39% at ID(50) 0.33 mg/kg and also inhibited by 61% (ID(50) 5.0mg/kg) total cell migration and by 32% peritoneal capillary permeability, which is related to the anti-inflammatory effect. The small differences in chemical structure in these polysaccharides thus modified their biological activities. (c) 2010. Published by Elsevier Ltd.

  15. Role of glycogen synthase kinase-3 beta in the inflammatory response caused by bacterial pathogens

    Directory of Open Access Journals (Sweden)

    Cortés-Vieyra Ricarda

    2012-06-01

    Full Text Available Abstract Glycogen synthase kinase 3β (GSK3β plays a fundamental role during the inflammatory response induced by bacteria. Depending on the pathogen and its virulence factors, the type of cell and probably the context in which the interaction between host cells and bacteria takes place, GSK3β may promote or inhibit inflammation. The goal of this review is to discuss recent findings on the role of the inhibition or activation of GSK3β and its modulation of the inflammatory signaling in monocytes/macrophages and epithelial cells at the transcriptional level, mainly through the regulation of nuclear factor-kappaB (NF-κB activity. Also included is a brief overview on the importance of GSK3 in non-inflammatory processes during bacterial infection.

  16. Central and peripheral haemodynamic effects of non-steroidal anti-inflammatory drugs in man.

    Science.gov (United States)

    Wennmalm, A; Carlsson, I; Edlund, A; Eriksson, S; Kaijser, L; Nowak, J

    1984-01-01

    The haemodynamic effects of non-steroidal anti-inflammatory (NSAI) drugs can be attributed either to their common property of inhibiting the formation of prostaglandins (PG) in the cardiovascular system, or to direct actions on the tone and sensitivity of the resistance vessels in various regions. Indomethacin (IND) is the most frequently studied NSAI drug, in animals and in man. Its cardiovascular effects differ somewhat from those of other NSAI, due to the fact that, besides inhibiting PG formation, IND acts as a direct vasoconstrictor. The stimulatory effect of IND in vascular smooth muscle results in an increased systemic vascular resistance which, although partially compensated by a decreased cardiac output, gives rise to a moderate increase in systemic blood pressure. The vasoconstrictor effect of IND is of particular interest in patients with ischemic heart disease, since it lowers their already decreased coronary flow, and may thereby accentuate the risk of myocardial infarction. Administration of IND also leads to a decreased blood flow in the splanchnic region, the kidneys, and the brain. The cerebral blood flow is lowered by 25-35%; in addition, IND almost entirely erases the hyperemic flow response to hypercapnia. Of other NSAI drugs, at least aspirin and naproxen are completely devoid of such actions on the cerebral circulation. A common vascular effect of all NSAI drugs is a diminution of reactive hyperemia, the local hyperemia that develops in a tissue subjected to a short period of arterial occlusion. Part of this hyperemic response is dependent on an intact vascular PG formation and consequently it is inhibited when PG formation is blocked. In contrast, NSAI drugs do not affect the functional increase in the blood flow in working skeletal muscle.

  17. Curcumin modulates the inflammatory response and inhibits subsequent fibrosis in a mouse model of viral-induced acute respiratory distress syndrome.

    Science.gov (United States)

    Avasarala, Sreedevi; Zhang, Fangfang; Liu, Guangliang; Wang, Ruixue; London, Steven D; London, Lucille

    2013-01-01

    Acute Respiratory Distress Syndrome (ARDS) is a clinical syndrome characterized by diffuse alveolar damage usually secondary to an intense host inflammatory response of the lung to a pulmonary or extrapulmonary infectious or non-infectious insult often leading to the development of intra-alveolar and interstitial fibrosis. Curcumin, the principal curcumoid of the popular Indian spice turmeric, has been demonstrated as an anti-oxidant and anti-inflammatory agent in a broad spectrum of diseases. Using our well-established model of reovirus 1/L-induced acute viral pneumonia, which displays many of the characteristics of the human ALI/ARDS, we evaluated the anti-inflammatory and anti-fibrotic effects of curcumin. Female CBA/J mice were treated with curcumin (50 mg/kg) 5 days prior to intranasal inoculation with 10(7)pfu reovirus 1/L and daily, thereafter. Mice were evaluated for key features associated with ALI/ARDS. Administration of curcumin significantly modulated inflammation and fibrosis, as revealed by histological and biochemical analysis. The expression of IL-6, IL-10, IFNγ, and MCP-1, key chemokines/cytokines implicated in the development of ALI/ARDS, from both the inflammatory infiltrate and whole lung tissue were modulated by curcumin potentially through a reduction in the phosphorylated form of NFκB p65. While the expression of TGFß1 was not modulated by curcumin, TGFß Receptor II, which is required for TGFß signaling, was significantly reduced. In addition, curcumin also significantly inhibited the expression of α-smooth muscle actin and Tenascin-C, key markers of myofibroblast activation. This data strongly supports a role for curcumin in modulating the pathogenesis of viral-induced ALI/ARDS in a pre-clinical model potentially manifested through the alteration of inflammation and myofibroblast differentiation.

  18. Preparation and evaluation of enrofloxacin microspheres and tissue distribution in rats.

    Science.gov (United States)

    Yang, Fan; Kang, Jijun; Yang, Fang; Zhao, Zhensheng; Kong, Tao; Zeng, Zhenling

    2015-01-01

    New enrofloxacin microspheres were formulated, and their physical properties, lung-targeting ability, and tissue distribution in rats were examined. The microspheres had a regular and round shape. The mean diameter was 10.06 µm, and the diameter of 89.93% of all microspheres ranged from 7.0 µm to 30.0 µm. Tissue distribution of the microspheres was evaluated along with a conventional enrofloxacin preparation after a single intravenous injection (7.5 mg of enrofloxacin/kg bw). The results showed that the elimination half-life (t1/2β) of enrofloxacin from lung was prolonged from 7.94 h for the conventional enrofloxacin to 13.28 h for the microspheres. Area under the lung concentration versus time curve from 0 h to ∞ (AUC00∞) was increased from 11.66 h·µg/g to 508.00 h·µg/g. The peak concentration (Cmax) in lung was increased from 5.95 µg/g to 93.36 µg/g. Three lung-targeting parameters were further assessed and showed that the microspheres had remarkable lung-targeting capabilities.

  19. Biodegradable microsphere-mediated cell perforation in microfluidic channel using femtosecond laser

    Science.gov (United States)

    Ishii, Atsuhiro; Ariyasu, Kazumasa; Mitsuhashi, Tatsuki; Heinemann, Dag; Heisterkamp, Alexander; Terakawa, Mitsuhiro

    2016-05-01

    The use of small particles has expanded the capability of ultrashort pulsed laser optoinjection technology toward simultaneous treatment of multiple cells. The microfluidic platform is one of the attractive systems that has obtained synergy with laser-based technology for cell manipulation, including optoinjection. We have demonstrated the delivery of molecules into suspended-flowing cells in a microfluidic channel by using biodegradable polymer microspheres and a near-infrared femtosecond laser pulse. The use of polylactic-co-glycolic acid microspheres realized not only a higher optoinjection ratio compared to that with polylactic acid microspheres but also avoids optical damage to the microfluidic chip, which is attributable to its higher optical intensity enhancement at the localized spot under a microsphere. Interestingly, optoinjection ratios to nucleus showed a difference for adhered cells and suspended cells. The use of biodegradable polymer microspheres provides high throughput optoinjection; i.e., multiple cells can be treated in a short time, which is promising for various applications in cell analysis, drug delivery, and ex vivo gene transfection to bone marrow cells and stem cells without concerns about residual microspheres.

  20. Changes in circulating inflammatory markers following febrile non-haemolytic transfusion reactions to leucoreduced red cells

    DEFF Research Database (Denmark)

    Larsen, R; Sandhu, N; Heegaard, N H H

    2018-01-01

    It would be desirable to be able to distinguish fever as a result of febrile non-haemolytic transfusion reactions (FNHTR) from other febrile conditions. To further characterize the inflammatory feature of FNHTR, we measured a large panel of inflammatory markers in pre- and posttransfusion plasma...

  1. Development and evaluation of intestinal targeted mucoadhesive microspheres of Bacillus coagulans.

    Science.gov (United States)

    Alli, Sk Md Athar; Ali, Sk Md Ajhar; Samanta, Amalesh

    2011-11-01

    Intestinal targeted mucoadhesive microsphere of probiotics may provide numerous associated health benefits. To develop mucoadhesive microspheres that will deliver viable probiotic cells into gut protectively against harsh environmental conditions of stomach for extended period. Core mucoadhesive microspheres of Bacillus coagulans were prepared using hypromellose, following coacervation and phase separation technique and were then coated with hypromellose phthalate to achieve their site-specific release. Microspheres were evaluated for percent yield, entrapment efficiency, surface morphology, particle size and size distribution, flow property, swelling property, mucoadhesion property by the in vitro wash-off and the ex vivo mucoadhesive strength tests, in vitro release profile and release kinetic, in vivo probiotic activity, and stability. The values for kinetic constant and regression coefficient of model-dependent approaches and the difference factor, the similarity factor, and the Rescigno index of model-independent approaches were determined for accessing and comparing in vitro performance. Microsphere formulation batches have percent yield value between 56.26% and 69.13% and entrapment efficiency value between 66.95% and 77.89%. Microspheres were coarser with spherical shape having mean particle size from 28.03 to 48.31 μm. In vitro B. coagulans release profile follows zero-order kinetics and depends on the grade of hypromellose and the B. coagulans-to-hypromellose ratio. Experimental microspheres rendered adequate stability to B. coagulans at room temperature. Microspheres had delivered B. coagulans in simulated intestinal condition following zero-order kinetics, protectively in simulated gastric condition, exhibiting appreciable mucoadhesion in intestinal condition, which could be useful to achieve site-specific delivery for extended period.

  2. Anti-Inflammatory Action of an Antimicrobial Model Peptide That Suppresses the TRIF-Dependent Signaling Pathway via Inhibition of Toll-Like Receptor 4 Endocytosis in Lipopolysaccharide-Stimulated Macrophages.

    Directory of Open Access Journals (Sweden)

    Do-Wan Shim

    Full Text Available Antimicrobial peptides (AMPs, also called host defense peptides, particularly those with amphipathic helical structures, are emerging as target molecules for therapeutic development due to their immunomodulatory properties. Although the antimicrobial activity of AMPs is known to be exerted primarily by permeation of the bacterial membrane, the mechanism underlying its anti-inflammatory activity remains to be elucidated. We report potent anti-inflammatory activity of WALK11.3, an antimicrobial model peptide with an amphipathic helical conformation, in lipopolysaccharide (LPS-stimulated RAW264.7 cells. This peptide inhibited the expression of inflammatory mediators, including nitric oxide, COX-2, IL-1β, IL-6, INF-β, and TNF-α. Although WALK11.3 did not exert a major effect on all downstream signaling in the MyD88-dependent pathway, toll-like receptor 4 (TLR4- mediated pro-inflammatory signals were markedly attenuated in the TRIF-dependent pathway due to inhibition of the phosphorylation of STAT1 by attenuation of IRF3 phosphorylation. WALK11.3 specifically inhibited the endocytosis of TLR4, which is essential for triggering TRIF-mediated signaling in macrophage cells. Hence, we suggest that specific interference with TLR4 endocytosis could be one of the major modes of the anti-inflammatory action of AMPs. Our designed WALK11 peptides, which possess both antimicrobial and anti-inflammatory activities, may be promising molecules for the development of therapies for infectious inflammation.

  3. Ganoderma lucidum ethanol extract inhibits the inflammatory response by suppressing the NF-κB and toll-like receptor pathways in lipopolysaccharide-stimulated BV2 microglial cells.

    Science.gov (United States)

    Yoon, Hyun-Min; Jang, Kyung-Jun; Han, Min Seok; Jeong, Jin-Woo; Kim, Gi Young; Lee, Jai-Heon; Choi, Yung Hyun

    2013-03-01

    Ganoderma lucidum is a traditional Oriental medicine that has been widely used as a tonic to promote longevity and health in Korea and other Asian countries. Although a great deal of work has been carried out on the therapeutic potential of this mushroom, the pharmacological mechanisms of its anti-inflammatory actions remain unclear. In this study, we evaluated the inhibitory effects of G. lucidum ethanol extract (EGL) on the production of inflammatory mediators and cytokines in lipopolysaccharide (LPS)-stimulated murine BV2 microglia. We also investigated the effects of EGL on the LPS-induced activation of nuclear factor kappaB (NF-κB) and upregulation of toll-like receptor 4 (TLR4) and myeloid differentiation factor 88 (MyD88). Elevated levels of nitric oxide (NO), prostaglandin E(2) (PGE(2)) and pro-inflammatory cytokine production were detected in BV2 microglia following LPS stimulation. We identifed that EGL significantly inhibits the excessive production of NO, PGE(2) and pro-inflammatory cytokines, including interleukin (IL)-1β and tumor necrosis factor-α in a concentration-dependent manner without causing cytotoxicity. In addition, EGL suppressed NF-κB translocation and transcriptional activity by blocking IκB degradation and inhibiting TLR4 and MyD88 expression in LPS-stimulated BV2 cells. Our results indicate that the inhibitory effects of EGL on LPS-stimulated inflammatory responses in BV2 microglia are associated with the suppression of the NF-κB and TLR signaling pathways. Therefore, EGL may be useful in the treatment of neurodegenerative diseases by inhibiting inflammatory mediator responses in activated microglia.

  4. ADRIAMYCIN-LOADED ALBUMIN-HEPARIN CONJUGATE MICROSPHERES FOR INTRAPERITONEAL CHEMOTHERAPY

    NARCIS (Netherlands)

    CREMERS, HFM; SEYMOUR, LW; LAM, K; LOS, G; KWON, G; BAE, YH; KIM, SW; FEIJEN, J

    1994-01-01

    Adriamycin-loaded albumin-heparin conjugate microspheres (ADR-AHCMS) were evaluated as possible intraperitoneal (i.p.) delivery systems for site-specific cytotoxic action. The biocompatibility of the microspheres after intraperitoneal injection was tested first. 1 day after i.p. administration of

  5. A substance P antagonist, [D-Pro2, D-Trp7,9]SP, inhibits inflammatory responses in the rabbit eye

    International Nuclear Information System (INIS)

    Holmdahl, G.; Hakanson, R.; Leander, S.; Rosell, S.; Folkers, K.; Sundler, F.

    1981-01-01

    Neurogenic factors released by antidromic nerve stimulation are thought to be in part responsible for the vasodilation and breakdown of the blood-aqueous barrier that follows trauma to the eye. Substance P is one candidate for the mediation of the inflammatory response since it is thought to be a neurotransmitter in sensory afferents and since exogenous substance P is capable of eliciting a response characteristic of inflammation. In rabbits, intravitreal or topical application onto the eye of a specific substance P antagonist, [d-Pro2, D-Trp7,9]SP, inhibited not only the irritant effects of exogenous substance P but also the inflammatory response to a standardized trauma (infrared irradiation of the iris). These observations suggest that substance P, or a related peptide, is a neurogenic mediator of the inflammatory response in the eye

  6. Biomimetic mineralization of calcium carbonate/carboxymethylcellulose microspheres for lysozyme immobilization

    International Nuclear Information System (INIS)

    Lu Zheng; Zhang Juan; Ma Yunzi; Song Siyue; Gu Wei

    2012-01-01

    Porous calcium carbonate/carboxymethylcellulose (CaCO 3 /CMC) microspheres were prepared by the biomimetic mineralization method for lysozyme immobilization via adsorption. The size and morphology of CaCO 3 /CMC microspheres were characterized by transmitted electron microscopy (TEM) and zeta potential measurement. The lysozyme immobilization was verified by Fourier transform infrared (FTIR) spectroscopy. The effects of pHs and temperatures on lysozyme adsorption were investigated as well. It was revealed that CaCO 3 /CMC microspheres could immobilize lysozyme efficiently via electrostatic interactions and a maximum adsorption capacity of 450 mg/g was achieved at pH 9.2 and 25 °C. Moreover, it was found that the adsorption process fitted well with the Langmuir isothermal model. In addition, UV, fluorescence, and circular dichroism (CD) spectroscopic studies showed that lysozyme maintained its original secondary structure during the adsorption/desorption process. Our study therefore demonstrated that CaCO 3 /CMC microsphere can be used as a cost-effective and efficient support for lysozyme immobilization. - Graphical abstract: CaCO 3 /CMC microsphere was prepared by a facile biomimetic mineralization method and can be used as an efficient and cost-effective support for lysozyme immobilization. Highlights: ► CaCO 3 /CMC microspheres were prepared by the biomimetic mineralization method. ► Lysozyme was efficiently immobilized to CaCO 3 /CMC microspheres via adsorption. ► A maximum adsorption capacity of 450 mg/g was obtained at pH 9.2 and 25 °C. ► The original secondary structure of lysozyme was maintained upon immobilization.

