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Sample records for dextran microsphere formulation

  1. Preclinical and Clinical In Vitro In Vivo Correlation of an hGH Dextran Microsphere Formulation

    OpenAIRE

    2007-01-01

    Purpose To investigate the in vitro in vivo correlation of a sustained release formulation for human growth hormone (hGH) based on hydroxyethyl methacrylated dextran (dex-HEMA) microspheres in Pit-1 deficient Snell dwarf mice and in healthy human volunteers. Materials and Methods A hGH-loaded microsphere formulation was developed and tested in Snell dwarf mice (pharmacodynamic study) and in healthy human volunteers (pharmacokinetic study). Results Single subcutaneous administration of the mic...

  2. Preclinical and Clinical In Vitro In Vivo Correlation of an hGH Dextran Microsphere Formulation

    Science.gov (United States)

    de Vrueh, R.; Gresnigt, M. G.; Hoogerbrugge, C. M.; van Buul-Offers, S. C.; de Leede, L. G. J.; Sterkman, L. G. W.; Crommelin, D. J. A.; Hennink, W. E.; Verrijk, R.

    2007-01-01

    Purpose To investigate the in vitro in vivo correlation of a sustained release formulation for human growth hormone (hGH) based on hydroxyethyl methacrylated dextran (dex-HEMA) microspheres in Pit-1 deficient Snell dwarf mice and in healthy human volunteers. Materials and Methods A hGH-loaded microsphere formulation was developed and tested in Snell dwarf mice (pharmacodynamic study) and in healthy human volunteers (pharmacokinetic study). Results Single subcutaneous administration of the microspheres in mice resulted in a good correlation between hGH released in vitro and in vivo effects for the hGH-loaded microsphere formulation similar to daily injected hGH indicating a retained bioactivity. Testing the microspheres in healthy volunteers showed an increase (over 7–8 days) in hGH serum concentrations (peak concentrations: 1–2.5 ng/ml). A good in vitro in vivo correlation was obtained between the measured and calculated (from in vitro release data) hGH serum concentrations. Moreover, an increased serum concentration of biomarkers (insulin-like growth factor-I (IGF-I), IGF binding protein-3 (IGFBP-3) was found again indicating that bioactive hGH was released from the microspheres. Conclusions Good in vitro in vivo correlations were obtained for hGH-loaded dex-HEMA microspheres, which is an important advantage in predicting the effect of the controlled drug delivery product in a clinical situations. PMID:17929148

  3. Dextran-based microspheres as controlled delivery systems for proteins

    NARCIS (Netherlands)

    Vlugt-Wensink, K.D.F.

    2007-01-01

    Dextran-based microspheres as controlled delivery systems for proteins Dextran based microspheres are investigated as controlled delivery system for proteins. Microspheres were prepared by polymerization of dex-HEMA in an aqueous two-phase system of dex-HEMA and PEG. Protein loaded microspheres are

  4. PREPARATION AND ADSORBABILITY OF DEXTRAN MICROSPHERES WITH UNIFORM DIAMETER

    Institute of Scientific and Technical Information of China (English)

    Ri-sheng Yao; Wen-xia Gao; Jing Sun; Ya-hua You

    2005-01-01

    The method of preparing uniform dextran microspheres with a narrow diameter distribution was introduced and the adsorbability of these microspheres was evaluated. The microspheres were prepared in W/O microemulsion using 0.5% dextran solution as the aqueous phase and n-hexane as the oil phase. Characteristics of the prepared dextran microspheres were examined with laser light blocking technique, optical microscope and ultraviolet spectrometer. The results show that the prepared dextran microspheres have uniform morphology and narrow diameter distribution, nearly 92% of them having a diameter of 56.6 μm. In vitro evaluation of adsorbability, wet dextran microspheres have good adsorption of 98.32 mg/g of model drug methylene blue in 20.86 mg/L methylene blue solution at 25℃. The adsorption of dried dextran microspheres under the same condition is 132.15 mg/g, which is even higher. And the adsorbability of dextran microspheres has significant relationship with the concentration of methylene blue and temperature. The adsorbability is better at lower temperature and higher concentration of methylene blue.

  5. Dextran Microsphere Hepatic Artery Embolization for Hepatoma: Pathological Assessment of Its Efficacy in Resected Cases

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Objective To evaluate the therapeutic effect and the mechanism of dextran microsphere hepatic artery embolization for hepatoma. Methods Partial hepatectomy was performed in 11 patients with hepatoma pretreated with dextran microsphere hepatic artery embolization. All specimens were for histopathologic studies in order to observe the destiny of dextran microspheres and necrotic degree of the tumor. Results complete necrosis of the tumor was found in seven cases and incomplete necrosis of the tumor in the rest 4. Tumors in the later were near to areas rich in arterial collateral anastomoses. The extent of tumor necrosis was unrelated to the presence and thickness of tumor capsule and capsular invasions. Dextran microspheres could cause permanent embolization of distal arterioles. The microspheres were very biocompatible and cause little foreign body reaction. No inflammatory changes were seen both inside and outside of the embolized artery 191 days after embolization. Dextran microspheres were not absorbed and the vessel recanalization was also not seen. Dextran microsphere was not found in portal veins. Conclusion Some hepatomas distant from the collateral circulation of arteries could be cured with dextran microsphere hepatic artery embolization alone.

  6. 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.

  7. Preparation and Characterization of Quaternized Chitosan Coated Alginate Microspheres for Blue Dextran Delivery

    Directory of Open Access Journals (Sweden)

    Kuo-Yu Chen

    2017-06-01

    Full Text Available In this study, 2-[(Acryloyloxyethyl]trimethylammonium chloride was graft polymerized onto chitosan (CS to form quaternary ammonium CS (QAC by using ammonium persulfate as a redox initiator. Alginate (ALG microspheres loaded with a water-soluble macromolecular model drug, blue dextran (BD, were obtained by corporation of coaxial gas-flow method and ionic gelation process. CS and QAC were then coated on the surfaces of ALG microspheres to generate core/shell structured CS/ALG and QAC/ALG microspheres, respectively. The experiment result showed that QAC/ALG microspheres had a smaller particle size due to the stronger electrostatic interactions between QAC and ALG molecules. In vitro drug release studies at pH 7.4 and pH 9.0 exhibited that the release rate of BD was significantly decreased after ALG microspheres coating with CS and QAC. Moreover, ALG microspheres coated with QAC showed a prolonged release profile for BD at pH 9.0. Therefore, QAC/ALG microspheres may be a promising hydrophilic macromolecular drug carrier for a prolonged and sustained delivery.

  8. Immunoadjuvant potential of cross-linked dextran microspheres mixed with chitosan nanospheres encapsulated with tetanus toxoid.

    Science.gov (United States)

    Pirouzmand, Haniyeh; Khameneh, Bahman; Tafaghodi, Mohsen

    2017-12-01

    Nasal mucosa is a desirable route for mucosal vaccine delivery. Mucosal co-administration of chitosan nanoparticles with absorption enhancers such as cross-linked dextran microspheres (CDM, Sephadex(®)) is a promising antigen delivery system. In the current study, the chitosan nanospheres loaded with tetanus toxoid (CHT:TT NPs) was prepared and characterized. The immune responses against tetanus toxoid after nasal administration of CHT:TT NPs alone or mixed with CDM were also determined. Chitosan nanospheres were prepared by ionic gelation method. Particle size, releasing profile and antigen stability were evaluated by dynamic light scattering, diffusion chamber and SDS-PAGE methods, respectively. Rabbits were nasally immunized with different formulations loaded with 40 Lf TT. After three times immunizations with 2 weeks intervals, sera IgG titres and nasal lavage sIgA titres were determined. Mean size of CHT NPs and CHT:TT NPs were 205 ± 42 nm and 432 ± 85 nm, respectively. The release profile showed that 42.4 ± 10.5% of TT was released after 30 min and reached to a steady state after 1.5 h. Stability of encapsulated TT in nanospheres was confirmed by SDS-PAGE. The antibody titres showed that CHT:TT NPs-induced antibody titres were higher than TT solution. CHT NPs mixed with CDM induced the systemic IgG and nasal lavage sIgA titres higher than intranasal administration of TT solution (p < 0.001). As the results indicated, these CHT:TT NPs when co-administered with CDM were able to induce more immune responses and have the potential to be used in mucosal immunization.

  9. Formulation, optimization and evaluation of sustained release microsphere of ketoprofen

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    V Chirag Prajapati

    2012-01-01

    Full Text Available The objective of this study is to formulate ketoprofen loaded microspheres of Acrycoat S100 by an o/w emulsion solvent evaporation method. It potently inhibits the enzyme cyclooxygenase resulting in prostaglandin synthesis inhibition. Ketoprofen causes an irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. The half-life in plasma is about 1-2hrs. This makes ketoprofen a very good candidate for the formulation of controlled release dosage forms. Ketoprofen microspheres help to protect the gastric mucous membrane from drug irritation and to mask its taste. The prepared microspheres were evaluated for micromeritic properties, particle size, effect of surfactant concentration, percentage yield, incorporation efficiency, drug polymer compatibility (IR and DSC study, scanning electron microscopy and in vitro drug release. The microspheres produced exhibited good encapsulation efficiencies and micromeritic properties. Encapsulation efficiency of microsphere is around 78%. The mean diameters of microspheres were found in required micrometer range. The results of optimized formulations showed a narrow size distribution and smooth surface. The DSC and the FTIR analysis showed the absence of any potent incompatibility between the drug and the polymer. In-vitro release showed 86.4% drug release after 12 hours. Results of present study suggest that Acrycoat S100 loaded microsphere of ketoprofen can be successfully designed to develop sustained drug delivery system. The solvent evaporation method is a suitable technique for the preparation of Acrycoat S100 microspheres for controlling the release of Ketoprofen for a prolonged duration.

  10. Preparation of recombinant human bone morphogenetic protein-2 loaded dextran-based microspheres and their characteristics

    Institute of Scientific and Technical Information of China (English)

    Fa-ming CHEN; Zhi-fen WU; Qin-tao WANG; Hong WU; Yong-jie ZHANG; Xin NIE; Yan JIN

    2005-01-01

    Aim: To prepare new pharmaceutical forms with sustained delivery properties of recombinant human bone morphogenetic protein-2 (rhBMP2) for tissue engineering and guided tissue regeneration (GTR) use. Methods: rhBMP2-1oaded dextranbased hydrogel microspheres (rhBMP2-MPs), which aimed to keep rhBMP2 bioactivity and to achieve long-term sustained release of rhBMP2, were prepared by double-phase emulsified condensation polymerization. The physical, chemical performances and biological characteristics of those microspheres were studied both in vitro and in vivo. Results: The microspheres' average diameter was 30.33±4.32 μm with 75.4% ranging from 20 μm to 40 μm and the drug loading and encapsulation efficiency were 7.82% and 82.25%, respectively. The rhBMP2-releasing profiles in vitro showed that rhBMP2 release could be maintained more than 10 d. The rhBMP2-MPs, with good swelling and biodegradation behavior,could be kept for 6 months at below 4 ℃ without significant characteristic change or bioactivity loss. Cytology studies showed that rhBMP2-MPs could promote the proliferation of periodontal ligament cells (PDLCs) approximately 10 d, while the bioactivity of concentrated rhBMP2 solution could keep no more than 3 d.Scanning electron microscope showed that rhBMP2-MPs could be enchased into the porous structure of calcium phosphate ceremic (CPC) and the eugonic growth of PDLCs in CPC/rhBMP2-MPs scaffolds. Animal experiments indicated that using CPC/rhBMP2-MPs scaffolds could gain more periodontal tissue regeneration than using rhBMP2 compound firsthand with CPC (CPC/rhBMP2). Conclusion:By encapsulating rhBMP2 into dextran-based microspheres, a small quantity of rhBMP2 could achieve equivalent effects to the concentrated rhBMP2 solution and at the same time, could prolong rhBMP2 retention both in vitro and in vivo.

  11. Protein-loaded microspheres prepared by sequential adsorption of dextran sulphate and protamine on melamine formaldehyde core.

    Science.gov (United States)

    Balabushevich, Nadezda G; Larionova, Natalia I

    2009-11-01

    Polyelectrolyte multilayer microspheres were fabricated by layer-by-layer self-assembly of a dextran sulphate and a protamine on melamine formaldehyde cores, followed by the partial decomposition of the core. Effects of pH on the encapsulation of proteins and enzymes with different physico-chemical properties (insulin, aprotinin, peroxidase, glucose oxidase (GOD), catalase (Cat)) in the prepared microspheres were then studied. This method of protein encapsulation demonstrated a high loading capacity and efficiency. The protein incorporation and release was regulated by the pH of the solution. Encapsulated enzymes retained a high specific activity depending on the amount of protein incorporated. Bienzyme system GOD/Cat immobilized in the microspheres was suitable for the glucose content assay.

  12. FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF PIOGLITAZONE HYDROCHLORIDE USING A NATURAL POLYMER

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    Mobeen Mohd.

    2015-04-01

    Full Text Available The objective of the present investigation was to design a controlled release dosage form for a thiazolidinedione oral hypoglycemic drug i.e., pioglitazone hydrochloride employing a natural polymer. The present study was also aimed to increase the biological half-life by developing it in the form of sustained release microspheres. The present study aimed at employing a natural polymer in formulating the mucoadhesive microspheres and estimate its effect over the controlled release of the drug from the formulation. The microspheres of pioglitazone hydrochloride were prepared by employing sodium alginate as a cell forming polymer and by using a natural bio-adhesive polymer viz. goru gum in the ratios of 1:1, 1:1.5 and 1:2, by orifice ion gelation method with varying concentrations of calcium chloride. Six batches of microspheres (MS1 – MS6 were prepared. The microspheres were evaluated for various micromeritic properties and it was observed that all the batches exhibited free-flowing properties. Scanning electron microscopy results showed that the microspheres were almost spherical in shape and discrete. The FTIR results showed that there were no interactions between the drug and the excipients. The in vitro release profile indicated that all the batches of microspheres showed controlled and prolonged drug release over an extended period, with acceptable release kinetics. The work demonstrated that among all the formulations of microspheres, the microspheres of the formulation MS4 are promising candidates for the sustained release of pioglitazone hydrochloride.

  13. Self-assembling microsphere-based dextran hydrogels for pharmaceutical applications

    NARCIS (Netherlands)

    Van Tomme, S.R.

    2007-01-01

    In this thesis novel self-assembling hydrogels, based on physical interactions between dextran microgels, potentially suitable for controlled drug delivery and tissue engineering, are presented. Two different approaches to self-assemble the hydrogels were investigated: ionic interactions and hydroph

  14. Multifunctional microsphere formulation of fluorescent magnetic properties for drug delivery system

    Science.gov (United States)

    Kusrini, Eny; Prassanti, Riesna; Nurjaya, Dwi Marta; Gunawan, Cindy

    2017-02-01

    The microsphere formulations of Chit/TPP/Sm/Fe3O4/Rn were prepared by an ionic gelation technique, where Chit=chitosan, TPP=tripolyphosphate, Sm=samarium and Rn=ranitidine. Optimum of microsphere formulation exhibit magnetic and fluorescent properties with adsorption efficiency of ˜92% was obtained for Chit/TPP/Sm/Fe3O4/Rn with ratio 400:500:50:1:20. Fluorescence intensity of microsphere formulations increased with the cumulative amount release of ranitidine, so that the changing of fluorescence intensity at wavelength of 590 nm referring to the Sm3+ ion could be used as indicator in DDS. With the demonstration of sustained release from microsphere formulation, it allows to investigate the applications to other drugs.

  15. Sustained Release Floating Microspheres Of Acyclovir: Formulation, Optimization, Characterization And In Vitro Evaluation

    Directory of Open Access Journals (Sweden)

    Parmar Kunal Vinodbhai

    2011-03-01

    Full Text Available The aim of the present work was to prepare floating microspheres of acyclovir to prolong residence time in stomach and to sustain the release of acyclovir. Acyclovir loaded floating microspheres were prepared by double emulsion solvent evaporation method. The 32 full factorial design was applied to optimize the formulation. The resultant microspheres were evaluated for average particle size, percentage encapsulation efficiency, in vitro drug release and model fitting kinetics. Scanning electron microscopy, Fourier transform infrared (FTIR spectroscopy and differential scanning calorimetry were used to investigate the physical state of the drug in the microspheres. The particle size of microspheres was in the range of 275-340 µm. Percentage encapsulation efficiency was between 59%-77% w/w. Microspheres remained buoyant for more than about 12 h. The results of FT-IR spectroscopy and differential scanning calorimetry indicated the stable character of acyclovir in microspheres and also revealed absence of drugpolymer interaction. The in vitro drug release study showed that acyclovir release from the microspheres was slow and sustained for more than about 10 h. Drug release followed Korsemeyer-peppas model. The results of factorial batches revealed that the concentration of ethyl cellulose and stirring speed significantly affected drug encapsulation efficiency and particle size of the microspheres. Thus we can conclude that floating microspheres can successfully be developed to sustain the drug release.

  16. 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 mean...... diameter, encapsulation efficiency and FA released from the microspheres were determined. The solid-state and phase separation properties of the microspheres were characterized using DSC, XRPD, Raman spectroscopy, SEM, laser confocal and real time recording of single microspheres formation. Above a loading...... of 1% (w/w) FA phase separated from PLGA polymer and formed distinct spherical FA-rich amorphous microdomains throughout the PLGA microsphere. For FA-loaded PLGA microspheres, encapsulation efficiency and cumulative release increased with initial drug loading. Similarly, cumulative release from FA...