  7. Cholinergic anti-inflammatory pathway in the non-obese diabetic mouse model

    NARCIS (Netherlands)

    Koopman, F. A.; Vosters, J. L.; Roescher, N.; Broekstra, N.; Tak, P. P.; Vervoordeldonk, M. J.

    2015-01-01

    Activation of the cholinergic anti-inflammatory pathway (CAP) has been shown to reduce inflammation in animal models, while abrogation of the pathway increases inflammation. We investigated whether modulation of CAP influences inflammation in the non-obese diabetic (NOD) mouse model for Sjögren's

  8. Formulation and Evaluation of Microsphere Based Oro Dispersible Tablets of Itopride Hcl

    Directory of Open Access Journals (Sweden)

    S.S Agrawal

    2012-09-01

    Full Text Available Background The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing.Methods:With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. Results:The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8 and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. ConclusionsEffective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  9. Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl

    Directory of Open Access Journals (Sweden)

    Shah Sanjay

    2012-09-01

    Full Text Available Abstract Background The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing. Methods With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. Results The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8 and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. Conclusions Effective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  10. Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl.

    Science.gov (United States)

    Shah, Sanjay; Madan, Sarika; Agrawal, Ss

    2012-09-03

    The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT) of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing. With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8) and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. Effective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  11. Kefir-isolated bacteria and yeasts inhibit Shigella flexneri invasion and modulate pro-inflammatory response on intestinal epithelial cells.

    Science.gov (United States)

    Bolla, P A; Abraham, A G; Pérez, P F; de Los Angeles Serradell, M

    2016-02-01

    The aim of this work was to evaluate the ability of a kefir-isolated microbial mixture containing three bacterial and two yeast strains (MM) to protect intestinal epithelial cells against Shigella flexneri invasion, as well as to analyse the effect on pro-inflammatory response elicited by this pathogen. A significant decrease in S. flexneri strain 72 invasion was observed on both HT-29 and Caco-2 cells pre-incubated with MM. Pre-incubation with the individual strains Saccharomyces cerevisiae CIDCA 8112 or Lactococcus lactis subsp. lactis CIDCA 8221 also reduced the internalisation of S. flexneri into HT-29 cells although in a lesser extent than MM. Interestingly, Lactobacillus plantarum CIDCA 83114 exerted a protective effect on the invasion of Caco-2 and HT-29 cells by S. flexneri. Regarding the pro-inflammatory response on HT-29 cells, S. flexneri infection induced a significant activation of the expression of interleukin 8 (IL-8), chemokine (C-C motif) ligand 20 (CCL20) and tumour necrosis factor alpha (TNF-α) encoding genes (P<0.05), whereas incubation of cells with MM did not induce the expression of any of the mediators assessed. Interestingly, pre-incubation of HT-29 monolayer with MM produced an inhibition of S. flexneri-induced IL-8, CCL20 and TNF-α mRNA expression. In order to gain insight on the effect of MM (or the individual strains) on this pro-inflammatory response, a series of experiments using a HT-29-NF-κB-hrGFP reporter system were performed. Pre-incubation of HT-29-NF-κB-hrGFP cells with MM significantly dampened Shigella-induced activation. Our results showed that the contribution of yeast strain Kluyveromyces marxianus CIDCA 8154 seems to be crucial in the observed effect. In conclusion, results presented in this study demonstrate that pre-treatment with a microbial mixture containing bacteria and yeasts isolated from kefir, resulted in inhibition of S. flexneri internalisation into human intestinal epithelial cells, along with the

  12. Postoperative use of non-steroidal anti-inflammatory drugs in patients with anastomotic leakage requiring reoperation after colorectal resection

    DEFF Research Database (Denmark)

    Klein, Mads; Gögenur, Ismail; Rosenberg, Jacob

    2012-01-01

    To evaluate the effect of postoperative use of non-steroidal anti-inflammatory drugs (NSAIDs) on anastomotic leakage requiring reoperation after colorectal resection.......To evaluate the effect of postoperative use of non-steroidal anti-inflammatory drugs (NSAIDs) on anastomotic leakage requiring reoperation after colorectal resection....

  13. Anti-Inflammatory Benefits of Antibiotics: Tylvalosin Induces Apoptosis of Porcine Neutrophils and Macrophages, Promotes Efferocytosis, and Inhibits Pro-Inflammatory CXCL-8, IL1α, and LTB4 Production, While Inducing the Release of Pro-Resolving Lipoxin A4 and Resolvin D1.

    Science.gov (United States)

    Moges, Ruth; De Lamache, Dimitri Desmonts; Sajedy, Saman; Renaux, Bernard S; Hollenberg, Morley D; Muench, Gregory; Abbott, Elizabeth M; Buret, Andre G

    2018-01-01

    Excessive accumulation of neutrophils and their uncontrolled death by necrosis at the site of inflammation exacerbates inflammatory responses and leads to self-amplifying tissue injury and loss of organ function, as exemplified in a variety of respiratory diseases. In homeostasis, neutrophils are inactivated by apoptosis, and non phlogistically removed by neighboring macrophages in a process known as efferocytosis, which promotes the resolution of inflammation. The present study assessed the potential anti-inflammatory and pro-resolution benefits of tylvalosin, a recently developed broad-spectrum veterinary macrolide derived from tylosin. Recent findings indicate that tylvalosin may modulate inflammation by suppressing NF-κB activation. Neutrophils and monocyte-derived macrophages were isolated from fresh blood samples obtained from 12- to 22-week-old pigs. Leukocytes exposed to vehicle or to tylvalosin (0.1, 1.0, or 10 µg/mL; 0.096-9.6 µM) were assessed at various time points for apoptosis, necrosis, efferocytosis, and changes in the production of cytokines and lipid mediators. The findings indicate that tylvalosin increases porcine neutrophil and macrophage apoptosis in a concentration- and time-dependent manner, without altering levels of necrosis or reactive oxygen species production. Importantly, tylvalosin increased the release of pro-resolving Lipoxin A 4 (LXA 4 ) and Resolvin D1 (RvD 1 ) while inhibiting the production of pro-inflammatory Leukotriene B4 (LTB 4 ) in Ca 2+ ionophore-stimulated porcine neutrophils. Tylvalosin increased neutrophil phospholipase C activity, an enzyme involved in releasing arachidonic acid from membrane stores. Tylvalosin also inhibited pro-inflammatory chemokine (C-X-C motif) ligand 8 (CXCL-8, also known as Interleukin-8) and interleukin-1 alpha (IL-1α) protein secretion in bacterial lipopolysaccharide-stimulated macrophages. Together, these data illustrate that tylvalosin has potent immunomodulatory effects in porcine

  14. Anti-Inflammatory Benefits of Antibiotics: Tylvalosin Induces Apoptosis of Porcine Neutrophils and Macrophages, Promotes Efferocytosis, and Inhibits Pro-Inflammatory CXCL-8, IL1α, and LTB4 Production, While Inducing the Release of Pro-Resolving Lipoxin A4 and Resolvin D1

    Directory of Open Access Journals (Sweden)

    Ruth Moges

    2018-04-01

    Full Text Available Excessive accumulation of neutrophils and their uncontrolled death by necrosis at the site of inflammation exacerbates inflammatory responses and leads to self-amplifying tissue injury and loss of organ function, as exemplified in a variety of respiratory diseases. In homeostasis, neutrophils are inactivated by apoptosis, and non phlogistically removed by neighboring macrophages in a process known as efferocytosis, which promotes the resolution of inflammation. The present study assessed the potential anti-inflammatory and pro-resolution benefits of tylvalosin, a recently developed broad-spectrum veterinary macrolide derived from tylosin. Recent findings indicate that tylvalosin may modulate inflammation by suppressing NF-κB activation. Neutrophils and monocyte-derived macrophages were isolated from fresh blood samples obtained from 12- to 22-week-old pigs. Leukocytes exposed to vehicle or to tylvalosin (0.1, 1.0, or 10 µg/mL; 0.096–9.6 µM were assessed at various time points for apoptosis, necrosis, efferocytosis, and changes in the production of cytokines and lipid mediators. The findings indicate that tylvalosin increases porcine neutrophil and macrophage apoptosis in a concentration- and time-dependent manner, without altering levels of necrosis or reactive oxygen species production. Importantly, tylvalosin increased the release of pro-resolving Lipoxin A4 (LXA4 and Resolvin D1 (RvD1 while inhibiting the production of pro-inflammatory Leukotriene B4 (LTB4 in Ca2+ ionophore-stimulated porcine neutrophils. Tylvalosin increased neutrophil phospholipase C activity, an enzyme involved in releasing arachidonic acid from membrane stores. Tylvalosin also inhibited pro-inflammatory chemokine (C–X–C motif ligand 8 (CXCL-8, also known as Interleukin-8 and interleukin-1 alpha (IL-1α protein secretion in bacterial lipopolysaccharide-stimulated macrophages. Together, these data illustrate that tylvalosin has potent immunomodulatory effects

  15. Biotemplate synthesis of monodispersed iron phosphate hollow microspheres

    International Nuclear Information System (INIS)

    Cao Feng; Li Dongxu

    2010-01-01

    Monodispersed iron phosphate hollow microspheres with a high degree of crystallization were prepared through a facile in situ deposition method using rape pollen grains as a biotemplate. The functional group on the surface of the pollen grains could adsorb Fe 3+ , which provided the nucleation sites for growth of iron phosphate nanoparticles. After being sintered at 600 deg. C for 10 h, the pollen grains were removed and iron phosphate hollow microspheres were obtained. A scanning electron microscope and x-ray diffraction were applied to characterize the morphology and crystalline structure of the pollen grains, iron phosphate-coated pollen grains and iron phosphate hollow microspheres. Differential scanning calorimetry and thermogravity analyses were performed to investigate the thermal behavior of the iron phosphate-coated pollen grains during the calcinations. Energy dispersive spectroscopy and Fourier transform infrared spectroscopy were utilized to investigate the interaction between the pollen grains and iron phosphate. The effect of the pollen wall on the surface morphology of these iron phosphate hollow microspheres was also proven in this work.

  16. Biotemplate synthesis of monodispersed iron phosphate hollow microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Cao Feng; Li Dongxu, E-mail: dongxuli@njut.edu.c [College of Materials Science and Engineering, Nanjing University of Technology, Jiangsu Nanjing 210009 (China)

    2010-03-15

    Monodispersed iron phosphate hollow microspheres with a high degree of crystallization were prepared through a facile in situ deposition method using rape pollen grains as a biotemplate. The functional group on the surface of the pollen grains could adsorb Fe{sup 3+}, which provided the nucleation sites for growth of iron phosphate nanoparticles. After being sintered at 600 deg. C for 10 h, the pollen grains were removed and iron phosphate hollow microspheres were obtained. A scanning electron microscope and x-ray diffraction were applied to characterize the morphology and crystalline structure of the pollen grains, iron phosphate-coated pollen grains and iron phosphate hollow microspheres. Differential scanning calorimetry and thermogravity analyses were performed to investigate the thermal behavior of the iron phosphate-coated pollen grains during the calcinations. Energy dispersive spectroscopy and Fourier transform infrared spectroscopy were utilized to investigate the interaction between the pollen grains and iron phosphate. The effect of the pollen wall on the surface morphology of these iron phosphate hollow microspheres was also proven in this work.

  17. Electrodepositing of Au on hollow PS micro-spheres

    International Nuclear Information System (INIS)

    Sun Jingyuan; Zhang Yunwang; Du Kai; Wan Xiaobo; Xiao Jiang; Zhang Wei; Zhang Lin; Chen Jing

    2010-01-01

    Using the self-regulating new micro-sphere electrodepositing device, the techniques of electrodepositing gold on hollow PS micro-spheres were established. The experiment was carried out under the following conditions: voltage was about 0.7 ∼ 0.8 V, current density was 2.0 mA · cm -2 , the temperature was 45 degree C, cathode rotating rate was 250 r · min -1 , flow rate of the solution was 7 mL · min -1 · cm -2 . Hollow gold-plated micro-spheres were prepared with well spherical symmetry, uniform thickness and surface smoothness under 500 nm. The speed of the gold depositing was 6 μm · h -1 . (authors)

  18. MRI of the SI joints commonly shows non-inflammatory disease in patients clinically suspected of sacroiliitis

    Energy Technology Data Exchange (ETDEWEB)

    Jans, L., E-mail: lennartjans@hotmail.com [Department of Radiology and Medical Imaging, Ghent University Hospital, De Pintelaan 185, 9000 Gent (Belgium); Van Praet, L.; Elewaut, D.; Van den Bosch, F.; Carron, P. [Department of Rheumatology, Ghent University Hospital, De Pintelaan 185, 9000 Gent (Belgium); Jaremko, J.L. [Department of Radiology, University of Alberta Hospital, 8440-112 Street, Edmonton T6G 2B7, Alberta (Canada); Behaeghe, M.; Denis, A.; Huysse, W.; Lambrecht, V.; Verstraete, K. [Department of Radiology and Medical Imaging, Ghent University Hospital, De Pintelaan 185, 9000 Gent (Belgium)

    2014-01-15

    Purpose: To determine the prevalence of clinically relevant non-inflammatory disease on MRI of the sacroiliac (SI) joints in patients suspected of sacroiliitis. To assess the added value of axial imaging of the pelvis in these patients. Methods: In a retrospective study of 691 patients undergoing MRI of the SI joints from January 2006 to December 2012 for inflammatory back pain the prevalence of sacroiliitis and non-inflammatory disease was recorded. Results: In 285 (41%) patients MRI did not show any abnormal findings. In 36% of patients MRI features of sacroiliitis were present. Spinal degenerative changes were the most common non-inflammatory finding in 305 patients (44.1%) and consisted of disc degeneration in 222 (32%) patients, facet joint arthrosis in 58 (8.4%) patients and disc herniation in 25 (3.6%) patients. Hip joint disease in 44 (6.4%) patients, lumbosacral transitional anomaly in 41 (5.9%) patients, SI joint degenerative changes in 25 (3.6%) patients and diffuse idiopathic skeletal hyperostosis in 24 (3.5%) patients were also common. Osteitis condensans ilii in 17 (2.5%) patients, tumour in 11 (1.6%) patients, fracture in 8 (1.2%) patients, infection in 4 (0.6%) patients and acute spondylolysis in 2 patients (0.3%) were less frequently seen. Conclusion: Our study shows that non-inflammatory disease is more common than true sacroiliitis on MRI of the SI joints in patients with inflammatory type back pain. Axial pulse sequences may demonstrate unexpected findings that remain undetected if only coronal images are obtained. Clinical relevance statement:, MRI of the SI joints may demonstrate conditions that clinically mimic sacroiliitis. Axial imaging of the pelvis may help detect these unexpected findings.

  19. MRI of the SI joints commonly shows non-inflammatory disease in patients clinically suspected of sacroiliitis

    International Nuclear Information System (INIS)

    Jans, L.; Van Praet, L.; Elewaut, D.; Van den Bosch, F.; Carron, P.; Jaremko, J.L.; Behaeghe, M.; Denis, A.; Huysse, W.; Lambrecht, V.; Verstraete, K.