  17. Floating microspheres of valacyclovir HCl: Formulation, optimization, characterization, in vitro and in vivo floatability studies

    Directory of Open Access Journals (Sweden)

    Nilamgiri Goswami

    2012-01-01

    Full Text Available Floating microspheres are multiple unit Gastroretentive drug delivery systems. Valacyclovir hydrochloride (VCH is L-valyl ester prodrug of acyclovir. VCH degrades in intestinal fluid. The objective was to develop floating microspheres of VCH to localise the drug at upper part of GIT, for improved absorption. Floating microspheres were prepared by W/O emulsification solvent evaporation method using Ethylcellulose (EC as polymer. Particle size and % EE were 550.021±0.241 μm, 79.88±2.236% respectively. in vitro and in vivo floatability studies confirmed floating behaviour of microspheres. VCH loaded floating microspheres can be a suitable alternative to the conventional formulation, by localizing the drug at upper GIT.

  18. Formulation and evalution of montelukast sodium - chitosan based spray dried microspheres for pulmonary drug delivery

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    Rushi Panchal

    2012-01-01

    Full Text Available The objective of present work was to prepare microspheres of montelukast sodium using a natural polymer- chitosan by spray drying method by using glutaraldehyde as a cross linking agent. The microspheres were characterized for size, shape, dissolution, swelling and mucoadhesion. It was observed that, all microspheres were spherical in shape with narrow size distribution. Microspheres had mean particle size of 7-12 μm, with % encapsulation efficiency of 78-86%. The % yield was 32-49% and drug load was 48-53%. With the increase in proportion of chitosan in formulation mucoadhesive strength was increase and also increased in particle size of microspheres. As the drug:polymer ratio increase drug loading was increase and % encapsulation efficiency was also increase.

  19. Formulation and characterization of albumin microspheres containing norcantharidate for liver tumor targeting.

    Science.gov (United States)

    Yan, Fang; Li, Bo; Shen, Fengping; Fu, Qiang

    2015-01-01

    The objectives of this study were first to encapsulate norcantharidate into albumin microspheres by the emulsion crosslinking method and second to characterize the microspheres in terms of the morphological examination, particle size, and encapsulation efficiency. The in vitro release of norcantharidate from the microspheres was studied by using the dialysis bag method. Pharmacokinetics and biodistribution studies were used to evaluate the advantages of microspheres than the conventional formulations. The microspheres prepared by crosslink emulsion were with uniform size, smooth surface, spherical shape, and disperse evenly. The particle size was uniform (13.3 ± 0.4 µm) and the encapsulation efficiency was 54.3 ± 4.18%. In vitro release indicated that the norcantharidate microspheres had a well-sustained release efficacy and fitted Korsmeyer's Peppas release model. In vivo studies showed that pharmacokinetics of norcantharidate microspheres could be described by the model of two-compartment after i.v. administration and had higher AUC inside liver and spleen than the injection group. No histological change occurred to the rat liver after the administration of norcantharidate microspheres.

  20. Formulation and evaluation of Zidovudine loaded chitosan Microspheres for controlled release

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    Kesari Asha

    2012-03-01

    Full Text Available The aim of this study was to formulate and evaluate zidovudine loaded chitosan microspheres for controlled drug release. Microspheres were prepared by emulsification method using gluteraldehyde as crosslinking agent. The prepared microspheres were characterized for their yield and drug loading, as well by Fourier transform infrared spectroscopy (FTIR, X-ray powder diffractometry and Scanning electron microscopy. The in vitro release studies were performed in pH 7.4, phosphate buffer. The prepared microspheres were free flowing and spherical in shape. The drugloaded microspheres showed 72-94% of entrapment and release was extended up to 12h. The infrared spectra showed stable character of zidovudine in the drugloaded microspheres and revealed the absence of drugpolymer interactions. X-ray diffraction patterns showed that there was decrease in crystallinity of the drug. Scanning electron microscopy study revealed that the microspheres were spherical and porous in nature. It was found that the drug: polymer ratio, the stirring speed, the concentration of surfactant, and the amount of gluteraldehyde used for crosslinking were the most significant variables which influenced the size of the chitosan microspheres under the applied experimental condition.

  1. Formulation and evaluation of albumin microspheres and its enteric coating using a spray-dryer.

    Science.gov (United States)

    Bejugam, Naveen K; Uddin, Akm N; Gayakwad, Sanjay G; D'Souza, Martin J

    2008-12-01

    This study optimized and evaluated the conditions for surface coating of microspheres using a spray-dryer. Four formulations of Bromophenol blue (BPB)-loaded albumin microspheres were prepared using a spray-dryer, cross-linked at different concentrations and time periods. One of the optimized formulations with the desired characteristics was selected for enteric coating with Eudragit L100-55. The procedure involved suspending BPB microspheres in polymer solution and spray-drying it. Four enteric coated formulations were prepared with different concentrations of microspheres in suspension (0.25 and 0.5%w/v) and polymer concentrations (0.25 and 0.5%w/v). Change in the mean particle size after coating was determined using a Laser Particle Counter. The surface coating technique employed did not significantly increase the particle size. Enteric coating efficiency was determined in simulated gastric fluid. Compared to the uncoated microspheres the cumulative amount of drug released from coated microspheres was significantly lower for 3 h, implying efficient surface coating.

  2. FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF NIFEDIPINE

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    G.V. Radha

    2012-10-01

    Full Text Available In the present study, an attempt has been made to evaluate mucoadhesive microspheres of nifedipine by orifice ionic gelation method employing sodium alginate and different mucoadhesive polymers (HPMC, carbopol alone and in combination of different proportions. The compatibility study was done between drug and polymer by FTIR which shows no interaction between the drug and polymer. The prepared microspheres were evaluated for particle size ,angle of repose, carrs index, swelling index, microencapsulation efficiency, percent drug content, drug release, kinetics and mechanism of drug release. The microspheres were found discrete, spherical, free flowing and the particle size was found in the range of 765 to 792µ. The encapsulation efficiency was found in the range of 55 to 69 %. Percent drug content was found to be in the range of 96 to 99 %. All the microspheres showed good muco adhesive property in the in vitro wash off test. Drug release from the microspheres was found slow, followed first order kinetics with non fickian release mechanism and release dependent on nature and concentration of polymers.

  3. Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl

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    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.

  4. Formulation and Evaluation of Microsphere Based Oro Dispersible Tablets of Itopride Hcl

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    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.

  5. 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 mean...

  6. Effects of formulation variables and characterization of guaifenesin wax microspheres for controlled release.

    Science.gov (United States)

    Mani, Narasimhan; Park, M O; Jun, H W

    2005-01-01

    Sustained-release wax microspheres of guaifenesin, a highly water-soluble drug, were prepared by the hydrophobic congealable disperse method using a salting-out procedure. The effects of formulation variables on the loading efficiency, particle properties, and in-vitro drug release from the microspheres were determined. The type of dispersant, the amount of wetting agent, and initial stirring time used affected the loading efficiency, while the volume of external phase and emulsification speed affected the particle size of the microspheres to a greater extent. The crystal properties of the drug in the wax matrix and the morphology of the microspheres were studied by differential scanning calorimetry (DSC), powder x-ray diffraction (XRD), and scanning electron microscopy (SEM). The DSC thermograms of the microspheres showed that the drug lost its crystallinity during the microencapsulation process, which was further confirmed by the XRD data. The electron micrographs of the drug-loaded microspheres showed well-formed spherical particles with a rough exterior.

  7. Formulation and characterization of microspheres loaded with imatinib for sustained delivery.

    Science.gov (United States)

    Ramazani, F; Chen, W; Van Nostrum, C F; Storm, G; Kiessling, F; Lammers, T; Hennink, W E; Kok, R J

    2015-03-30

    The aim of this study was the development of imatinib-loaded poly(d,l-lactide-co-glycolide) (PLGA) microspheres with high loading efficiency which can afford continuous release of imatinib over a prolonged period of time. Imatinib mesylate loaded PLGA microspheres with a size of 6-20 μm were prepared by a double emulsion (W1/O/W2) method using dichloromethane as volatile solvent. It was found that the microspheres were spherical with a non-porous surface; imatinib loading efficiency (LE) was highly dependent on the pH of the external water phase (W2). By increasing the pH of W2 phase above the highest pKa of imatinib (pKa 8.1), at which imatinib is mainly uncharged, the LE increased from 10% to 90% (pH 5.0 versus pH 9.0). Conversely, only 4% of its counter ion, mesylate, was retained in the microspheres at the same condition (pH 9.0). Since mesylate is highly water soluble, it is unlikely that it partitions into the organic phase. We demonstrated, using differential scanning calorimetry (DSC), that imatinib was molecularly dispersed in the polymeric matrix at loadings up to 8.0%. At higher drug loading, imatinib partially crystallized in the matrix. Imatinib microspheres released their cargo during three months by a combination of diffusion through the polymer matrix and polymer erosion. In conclusion, we have formulated imatinib microspheres with high LE and LC. Although we started with a double emulsion of imatinib mesylate, the obtained microspheres contained imatinib base which was mainly molecularly dispersed in the polymer matrix. These microspheres release imatinib over a 3-month period which is of interest for local treatment of cancer.

  8. Formulation and evaluation of controlled release floating microspheres of tolperisone hydrochloride

    Directory of Open Access Journals (Sweden)

    Pooja Jani

    2012-01-01

    Full Text Available Main aim of this study was to develop controlled release (CR floating multiparticulate drug delivery system of tolperisone hydrochloride. Microspheres were prepared by nonaqueous solvent evaporation technique consisting of porous calcium silicate (Florite or FLR as porous carrier, tolperisone hydrochloride (API, Ethyl cellulose (EC, and HPMC 15 cPs as rate controlling polymers. 2 3 full factorial design was applied for optimization of formulation. The effect of various formulation and process variables on the particle morphology, micromeritic properties, in vitro floating behavior, entrapment efficiency, and in vitro drug release were studied. The size of microspheres was varied from 300 to 500 μm. The microspheres were found to be highly porous and regular in shape. All the formulations showed excellent flow properties. The percentage entrapment efficiency of all batches was greater than 80%. The percentage buoyancy varied from 85% to 98% at the end of 12 h. The release rate was determined in simulated gastric fluids. The formulation demonstrated favorable in vitro floating and release characteristics. Different kinetic models were applied to study the release mechanism. All formulations followed Higuchi model, which indicates the diffusion control release of water soluble drug from polymer matrix. Multiple regression analysis was applied for study of the effect of independent variables on the dependent variables.

  9. Study of formulation variables on properties of glipizide mucoadhesive microspheres by factorial design

    Directory of Open Access Journals (Sweden)

    Hosmani A.H

    2009-12-01

    Full Text Available "nBackground and the Purpose of the study:The purpose of the study was formulate and systemsystematic evaluation in-vitro and in-vivo behaviour of Glipizide mucoadhesive microspheres using 32 full factorial design. "nMethods:Concentration of Polycarbophil and Sodium Alginate were selected as independent variables and the effects were checked on dependent variables like swelling index, mucoadhesion, drug entrapment efficiency and T75. In vivo studies were also performed to determine hypoglycemic activity of the mucoadhesive microspheres. "nResults:The best batch exhibited drug entrapment efficiency of 75%, swelling index of 1.8 and mucoadhesion was 100%. The drug release from the microspheres was also sustained for more than 9 hrs. Conclusion:The concentration of polycarbophil and sodium alginate had highly significant effects on dependent variables. In-vivo testing demonstrated a significant hypoglycemic effect of glipizide.

  10. Comparison of drug release from poly(lactide-co-glycolide) microspheres and novel fibre formulations.

    Science.gov (United States)

    Campbell, Christopher S J; Delgado-Charro, M Begoña; Camus, Olivier; Perera, Semali

    2016-03-01

    Intraperitoneal cisplatin delivery has recently been shown to benefit ovarian cancer patients. Cisplatin-containing poly(lactide-co-glycolide) (PLGA) microspheres have been proposed for cisplatin delivery. The drug loading of cisplatin containing microspheres produced elsewhere is 3-10%w. Similar microspheres are reported here with a mean diameter of 38.8 µm, and a drug loading of 11.7%w, but using ethyl acetate as a safer solvent. In addition, novel formulations of cisplatin-containing solid and hollow PLGA 65:35 (lactide:glycolide) fibres were prepared and are reported here for the first time. PLGA hollow fibres were produced by phase inversion with a high drug loading of 27%w. Mechanistic mathematical models were applied to the cisplatin release profiles to allow quantitative comparison of microsphere, solid fibre and hollow fibre formulations. The diffusion coefficient of cisplatin eluting from a typical batch of PLGA microspheres was 4.8 × 10(-13) cm(2) s(-1); this low diffusivity of cisplatin in microspheres was caused by the low porosity of the polymer matrix. The diffusion coefficients of cisplatin eluting from a batch of PLGA solid fibres and hollow fibres were 6.1 × 10(-10) and 3.3 × 10(-10) cm(2) s(-1), respectively. These fibres allowed the controlled release of high doses of cisplatin over four days and may represent an improvement in slow release technology for treatment of ovarian cancer.

  11. FORMULATION AND EVALUATION OF TIZANIDINE HYDROCHLORIDE MICROSPHERES BY USING 32 FULL FACTORIAL DESIGNS

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    Adimoolam Senthil

    2011-09-01

    Full Text Available Tizanidine hydrochloride is a centrally acting α-2 adrenergic agonist muscle relaxant. In the present study an attempt has been made to formulate and evaluate tizanidine hydrochloride microspheres by using hydroxypropylmethylcellulose K4M and carboxymethyl cellulose as polymers. Tizanidine hydrochloride microspheres were prepared by simple emulsification phase separation technique using glutaraldehyde as a cross-linking agent. Twenty preliminary trial batches, B1-B20 batches of microspheres were prepared by using different volume (2 to 10 ml of glutaraldehyde as cross-linking agent, cross-linking time 1 to 4 hours and 3:1 ratio of polymer-to-drug with two different polymers. From these twenty batches of each polymer, the optimized formulation is selected based on the percentage of mucoadhesion, drug entrapment efficiency and sphericity of microspheres. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X1, and stirring speed (X2 on dependent variables percentage of mucoadhesion, drug entrapment efficiency, swelling index and in-vitro drug release study. The drug polymer compatibility studies were carried out using FTIR. Among the two polymers hydroxypropylmethyl cellulose K4M exhibited a high drug entrapment efficiency of 79% and a swelling index 1.260, percentage of mucoadhesive after 1hour was 80% and the drug release was also sustained for more than 10 hours.

  12. Formulation and evaluation of clarithromycin microspheres for eradication of Helicobacter pylori.

    Science.gov (United States)

    Rajinikanth, Paruvathanahalli Siddalingam; Karunagaran, Lakshmi Narayanan; Balasubramaniam, Jagdish; Mishra, Brahmeshwar

    2008-12-01

    The objective of the study was to develop a stomach-specific drug delivery system for controlled release of clarithromycin for eradication of Helicobacter pylori (H. pylori). Floating-bioadhesive microspheres of clarithromycin (FBMC) were prepared by emulsification-solvent evaporation method using ethylcellulose as matrix polymer and Carbopol 934P as mucoadhesive polymer. The prepared microspheres were subjected to evaluation for particle size, incorporation efficiency, in vitro buoyancy, in vitro mucoadhesion and in vitro drug release characteristics. The prepared microspheres showed a strong mucoadhesive property with good buoyancy. The formulation variables like polymer concentration and drug concentration influenced the in vitro drug release significantly in simulated gastric fluid (pH. 2.0). The in vivo H. pylori clearance efficiency of prepared FBMC in reference to clarithromycin suspension following repeated oral administration to H. pylori infected Mongolian gerbils was examined by polymerase chain reaction (PCR) technique and by a microbial culture method. The FBMC showed a significant anti-H. pylori effect in the in vivo gerbil model. It was also noted that the required amount of clarithromycin for eradication of H. pylori was significantly less in FBMC than from corresponding clarithromycin suspension. The results further substantiated that FBMC improved the gastric stability of clarithromycin (due to entrapment within the microsphere) and eradicated H. pylori from the gastrointestinal tract more effectively than clarithromycin suspension because of the prolonged gastrointestinal residence time of the formulation.

  13. Study of formulation variables on properties of glipizide mucoadhesive microspheres by factorial design

    OpenAIRE

    Hosmani A.H; Kasture, P. V.; ID Gonjari; A.B. Karmarkar

    2009-01-01

    "nBackground and the Purpose of the study:The purpose of the study was formulate and systemsystematic evaluation in-vitro and in-vivo behaviour of Glipizide mucoadhesive microspheres using 32 full factorial design. "nMethods:Concentration of Polycarbophil and Sodium Alginate were selected as independent variables and the effects were checked on dependent variables like swelling index, mucoadhesion, drug entrapment efficiency and T75. In vivo studies were also performed to determine ...

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

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    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

  15. Influence of Formulation Components on Aerosolization Properties of Isoniazid Loaded Chitosan Microspheres

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    Aliasgar J. Kundawala

    2011-10-01

    Full Text Available The objective of the present study was to prepare microspheres with small size and good sphericity by spray drying technology using Isoniazid (INH as model drug, chitosan as encapsulating polymer; lactose and L Leucine as bulking and dispersing agent respectively. Influence of formulation components on physical properties and aerosol performance were studied. The spray dried powders obtained were characterized for morphological characteristics, compatibility using scanning electron microscopy and Differential Scanning calorimetery respectively. Tapped density; bulk density and aerosol properties like Fine particle fraction, mass median aerodynamic diameter etc were also evaluated. The smooth microspheres with particle size ranging between 4 to 6 µm were obtained. The drug content of chitosan microspheres loaded with Isoniazid were in the range of 88 % to 108 %. The drug release studies showed that more than 90% of drug released from the chitosan microsphere matrix within one hour. The fine particle fraction observed between 55 to 67 % which indicate good lung deposition. Results of Fine particle fraction also revealed addition of L Leucine found to enhance powder dispersibility.