    2014-01-01

    Purpose: To determine the prevalence of clinically relevant non-inflammatory disease on MRI of the sacroiliac (SI) joints in patients suspected of sacroiliitis. To assess the added value of axial imaging of the pelvis in these patients. Methods: In a retrospective study of 691 patients undergoing MRI of the SI joints from January 2006 to December 2012 for inflammatory back pain the prevalence of sacroiliitis and non-inflammatory disease was recorded. Results: In 285 (41%) patients MRI did not show any abnormal findings. In 36% of patients MRI features of sacroiliitis were present. Spinal degenerative changes were the most common non-inflammatory finding in 305 patients (44.1%) and consisted of disc degeneration in 222 (32%) patients, facet joint arthrosis in 58 (8.4%) patients and disc herniation in 25 (3.6%) patients. Hip joint disease in 44 (6.4%) patients, lumbosacral transitional anomaly in 41 (5.9%) patients, SI joint degenerative changes in 25 (3.6%) patients and diffuse idiopathic skeletal hyperostosis in 24 (3.5%) patients were also common. Osteitis condensans ilii in 17 (2.5%) patients, tumour in 11 (1.6%) patients, fracture in 8 (1.2%) patients, infection in 4 (0.6%) patients and acute spondylolysis in 2 patients (0.3%) were less frequently seen. Conclusion: Our study shows that non-inflammatory disease is more common than true sacroiliitis on MRI of the SI joints in patients with inflammatory type back pain. Axial pulse sequences may demonstrate unexpected findings that remain undetected if only coronal images are obtained. Clinical relevance statement:, MRI of the SI joints may demonstrate conditions that clinically mimic sacroiliitis. Axial imaging of the pelvis may help detect these unexpected findings

  20. Microspheres with Ultrahigh Holmium Content for Radioablation of Malignancies

    NARCIS (Netherlands)

    Bult, W.; Seevinck, P.R.; Krijger, G.C.; Visser, T.; Kroon-Batenburg, L.M.J.; Bakker, C.J.G.; Hennink, W.E.; van het Schip, A.D.; Nijsen, J.F.W.

    2009-01-01

    The aim of this study was to develop microspheres with an ultra high holmium content which can be neutron activated for radioablation of malignancies. These microspheres are proposed to be delivered selectively through either intratumoral injections into solid tumors or administered via an

  1. Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon.

    Science.gov (United States)

    Rai, Gopal; Yadav, Awesh K; Jain, Narendra K; Agrawal, Govind P

    2016-01-01

    Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.

  2. Optical diffraction by ordered 2D arrays of silica microspheres

    International Nuclear Information System (INIS)

    Shcherbakov, A.A.; Shavdina, O.; Tishchenko, A.V.; Veillas, C.; Verrier, I.; Dellea, O.; Jourlin, Y.

    2017-01-01

    The article presents experimental and theoretical studies of angular dependent diffraction properties of 2D monolayer arrays of silica microspheres. High-quality large area defect-free monolayers of 1 μm diameter silica microspheres were deposited by the Langmuir-Blodgett technique under an accurate optical control. Measured angular dependencies of zeroth and one of the first order diffraction efficiencies produced by deposited samples were simulated by the rigorous Generalized Source Method taking into account particle size dispersion and lattice nonideality. - Highlights: • High quality silica microsphere monolayer was fabricated. • Accurate measurements of diffraction efficiency angular dependencies. • Rigorous diffraction simulation of both ideal hexagonal and realistic microsphere arrangements. • Qualitative rationalization of the obtained results and the observed differences between the experiment and the theory.

  3. Effects of non-pharmacological interventions on inflammatory biomarker expression in patients with fibromyalgia: a systematic review.

    Science.gov (United States)

    Sanada, Kenji; Díez, Marta Alda; Valero, Montserrat Salas; Pérez-Yus, María Cruz; Demarzo, Marcelo M P; García-Toro, Mauro; García-Campayo, Javier

    2015-09-26

    Fibromyalgia (FM) is a prevalent disorder. However, few studies have evaluated the effect of treatment interventions on biomarker expression. The aim of this review was to explore the efficacy of non-pharmacological interventions on inflammatory biomarker expression, specifically cytokines, neuropeptides and C-reactive protein (CRP), in FM patients. A literature search using PubMed, EMBASE, PsycINFO and the Cochrane library was performed from January 1990 to March 2015. Randomized controlled trials (RCTs) and non-RCTs published in English, French or Spanish were eligible. Twelve articles with a total of 536 participants were included. After exercise, multidisciplinary, or dietary interventions in FM patients, interleukin (IL) expression appeared reduced, specifically serum IL-8 and IL-6 (spontaneous, lipopolysaccharide (LPS)-induced, or serum). Furthermore, the changes to insulin-like growth factor 1 (IGF-1) levels might indicate a beneficial role for fatigue in obese FM patients. In contrast, evidence of changes in neuropeptide and CRP levels seemed inconsistent. Despite minimal evidence, our findings indicate that exercise interventions might act as an anti-inflammatory treatment in FM patients and ameliorate inflammatory status, especially for pro-inflammatory cytokines. Additional RCTs focused on the changes to inflammatory biomarker expression after non-pharmacological interventions in FM patients are needed.

  4. Naja naja atra venom ameliorates pulmonary fibrosis by inhibiting inflammatory response and oxidative stress.

    Science.gov (United States)

    Cui, Kui; Kou, Jian-Qun; Gu, Jin-Hua; Han, Rong; Wang, Guanghui; Zhen, Xuechu; Qin, Zheng-Hong

    2014-12-02

    Naja naja atra venom (NNAV) displays diverse pharmacological actions including analgesia, anti-inflammation and immune regulation.In this study, we investigated the effects of NNAV on pulmonary fibrosis and its mechanisms of action. To determine if Naja naja atra venom (NNAV) can produce beneficial effects on pulmonary fibrosis, two marine models of pulmonary fibrosis were produced with bleomycin (BLM) and lipopolysaccharide (LPS). NNAV (30, 90, 270 μg/kg) was orally administered once a day started five days before BLM and LPS until to the end of experiment. The effects of NNAV treatment on pulmonary injury were evaluated with arterial blood gas analysis, hydroxyproline (HYP) content assessment and HE/Masson staining. The effects of NNAV treatment on inflammatory related cytokines, fibrosis related TGF-β/Smad signaling pathway and oxidative stress were examined. The results showed that NNAV improved the lung gas-exchange function and attenuated the fibrotic lesions in lung. NNAV decreased IL-1β and TNF-α levels in serum in both pulmonary fibrosis models. NNAV inhibited the activation of NF-κB in LPS-induced and TGF-β/Smad pathway in BLM-induced pulmonary fibrosis. Additionally, NNAV also increased the levels of SOD and GSH and reduced the levels of MDA in BLM-induced pulmonary fibrosis model. The present study indicates that NNAV attenuates LPS- and BLM-induced lung fibrosis. Its mechanisms of action are associated with inhibiting inflammatory response and oxidative stress. The study suggests that NNAV might be a potential therapeutic drug for treatment of pulmonary fibrosis.

  5. Evaluation of the Thermosensitive Release Properties of Microspheres Containing an Agrochemical Compound.

    Science.gov (United States)

    Terada, Takatoshi; Ohtsubo, Toshiro; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2017-01-01

    The purpose of this study was to develop a deeper understanding of the key physicochemical parameters involved in the release profiles of microsphere-encapsulated agrochemicals at different temperatures. Microspheres consisting of different polyurethanes (PUs) were prepared using our previously reported solventless microencapsulation technique. Notably, these microspheres exhibited considerable differences in their thermodynamic characteristics, including their glass transition temperature (T g ), extrapolated onset temperature (T o ) and extrapolated end temperature (T e ). At test temperatures below the T o of the PU, only 5-10% of the agrochemical was rapidly released from the microspheres within 1 d, and none was released thereafter. However, at test temperatures above the T o of the PU, the rate of agrochemical release gradually increased with increasing temperatures, and the rate of release from the microspheres was dependent on the composition of the PU. Taken together, these results show that the release profiles of the microspheres were dependent on their thermodynamic characteristics and changes in their PU composition.

  6. Reduced Graphene Oxide Decorated Na3V2(PO43 Microspheres as Cathode Material With Advanced Sodium Storage Performance

    Directory of Open Access Journals (Sweden)

    Hezhang Chen

    2018-05-01

    Full Text Available Reduced graphene oxide (rGO sheet decorated Na3V2(PO43 (NVP microspheres were successfully synthesized by spray-drying method. The NVP microspheres were embedded by rGO sheets, and the surface of the particles were coated by rGO sheets and amorphous carbon. Thus, the carbon conductive network consisted of rGO sheets and amorphous carbon generated in the cathode material. NVP microspheres decorated with different content of rGO (about 0, 4, 8, and 12 wt% were investigated in this study. The electrochemical performance of NVP exhibited a significant enhancement after rGO introduction. The electrode containing about 8 wt% rGO (NVP/G8 showed the best rate and cycle performance. NVP/G8 electrode exhibited the discharge capacity of 64.0 mAh g−1 at 70°C, and achieved high capacity retention of 95.5% after cycling at 10°C for 100 cycles. The polarization of the electrode was inhibited by the introduction of rGO sheets. Meanwhile, compared with the pristine NVP electrode, NVP/G8 electrode exhibited small resistance and high diffusion coefficient of sodium ions.

  7. Pharmacological Regulation of Neuropathic Pain Driven by Inflammatory Macrophages

    Directory of Open Access Journals (Sweden)

    Norikazu Kiguchi

    2017-11-01

    Full Text Available Neuropathic pain can have a major effect on quality of life but current therapies are often inadequate. Growing evidence suggests that neuropathic pain induced by nerve damage is caused by chronic inflammation. Upon nerve injury, damaged cells secrete pro-inflammatory molecules that activate cells in the surrounding tissue and recruit circulating leukocytes to the site of injury. Among these, the most abundant cell type is macrophages, which produce several key molecules involved in pain enhancement, including cytokines and chemokines. Given their central role in the regulation of peripheral sensitization, macrophage-derived cytokines and chemokines could be useful targets for the development of novel therapeutics. Inhibition of key pro-inflammatory cytokines and chemokines prevents neuroinflammation and neuropathic pain; moreover, recent studies have demonstrated the effectiveness of pharmacological inhibition of inflammatory (M1 macrophages. Nicotinic acetylcholine receptor ligands and T helper type 2 cytokines that reduce M1 macrophages are able to relieve neuropathic pain. Future translational studies in non-human primates will be crucial for determining the regulatory mechanisms underlying neuroinflammation-associated neuropathic pain. In turn, this knowledge will assist in the development of novel pharmacotherapies targeting macrophage-driven neuroinflammation for the treatment of intractable neuropathic pain.

  8. Development and evaluation of floating microspheres of curcumin in ...

    African Journals Online (AJOL)

    Purpose: To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence and to study their effect on alloxan-induced diabetic rats. Methods: Floating microsphere were prepared by emulsion-solvent diffusion method, using hydroxylpropyl methylcellulose, chitosan and Eudragit S 100 polymer in ...

  9. Microspheres with ultrahigh holmium content for radioablation of malignancies

    NARCIS (Netherlands)

    Bult, W; Seevinck, P R; Krijger, G C; Visser, T; Kroon-Batenburg, L M J; Bakker, C J G; Hennink, W E; van het Schip, A D; Nijsen, J F W

    PURPOSE: The aim of this study was to develop microspheres with an ultra high holmium content which can be neutron activated for radioablation of malignancies. These microspheres are proposed to be delivered selectively through either intratumoral injections into solid tumors or administered via an

  10. Microspheres with Ultrahigh Holmium Content for Radioablation of Malignancies

    NARCIS (Netherlands)

    Bult, W.; Seevinck, P.R.; Krijger, G.C.; Visser, T.; Kroon-Batenburg, L.M.J.; Bakker, C.J.G.; Hennink, W.E.; Van het Schip, A.D.; Nijsen, J.F.W.

    Purpose The aim of this study was to develop microspheres with an ultra high holmium content which can be neutron activated for radioablation of malignancies. These microspheres are proposed to be delivered selectively through either intratumoral injections into solid tumors or administered via an

  11. INVESTIGATION OF DRUG RELEASE FROM BIODEGRADABLE PLG MICROSPHERES: EXPERIMENT AND THEORY

    Energy Technology Data Exchange (ETDEWEB)

    ANDREWS, MALCOLM J. [Los Alamos National Laboratory; BERCHANE, NADER S. [Los Alamos National Laboratory; CARSON, KENNETH H. [Los Alamos National Laboratory; RICE-FICHT, ALLISON C. [Los Alamos National Laboratory

    2007-01-30

    Piroxicam containing PLG microspheres having different size distributions were fabricated, and in vitro release kinetics were determined for each preparation. Based on the experimental results, a suitable mathematical theory has been developed that incorporates the effect of microsphere size distribution and polymer degradation on drug release. We show from in vitro release experiments that microsphere size has a significant effect on drug release rate. The initial release rate decreased with an increase in microsphere size. In addition, the release profile changed from first order to concave-upward (sigmoidal) as the system size was increased. The mathematical model gave a good fit to the experimental release data.

  12. Method for selecting hollow microspheres for use in laser fusion targets

    Science.gov (United States)

    Farnum, Eugene H.; Fries, R. Jay; Havenhill, Jerry W.; Smith, Maurice Lee; Stoltz, Daniel L.

    1976-01-01

    Hollow microspheres having thin and very uniform wall thickness are useful as containers for the deuterium and tritium gas mixture used as a fuel in laser fusion targets. Hollow microspheres are commercially available; however, in commercial lots only a very small number meet the rigid requirements for use in laser fusion targets. Those meeting these requirements may be separated from the unsuitable ones by subjecting the commercial lot to size and density separations and then by subjecting those hollow microspheres thus separated to an external pressurization at which those which are aspherical or which have nonuniform walls are broken and separating the sound hollow microspheres from the broken ones.

  13. Chitosan microspheres in novel drug delivery systems.

    Science.gov (United States)

    Mitra, Analava; Dey, Baishakhi

    2011-07-01

    The main aim in the drug therapy of any disease is to attain the desired therapeutic concentration of the drug in plasma or at the site of action and maintain it for the entire duration of treatment. A drug on being used in conventional dosage forms leads to unavoidable fluctuations in the drug concentration leading to under medication or overmedication and increased frequency of dose administration as well as poor patient compliance. To minimize drug degradation and loss, to prevent harmful side effects and to increase drug bioavailability various drug delivery and drug targeting systems are currently under development. Handling the treatment of severe disease conditions has necessitated the development of innovative ideas to modify drug delivery techniques. Drug targeting means delivery of the drug-loaded system to the site of interest. Drug carrier systems include polymers, micelles, microcapsules, liposomes and lipoproteins to name some. Different polymer carriers exert different effects on drug delivery. Synthetic polymers are usually non-biocompatible, non-biodegradable and expensive. Natural polymers such as chitin and chitosan are devoid of such problems. Chitosan comes from the deacetylation of chitin, a natural biopolymer originating from crustacean shells. Chitosan is a biocompatible, biodegradable, and nontoxic natural polymer with excellent film-forming ability. Being of cationic character, chitosan is able to react with polyanions giving rise to polyelectrolyte complexes. Hence chitosan has become a promising natural polymer for the preparation of microspheres/nanospheres and microcapsules. The techniques employed to microencapsulate with chitosan include ionotropic gelation, spray drying, emulsion phase separation, simple and complex coacervation. This review focuses on the preparation, characterization of chitosan microspheres and their role in novel drug delivery systems.

  14. Modified composite microspheres of hydroxyapatite and poly(lactide-co-glycolide) as an injectable scaffold

    Energy Technology Data Exchange (ETDEWEB)

    Hu, Xixue [BNLMS, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190 (China); CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Beijing 100190 (China); Shen, Hong, E-mail: shenhong516@iccas.ac.cn [BNLMS, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190 (China); Yang, Fei [BNLMS, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190 (China); Liang, Xinjie [CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Beijing 100190 (China); Wang, Shenguo, E-mail: wangsg@iccas.ac.cn [BNLMS, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190 (China); Wu, Decheng, E-mail: dcwu@iccas.ac.cn [BNLMS, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190 (China)

    2014-02-15

    The compound of hydroxyapatite-poly(lactide-co-glycolide) (HA-PLGA) was prepared by ionic bond between HA and PLGA. HA-PLGA was more stable than the simple physical blend of hydroxyapatite and poly(lactide-co-glycolide) (HA/PLGA). The surface of HA-PLGA microsphere fabricated by an emulsion–solvent evaporation method was rougher than that of HA/PLGA microspheres. Moreover, surface HA content of HA-PLGA microspheres was more than that of HA/PLGA microspheres. In vitro mouse OCT-1 osteoblast-like cell culture results showed that the HA-PLGA microspheres clearly promoted osteoblast attachment, proliferation and alkaline phosphatase activity. It was considered that surface rich HA component and rough surface of HA-PLGA microsphere enhanced cell growth and differentiation. The good cell affinity of the HA-PLGA microspheres indicated that they could be used as an injectable scaffold for bone tissue engineering.