  16. Microspheres

    Science.gov (United States)

    1990-01-01

    Vital information on a person's physical condition can be obtained by identifying and counting the population of T-cells and B-cells, lymphocytes of the same shape and size that help the immune system protect the body from the invasion of disease. The late Dr. Alan Rembaum developed a method for identifying the cells. The method involved tagging the T-cells and B-cells with microspheres of different fluorescent color. Microspheres, which have fluorescent dye embedded in them, are chemically treated so that they can link with antibodies. With the help of a complex antibody/antigen reaction, the microspheres bind themselves to specific 'targets,' in this case the T-cells or B-cells. Each group of cells can then be analyzed by a photoelectronic instrument at different wavelengths emitted by the fluorescent dyes. Same concept was applied to the separation of cancer cells from normal cells. Microspheres were also used to conduct many other research projects. Under a patent license Magsphere, Inc. is producing a wide spectrum of microspheres on a large scale and selling them worldwide for various applications.

  17. Formulation and evaluation of novel stomach specific floating microspheres bearing famotidine for treatment of gastric ulcer and their radiographic study

    Institute of Scientific and Technical Information of China (English)

    Rishikesh; Gupta; Sunil; Kumar; Prajapati; Snigdha; Pattnaik; Peeyush; Bhardwaj

    2014-01-01

    Objective:To develop and characterize multiple-unit-type oral floating microsphere of famotidine to prolong gastric residence time and to target stomach ulcer.Methods:The floating microspheres were prepared by modified solvent evaporation method,Eudragil S-100 was used as polymer.Microspheres were characterized for the micromeritic properties,floating behavior,entrapment efficiency and scanning electron microscopy.The invitro release studies and floating behavior were studied in simulated gastric fluid at pH 1.2.Different drug release kinetics models were also applied for all the batches.Selected formulations were also subjected for X-ray radiographic study.Results:Floating microspheres were successfully prepared by modified solvent evaporation technique.Microspheres showed passable flow properties.The maximum yield of microspheres was up to(95.11±0.35)%.On the basis of optical microscopy particle size range was found to be ranging from(52.18±182.00) to(91.64±5.16) μm.Scanning electron microscopy showed their spherical size,perforated smooth surface and a cavity inside microspheres.Microspheres were capable to float up to 20 h in simulated gastric fluid.X-ray radiographic studies also proved its better retention in the stomach.Conclusions:On the basis of the results,such dosage forms may be a good candidate for stomach targeting and may be dispensed in hard gelatin capsules.

  18. Formulation and evaluation of novel stomach specific floating microspheres bearing famotidine for treatment of gastric ulcer and their radiographic study

    Institute of Scientific and Technical Information of China (English)

    Rishikesh Gupta; Sunil Kumar Prajapati; Snigdha Pattnaik; Peeyush Bhardwaj

    2014-01-01

    Objective: To develop and characterize multiple-unit-type oral floating microsphere of famotidine to prolong gastric residence time and to target stomach ulcer. Methods: The floating microspheres were prepared by modified solvent evaporation method. Eudragit S-100 was used as polymer. Microspheres were characterized for the micromeritic properties, floating behavior, entrapment efficiency and scanning electron microscopy. The in-vitro release studies and floating behavior were studied in simulated gastric fluid at pH 1.2. Different drug release kinetics models were also applied for all the batches. Selected formulations were also subjected for X-ray radiographic study. Results: Floating microspheres were successfully prepared by modified solvent evaporation technique. Microspheres showed passable flow properties. The maximum yield of microspheres was up to (95.11±0.35)%. On the basis of optical microscopy particle size range was found to be ranging from (52.18±182.00) to (91.64±5.16) µm. Scanning electron microscopy showed their spherical size, perforated smooth surface and a cavity inside microspheres. Microspheres were capable to float up to 20 h in simulated gastric fluid. X-ray radiographic studies also proved its better retention in the stomach. Conclusions:On the basis of the results, such dosage forms may be a good candidate for stomach targeting and may be dispensed in hard gelatin capsules.

  19. Formulation and in vitro characterization of alginate microspheres loaded with diloxanide furoate for colon- specific drug delivery

    Directory of Open Access Journals (Sweden)

    Shukla Shailendra

    2010-01-01

    Full Text Available The aim of the research work was to develop cyst-targeted alginates microspheres of diloxanide furoate (DF for the effective treatment of amoebiasis. Calcium alginates microspheres of DF were prepared using emulsification method using calcium chloride as a cross-linking agent. Alginate is a natural polysaccharide found in brown algae. Alginates are widely used in the food and pharmaceutical industries and have been employed as a matrix for the entrapment of drugs, macromolecules and biological cells. Alginate microspheres produced by the emulsification method using calcium chloride. Formulations were characterized for particle size and shape, surface morphology, entrapment efficiency, and in vitro drug release in simulated gastrointestinal fluids. XRD and differential scanning calorimetery were used to confirm successful entrapment of DF into the alginates microspheres. All the microsphere formulations showed good % drug entrapment (73.82΁1.99. Calcium alginate retarded the release of DF at low pH (1.2 and 4.5 and released microspheres slowly at pH 7.4 in the colon without colonic enzymes.

  20. Physicochemical characterization of camptothecin membrane binding properties and polymeric microsphere formulations

    Science.gov (United States)

    Selvi, Bilge

    acidic media CPT-loaded microspheres were prepared in a 10 N HCl-methylene chloride mixture using the H-series of poly(D,L-lactide-co-glycolide) (H-PLGA). The system was then compared with a standard microsphere formation method and the results were evaluated with respect to particle morphology and drug release profile. Rough surface of the particles were obtained from the preparation method where a 10 N HCl solution was used. The release pattern of CPT was biphasic comprising a first burst effect followed by zero order release for all the formulations. However, the release of the drug was slightly faster from the microspheres formed with the modified method compared to the standard. Until now clinical application of CPT has been highly restricted by the insolubility and instability of the drug in its active lactone form, resulting in less antitumor potency and poor bioavailability. The pH-dependent release of the CPT-loaded microspheres was also compared and faster initial release (burst phase) was found at neutral pH, whereas at low pH the release was zero order for all the formulations. The results indicate that the stabilization and sustained release of CPT from H-PLGA microspheres might reduce local toxicity while simultaneously prolonging efficiency, suggesting new perspectives in CPT chemotherapy.

  1. Development and evaluation of sustained-release ibuprofen-wax microspheres. I. Effect of formulation variables on physical characteristics.

    Science.gov (United States)

    Adeyeye, C M; Price, J C

    1991-11-01

    A congealable disperse phase encapsulation method was used to prepare sustained-release ibuprofen-wax microspheres. Microspheres prepared with paraffin wax, such as ceresine and microcrystalline waxes, using polyvinylpyrrolidone (PVP) as dispersant had a tendency to aggregate, but the addition of wax modifiers (stearyl alcohol and glyceryl monostearate) greatly reduced aggregation. Optimum modifier and dispersant concentrations were 20% (w/w) and 5% (w/v), respectively. The particle size distribution of the microspheres was log-normal. An increase in modifier, dispersant concentration, emulsification stirring speed, or temperature shifted the size distribution toward finer particles. Microcrystalline wax required a higher emulsification temperature and produced finer particles than ozokerite wax. The recovery of drug from the different microsphere formulations varied between 71 and 92%. Differential scanning calorimetry (DSC) of the single components and physical mixtures showed endothermic peaks at the respective melting-point ranges. The DSC of the ceresine and microcrystalline wax microspheres was similar to rescans of ternary mixtures of components of the microspheres with less prominent and lower melting temperatures than individual components or physical mixtures.

  2. Formulation, characterization and in vitro evaluation of floating microspheres of famotidine as a gastro retentive dosage form

    Directory of Open Access Journals (Sweden)

    Jain Abhishek

    2009-01-01

    Full Text Available The present study involves preparation and evaluation of floating microspheres using famotidine (FM as a model drug for prolongation of the gastric retention time. The microspheres were prepared by the solvent evaporation method using different polymers, i.e. acrycoat S100 and cellulose acetate. The size or average diameter (d avg and surface morphology of the prepared microspheres were recognized and characterized by the optical and scanning electron microscopic methods, respectively. In vitro drug release studies were performed and the drug release kinetics were evaluated using the linear regression method. Effects of the stirring rate during preparation, polymer concentration on the size of the microspheres and drug release were also observed. The prepared microspheres exhibited prolonged drug release (18 h and remained buoyant for more than 12 h. The mean particle size increased and the drug release rate decreased at a higher polymer concentration. No significant effect of the stirring rate during preparation on drug release was observed. In vitro studies demonstrated a diffusion-controlled drug release from the microspheres. The objective of the present study was to develop floating microspheres of FM in order to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The prepared microspheres were evaluated for particle size, in vitro release and buoyancy and incorporation efficiency. The effect of various formulation variables on the size and drug release was investigated. In vitro drug release studies were performed and the drug release kinetics were evaluated using the linear regression method. FM was obtained as a gift sample from Intas Pharmaceuticals, Ahmedabad, India. Polyvinyl alcohol was obtained from S.D. Fine Chemicals Ltd., Mumbai, India. Dichloromethane, acrycoat S100, cellulose acetate and Tween 80 were obtained from Central Drug House (P

  3. Determination of Ideal Broth Formulations Needed to Prepare Hydrous Cerium Oxide Microspheres via the Internal Gelation Process

    Energy Technology Data Exchange (ETDEWEB)

    Collins, Jack Lee [ORNL; Chi, Anthony [ORNL

    2009-02-01

    A simple test tube methodology was used to determine optimum process parameters for preparing hydrous cerium oxide microspheres via the internal gelation process.1 Broth formulations of cerium ammonium nitrate [(NH4)2Ce(NO3)6], hexamethylenetetramine, and urea were found that can be used to prepare hydrous cerium oxide gel spheres in the temperature range of 60 to 90 C. A few gel-forming runs were made in which microspheres were prepared with some of these formulations to be able to equate the test-tube gelation times to actual gelation times. These preparations confirmed that the test-tube methodology is reliable for determining the ideal broth formulations.

  4. Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study

    Directory of Open Access Journals (Sweden)

    Praveen Kumar Gaur

    2014-12-01

    Full Text Available The aim of this work was to design a controlled-release drug-delivery system for the angiotensin-II receptor antagonist drug telmisartan. Telmisartan was encapsulated with different EUDRAGIT polymers by an emulsion solvent evaporation technique and the physicochemical properties of the formulations were characterized. Using a solvent evaporation method, white spherical microspheres with particle sizes of 629.9–792.1 μm were produced. The in vitro drug release was studied in three different pH media (pH 1.2 for 2 hours, pH 6.8 for 4 hours, and pH 7.4 for 18 hours. The formulations were then evaluated for their pharmacokinetic parameters. The entrapment efficiency of these microspheres was between 58.6% and 90.56%. The obtained microspheres showed good flow properties, which were evaluated in terms of angle of repose (15.29–26.32, bulk and tapped densities (0.37–0.53 and 0.43–0.64, respectively, Carr indices and Hausner ratio (12.94–19.14% and 1.14–1.23, respectively. No drug release was observed in the simulated gastric medium up to 2 hours; however, a change in pH from 1.2 to 6.8 increased the drug release. At pH 7.4, formulations with EUDRAGIT RS 100 showed a steady drug release. The microsphere formulation TMRS-3 (i.e., microspheres containing 2-mg telmisartan gave the highest Cmax value (6.8641 μg/mL at 6 hours, which was three times higher than Cmax for telmisartan oral suspension (TOS. Correspondingly, the area under the curve for TMRS-3 was 8.5 times higher than TOS. Particle size and drug release depended on the nature and content of polymer used. The drug release mechanism of the TMRS-3 formulation can be explained using the Higuchi model. The controlled release of drug from TMRS-3 also provides for higher plasma drug content and improved bioavailability.

  5. Formulation of mucoadhesive microspheres of rosiglitazone maleate and its in vitro evaluation using ionotropic gelation technique

    Directory of Open Access Journals (Sweden)

    Akanksha Garud

    2015-01-01

    Full Text Available Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies, morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiency was 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of coat. Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release of Rosiglitazone maleate and thereby help in the management of type II diabetes mellitus.

  6. Sustained-release microsphere formulation containing an agrochemical by polyurethane polymerization during an agitation granulation process.

    Science.gov (United States)

    Terada, Takatoshi; Tagami, Manabu; Ohtsubo, Toshiro; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2016-07-25

    In this report, a new solventless microencapsulation method by synthesizing polyurethane (PU) from polyol and isocyanate during an agglomeration process in a high-speed mixing apparatus was developed. Clothianidin (CTD), which is a neonicotinoid insecticide and highly effective against a wide variety of insect pests, was used as the model compound. The microencapsulated samples covered with PU (CTD microspheres) had a median diameter of dispersed in PU. Although voids appeared in the CTD microspheres after CTD release, the spherical shape of the microspheres remained stable and no change in its framework was observed. The experimental release data were highly consistent with the Baker-Lonsdale model derived from drug release of spherical monolithic dispersions and consistent with the computed tomography measurements.

  7. Influence of some formulation variables on the optimization of pH-dependent, colon-targeted, sustained-release mesalamine microspheres.

    Science.gov (United States)

    El-Bary, Ahmed Abd; Aboelwafa, Ahmed A; Al Sharabi, Ibrahim M

    2012-03-01

    The aim of this work was to understand the influence of different formulation variables on the optimization of pH-dependent, colon-targeted, sustained-release mesalamine microspheres prepared by O/O emulsion solvent evaporation method, employing pH-dependent Eudragit S and hydrophobic pH-independent ethylcellulose polymers. Formulation variables studied included concentration of Eudragit S in the internal phase and the ratios between; internal to external phase, drug to Eudragit S and Eudragit S to ethylcellulose to mesalamine. Prepared microspheres were evaluated by carrying out in vitro release studies and determination of particle size, production yield, and encapsulation efficiency. In addition, morphology of microspheres was examined using optical and scanning electron microscopy. Emulsion solvent evaporation method was found to be sensitive to the studied formulation variables. Particle size and encapsulation efficiency increased by increasing Eudragit S concentration in the internal phase, ratio of internal to external phase, and ratio of Eudragit S to the drug. Employing Eudragit S alone in preparation of the microspheres is only successful in forming acid-resistant microspheres with pulsatile release pattern at high pH. Eudragit S and ethylcellulose blend microspheres were able to control release under acidic condition and to extend drug release at high pH. The stability studies carried out at 40°C/75% RH for 6 months proved the stability of the optimized formulation. From the results of this investigation, microencapsulation of mesalamine in microspheres using blend of Eudragit S and ethylcellulose could constitute a promising approach for site-specific and controlled delivery of drug in colon.

  8. Development of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres: Formulation optimization, characterization, and vitro release.

    Science.gov (United States)

    Lin, Qiang; Huo, Qing; Qin, Yingzhe; Zhao, Zhuo; Tao, Fengyun

    2017-01-02

    This study investigates the preparation of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres. This experiment investigates effects of the ratio of carboxymethyl chitosan and collagen blend, water to oil ratio, stirring speed, and other factors on the microsphere properties. The experiment had the following conditions: a 1:2 proportion of carboxymethyl chitosan and collagen, a 1:2 proportion of drugs and materials, a 5:1 proportion of oil phase and water phase, 0.5% of span80, a 600r/min stirring speed, 3 ml of a cross-linking agent, 3 h of cross-linking curing, 1.25 ± 0.05 mm diameter LTH microcapsules, a 54.08% envelop rate, and a 14.16% carrier rate. The microspheres release rate reached 66% within 1 h, then steadily released within 5 h in vitro. The experimental results showed that the ligustrazine hydrochloride microsphere production process was stable and exhibited a good release effect compared with other ligustrazine hydrochloride tablets and pills.

  9. Spray drying formulation of albendazole microspheres by experimental design. In vitro-in vivo studies.

    Science.gov (United States)

    García, Agustina; Leonardi, Darío; Piccirilli, Gisela N; Mamprin, María E; Olivieri, Alejandro C; Lamas, María C

    2015-02-01

    Both an experimental design and optimization techniques were carried out for the development of chitosan-pectin-carboxymethylcellulose microspheres to improve the oral absorption of albendazole as a model drug. The effect of three different factors (chitosan, pectin and carboxy methyl cellulose concentrations) was studied on five responses: yield, morphology, dissolution rate at 30 and 60 min, and encapsulation efficiency of the microspheres. During the screening phase, the factors were evaluated in order to identify those which exert a significant effect. Simultaneous multiple response optimizations were then used to find out experimental conditions where the system shows the most adequate results. The optimal conditions were found to be: chitosan concentration, 1.00% w/v, pectin concentration 0.10% w/v and carboxymethylcellulose concentration 0.20% w/v. The bioavailability of the loaded drug in the optimized microspheres was evaluated in Wistar rats which showed an area under curve (AUC) almost 10 times higher than the pure drug.

  10. Development of Recombinant Human Growth Hormone (rhGH) sustained-release microspheres by a low temperature aqueous phase/aqueous phase emulsion method.

    Science.gov (United States)

    Kang, Jian; Wu, Fei; Cai, Yunpeng; Xu, Mingxin; He, Mu; Yuan, Weien

    2014-10-01

    A novel method has been developed to protect Recombinant Human Growth Hormone (rhGH) in poly (lactic-co-glycolic acid) (PLGA) microspheres using an aqueous phase/aqueous phase emulsion and S/O/W multi-emulsion method. This method develops a novel rhGH sustained-release system, which is based on the combination of rhGH-loaded dextran microparticles and PLGA microspheres. The process to fabricate rhGH-loaded dextran microparticles involves an aqueous phase/aqueous phase emulsion system formed at the reduced temperature. RhGH was first dissolved in water together with dextran and polyethylene glycol, followed by stirring at the speed of 2000 rpm for 20-30s at 0°C, and then a freezing process could enable the dextran phase to separate from the continuous PEG phase and rhGH could preferentially be loaded with dextran. The sample after freezing and phase separation was then lyophilized to powder and washed with dichloromethane to remove the PEG. Once loaded in the dextran microparticles (1-4 μm in diameter), rhGH gained resistance to interface tensions and was encapsulated into PLGA microspheres without aggregation thereafter. RhGH released from PLGA microspheres was in a sustained manner with minimal burst and maximally reduced incomplete release in vitro. Single subcutaneous injection of rhGH-loaded PLGA microspheres to rats resulted in a stable plasma concentration for 30 days avoiding the drug concentration fluctuations after multiple injections of protein solutions. In a hypophysectomized rat model, the IGF-1 and bodyweight results showed that there were higher than the levels obtained for the sustained release formulation by W/O/W for 40 days. These results suggest that the microsphere delivery system had the potential to be an injectable depot for sustained-release of the biocompatible protein of rhGH.