  15. Controlled Synthesis of Hierarchically Assembled Porous ZnO Microspheres with Enhanced Gas-Sensing Properties

    Directory of Open Access Journals (Sweden)

    Shengsheng You

    2015-01-01

    Full Text Available The ZnO microspheres constructed by porous nanosheets were successfully synthesized by calcinating zinc hydroxide carbonate (ZHC microspheres obtained by a sample hydrothermal method. The samples were characterized in detail with scanning electron microscopy (SEM, transmission electron microscopy (TEM, X-ray diffraction (XRD, and thermogravimetric and differential scanning calorimetry (TG-DSC. The results indicated that the prepared ZnO microspheres were well crystalline with wurtzite hexagonal phase. The effects of reaction time, temperature, the amount of trisodium citrate, and urea on the morphology of ZnO microspheres were studied. The formation mechanism of porous ZnO microspheres was discussed. Furthermore, the gas-sensing properties for detection of organic gas of the prepared porous ZnO microspheres were investigated. The results indicated that the prepared porous ZnO microspheres exhibited high gas-sensing properties for detection of ethanol gas.

  16. Modified composite microspheres of hydroxyapatite and poly(lactide-co-glycolide) as an injectable scaffold

    International Nuclear Information System (INIS)

    Hu, Xixue; Shen, Hong; Yang, Fei; Liang, Xinjie; Wang, Shenguo; Wu, Decheng

    2014-01-01

    The compound of hydroxyapatite-poly(lactide-co-glycolide) (HA-PLGA) was prepared by ionic bond between HA and PLGA. HA-PLGA was more stable than the simple physical blend of hydroxyapatite and poly(lactide-co-glycolide) (HA/PLGA). The surface of HA-PLGA microsphere fabricated by an emulsion–solvent evaporation method was rougher than that of HA/PLGA microspheres. Moreover, surface HA content of HA-PLGA microspheres was more than that of HA/PLGA microspheres. In vitro mouse OCT-1 osteoblast-like cell culture results showed that the HA-PLGA microspheres clearly promoted osteoblast attachment, proliferation and alkaline phosphatase activity. It was considered that surface rich HA component and rough surface of HA-PLGA microsphere enhanced cell growth and differentiation. The good cell affinity of the HA-PLGA microspheres indicated that they could be used as an injectable scaffold for bone tissue engineering.

  17. Gastrointestinal Complications Depending on the Selectivity of Non-Steroidal Anti-Inflammatory Drug

    Directory of Open Access Journals (Sweden)

    G.V. Dzyak

    2013-02-01

    Full Text Available The article deals with the problem of gastrointestinal complications during administration of nonsteroidal anti-inflammatory drugs, commonly used to treat a range of conditions, particularly rheumatic diseases. The results of own researches, which served to define the characteristics of changes in the state of gastric secretory function in patients receiving non-selective and selective anti-inflammatory agent and their comparative analysis, are provided. The data obtained demonstrated a certain contribution to the understanding of the mechanism of development of complications from the gastrointestinal tract when taken drugs of above group.

  18. [Optimization of riboflavin sodium phosphate loading to calcium alginate floating microspheres by response surface methodology].

    Science.gov (United States)

    Zhang, An-yang; Fan, Tian-yuan

    2009-12-18

    To investigate the preparation, optimization and in vitro properties of riboflavin sodium phosphate floating microspheres. The floating microspheres composed of riboflavin sodium phosphate and calcium alginate were prepared using ion gelatin-oven drying method. The properties of the microspheres were investigated, including the buoyancy, release, appearance and entrapment efficiency. The formulation was optimized by response surface methodology (RSM). The optimized microspheres were round. The entrapment efficiency was 57.49%. All the microspheres could float on the artificial gastric juice over 8 hours. The release of the drug from the microspheres complied with Fick's diffusion.

  19. Non-steroidal anti-inflammatory drugs and ulcer complications: a risk factor analysis for clinical decision-making

    DEFF Research Database (Denmark)

    Hansen, J M; Hallas, J; Lauritsen, Jens

    1996-01-01

    Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications.......Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications....

  20. Anti-inflammatory and antifibrotic effects of methyl palmitate

    International Nuclear Information System (INIS)

    El-Demerdash, Ebtehal

    2011-01-01

    Methyl palmitate (MP) has been shown earlier to inhibit Kupffer cells and rat peritoneal macrophages. To evaluate the potential of MP to inhibit the activation of other macrophages, RAW cells (macrophages of alveolar origin) were treated with varying concentrations of MP (0.25, 0.5, 1 mM). Assessment of cytotoxicity using MTT assay revealed that 0.25 and 0.5 mM are not toxic to RAW cells. MP was able to inhibit the phagocytic function of RAW cells. Treatment of cells with MP 24 hours prior to LPS stimulation significantly decreased nitric oxide release and altered the pattern of cytokines release; there was a significant decrease in TNF-α and a significant increase in IL-10 compared to the controls. However, there is a non-significant change in IL-6 level. Furthermore, phosphorylation of inhibitory kappa B (IκBα) protein was significantly decreased in RAW cells treated with 0.5 mM MP after LPS stimulation. Based upon the in-vitro results, it was examined whether MP treatment will be effective in preventing bleomycin-induced lung inflammation and fibrosis in-vivo. Bleomycin given by itself caused destruction of the lung architecture characterized by pulmonary fibrosis with collapse of air alveoli and emphysematous. Bleomycin induced a significant increase in hydroxyproline level and activated NF-κB, p65 expression in the lung. MP co-treatment significantly ameliorated bleomycin effects. These results suggest that MP has a potential of inhibiting macrophages in general. The present study demonstrated for the first time that MP has anti-inflammatory and antifibrotic effect that could be through NF-kB inhibition. Thus MP like molecule could be a promising anti-inflammatory and antifibrotic drug. - Research highlights: →Methyl palmitate is a universal macrophage inhibitor. →It could be a promising nucleus of anti-inflammatory and antifibrotic drugs. →The underlying mechanism of these effects could be through NF-kB inhibition.

  1. Covalently coating dextran on macroporous polyglycidyl methacrylate microsphere enabled rapid protein chromatographic separation

    International Nuclear Information System (INIS)

    Zhang, Rongyue; Li, Qiang; Li, Juan; Zhou, Weiqing; Ye, Peili; Gao, Yang; Ma, Guanghui; Su, Zhiguo

    2012-01-01

    Protein denaturation and nonspecific adsorption on polymer media as a chromatographic support have been a problem which needs to be overcome. Macroporous poly(glycidyl methacrylate–divinylbezene) (PGMA–DVB) microspheres prepared in this study were firstly covalently coated with dextran through a three-step method. The dextran was firstly adsorbed onto the microspheres and then covalently bound to the PGMA–DVB microsphere through ether bonds which were formed by hydroxyl group reacting with epoxy group at the presence of 4-(Dimethylamino) pyridine. Finally, the coating dextran layer was crosslinked by ethylene glycol diglycidyl ether to form the continuous network coating. The coated microspheres were characterized by Fourier transform infrared spectra, scanning electron microscope, mercury porosimetry measurements, laser scanning confocal microscope, and protein adsorption experiments. Results showed that PGMA–DVB microspheres coated with dextran successfully maintained the macroporous structure and high permeability. The backpressure was only 1.69 MPa at a high flow rate of 2891 cm/h. Consequently, the hydrophilicity and biocompatibility of modified microspheres were greatly improved, and the contact angle decreased from 184° to 13°, and nonspecific adsorption of proteins was decreased to little or none. The clad dextran coating with large amounts of hydroxyl group was easily derived to be various functional groups. The derived media have great potential applications in rapid protein chromatography. - Highlights: ► Macroporous PGMA–DVB microspheres were covalently coated with dextran. ► The hydrophilicity of the coated microspheres was significantly improved. ► The irreversible adsorption of proteins was reduced to zero. ► The coated microspheres can maintain the macropore structure. ► The coated microspheres were applied to rapid protein separation.

  2. Peracetylated hydroxytyrosol, a new hydroxytyrosol derivate, attenuates LPS-induced inflammatory response in murine peritoneal macrophages via regulation of non-canonical inflammasome, Nrf2/HO1 and JAK/STAT signaling pathways.

    Science.gov (United States)

    Montoya, Tatiana; Aparicio-Soto, Marina; Castejón, María Luisa; Rosillo, María Ángeles; Sánchez-Hidalgo, Marina; Begines, Paloma; Fernández-Bolaños, José G; Alarcón-de-la-Lastra, Catalina

    2018-03-18

    The present study was designed to investigate the anti-inflammatory effects of a new derivative of hydroxytyrosol (HTy), peracetylated hydroxytyrosol (Per-HTy), compared with its parent, HTy, on lipopolysaccharide (LPS)-stimulated murine macrophages as well as potential signaling pathways involved. In particular, we attempted to characterize the role of the inflammasome underlying Per-HTy possible anti-inflammatory effects. Isolated murine peritoneal macrophages were treated with HTy or its derivative in the presence or absence of LPS (5 μg/ml) for 18 h. Cell viability was determined using sulforhodamine B (SRB) assay. Nitric oxide (NO) production was analyzed by Griess method. Production of pro-inflammatory cytokines was evaluated by enzyme-linked immunosorbent assay (ELISA) and inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway (STAT3), haem oxigenase 1 (HO1), nuclear factor (erythroid-derived 2)-like 2 (Nrf2) expression and mitogen-activated protein kinases (MAPKs) activation was determined by Western blot. Per-HTy significantly reduced the levels of NO and pro-inflammatory cytokines as well as both COX-2 and iNOS expressions. Furthermore, Per-HTy treatment inhibited STAT3 and increased Nrf2 and HO1 protein levels in murine macrophages exposed to LPS. In addition, Per-HTy anti-inflammatory activity was related with an inhibition of non-canonical nucleotide binding domain (NOD)-like receptor (NLRP3) inflammasome pathways by decreasing pro-inflammatory interleukin (IL)-1β and IL-18 cytokine levels as consequence of regulation of cleaved caspase-11 enzyme. These results support that this new HTy derivative may offer a new promising nutraceutical therapeutic strategy in the management of inflammatory-related pathologies. Copyright © 2018. Published by Elsevier Inc.

  3. Interleukin-6 inhibits apoptosis of exocrine gland tissues under inflammatory conditions.

    Science.gov (United States)

    Zhou, Jing; Jin, Jun-O; Patel, Ekta S; Yu, Qing

    2015-12-01

    Interleukin (IL)-6 is a multi-functional cytokine that can either promote or suppress tissue inflammation depending on the specific disease context. IL-6 is elevated in the exocrine glands and serum of patients with Sjögren's syndrome (SS), but the specific role of IL-6 in the pathogenesis of this disease has not been defined. In this study, we showed that IL-6 expression levels were increased with age in C56BL/6.NOD-Aec1Aec2 mice, a primary SS model, and higher than the control C57BL/6 mice. To assess the role of IL-6 during the immunological phase of SS development, a neutralizing anti-IL-6 antibody was administered into 16 week-old female C56BL/6.NOD-Aec1Aec2 mice, 3 times weekly for a consecutive 8 weeks. Neutralization of endogenous IL-6 throughout the immunological phase of SS development led to increased apoptosis, caspase-3 activation, leukocytic infiltration, and IFN-γ- and TNF-α production in the salivary gland. To further determine the effect of IL-6 on the apoptosis of exocrine gland cells, recombinant human IL-6 or the neutralizing anti-IL-6 antibody was injected into female C57BL/6 mice that received concurrent injection of anti-CD3 antibody to induce the apoptosis of exocrine gland tissues. Neutralization of IL-6 enhanced, whereas administration of IL-6 inhibited apoptosis and caspase-3 activation in salivary and lacrimal glands in this model. The apoptosis-suppressing effect of IL-6 was associated with up-regulation of Bcl-xL and Mcl-1 in both glands. Moreover, IL-6 treatment induced activation of STAT3 and up-regulated Bcl-xL and Mcl-1 gene expression in a human salivary gland epithelial cell line. In conclusion, IL-6 inhibits the apoptosis of exocrine gland tissues and exerts a tissue-protective effect under inflammatory conditions including SS. These findings suggest the possibility of using this property of IL-6 to preserve exocrine gland tissue integrity and function under autoimmune and inflammatory conditions. Copyright © 2015 Elsevier

  4. A novel approach to preparing magnetic protein microspheres with core-shell structure

    Energy Technology Data Exchange (ETDEWEB)

    Jiang Wei, E-mail: climentjw@126.co [National Special Superfine Powder Engineering Research Center, Nanjing University of Science and Technology, Nanjing 210094 (China); Sun Zhendong; Li Fengsheng [National Special Superfine Powder Engineering Research Center, Nanjing University of Science and Technology, Nanjing 210094 (China); Chen Kai; Liu Tianyu; Liu Jialing [Department of Physics, Nanjing University of Science and Technology, Nanjing 210094 (China); Zhou Tianle [Department of Materials Science and Engineering, Nanjing University of Science and Technology, Nanjing 210094 (China); Guo Rui [Department of Mechanical Engineering, Nanjing University of Science and Technology, Nanjing 210094 (China)

    2011-03-15

    Magnetic protein microspheres with core-shell structure were prepared through a novel approach based on the sonochemical method and the emulsion solvent evaporation method. The microspheres are composed of the oleic acid and undecylenic acid modified Fe{sub 3}O{sub 4} cores and coated with globular bovine serum albumin (BSA). Under an optimized condition, up to 57.8 wt% of approximately 10 nm superparamagnetic Fe{sub 3}O{sub 4} nanoparticles could be uniformly encapsulated into the BSA microspheres with the diameter of approximately 160 nm and the high saturation magnetization of 38.5 emu/g, besides of the abundant functional groups. The possible formation mechanism of magnetic microspheres was discussed in detail. - Research Highlights: Magnetic protein microspheres with core-shell structure were prepared through a novel approach based on the sonochemical method and the emulsion solvent evaporation method. The microspheres are composed of the oleic acid and undecylenic acid modified Fe{sub 3}O{sub 4} cores and coated with globular bovine serum albumin (BSA). 57.8 wt% of approximately 10 nm superparamagnetic Fe{sub 3}O{sub 4} nanoparticles could be uniformly encapsulated into the BSA microspheres with the diameter of approximately 160 nm and the high saturation magnetization of 38.5 emu/g, besides the abundant functional groups.

  5. A novel approach to preparing magnetic protein microspheres with core-shell structure

    International Nuclear Information System (INIS)

    Jiang Wei; Sun Zhendong; Li Fengsheng; Chen Kai; Liu Tianyu; Liu Jialing; Zhou Tianle; Guo Rui

    2011-01-01

    Magnetic protein microspheres with core-shell structure were prepared through a novel approach based on the sonochemical method and the emulsion solvent evaporation method. The microspheres are composed of the oleic acid and undecylenic acid modified Fe 3 O 4 cores and coated with globular bovine serum albumin (BSA). Under an optimized condition, up to 57.8 wt% of approximately 10 nm superparamagnetic Fe 3 O 4 nanoparticles could be uniformly encapsulated into the BSA microspheres with the diameter of approximately 160 nm and the high saturation magnetization of 38.5 emu/g, besides of the abundant functional groups. The possible formation mechanism of magnetic microspheres was discussed in detail. - Research Highlights: → Magnetic protein microspheres with core-shell structure were prepared through a novel approach based on the sonochemical method and the emulsion solvent evaporation method.→ The microspheres are composed of the oleic acid and undecylenic acid modified Fe 3 O 4 cores and coated with globular bovine serum albumin (BSA).→ 57.8 wt% of approximately 10 nm superparamagnetic Fe 3 O 4 nanoparticles could be uniformly encapsulated into the BSA microspheres with the diameter of approximately 160 nm and the high saturation magnetization of 38.5 emu/g, besides the abundant functional groups.