  11. [Impact of formulation and process parameters on the properties of chitosan-based microspheres prepared by external ionic gelation].

    Science.gov (United States)

    Kubánková, Romana; Vysloužil, Jakub; Kejdušová, Martina; Vetchý, David; Dvořáčková, Kateřina

    2014-06-01

    The aim of this experimental study was to optimize a preparation of microspheres from high viscosity chitosan by external ion gelation and to evaluate selected aspects of their preparation. For drug-free microparticles, the concentration of chitosan dispersions was chosen as a formulation variable; the position of instrument for a dispersion extrusion (horizontal vs. vertical) was evaluated as a process variable. On the basis of sphericity and equivalent diameter results, three different concentrations of chitosan dispersions were used for 5-aminosalicylic acid (5-ASA) encapsulation with the extrusion instrument in horizontal position, which was considered as the optimal. In consequent drug-loaded microparticle preparation, the influence of the concentration of chitosan dispersions and composition of hardening solution (10% sodium tripolyphosphate (TPP) vs. 10% TPP containing drug) was evaluated. In prepared 5-ASA microspheres it was found that the equivalent diameter increased with increasing chitosan concentration. In the case of sphericity, significant differences were not found. Samples prepared with the drug in both chitosan dispersion and hardening solution had a higher drug content, a smaller equivalent diameter and they showed a faster in vitro drug release in comparison with the samples prepared with the drug in chitosan dispersion only.

  12. Process and formulation variables of pregabalin microspheres prepared by w/o/o double emulsion solvent diffusion method and their clinical application by animal modeling studies.

    Science.gov (United States)

    Aydogan, Ebru; Comoglu, Tansel; Pehlivanoglu, Bilge; Dogan, Murat; Comoglu, Selcuk; Dogan, Aysegul; Basci, Nursabah

    2015-01-01

    Pregabalin is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. In conventional therapy recommended dose for pregabalin is 75 mg twice daily or 50 mg three times a day, with maximum dosage of 600 mg/d. To achieve maximum therapeutic effect with a low risk of adverse effects and to reduce often drug dosing, modified release preparations; such as microspheres might be helpful. However, most of the microencapsulation techniques have been used for lipophilic drugs, since hydrophilic drugs like pregabalin, showed low-loading efficiency and rapid dissolution of compounds into the aqueous continous phase. The purpose of this study was to improve loading efficiency of a water-soluble drug and modulate release profiles, and to test the efficiency of the prepared microspheres with the help of animal modeling studies. Pregabalin is a water soluble drug, and it was encapsulated within anionic acrylic resin (Eudragit S 100) microspheres by water in oil in oil (w/o/o) double emulsion solvent diffusion method. Dichloromethane and corn oil were chosen primary and secondary oil phases, respectively. The presence of internal water phase was necessary to form stable emulsion droplets and it accelerated the hardening of microspheres. Tween 80 and Span 80 were used as surfactants to stabilize the water and corn oil phases, respectively. The optimum concentration of Tween 80 was 0.25% (v/v) and Span 80 was 0.02% (v/v). The volume of the continous phase was affected the size of the microspheres. As the volume of the continous phase increased, the size of microspheres decreased. All microsphere formulations were evaluated with the help of in vitro characterization parameters. Microsphere formulations (P1-P5) exhibited entrapment efficiency ranged between 57.00 ± 0.72 and 69.70 ± 0.49%; yield ranged between 80.95 ± 1.21 and 93.05 ± 1.42%; and mean particle size were

  13. Gellan gum-based mucoadhesive microspheres of almotriptan for nasal administration: Formulation optimization using factorial design, characterization, and in vitro evaluation

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    Zaheer Abbas

    2014-01-01

    Full Text Available Background: Almotriptan malate (ALM, indicated for the treatment of migraine in adults is not a drug candidate feasible to be administered through the oral route during the attack due to its associated symptoms such as nausea and vomiting. This obviates an alternative dosage form and nasal drug delivery is a good substitute to oral and parenteral administration. Materials and Methods: Gellan gum (GG microspheres of ALM, for intranasal administration were prepared by water-in-oil emulsification cross-linking technique employing a 2 3 factorial design. Drug to polymer ratio, calcium chloride concentration and cross-linking time were selected as independent variables, while particle size and in vitro mucoadhesion of the microspheres were investigated as dependent variables. Regression analysis was performed to identify the best formulation conditions. The microspheres were evaluated for characteristics such as practical percentage yield, particle size, percentage incorporation efficiency, swellability, zeta potential, in vitro mucoadhesion, thermal analysis, X-ray diffraction study, and in vitro drug diffusion studies. Results: The shape and surface characteristics of the microspheres were determined by scanning electron microscopy, which revealed spherical nature and nearly smooth surface with drug incorporation efficiency in the range of 71.65 ± 1.09% - 91.65 ± 1.13%. In vitro mucoadhesion was observed the range of 79.45 ± 1.69% - 95.48 ± 1.27%. Differential scanning calorimetry and X-ray diffraction results indicated a molecular level dispersion of drug in the microspheres. In vitro drug diffusion was Higuchi matrix controlled and the release mechanism was found to be non-Fickian. Stability studies indicated that there were no significant deviations in the drug content, in vitro mucoadhesion and in vitro drug diffusion characteristics. Conclusion: The investigation revealed promising potential of GG microspheres for delivering ALM

  14. Formulation and evaluation of hydroxyzine hydrochloride sustained release microspheres by ionotropic gelation technique using Carbopol 934P

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    Soumyadeep Ghosh

    2014-01-01

    Full Text Available Preparation of sustained release microspheres of hydroxyzine hydrochloride by ionotropic gelation technique and evaluation. Microspheres of hydroxyzine hydrochloride were prepared by ionotropic gelation method using sodium alginate, Carbopol 934P and calcium chloride. The powders were evaluated for their flow properties. Hydroxyzine hydrochloride microspheres were characterized by Fourier transform infrared and in vitro dissolution studies. The drug release study of hydroxyzine hydrochloride microspheres was evaluated using basket type dissolution test apparatus. The release rate of Hydroxyzine hydrochloride microspheres was studied for 12 h in pH 7.4 phosphate buffer media. From the five batches F5 batch showed good release behavior 91.08% of drug is released over 12 h, and r2 = 0.987 in zero-order kinetics. The microspheres were prepared without the use of organic solvents. Microspheres of hydroxyzine hydrochloride decrease the incidence of side effects and also improve patient compliance by reducing the number of dosing and by reducing the fluctuations of drug in the blood. This entire attributed attitude proves that microsphere technology from novel drug delivery can be very much effective in reducing dosage frequency, dose dumping, and better patient compliance and economical to the patient. In the future, natural, biodegradable polymers can be used to improve therapeutic efficacy of the drug and further minimizing side-effects.

  15. Polymeric microspheres

    Science.gov (United States)

    Walt, David R.; Mandal, Tarun K.; Fleming, Michael S.

    2004-04-13

    The invention features core-shell microsphere compositions, hollow polymeric microspheres, and methods for making the microspheres. The microspheres are characterized as having a polymeric shell with consistent shell thickness.

  16. A comparative biocompatibility study of micropheres based on crosslinked dextran or poly(lactic-co-glycolic)acid after subcutaneous injection in rats

    NARCIS (Netherlands)

    Cadee, JA; Brouwer, LA; den Otter, W; Hennink, WE; van Luyn, MJA

    2001-01-01

    Microspheres based on methacrylated dextran (dex-MA), dextran derivatized with lactate-hydroxyethyl methacrylate (dex-lactate-HEMA) or derivatized with HEMA (dex-HEMA) were prepared. The microspheres were injected subcutaneously in rats and the effect of the particle size and network characteristics

  17. A comparative biocompatibility study of micropheres based on crosslinked dextran or poly(lactic-co-glycolic)acid after subcutaneous injection in rats

    NARCIS (Netherlands)

    Cadee, JA; Brouwer, LA; den Otter, W; Hennink, WE; van Luyn, MJA

    2001-01-01

    Microspheres based on methacrylated dextran (dex-MA), dextran derivatized with lactate-hydroxyethyl methacrylate (dex-lactate-HEMA) or derivatized with HEMA (dex-HEMA) were prepared. The microspheres were injected subcutaneously in rats and the effect of the particle size and network characteristics

  18. Iron Dextran Injection

    Science.gov (United States)

    ... allergic to iron dextran injection; any other iron injections such as ferric carboxymaltose (Injectafer), ferumoxytol (Feraheme), iron sucrose (Venofer), or sodium ferric gluconate (Ferrlecit);any other ...

  19. Efficient fabrication of high-capacity immobilized metal ion affinity chromatographic media: The role of the dextran-grafting process and its manipulation.