  6. Occupational radiation exposure of medical staff performing 90Y-loaded microsphere radioembolization

    International Nuclear Information System (INIS)

    Laffont, Sophie; Ardisson, Valerie; Lenoir, Laurence; Rolland, Yan; Rohou, Tanguy; Edeline, Julien; Pracht, Marc; Sourd, Samuel Le; Lepareur, Nicolas; Garin, Etienne

    2016-01-01

    Radioembolization of liver cancer with 90 Y-loaded microspheres is increasingly used but data regarding hospital staff exposure are scarce. We evaluated the radiation exposure of medical staff while preparing and injecting 90 Y-loaded glass and resin microspheres especially in view of the increasing use of these products. Exposure of the chest and finger of the radiopharmacist, nuclear medicine physician and interventional radiologist during preparation and injection of 78 glass microsphere preparations and 16 resin microsphere preparations was monitored. Electronic dosimeters were used to measure chest exposure and ring dosimeters were used to measure finger exposure. Chest exposure was very low for both products used (<10 μSv from preparation and injection). In our experience, finger exposure was significantly lower than the annual limit of 500 mSv for both products. With glass microspheres, the mean finger exposure was 13.7 ± 5.2 μSv/GBq for the radiopharmacist, and initially 17.9 ± 5.4 μSv/GBq for the nuclear medicine physician reducing to 13.97 ± 7.9 μSv/GBq with increasing experience. With resin microspheres, finger exposure was more significant: mean finger exposure for the radiopharmacist was 295.1 ± 271.9 μSv/GBq but with a reduction with increasing experience to 97.5 ± 35.2 μSv/GBq for the six most recent dose preparations. For administration of resin microspheres, the greatest mean finger exposure for the nuclear medicine physician (the most exposed operator) was 235.5 ± 156 μSv/GBq. Medical staff performing 90 Y-loaded microsphere radioembolization procedures are exposed to safe levels of radiation. Exposure is lower than that from treatments using 131 I-lipiodol. The lowest finger exposure is from glass microspheres. With resin microspheres finger exposure is acceptable but could be optimized in accordance with the ALARA principle, and especially in view of the increasing use of radioembolization. (orig.)

  7. Porous-wall hollow glass microspheres as carriers for biomolecules

    Science.gov (United States)

    Li, Shuyi; Dynan, William S; Wicks, George; Serkiz, Steven

    2013-09-17

    The present invention includes compositions of porous-wall hollow glass microspheres and one or more biomolecules, wherein the one or more biomolecules are positioned within a void location within the hollow glass microsphere, and the use of such compositions for the diagnostic and/or therapeutic delivery of biomolecules.

  8. Carboxyl-Functionalized Polymeric Microspheres Prepared by One-Stage Photoinitiated RAFT Dispersion Polymerization

    Directory of Open Access Journals (Sweden)

    Jianbo Tan

    2017-12-01

    Full Text Available Herein, we report a photoinitiated reversible addition-fragmentation chain transfer (RAFT dispersion copolymerization of methyl methacrylate (MMA and methyl methacrylic (MAA for the preparation of highly monodisperse carboxyl-functionalized polymeric microspheres. High rates of polymerization were observed, with more than 90% particle yields being achieved within 3 h of UV irradiation. Effects of reaction parameters (e.g., MAA concentration, RAFT agent concentration, photoinitiator concentration, and solvent composition were studied in detail, and highly monodisperse polymeric microspheres were obtained in most cases. Finally, silver (Ag composite microspheres were prepared by in situ reduction of AgNO3 using the carboxyl-functionalized polymeric microspheres as the template. The obtained Ag composite microspheres were able to catalyze the reduction of methylene blue (MB with NaBH4 as a reductant.

  9. Preparation of berbamine loaded chitosan-agarose microspheres and in vitro release study

    Directory of Open Access Journals (Sweden)

    Zhang Hu

    2012-01-01

    Full Text Available Berbamine loaded chitosan-agarose microspheres were prepared using a water-in-oil emulsion technique. Optimum preparing parameters were determined by orthogonal experiments as follows: ratio of berbamine to chitosan (w/w is 1:10; percentage of emulsifier (span 80, v/v is 6%; volume of glutaraldehyde is 2 mL; and reaction temperature is 70 ºC. Under these optimal conditions, the encapsulation efficiency and loading capacity of microspheres are 84.57% and 8.44%, respectively. The swelling tests showed that the microspheres possessed higher swelling ratio at pH 7.4 than at pH 1.2. FTIR indicated that berbamine had been successfully loaded in the chitosan-agarose microspheres by physical entrapment. In vitro release studies showed that berbamine was released from microspheres in a significantly sustained fashion.

  10. Flavonoids Identified from Korean Scutellaria baicalensis Georgi Inhibit Inflammatory Signaling by Suppressing Activation of NF-κB and MAPK in RAW 264.7 Cells

    Directory of Open Access Journals (Sweden)

    Gyeong-Eun Hong

    2013-01-01

    Full Text Available Scutellaria baicalensis Georgi has been used as traditional medicine for treating inflammatory diseases, hepatitis, tumors, and diarrhea in Asia. Hence, we investigated the anti-inflammatory effect and determined the molecular mechanism of action of flavonoids isolated from Korean S. baicalensis G. in lipopolysaccharide- (LPS- stimulated RAW 264.7 macrophages. A 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide assay was performed to examine cytotoxicity of the flavonoids at various concentrations of 10, 40, 70, and 100 µg/mL. No cytotoxicity was observed in RAW 264.7 cells at these concentrations. Furthermore, the flavonoids decreased production of inflammatory mediators such as inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6, and tumor necrosis factor-alpha and inhibited phosphorylation of nuclear factor-kappa B (NF-κB and mitogen-activated protein kinases (MAPKs in LPS-induced RAW 264.7 cells. Moreover, to identify the differentially expressed proteins in RAW 264.7 cells of the control, LPS-treated, and flavonoid-treated groups, two-dimensional gel electrophoresis and mass spectrometry were conducted. The identified proteins were involved in the inflammatory response and included PRKA anchor protein and heat shock protein 70 kD. These findings suggest that the flavonoids isolated from S. baicalensis G. might have anti-inflammatory effects that regulate the expression of inflammatory mediators by inhibiting the NF-κB signaling pathway via the MAPK signaling pathway in RAW 264.7 cells.

  11. Mucoadhesive microspheres: a promising tool in drug delivery.

    Science.gov (United States)

    Patil, Sanjay B; Sawant, Krutika K

    2008-10-01

    Mucoadhesive polymers have recently gained interest among pharmaceutical scientists as a means of improving drug delivery by promoting the residence time and contact time of the dosage form with the mucous membranes. Mucoadhesion is the process whereby synthetic and natural polymers adhere to mucosal surfaces in the body. If these materials are then incorporated into pharmaceutical formulations, drug absorption by mucosal cells may be enhanced or the drug will be released at the site for an extended period of time. Microspheres, in general, have the potential to be used for targeted and controlled release drug delivery; however, coupling of mucoadhesive properties to microspheres has additional advantages like, a much more intimate contact with the mucus layer, efficient absorption and enhanced bioavailability of the drugs due to a high surface to volume ratio. The present review describes the potential applications of mucoadhesive microspheres as a novel carrier system to improve drug delivery by various routes of administration like buccal, oral, nasal, ocular, vaginal and rectal, either for systemic or for local effects. The mucoadhesive polymers, methods of preparation of microspheres and their in vitro and in vivo evaluation are also described.

  12. Preparation of cellulose based microspheres by combining spray coagulating with spray drying.

    Science.gov (United States)

    Wang, Qiao; Fu, Aiping; Li, Hongliang; Liu, Jingquan; Guo, Peizhi; Zhao, Xiu Song; Xia, Lin Hua

    2014-10-13

    Porous microspheres of regenerated cellulose with size in range of 1-2 μm and composite microspheres of chitosan coated cellulose with size of 1-3 μm were obtained through a two-step spray-assisted approach. The spray coagulating process must combine with a spray drying step to guarantee the formation of stable microspheres of cellulose. This approach exhibits the following two main virtues. First, the preparation was performed using aqueous solution of cellulose as precursor in the absence of organic solvent and surfactant; Second, neither crosslinking agent nor separated crosslinking process was required for formation of stable microspheres. Moreover, the spray drying step also provided us with the chance to encapsulate guests into the resultant cellulose microspheres. The potential application of the cellulose microspheres acting as drug delivery vector has been studied in two PBS (phosphate-buffered saline) solution with pH values at 4.0 and 7.4 to mimic the environments of stomach and intestine, respectively. Copyright © 2014 Elsevier Ltd. All rights reserved.

  13. Bee Venom Inhibits Porphyromonas gingivalis Lipopolysaccharides-Induced Pro-Inflammatory Cytokines through Suppression of NF-κB and AP-1 Signaling Pathways.

    Science.gov (United States)

    Kim, Woon-Hae; An, Hyun-Jin; Kim, Jung-Yeon; Gwon, Mi-Gyeong; Gu, Hyemin; Park, Jae-Bok; Sung, Woo Jung; Kwon, Yong-Chul; Park, Kyung-Duck; Han, Sang Mi; Park, Kwan-Kyu

    2016-11-10

    Periodontitis is a chronic inflammatory disease that leads to destruction of tooth supporting tissues. Porphyromonas gingivalis ( P. gingivalis ), especially its lipopolysaccharides (LPS), is one of major pathogens that cause periodontitis. Bee venom (BV) has been widely used as a traditional medicine for various diseases. Previous studies have demonstrated the anti-inflammatory, anti-bacterial effects of BV. However, a direct role and cellular mechanism of BV on periodontitis-like human keratinocytes have not been explored. Therefore, we investigated the anti-inflammatory mechanism of BV against P. gingivalis LPS (PgLPS)-induced HaCaT human keratinocyte cell line. The anti-inflammatory effect of BV was demonstrated by various molecular biological methods. The results showed that PgLPS increased the expression of Toll-like receptor (TLR)-4 and pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, IL-8, and interferon (IFN)-γ. In addition, PgLPS induced activation of the signaling pathways of inflammatory cytokines-related transcription factors, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and activator protein 1 (AP-1). BV effectively inhibited those pro-inflammatory cytokines through suppression of NF-κB and AP-1 signaling pathways. These results suggest that administration of BV attenuates PgLPS-induced inflammatory responses. Furthermore, BV may be a useful treatment to anti-inflammatory therapy for periodontitis.

  14. Development of nuclear fuel microsphere handling techniques and equipment

    International Nuclear Information System (INIS)

    Mack, J.E.; Suchomel, R.R.; Angelini, P.

    1979-01-01

    Considerable progress has been made in the development of microsphere handling techniques and equipment for nuclear applications. Work at Oak Ridge National Laboratory with microspherical fuel forms dates back to the early sixties with the development of the sol-gel process. Since that time a number of equipment items and systems specifically related to microsphere handling and characterization have been identified and developed for eventual application in a remote recycle facility. These include positive and negative pressure transfer systems, samplers, weighers, a blender-dispenser, and automated devices for particle size distribution and crushing strength analysis. The current status of these and other components and systems is discussed

  15. Research progress of fabricating polyvinyl alcohol coating on plastic microsphere

    International Nuclear Information System (INIS)

    Su Lin; Chen Sufen; Liu Meifang; Zhang Zhanwen; Yao Hong; Li Bo; Liu Yiyang

    2012-01-01

    In the procedures of designing polystyrene-polyvinyl alcohol-CH (carbon and hydrogen elements) (PS-PVA-CH) triple-layer microspheres, there are many methods such as drop-tower technique, emulsion micro-encapsulation, dip (spin) coating, interfacial polycondensation, and spraying technique to prepare the PVA coating. Drop-tower technique, emulsion micro-encapsulation and dip (spin) coating are most-commonly used. The advantages, disadvantages and the research progress of the three methods are summarized in this paper. Emulsion micro-encapsulation is suitable for preparing double-layer microspheres of sizes smaller then 500 μm, with high survival ratio and good quality. However, the preparation process is easily influenced by artificial factors. Small-sized double-layer microspheres can also be prepared by the drop-tower technique, and the preparation period is short. But there are still some problems such as the difficulty in designing the droplet generator, uneven PVA coating and the difficulty in preparing large-sized microspheres. Dip (spin) coating technique can be used to prepare PS-PVA microspheres with sizes larger than 1000 μm, but the spread of PVA coating is affected by many factors in this method, and the prepared PVA coating is too thin and not uniform. (authors)

  16. Allosteric Inhibition of Factor XIIIa. Non-Saccharide Glycosaminoglycan Mimetics, but Not Glycosaminoglycans, Exhibit Promising Inhibition Profile.

    Directory of Open Access Journals (Sweden)

    Rami A Al-Horani

    Full Text Available Factor XIIIa (FXIIIa is a transglutaminase that catalyzes the last step in the coagulation process. Orthostery is the only approach that has been exploited to design FXIIIa inhibitors. Yet, allosteric inhibition of FXIIIa is a paradigm that may offer a key advantage of controlled inhibition over orthosteric inhibition. Such an approach is likely to lead to novel FXIIIa inhibitors that do not carry bleeding risks. We reasoned that targeting a collection of basic amino acid residues distant from FXIIIa's active site by using sulfated glycosaminoglycans (GAGs or non-saccharide GAG mimetics (NSGMs would lead to the discovery of the first allosteric FXIIIa inhibitors. We tested a library of 22 variably sulfated GAGs and NSGMs against human FXIIIa to discover promising hits. Interestingly, although some GAGs bound to FXIIIa better than NSGMs, no GAG displayed any inhibition. An undecasulfated quercetin analog was found to inhibit FXIIIa with reasonable potency (efficacy of 98%. Michaelis-Menten kinetic studies revealed an allosteric mechanism of inhibition. Fluorescence studies confirmed close correspondence between binding affinity and inhibition potency, as expected for an allosteric process. The inhibitor was reversible and at least 9-fold- and 26-fold selective over two GAG-binding proteins factor Xa (efficacy of 71% and thrombin, respectively, and at least 27-fold selective over a cysteine protease papain. The inhibitor also inhibited the FXIIIa-mediated polymerization of fibrin in vitro. Overall, our work presents the proof-of-principle that FXIIIa can be allosterically modulated by sulfated non-saccharide agents much smaller than GAGs, which should enable the design of selective and safe anticoagulants.

  17. Covalently coating dextran on macroporous polyglycidyl methacrylate microsphere enabled rapid protein chromatographic separation

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Rongyue; Li, Qiang; Li, Juan; Zhou, Weiqing; Ye, Peili; Gao, Yang; Ma, Guanghui, E-mail: ghma@home.ipe.ac.cn; Su, Zhiguo

    2012-12-01

    Protein denaturation and nonspecific adsorption on polymer media as a chromatographic support have been a problem which needs to be overcome. Macroporous poly(glycidyl methacrylate-divinylbezene) (PGMA-DVB) microspheres prepared in this study were firstly covalently coated with dextran through a three-step method. The dextran was firstly adsorbed onto the microspheres and then covalently bound to the PGMA-DVB microsphere through ether bonds which were formed by hydroxyl group reacting with epoxy group at the presence of 4-(Dimethylamino) pyridine. Finally, the coating dextran layer was crosslinked by ethylene glycol diglycidyl ether to form the continuous network coating. The coated microspheres were characterized by Fourier transform infrared spectra, scanning electron microscope, mercury porosimetry measurements, laser scanning confocal microscope, and protein adsorption experiments. Results showed that PGMA-DVB microspheres coated with dextran successfully maintained the macroporous structure and high permeability. The backpressure was only 1.69 MPa at a high flow rate of 2891 cm/h. Consequently, the hydrophilicity and biocompatibility of modified microspheres were greatly improved, and the contact angle decreased from 184 Degree-Sign to 13 Degree-Sign , and nonspecific adsorption of proteins was decreased to little or none. The clad dextran coating with large amounts of hydroxyl group was easily derived to be various functional groups. The derived media have great potential applications in rapid protein chromatography. - Highlights: Black-Right-Pointing-Pointer Macroporous PGMA-DVB microspheres were covalently coated with dextran. Black-Right-Pointing-Pointer The hydrophilicity of the coated microspheres was significantly improved. Black-Right-Pointing-Pointer The irreversible adsorption of proteins was reduced to zero. Black-Right-Pointing-Pointer The coated microspheres can maintain the macropore structure. Black-Right-Pointing-Pointer The coated microspheres

  18. Prostaglandin E(2) synthase inhibition as a therapeutic target.

    Science.gov (United States)

    Iyer, Jitesh P; Srivastava, Punit K; Dev, Rishabh; Dastidar, Sunanda G; Ray, Abhijit

    2009-07-01

    Most NSAIDs function by inhibiting biosynthesis of PGE(2) by inhibition of COX-1 and/or COX-2. Since COX-1 has a protective function in the gastro-intestinal tract (GIT), non-selective inhibition of both cycloxy genases leads to moderate to severe gastro-intestinal intolerance. Attempts to identify selective inhibitors of COX-2, led to the identification of celecoxib and rofecoxib. However, long-term use of these drugs has serious adverse effects of sudden myocardial infarction and thrombosis. Drug-mediated imbalance in the levels of prostaglandin I(2) (PGI(2)) and thromboxane A(2) (TXA(2)) with a bias towards TXA(2) may be the primary reason for these events. This resulted in the drugs being withdrawn from the market, leaving a need for an effective and safe anti-inflammatory drug. Recently, the focus of research has shifted to enzymes downstream of COX in the prosta glandin biosynthetic pathway such as prostaglandin E(2) synthases. Microsomal prostaglandin E(2) synthase-1 (mPGES-1) specifically isomerizes PGH(2) to PGE(2), under inflammatory conditions. In this review, we examine the biology of mPGES-1 and its role in disease. Progress in designing molecules that can selectively inhibit mPGES-1 is reviewed. mPGES-1 has the potential to be a target for anti-inflammatory therapy, devoid of adverse GIT and cardiac effects and warrants further investigation.

  19. A microsphere suspension model of metamaterial fluids

    Directory of Open Access Journals (Sweden)

    Qian Duan

    2017-05-01

    Full Text Available Drawing an analogy to the liquid phase of natural materials, we theoretically propose a microsphere suspension model to realize a metamaterial fluid with artificial electromagnetic indexes. By immersing high-ε, micrometer-sized dielectric spheres in a low-ε insulating oil, the structured fluid exhibits liquid-like properties from dispersing phase as well as the isotropic negative electromagnetic parameters caused by Mie resonances from dispersed microspheres. The work presented here will benefit the development of structured fluids toward metamaterials.

  20. Iron Nanoparticles-Encapsulating Silica Microspheres for Arterial Embolization Hyperthermia

    Energy Technology Data Exchange (ETDEWEB)

    Li, Z; Kawashita, M, E-mail: zhixia@ecei.tohoku.ac.jp [Graduate School of Biomedical Engineering, Tohoku University (Japan)

    2011-10-29

    We attempted to prepare {alpha}-Fe-encapsulating silica ({alpha}FeSi) microspheres by a sol-gel process using tetramethoxysilane (TMOS) in water-in-oil emulsion. The effect of preparation conditions on the structure, magnetic and heating properties of resultant products were investigated. Oil phase consisted of kerosene with 32 wt% of surfactants (sorbitan monooleate / sorbitan monostearate in 3:1 weight ratio). Water phase consisted of TMOS, ethanol (CH{sub 2}CH{sub 3}OH), water and iron nitrate (Fe(NO{sub 3}){sub 3{center_dot}}9H{sub 2}O) with TMOS / CH{sub 2}CH{sub 3}OH/H{sub 2}O/Fe{sup 3+} in 1:7.4:16.2:0.4{approx}1.2 molar ratio. Fe{sup 3+}-containing silica gel (FeSiG) microspheres 5 to 30 {mu}m in size were successfully obtained by adding the water phase into the oil phase at 60 deg. C under stirring of 1500 rpm for 100 min. {alpha}FeSi microspheres was obtained by heating the FeSiG microspheres at 850deg. C in argon atmosphere. The obtained {alpha}FeSi microspheres have a saturation magnetization (Ms) up to 21 emu g{sup -1} and a coercive force (Hc) of 133 Oe. The in vitro heating generation was evaluated under an alternating current (AC) magnetic field of 300 Oe and 100 kHz.

  1. Amides of non-steroidal anti-inflammatory drugs with thiomorpholine can yield hypolipidemic agents with improved anti-inflammatory activity.

    Science.gov (United States)

    Theodosis-Nobelos, Panagiotis; Kourti, Malamati; Gavalas, Antonios; Rekka, Eleni A

    2016-02-01

    Novel amides of non steroidal anti-inflammatory drugs (NSAIDs), α-lipoic acid and indole-3-acetic acid with thiomorpholine were synthesised by a simple method and at high yields (60-92%). All the NSAID derivatives highly decreased lipidemic indices in the plasma of Triton treated hyperlipidemic rats. The most potent compound was the indomethacin derivative, which decreased total cholesterol, triglycerides and LDL cholesterol by 73%, 80% and 83%, respectively. They reduced acute inflammation equally or more than most parent acids. Hence, it could be concluded that amides of common NSAIDs with thiomorpholine acquire considerable hypolipidemic potency, while they preserve or augment their anti-inflammatory activity, thus addressing significant risk factors for atherogenesis. Copyright © 2015 Elsevier Ltd. All rights reserved.

  2. Chitosan and Nanohydroxyapatite Roles in Physical and Chemical Characteristics of Gelatin/Chitosan/Nanohydroxyapatite Microspheres

    Directory of Open Access Journals (Sweden)

    S. Bagheri-Khoulenjani

    2010-12-01

    Full Text Available The effects of chitosan/biopolymer (C/P and nanohydroxyapatite/ biopolymer (nHA/P weight ratios on particle size and its uniformity, cross-linking density and NH2 content of nano-hydroxyapatite/chitosan/gelatin (nHA/C/G microspheres were investigated. Microspheres were fabricated using water-in-oil emulsion. Cross-linking of microspheres was performed using water soluble carbodiimide. Particle size and its uniformity were evaluated using an optical microscope. The morphology of microspheres was studied by scanning electron microscopy. The obtained data from particle size measurements revealed that increments in C/P ratio increased the particle size while reducing its uniformity, and increased the NH2 content and cross linking density of the microspheres. It was shown that incremental increase in nHA/P ratio increased the particle size and its uniformity and reduced the NH2 content and cross-linking density of the microspheres.Morphological studies showed that the fabricated microspheres had spherical shape in medium level of C/P ratio and nHA/P ratio. However, increasing in chitosan/biopolymer ratio induced some micro-cracks into the structure of microspheres.

  3. Toward quantum-limited position measurements using optically levitated microspheres

    International Nuclear Information System (INIS)

    Libbrecht, Kenneth G.; Black, Eric D.

    2004-01-01

    We propose the use of optically levitated microspheres as test masses in experiments aimed at reaching and potentially exceeding the standard quantum limit for position measurements. Optically levitated microspheres have low mass and are essentially free of suspension thermal noise, making them well suited for experimentally testing our understanding of quantum-limited measurements

  4. Toward quantum-limited position measurements using optically levitated microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Libbrecht, Kenneth G.; Black, Eric D

    2004-01-26

    We propose the use of optically levitated microspheres as test masses in experiments aimed at reaching and potentially exceeding the standard quantum limit for position measurements. Optically levitated microspheres have low mass and are essentially free of suspension thermal noise, making them well suited for experimentally testing our understanding of quantum-limited measurements.

  5. Synthesis and characterization of magnesium gluconate contained poly(lactic-co-glycolic acid)/chitosan microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rahman, Shekh M. [Department of Chemical, Biological and Bioengineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Mahoney, Christopher [Department of Bioengineering, University of Pittsburgh, 4200 Fifth Avenue, Pittsburgh, PA 15250 (United States); Sankar, Jagannathan [NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Department of Mechanical Engineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); Marra, Kacey G. [NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Department of Bioengineering, University of Pittsburgh, 4200 Fifth Avenue, Pittsburgh, PA 15250 (United States); Department of Plastic Surgery, University of Pittsburgh, 200 Lothrop Street, Pittsburgh, PA 15250 (United States); McGowan Institute for Regenerative Medicine, University of Pittsburgh, 450 Technology Drive, Pittsburgh, PA 15250 (United States); Bhattarai, Narayan, E-mail: nbhattar@ncat.edu [Department of Chemical, Biological and Bioengineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States)

    2016-01-15

    Graphical abstract: - Highlights: • Magnesium gluconate contained PLGA/chitosan microspheres were fabricated. • In vitro release of magnesium ions was performed using Xylidyl Blue assay. • Chitosan coated PLGA can significantly control the release of magnesium ions. • Cellular compatibility was tested using adipose-derived stem cells and PC12 cells. • The cells encounter acceptably low levels of damage in contact with microspheres. - Abstract: The goal of this study was to fabricate and investigate the chitosan coated poly(lactic-co-glycolic acid) (PLGA) microspheres for the development of controlled release magnesium delivery system. PLGA based microspheres are ideal vehicles for many controlled release drug delivery applications. Chitosan is a naturally occurring biodegradable and biocompatible polysaccharide, which can coat the surface of PLGA to alter the release of drugs. Magnesium gluconate (MgG) was encapsulated in the PLGA and PLGA/chitosan microspheres by utilizing the double emulsion solvent evaporation technique for controlled release study. The microspheres were tested with respect to several physicochemical and biological properties, including morphology, chemical structure, chitosan adsorption efficiency, magnesium encapsulation efficiency, in vitro release of magnesium ions, and cellular compatibility using both human adipose-derived stem cells (ASCs) and PC12 cells. Chitosan coated PLGA microspheres can significantly control the release of magnesium ions compared to uncoated PLGA microspheres. Both coated and uncoated microspheres showed good cellular compatibility.

  6. STRUCTURING OF DIAMOND FILMS USING MICROSPHERE LITHOGRAPHY

    Directory of Open Access Journals (Sweden)

    Mária Domonkos

    2014-10-01

    Full Text Available In this study, the structuring of micro- and nanocrystalline diamond thin films is demonstrated. The structuring of the diamond films is performed using the technique of microsphere lithography followed by reactive ion etching. Specifically, this paper presents a four-step fabrication process: diamond deposition (microwave plasma assisted chemical vapor deposition, mask preparation (by the standard Langmuir-Blodgett method, mask modification and diamond etching. A self-assembled monolayer of monodisperse polystyrene (PS microspheres with close-packed ordering is used as the primary template. Then the PS microspheres and the diamond films are processed in capacitively coupled radiofrequency plasma  using different plasma chemistries. This fabrication method illustrates the preparation of large arrays of periodic and homogeneous hillock-like structures. The surface morphology of processed diamond films is characterized by scanning electron microscopy and atomic force microscope. The potential applications of such diamond structures in various fields of nanotechnology are also briefly discussed.

  7. Adsorption behavior of protein onto siloxane microspheres

    International Nuclear Information System (INIS)

    Liu Bailing; Cao Shunsheng; Deng Xiaobo; Li Songjun; Luo Rong

    2006-01-01

    The siloxane microspheres with core-shell structure (PMMA/PMPS) (MMA, methyl methacrylate; MPS, 3-methacryloxypropyl-trimethoxysilane) have been prepared by dispersion polymerization as described in our previous work. In this paper, the developed poly(MMA-MPS) microspheres, as a carrier, are used to investigate the adsorption behavior of bovine serum albumin (BSA) on them. The Langmuir and Freundlich models have been applied to describe the adsorption behavior. The experimental results indicated that the presence of PMPS evidently increases the adsorption rate and the amount of protein, and it also influences the interaction of BSA molecules. The adsorption of BSA on the poly(MMA-MPS) microspheres seems to be sensitive to pH and ionic strength. The fittings curves from Langmuir and Freundlich models showed that the adsorption was actually more complicated than ideal situation because one or more interactions were involved in the process. For understanding the electronic contribution, the Zeta potential was used to measure the reactive system before and after protein adsorption

  8. Adsorption behavior of protein onto siloxane microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Liu Bailing [Chengdu Institute of Organic Chemistry, Graduate School of CAS, Chinese Academy of Sciences, Chengdu 610041 (China)]. E-mail: Blliuchem@hotmail.com; Cao Shunsheng [Chengdu Institute of Organic Chemistry, Graduate School of CAS, Chinese Academy of Sciences, Chengdu 610041 (China); Deng Xiaobo [Chengdu Institute of Organic Chemistry, Graduate School of CAS, Chinese Academy of Sciences, Chengdu 610041 (China); Li Songjun [Chengdu Institute of Organic Chemistry, Graduate School of CAS, Chinese Academy of Sciences, Chengdu 610041 (China); Luo Rong [Chengdu Institute of Organic Chemistry, Graduate School of CAS, Chinese Academy of Sciences, Chengdu 610041 (China)

    2006-09-15

    The siloxane microspheres with core-shell structure (PMMA/PMPS) (MMA, methyl methacrylate; MPS, 3-methacryloxypropyl-trimethoxysilane) have been prepared by dispersion polymerization as described in our previous work. In this paper, the developed poly(MMA-MPS) microspheres, as a carrier, are used to investigate the adsorption behavior of bovine serum albumin (BSA) on them. The Langmuir and Freundlich models have been applied to describe the adsorption behavior. The experimental results indicated that the presence of PMPS evidently increases the adsorption rate and the amount of protein, and it also influences the interaction of BSA molecules. The adsorption of BSA on the poly(MMA-MPS) microspheres seems to be sensitive to pH and ionic strength. The fittings curves from Langmuir and Freundlich models showed that the adsorption was actually more complicated than ideal situation because one or more interactions were involved in the process. For understanding the electronic contribution, the Zeta potential was used to measure the reactive system before and after protein adsorption.

  9. Inhibition of Lipopolysaccharide-Stimulated Neuro- Inflammatory ...

    African Journals Online (AJOL)

    ... (12): 2005-2010. ISSN: 1596-5996 (print); 1596-9827 (electronic) ... and production of inflammatory mediators, namely, nitric oxide (NO), inducible NO synthase (iNOS) and tumor necrosis ... TKE in a concentration-dependent manner. Conclusion: .... and incubated at room temperature for 10 min. .... Kuntze ethanol extract ...

  10. Retroperitoneal Inflammatory Liposarcoma in a Patient with Non-Hodgkin Lymphoma: A Report Highlighting Diagnostic Pitfalls

    Directory of Open Access Journals (Sweden)

    Cathy S. Lim

    2010-01-01

    Full Text Available Well differentiated liposarcoma (WDLS is the commonest subtype of liposarcoma. Recognised subtypes of WDLSs are lipoma-like, sclerosing, spindle cell and inflammatory. The inflammatory variant of WDLS also known as “lymphocyte-rich liposarcoma” is rare. We present a case of inflammatory WDLS occurring in the retroperitoneum, in a patient with a past history of non-Hodgkin lymphoma. We outline the histological features, discuss the differential diagnoses and highlight the diagnostic pitfalls in interpretation of this lesion on fine needle biopsy.

  11. Effect of rigidity of porous structure on electrochemical behavior of pristine Li4Ti5O12 microspheres

    International Nuclear Information System (INIS)

    Jia, Zhenyong; Zhou, Qun; Li, Xiaowei; Fu, Yu; Ming, Hai; Zheng, Junwei

    2015-01-01

    Highlights: • Rigid porous framework of Li 4 Ti 5 O 12 microspheres can be fabricated by mutual molten growth of primary particles. • Well-confined nanosized tortuous channels are formed inside Li 4 Ti 5 O 12 microspheres. • Li 4 Ti 5 O 12 microspheres with rigid porous structures exhibit greatly enhanced electrochemical performance. - Abstract: Highly controllable porous architecture is desirable to tailor the physical and chemical properties of functional materials in advanced lithium ion batteries. Here, porous microspheres of spinel lithium titanate (Li 4 Ti 5 O 12 ), a promising alternative anode material for lithium ion batteries, are fabricated by mutual molten growth method in a controllable manner. The key role of the rigidity of the porous structure on the performance of the electrode materials in lithium ion batteries is demonstrated. Rigid framework of the materials is formed by second growth of the primary particles that fused together to generate an interconnected nanopore system inside the spheres, leading to better electrolyte diffusion and lower interparticle contact resistance, relative to the non-porous counterpart. The pristine Li 4 Ti 5 O 12 microspheres with uniform pore distribution and continuous framework exhibit high tap density, remarkable reversible capacity and rate capability, as well as excellent cycling stability. The present method is scalable and may provide a new approach to fabricate other candidate electrode materials for applications that require both high power and high volumetric energy density

  12. Possibilities of the combined use of non-steroidal anti-inflammatory drugs and sulfhydryl compounds in radioprotection

    International Nuclear Information System (INIS)

    Kozubik, A.; Pospisil, M.; Netikova, J.

    1991-01-01

    The combined preirradiation administration of indomethacin and cystamine was found to enhance synergistically the recovery of hemopoiesis in sublethally gamma-irradiated mice. This effect can be explained by a common operation of two mechanisms of radioprotection, i.e. of an increased survival of hemopoietic stem cells due to cystamine action and of stimulatory effects of indomethacin on the proliferation of surviving cells, mediated by the inhibition of prostaglandin synthesis. Attempts to prove such enhancement of protective effects on irradiated mice in terms of postirradiation lethality were unsuccessful. The reason seems to be the influence of toxic effects of the indomethacin-cystamine combination on the gastrointestinal tract. When using the less toxic combination, i.e. diclofenac and WR-2721, the additivity of protective effects is manifested even in the survival of lethally irradiated mice. The results suggest that under suitable conditions avoiding the unfavourable toxic effects, non-steroidal anti-inflammatory drugs can be successfully used with the aim to enhance the efficiency of sulfhydryl radioprotectors. (orig.) [de

  13. Magnetic Ganoderma lucidum spore microspheres: A novel material to immobilize CotA multicopper oxidase for dye decolorization

    International Nuclear Information System (INIS)

    Fan, Lili; Wang, Yan; Zhao, Min; Song, Jinzhu; Wang, Jueyu; Jin, Zijing

    2016-01-01

    Highlights: • Hollow microspheres were obtained from Ganoderma lucidum spores. • Novel magnetic microspheres were prepared by load hollow spore microspheres with Fe_3O_4 nanoparticles. • CotA multicopper oxidase was immobilized on the magnetic spore microspheres for indigo carmine decolorization. • The immobilized CotA displayed higher decolorization capability and reusability. - Abstract: In this study, hollow microspheres were obtained from Ganoderma lucidum spores. Then the hollow microspheres were loaded with Fe_3O_4 nanoparticles to prepare novel magnetic spore microspheres. TEM images and X-ray diffractometry demonstrated that the Fe_3O_4 nanoparticles were incorporated throughout the spore microsphere. CotA multicopper oxidase was chosen as biomacromolecule to study the loading ability of the magnetic spore microspheres. The combination of the CotA enzyme with the microsphere was observed by laser scanning confocal microscope. The loaded amount of CotA on the microspheres was 75 mg/g when the CotA concentration was 1.2 mg/mL and the activity recovery of the immobilized CotA was 81%. The magnetic microspheres loaded with CotA, which can be easily and quickly recovered by an external magnetic field, were used for dye decolorization. After 1 h decolorization, 99% of the indigo carmine has been removed by 10 mg microspheres. In addition, the immobilized CotA retained 75% of activity after 10 consecutive cycles, which indicated that the magnetic spore microspheres are good support material for immobilization of the enzyme.

  14. Comparison of Clinicopathological Characteristics and Outcome of Inflammatory and Non-inflammatory Locally Advanced Breast Cancer: A Study in Iran

    Directory of Open Access Journals (Sweden)

    Saeed Arefanian

    2014-05-01

    Full Text Available Background: Inflammatory breast cancer (IBC, a subgroup of locally advanced breast cancer (LABC, is diagnosed based on clinical findings, and seems to be different from other types of LABC. The purpose of this study was to compare clinicopathological characteristics and outcomes between inflammatory and non-inflammatory LABC patients at Breast Cancer Research Center (BCRC, Tehran, Iran.Methods: The medical records of all patients who were diagnosed as LABC in BCRC  since  1997  to  2011  were  extracted  from  the database. Then,  clinical  and pathological characteristics and overall survival of IBC patients were compared with non-inflammatory LABC (NI-LABC.Results: A total number of 340 patients were identified as LABC from which 17 patients (5% were diagnosed as IBC. Menopausal status, body mass index (BMI, family history of breast cancer, nodal status, and Her2/neu and PR positivity were not statistically different between IBC and NI-LABC groups. The difference in estrogen receptor (ER between the two groups was significant (P = 0.028. Median duration of follow-up was 26.50 months. Patients with IBC had overall survival of 27.9 months (95% CI: 22.7–33.1 which was lower than patients in the NI-LABC group with a survival of 118.9 months (95% CI: 107.3–130.6 (P = 0.015. The difference between the disease-free survivals of the two groups were also statistically significant (P < 0.001.Conclusions: Compared to NI-LABC, IBC is more frequently ER negative and more commonly associated with lower survival rate. These findings reinforce the idea that IBC has a more aggressive biology and more unfavorable outcome than NI-LABC and needs close follow-up. Normal 0 false false false EN-US X-NONE X-NONE

  15. Synthesis and electrochemical properties of {alpha}-MnO{sub 2} microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Wang Hongen [College of Chemistry and Chemical Engineering, Central South University, Changsha 410083 (China); Zhengzhou Research Institute of CHALCO, Zhengzhou Research Institute of Light Metals, Zhengzhou 450041 (China); Qian Dong [College of Chemistry and Chemical Engineering, Central South University, Changsha 410083 (China)], E-mail: qiandong6@yahoo.com.cn

    2008-06-15

    We report the synthesis of {alpha}-MnO{sub 2} microspheres by a low-temperature hydrothermal method involving no templates or catalysts. The products were characterized by powder X-ray diffraction (XRD), scanning electron microscopy (SEM), Energy-dispersive X-ray spectrum (EDX), transmission electron microscopy (TEM), Fourier transform infrared spectrum (FT-IR), and Brunauer-Emmett-Teller (BET). The results show that the as-synthesized products are mainly composed of large quantities of {alpha}-MnO{sub 2} microspheres having a sea-urchin shape and a few microspheres constructed of small nanorods. Electrochemical characterization indicates that the resulting {alpha}-MnO{sub 2} microspheres display promising discharge properties than the commercial electrolytic manganese dioxides (EMD) when used as cathodes in alkaline Zn-MnO{sub 2} batteries.

  16. Release of proteins via ion exchange from albumin-heparin microspheres

    NARCIS (Netherlands)

    Kwon, Glen S.; Bae, You Han; Cremers, H.F.M.; Cremers, Harry; Feijen, Jan; Kim, Sung Wan

    1992-01-01

    Albumin-heparin and albumin microspheres were prepared as ion exchange gels for the controlled release of positively charged polypeptides and proteins. The adsorption isotherms of chicken egg and human lysozyme, as model proteins, on microspheres were obtained. An adsorption isotherm of chicken egg

  17. The effect of non-steroidal anti-inflammatory drugs on the metabolism of 14C-arachidonic acid by human gingival tissue in vitro

    International Nuclear Information System (INIS)

    Elattar, T.M.; Lin, H.S.; Tira, D.E.

    1983-01-01

    We investigated the effect of non-steroidal anti-inflammatory drugs on prostaglandins (PGs) and 12-hydroxyeicosatetraenoic acid (12-HETE) formation by inflamed human gingival tissues. Gingival tissue homogenates were incubated with 14 C-arachidonic acid in the presence of indomethacin, piroxicam, or ibuprofen, and the organic solvent extracts were chromatographed on silica gel plates with standards for radiometric assay. There was a significant negative trend between the doses (10(-7)-10(-3) M) of each of indomethacin, piroxicam, and ibuprofen, and the amounts of PGF2 alpha, PGE2, PGD2, and 15-keto-PGE2 produced. All three drugs have a significant inhibitory effect on PGs and 12-HETE production at 10(-3) M when compared with the control. The rank order effectiveness of the drugs, at 10(-3) M, on PG inhibition was indomethacin greater than piroxicam greater than ibuprofen, and on 12-HETE inhibition was indomethacin greater than ibuprofen greater than piroxicam

  18. Preparation of polymethacrylic acid-grafted HEMA/PVP microspheres and preliminary study on basic protein adsorption.

    Science.gov (United States)

    Gao, Baojiao; Hu, Hongyan; Guo, Jianfeng; Li, Yanbin

    2010-06-01

    The crosslinked copolymeric microspheres (HEMA/NVP) of N-vinylpyrrolidone (NVP) and 2-hydroxyethyl methacrylate (HEMA) were prepared using inverse suspension polymerization method. Subsequently, the reaction of methacryloyl chloride with the hydroxyl groups on the surfaces of HEMA/NVP microspheres was performed, leading to the introduction of polymerisable double bonds onto the surfaces of microspheres HEMA/NVP. Afterward, methacrylic acid was allowed to be graft-polymerized on microspheres HEMA/NVP in the manner of "grafting from", resulting in the grafted microspheres PMAA-HEMA/NVP. The grafted microspheres PMAA-HEMA/NVP were fully characterized with several means. The graft-polymerization of MAA on microspheres HEMA/NVP was studied in detail, and the optimal reaction conditions were determined. Thereafter, the adsorption property of the grafted microspheres PMAA-HEMA/NVP for lysozyme as a basic protein model was preliminarily examined to explore the feasibility of removing deleterious basic protein such as density lipoprotein from blood. The experimental results indicate that the PMAA grafting degree on microspheres HEMA/NVP is limited because an enwinding polymer layer as a kinetic barrier on the surfaces of HEMA/NVP microspheres will be formed during the graft-polymerization, and block the graft-polymerization. In order to enhance PMAA grafting degree, reaction temperature, monomer concentration and the used amount of initiator should be effectively controlled. The experimental results also reveal that the grafted microspheres PMAA-HEMA/NVP possess very strong adsorption ability for lysozyme by right of strong electrostatic interaction. Copyright 2010 Elsevier B.V. All rights reserved.

  19. In-vitro studies of enteric coated diclofenac sodium-carboxymethylcellulose microspheres.

    Science.gov (United States)

    Arica, B; Arica, M Y; Kaş, H S; Hincal, A A; Hasirci, V

    1996-01-01

    MIcrospheres containing diclofenac sodium (DS) were prepared using carboxymethylcellulose (CMC) as the main support material (1.0, 2.0, 3.0% (w/v)) and aluminum chloride as the crosslinker. Drug to polymer ratios of 1:1, 1:2 and 1:4 were used to obtain a range of microspheres. The microspheres were then coated with an enteric coating material, Eudragit S-100, efficiency, % yield value, particle sizes an in-vitro dissolution behaviour were investigated. The surface of the enteric coated microspheres seemed to be all covered with Eudragit S-100 from scanning electron microscopy observation. It was also observed that increasing the CMC concentration led to an increase in the encapsulation efficiency, % yield value and particle size and decreased the release rate. Eudragit S-100 coating did not significantly alter the size but the release rate was significantly lower even when the lower concentration solution was used.

  20. Biomimetic composite microspheres of collagen/chitosan/nano-hydroxyapatite: In-situ synthesis and characterization.

    Science.gov (United States)

    Teng, Shu-Hua; Liang, Mian-Hui; Wang, Peng; Luo, Yong

    2016-01-01

    The collagen/chitosan/hydroxyapatite (COL/CS/HA) composite microspheres with a good spherical form and a high dispersity were successfully obtained using an in-situ synthesis method. The FT-IR and XRD results revealed that the inorganic phase in the microspheres was crystalline HA containing carbonate ions. The morphology of the composite microspheres was dependent on the HA content, and a more desirable morphology was achieved when 20 wt.% HA was contained. The composite microspheres exhibited a narrow particle distribution, most of which ranged from 5 to 10 μm. In addition, the needle-like HA nano-particles were uniformly distributed in the composite microspheres, and their crystallinity and crystal size decreased with the HA content. Copyright © 2015 Elsevier B.V. All rights reserved.

  1. Electroacupuncture Inhibits the Activation of p38MAPK in the Central Descending Facilitatory Pathway in Rats with Inflammatory Pain

    Directory of Open Access Journals (Sweden)

    Man-Li Hu

    2017-01-01

    Full Text Available The mitogen-activated protein kinases (MAPKs, especially p38MAPK, play a pivotal role in chronic pain. Electroacupuncture (EA relieves inflammatory pain underlying the descending pathway, that is, the periaqueductal gray (PAG, the rostral ventromedial medulla (RVM, and the spinal cord dorsal horn (SCDH. However, whether EA antagonizes inflammatory pain through regulation of p38MAPK in this descending facilitatory pathway is unclear. Complete Freund’s adjuvant (CFA was injected into the hind paw of rats to establish inflammatory pain model. EA was administrated for 30 min at Zusanli and Kunlun acupoints at 0.5, 24.5, 48.5, and 72.5 h, respectively. The paw withdrawal threshold (PWT, paw edema, and Phosphor-p38MAPK-Immunoreactivity (p-p38MAPK-IR cells were measured before (0 h and at 1, 3, 5, 7, 25, and 73 h after CFA or saline injection. EA increased PWT at 1, 3, 25, and 73 h and inhibited paw edema at 25 and 73 h after CFA injection. Moreover, the increasing number of p-p38MAPK-IR cells which was induced by CFA was suppressed by EA stimulation in PAG and RVM at 3 and 5 h and in SCDH at 5, 7, 25, and 73 h. These results suggest that EA suppresses inflammation-induced hyperalgesia probably through inhibiting p38MAPK activation in the descending facilitatory pathway.

  2. Non-pharmacological interventions for preventing job loss in workers with inflammatory arthritis

    NARCIS (Netherlands)

    Hoving, Jan L.; Lacaille, Diane; Urquhart, Donna M.; Hannu, Timo J.; Sluiter, Judith K.; Frings-Dresen, Monique H. W.

    2014-01-01

    Work participation of patients with inflammatory arthritis (IA) is important not only economically but also for physical and psychological health. There is no Cochrane Review to date on studies of non-pharmacological interventions specifically aimed at preventing job loss in people with IA. To

  3. A sonochemical route for the encapsulation of drug in magnetic microspheres

    International Nuclear Information System (INIS)

    Wu Shixi; Jiang Wei; Zhang Xiaojuan; Sun Huan; Zhang Wenyao; Dai Junjun; Liu Li; Chen Xiaolong; Li Fengsheng

    2012-01-01

    This study focused on the preparation and characterization of magnetic targeted antibiotic microspheres (MTAMs). MTAMs were prepared by a sonochemical method in the presence of hydrophobic Fe 3 O 4 nanoparticles and tetracycline. The properties of MTAMs were characterized by transmission electron microscopy, Fourier-transform infrared spectrum, thermogravimetric analysis, vibration sample magnetometry, and bacteriostatic experiment. The results indicated that the superparamagnetic microspheres have ultrafine size (below 230 nm), high saturation magnetization (80.90 emu/g), high biocompatibility, biodegradability, controlled-release, and antibiotic effect. It has been proved that MTAMs can carry out the function of magnetic targeted drugs delivery system by putting together magnetic materials and antibiotics. The possible formation mechanism of MTAMs was also discussed. In summary, MTAMs had potential in medical imaging, drug targeting, and catalysis. - Highlights: → Microspheres carry out the function of magnetic targeted drugs delivery system. → Microspheres exhibit high saturation magnetization and antibiotic effect. → Microspheres have a potential application in the biomedical field. → The sonochemical method is well controlled for the synthesis.

  4. Preparation and photocatalytic activity of hollow ZnSe microspheres via Ostwald ripening

    International Nuclear Information System (INIS)

    Zhang Lihui; Yang Heqing; Xie Xiaoli; Zhang Fenghua; Li Li

    2009-01-01

    Hollow ZnSe microspheres were prepared via a facile hydrothermal reaction of Zn(AC) 2 .2H 2 O with Na 2 SeO 3 and ethylene glycol in NaOH solution at 180 deg. C for 12 h. The products were characterized by means of X-ray diffraction, scanning electron microscopy, transmission electron microscopy and Raman spectrum. The hollow microspheres with the diameters of about 2 μm are constructed from ZnSe nanoparticles with the cubic zinc blende structure, the size of hollow interiors and constituent ZnSe nanodots can be tuned by changing the reaction time. The hollow microspheres are formed via an Ostwald ripening process. Photoluminescence and photocatalytic activity of the hollow ZnSe microspheres were studied at room temperature. The results indicate that the hollow microspheres constructed from ZnSe nanoparticles display a strong near-band edge emission at 479 nm and a very weak deep defect (DD) related emission at 556 nm and a high photocatalytic activity in the photodegradation of methyl orange. The photodegradation of methyl orange catalyzed by the ZnSe microspheres is a pseudo first-order reaction

  5. Behaviour of (Th, U)O2 microspheres under compression tests and pelletization

    International Nuclear Information System (INIS)

    Ferreira, R.A.N.

    1982-12-01

    The interrelation between the behaviour of isolated microspheres in compression tests and the microstructure of sintered pellets obtained with these microspheres, was investigated. Various batches of (Th, 5 w/o U)O 2 microspheres were produced applying the so-called gel process. The production parameters were diversified both as to the composition and to the heat treatments. The resulting products underwent compression tests in an universal tension and compression machine as single microspheres and, as bulk material, were compacted and sintered. The results of the compression tests revealed the existence of two distinct classes of fragmentation behaviour. Each of these classes causes a distinct behaviour during the pelletization, too, resulting in fuel pellets with quite different microstructures. It was evidenced that there is a relationship between these differences in the microstructure and the behaviour of the single microspheres in the compression test. (Author) [pt

  6. Preparation of hydroxypropyl cyclosophoraose/dextran microspheres for the controlled release of ciprofloxacin

    International Nuclear Information System (INIS)

    Lee, Benel; Jeong, Da Ham; Joo, Sang Woo; Choi, Jae Min; Jung, Seung Ho; Cho, Eun Na; Lee, Jae Yung; Park, Se Yeon

    2016-01-01

    Hydroxypropyl cyclosophoraose/dextran (HPCys/dextran) microspheres were prepared using an emulsion polymerization method for use as drug carriers to achieve the controlled release of a poorly water-soluble antibacterial drug, ciprofloxacin (CFX). Cyclosophoraoses are cyclic (1 → 2)-β-d-glucans isolated from the Rhizobium species. Characteristics of HPCys/dextran microspheres were investigated using Fourier transform infrared analysis, solid-state 13C nuclear magnetic resonance spectroscopy, and field emission scanning electron microscopy. The amount of CFX released from these microspheres at pH 7.4 (intestinal phase pH) was about two times higher than that released at pH 1.2 (gastric phase pH). Furthermore, HPCys/dextran microspheres did not show any toxicity in human embryonic kidney cells. We propose that HPCys/dextran microspheres could be used as an effective pH-dependent release system for poorly water-soluble drugs such as CFX

  7. Preparation of hydroxypropyl cyclosophoraose/dextran microspheres for the controlled release of ciprofloxacin

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Benel; Jeong, Da Ham; Joo, Sang Woo; Choi, Jae Min; Jung, Seung Ho; Cho, Eun Na [Center for Biotechnology Research in UBITA (CBRU), Konkuk University, Seoul (Korea, Republic of); Lee, Jae Yung [Dept. Biological Science, Mokpo National University, Mokpo (Korea, Republic of); Park, Se Yeon [Dept. Applied Chemistry, Dongduk Women' s University, Seoul (Korea, Republic of)

    2016-12-15

    Hydroxypropyl cyclosophoraose/dextran (HPCys/dextran) microspheres were prepared using an emulsion polymerization method for use as drug carriers to achieve the controlled release of a poorly water-soluble antibacterial drug, ciprofloxacin (CFX). Cyclosophoraoses are cyclic (1 → 2)-β-d-glucans isolated from the Rhizobium species. Characteristics of HPCys/dextran microspheres were investigated using Fourier transform infrared analysis, solid-state 13C nuclear magnetic resonance spectroscopy, and field emission scanning electron microscopy. The amount of CFX released from these microspheres at pH 7.4 (intestinal phase pH) was about two times higher than that released at pH 1.2 (gastric phase pH). Furthermore, HPCys/dextran microspheres did not show any toxicity in human embryonic kidney cells. We propose that HPCys/dextran microspheres could be used as an effective pH-dependent release system for poorly water-soluble drugs such as CFX.

  8. PLGA and PHBV Microsphere Formulations and Solid-State Characterization

    DEFF Research Database (Denmark)

    Yang, Chiming; Plackett, David; Needham, David

    2009-01-01

    To develop and characterize the solid-state properties of poly(DL-lactic-co-glycolic acid) (PLGA) and poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) (PHBV) microspheres for the localized and controlled release of fusidic acid (FA). The effects of FA loading and polymer composition on the me...... of a DCM-FA-rich phase in the forming microsphere....

  9. A novel approach to preparing magnetic protein microspheres with core-shell structure

    Science.gov (United States)

    Jiang, Wei; Sun, Zhendong; Li, Fengsheng; Chen, Kai; Liu, Tianyu; Liu, Jialing; Zhou, Tianle; Guo, Rui

    2011-03-01

    Magnetic protein microspheres with core-shell structure were prepared through a novel approach based on the sonochemical method and the emulsion solvent evaporation method. The microspheres are composed of the oleic acid and undecylenic acid modified Fe 3O 4 cores and coated with globular bovine serum albumin (BSA). Under an optimized condition, up to 57.8 wt% of approximately 10 nm superparamagnetic Fe 3O 4 nanoparticles could be uniformly encapsulated into the BSA microspheres with the diameter of approximately 160 nm and the high saturation magnetization of 38.5 emu/g, besides of the abundant functional groups. The possible formation mechanism of magnetic microspheres was discussed in detail.

  10. CO2-assisted high pressure homogenization: a solvent-free process for polymeric microspheres and drug-polymer composites.

    Science.gov (United States)

    Kluge, Johannes; Mazzotti, Marco

    2012-10-15

    The study explores the enabling role of near-critical CO(2) as a reversible plasticizer in the high pressure homogenization of polymer particles, aiming at their comminution as well as at the formation of drug-polymer composites. First, the effect of near-critical CO(2) on the homogenization of aqueous suspensions of poly lactic-co-glycolic acid (PLGA) was investigated. Applying a pressure drop of 900 bar and up to 150 passes across the homogenizer, it was found that particles processed in the presence of CO(2) were generally of microspherical morphology and at all times significantly smaller than those obtained in the absence of a plasticizer. The smallest particles, exhibiting a median x(50) of 1.3 μm, were obtained by adding a small quantity of ethyl acetate, which exerts on PLGA an additional plasticizing effect during the homogenization step. Further, the study concerns the possibility of forming drug-polymer composites through simultaneous high pressure homogenization of the two relevant solids, and particularly the effect of near-critical CO(2) on this process. Therefore, PLGA was homogenized together with crystalline S-ketoprofen (S-KET), a non-steroidal anti-inflammatory drug, at a drug to polymer ratio of 1:10, a pressure drop of 900 bar and up to 150 passes across the homogenizer. When the process was carried out in the presence of CO(2), an impregnation efficiency of 91% has been reached, corresponding to 8.3 wt.% of S-KET in PLGA; moreover, composite particles were of microspherical morphology and significantly smaller than those obtained in the absence of CO(2). The formation of drug-polymer composites through simultaneous homogenization of the two materials is thus greatly enhanced by the presence of CO(2), which increases the efficiency for both homogenization and impregnation. Copyright © 2012 Elsevier B.V. All rights reserved.

  11. Magnetic Ganoderma lucidum spore microspheres: A novel material to immobilize CotA multicopper oxidase for dye decolorization

    Energy Technology Data Exchange (ETDEWEB)

    Fan, Lili [School of Chemistry and Chemical Engineering, Harbin Institute of Technology, Harbin 150001 (China); Wang, Yan, E-mail: wangy_msn@hit.edu.cn [School of Chemistry and Chemical Engineering, Harbin Institute of Technology, Harbin 150001 (China); Zhao, Min [College of Life Science, Northeast Forestry University, Harbin 150040 (China); Song, Jinzhu [School of Life Science and Technology, Harbin Institute of Technology, Harbin 150001 (China); Wang, Jueyu; Jin, Zijing [College of Life Science, Northeast Forestry University, Harbin 150040 (China)

    2016-08-05

    Highlights: • Hollow microspheres were obtained from Ganoderma lucidum spores. • Novel magnetic microspheres were prepared by load hollow spore microspheres with Fe{sub 3}O{sub 4} nanoparticles. • CotA multicopper oxidase was immobilized on the magnetic spore microspheres for indigo carmine decolorization. • The immobilized CotA displayed higher decolorization capability and reusability. - Abstract: In this study, hollow microspheres were obtained from Ganoderma lucidum spores. Then the hollow microspheres were loaded with Fe{sub 3}O{sub 4} nanoparticles to prepare novel magnetic spore microspheres. TEM images and X-ray diffractometry demonstrated that the Fe{sub 3}O{sub 4} nanoparticles were incorporated throughout the spore microsphere. CotA multicopper oxidase was chosen as biomacromolecule to study the loading ability of the magnetic spore microspheres. The combination of the CotA enzyme with the microsphere was observed by laser scanning confocal microscope. The loaded amount of CotA on the microspheres was 75 mg/g when the CotA concentration was 1.2 mg/mL and the activity recovery of the immobilized CotA was 81%. The magnetic microspheres loaded with CotA, which can be easily and quickly recovered by an external magnetic field, were used for dye decolorization. After 1 h decolorization, 99% of the indigo carmine has been removed by 10 mg microspheres. In addition, the immobilized CotA retained 75% of activity after 10 consecutive cycles, which indicated that the magnetic spore microspheres are good support material for immobilization of the enzyme.

  12. The Sirt1 activator SRT1720 attenuates angiotensin II-induced atherosclerosis in apoE{sup −/−} mice through inhibiting vascular inflammatory response

    Energy Technology Data Exchange (ETDEWEB)

    Chen, Yi xi; Zhang, Man; Cai, Yuehua; Zhao, Qihui; Dai, Wenjian, E-mail: wjdai@126.com

    2015-10-02

    Activation of the silent mating type information regulation 2 homolog 1 (SIRT1) has been shown consistent antiinflammatory function. However, little information is available on the function of SIRT1 during Angiotensin II (AngII)-induced atherosclerosis. Here we report atheroprotective effects of sirt1 activation in a model of AngII-accelerated atherosclerosis, characterized by suppression pro-inflammatory transcription factors Nuclear transcription factor (NF)-κB and Signal Transducers and Activators of Transcription. (STAT) signaling pathway, and atherosclerotic lesion macrophage content. In this model, administration of the SIRT1 agonist SRT1720 substantially attenuated AngII-accelerated atherosclerosis with decreasing blood pressure and inhibited NF-κB and STAT3 activation, which was associated with suppression of inflammatory factor and atherogenic gene expression in the artery. In vitro studies demonstrated similar changes in AngII-treated VSMCs and macrophages: SIRT1 activation inhibited the expression levels of proinflammatory factor. These studies uncover crucial proinflammatory mechanisms of AngII and highlight actions of SIRT1 activation to inhibit AngII signaling, which is atheroprotective. - Highlights: • SRT1720 reduced atherosclerotic lesion size in aortic arches and atherosclerotic lesion macrophage content. • SRT1720 could inhibit the phosphorylation of STAT3 and p65 phosphorylation and translocation. • SRT1720 could inhibit the expression of proinflammatory factor.

  13. Carbidopa/levodopa-loaded biodegradable microspheres: in vivo evaluation on experimental Parkinsonism in rats.

    Science.gov (United States)

    Arica, Betül; Kaş, H Süheyla; Moghdam, Amir; Akalan, Nejat; Hincal, A Atilla

    2005-02-16

    The purpose of this study was to prepare and characterize injectable carbidopa (CD)/levodopa (LD)-loaded Poly(L-lactides) (L-PLA), Poly(D,L-lactides) (D,L-PLA) and Poly(D,L-lactide-co-glycolide) (PLAGA) microspheres for the intracerebral treatment of Parkinson's disease. The microspheres were prepared by solvent evaporation method. The polymers' (L-PLA, D,L-PLA and PLAGA) concentrations were 10% (w/w) in the organic phase; the emulsifiers [sodium carboxymethylcellulose (NaCMC):sodium oleate (SO) and Polyvinyl alcohol (PVA):SO mixture (4:1 w/v)] concentrations were 0.75% in the aqueous phase. Microspheres were analyzed for morphological characteristics, size distribution, drug loading and in vitro release. The release profile of CD/LD from microspheres was characterized in the range of 12-35% within the first hour of the in vitro release experiment. The efficiency of CD- and LD-encapsulated microspheres to striatal transplantation and the altering of apomorphine-induced rotational behavior in the 6-hydroxydopamine (6-OHDA) unilaterally lesioned rat model were also tested. 6-OHDA/CD-LD-loaded microsphere groups exhibited lower rotation scores than 6-OHDA/Blank microsphere groups as early as 1 week postlesion. These benefits continued throughout the entire experimental period and they were statistically significant during the 1, 2 and 8 weeks (p<0.05). CD/LD-loaded microspheres were specifically prepared to apply as an injectable dosage forms for brain implantation.

  14. Fracture properties and heat resistance of ceramics consisting of microspheres of stabilized zirconium dioxide

    International Nuclear Information System (INIS)

    Krasulin, Yu.L.; Barinov, S.M.; Ivanov, A.B.; Timofeev, V.N.; Grevtsev, S.N.; Ivanov, D.A.

    1980-01-01

    Determined were effective specific fracture work, critical coefficient of stress intensity in the upper point of the fracture, strength and heat resistance during heat changes (20-1300 deg C) of the material produced by sintering stabilized zirconium dioxide microspheres. Dependence of these characteristics on granulometric composition of microspheres was determined. It was ascertained that the additional introduction of large microspheres into the bulk of small microspheres increased the metal fracture work. Specific work of material fracture progress exceeded specific work of fracture motion initiation. High value of fracture work together with high strength permits to use the material formed of microspheres as structural ceramics

  15. Non-steroidal anti-inflammatory drug use and risk of endometrial cancer

    DEFF Research Database (Denmark)

    Verdoodt, Freija; Friis, Søren; Dehlendorff, Christian

    2016-01-01

    OBJECTIVE: Non-steroidal anti-inflammatory drug (NSAID) use has been linked to a reduction in the risk of several cancer types. For endometrial cancer, however, results have been inconsistent. To summarize the available evidence on the risk of endometrial cancer associated with use of aspirin...... a random effects model. RESULTS: Six case-control and seven cohort studies were found eligible for our meta-analysis. We observed risk reductions in endometrial cancer associated with regular use of aspirin (case-control: 11%, cohort: 8%) and NA-NSAIDs (case-control: 9%, cohort: 6%), compared to non...

  16. Comparison of gas clearance and radioactive microspheres for pancreatic blood flow measurement

    International Nuclear Information System (INIS)

    DeMar, A.R.; Graham, L.S.; Lake, R.; Fink, A.S.

    1989-01-01

    Measurement of pancreatic blood flow (PBF) is technically demanding. Although radiolabeled microspheres are considered the gold standard for PBF assessment, they have practical limitations. In the current study, H 2 and xenon-133 gas clearance techniques were adapted to PBF measurement and compared to radiolabeled microsphere techniques. Simultaneous measurements of PBF were made using either hydrogen or xenon gas washout and radiolabeled microspheres. Measurements were made under basal, vasoconstricted (vasopressin 2U i.v. or nicotine 4 micrograms/kg/h) and stimulated (secretin 125 ng/kg/h or 2 U/kg i.v.) conditions (random order). Mean PBF was 26.9 +/- 5.3, 50.5 +/- 2.3 and 27.6 +/- 5.2 ml/min/100 g basally, 36.9 +/- 8.0, 90.1 +/- 18.9, and 81.7 +/- 14.5 ml/min/100 g in the stimulated state, and 24.2 +/- 7.8, 25.0 +/- 3.5, and 14.9 +/- 7.5 ml/min/100 g in the vasoconstricted state for hydrogen gas clearance, xenon gas clearance, and radiolabeled microspheres, respectively. The H 2 clearance technique resulted in tissue trauma, was complicated by frequent electrode displacement, and correlated poorly (r2 = 0.36, p greater than 0.05) with microsphere values. In contrast, xenon clearance measurement had no apparent effect on the pancreas and correlated well (r2 = 0.83, p less than 0.01) with microsphere data. We conclude that xenon clearance offers an attractive, validated alternative to radiolabeled microspheres for measuring pancreatic blood flow

  17. Preparation and characterization of gelatin–hydroxyapatite composite microspheres for hard tissue repair

    International Nuclear Information System (INIS)

    Chao, Shao Ching; Wang, Ming-Jia; Pai, Nai-Su; Yen, Shiow-Kang

    2015-01-01

    Gelatin–hydroxyapatite composite microspheres composed of 21% gelatin (G) and 79% hydroxyapatite (HA) with uniform morphology and controllable size were synthesized from a mixed solution of Ca(NO 3 ) 2 , NH 4 H 2 PO 4 and gelatin by a wet-chemical method. Material analyses such as X-ray diffraction (XRD), scanning/transmission electron microscopy examination (SEM/TEM) and inductively coupled plasma-mass spectroscopy (ICP-MS) were used to characterize G–HA microspheres by analyzing their crystalline phase, microstructure, morphology and composition. HA crystals precipitate along G fibers to form nano-rods with diameters of 6–10 nm and tangle into porous microspheres after blending. The cell culture indicates that G–HA composite microspheres without any toxicity could enhance the proliferation and differentiation of osteoblast-like cells. In a rat calvarial defect model, G–HA bioactive scaffolds were compared with fibrin glue (F) and Osteoset® Bone Graft Substitute (OS) for their capacity of regenerating bone. Four weeks post-implantation, new bone, mineralization, and expanded blood vessel area were found in G–HA scaffolds, indicating greater osteoconductivity and bioactivit