    Science.gov (United States)

    Zhao, Lan; Zhang, Jingfei; Huang, Yongdong; Li, Qiang; Zhang, Rongyue; Zhu, Kai; Suo, Jia; Su, Zhiguo; Zhang, Zhigang; Ma, Guanghui

    2016-03-01

    Novel high-capacity Ni(2+) immobilized metal ion affinity chromatographic media were prepared through the dextran-grafting process. Dextran was grafted to an allyl-activated agarose-based matrix followed by functionalization for the immobilized metal ion affinity chromatographic media. With elaborate regulation of the allylation degree, dextran was completely or partly grafted to agarose microspheres, namely, completely dextran-grafted agarose microspheres and partly dextran-grafted ones, respectively. Confocal laser scanning microscope results demonstrated that a good adjustment of dextran-grafting degree was achieved, and dextran was distributed uniformly in whole completely dextran-grafted microspheres, while just distributed around the outside of the partly dextran-grafted ones. Flow hydrodynamic properties were improved greatly after the dextran-grafting process, and the flow velocity increased by about 30% compared with that of a commercial chromatographic medium (Ni Sepharose FF). A significant improvement of protein binding performance was also achieved by the dextran-grafting process, and partly dextran-grafted Ni(2+) chelating medium had a maximum binding capacity for His-tagged lactate dehydrogenase about 2.5 times higher than that of Ni Sepharose FF. The results indicated that this novel chromatographic medium is promising for applications in high-efficiency and large-scale protein purification.

  20. Organic aerogel microspheres

    Science.gov (United States)

    Mayer, Steven T.; Kong, Fung-Ming; Pekala, Richard W.; Kaschmitter, James L.

    1999-01-01

    Organic aerogel microspheres which can be used in capacitors, batteries, thermal insulation, adsorption/filtration media, and chromatographic packings, having diameters ranging from about 1 micron to about 3 mm. The microspheres can be pyrolyzed to form carbon aerogel microspheres. This method involves stirring the aqueous organic phase in mineral oil at elevated temperature until the dispersed organic phase polymerizes and forms nonsticky gel spheres. The size of the microspheres depends on the collision rate of the liquid droplets and the reaction rate of the monomers from which the aqueous solution is formed. The collision rate is governed by the volume ratio of the aqueous solution to the mineral oil and the shear rate, while the reaction rate is governed by the chemical formulation and the curing temperature.

  1. Organic aerogel microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Mayer, S.T.; Kong, F.M.; Pekala, R.W.; Kaschmitter, J.L.

    1999-06-01

    Organic aerogel microspheres are disclosed which can be used in capacitors, batteries, thermal insulation, adsorption/filtration media, and chromatographic packings, having diameters ranging from about 1 micron to about 3 mm. The microspheres can be pyrolyzed to form carbon aerogel microspheres. This method involves stirring the aqueous organic phase in mineral oil at elevated temperature until the dispersed organic phase polymerizes and forms nonstick gel spheres. The size of the microspheres depends on the collision rate of the liquid droplets and the reaction rate of the monomers from which the aqueous solution is formed. The collision rate is governed by the volume ratio of the aqueous solution to the mineral oil and the shear rate, while the reaction rate is governed by the chemical formulation and the curing temperature.

  2. Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio

    Directory of Open Access Journals (Sweden)

    Piroska Szabó-Révész

    2011-11-01

    Full Text Available The objectives of this work were the formulation optimization of the preparation process parameters and to evaluate spray-dried sustained-release microspheres using ammonio methacrylate copolymer (AMC as a polymer matrix. The effects of log P and the concentrations of the cosolvents (acetone, methyl ethyl ketone and n-butyl acetate and different drug/copolymer ratios as independent variables on the physicochemical parameters (the W1/O emulsion viscosity, the microsphere production yield, the average particle size, the encapsulation efficiency and the cumulative in vitro drug release as dependent variables were studied. The optimization was carried out on the basis of the 33 factorial design study. The optimization process results showed that addition of polar cosolvents proved effective, linear relationships were observed between the independent and the dependent variables. The best conditions were achieved by microspheres prepared by using a low/medium cosolvent log P, cosolvent concentration of 25–50% v/v and a drug/copolymer ratio of 1:16. The microspheres ensured sustained release with Nernst and Baker-Lonsdale release profiles.

  3. Computer Modeling Assisted Design of Monodisperse PLGA Microspheres with Controlled Porosity Affords Zero Order Release of an Encapsulated Macromolecule for 3 Months

    NARCIS (Netherlands)

    Kazazi-Hyseni, Filis; Landin, Mariana; Lathuile, Audrey; Veldhuis, Gert J.; Rahimian, Sima; Hennink, Wim E.; Kok, Robbert Jan; van Nostrum, Cornelus F.

    2014-01-01

    Purpose The aim of this study was the development of poly(D,L-lactide-co-glycolide) (PLGA) microspheres with controlled porosity, to obtain microspheres that afford continuous release of a macromolecular model compound (blue dextran). Methods PLGA microspheres with a size of around 40 μm and narrow

  4. Synthesis, properties, and in vivo evaluation of sustained release albumin-mitoxantrone microsphere formulations for nonsystemic treatment of breast cancer and other high mortality cancers

    Science.gov (United States)

    Hadba, Ahmad Robert

    Methods for preparing mitoxantrone (MXN)-loaded albumin microspheres for the treatment of breast cancer were developed. The effect of processing conditions on the particle size of unloaded and MXN-loaded microspheres was evaluated using multivariate analyses. The data suggested that the particle size of unloaded microspheres increased as protein concentration increased or the steric stabilizer concentration decreased. In addition, synergy between these two variables was observed. In situ-loading of MXN achieved loading efficiencies in excess of 80%. Comparable efficiencies were achieved with postsynthesis loading when the microsphere were prepared from albumin-poly(glutamic acid) blends. In vitro release of MXN in phosphate buffered saline under infinite sink conditions showed that the total amount of drug released increased as the glutaraldehyde concentration decreased. This trend was reversed when the microspheres were incubated in plasma. Nanoparticles were also prepared using ethanol desolvation. These particles were dispersible in saline and easily modified with amino acids. In addition, particle size could be varied by use of different non-ionic surfactants in the preparation. The effect of intratumoral (IT) versus intravenous (IV) drug administration on tumor response and systemic toxicity was investigated in vivo using the 16/C murine mammary adenocarcinoma tumor model. The data suggested that IT-treated animals had significantly smaller tumors and lower weight loss when compared to IV-treated animals. Furthermore, the addition of surgery to the chemotherapy further improved the survival of the animals. Pilot studies using MXN-albumin microspheres suggested that microspheres could be safely administered IT in doses up to 48 mg/kg. However, there was no evidence that this higher dose resulted in improved long term survival when compared to the 32 mg/kg dose. The maximum tolerated dose of MAN given IT was approximately 12 mg/kg. The animal studies suggested

  5. Rheological Behavior of an Epoxy Resin with Hollow Glass Microspheres

    Science.gov (United States)

    Costa, Cleber C.; Calado, Verônica; Tavares, Frederico W.

    2008-07-01

    An investigation was carried out on the rheological behavior of a TET/DGEBA epoxy formulations with hollow glass microspheres using different types and different volume fractions of microspheres to manufacture composites. It was proposed an equation to describe viscosity as a function of microsphere volume fracion. The fit to the experimental data was excellent.

  6. 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.

  7. Polyacrolein microspheres

    Science.gov (United States)

    Rembaum, Alan (Inventor)

    1987-01-01

    Microspheres of acrolein homopolymers and copolymer with hydrophillic comonomers such as methacrylic acid and/or hydroxyethylmethacrylate are prepared by cobalt gamma irradiation of dilute aqueous solutions of the monomers in presence of suspending agents, especially alkyl sulfates such as sodium dodecyl sulfate. Amine or hydroxyl modification is achieved by forming adducts with diamines or alkanol amines. Carboxyl modification is effected by oxidation with peroxides. Pharmaceuticals or other aldehyde reactive materials can be coupled to the microspheres. The microspheres directly form antibody adducts without agglomeration.

  8. Effect of the formulation parameters on the encapsulation efficiency and release behavior of p-aminobenzoic acid-loaded ethylcellulose microspheres

    Directory of Open Access Journals (Sweden)

    Mouffok Meryem

    2016-01-01

    Full Text Available In the current study, p-aminobenzoic acid-loaded ethylcellulose microspheres were prepared under various conditions by solvent evaporation method (o/w. This preparation was carried out with different p-aminobenzoic acid:ethylcellulose (PABA:EC ratios, stirring speed, surfactant nature and concentration in order to investigate their effect on encapsulation efficiency and drug release kinetics. Scanning Electron Microscopy (SEM studies showed spherical microspheres with a porous surface and different structures. The mean diameter of Sauter (d32 of these microparticles is in the range from 47 to 165 μm with PVA and from 793 to 870 μm with Tween 80 by adjusting process parameters. However, the encapsulation efficiency varied from 37.52 to 79.05 % suitable for the adjustment of a p-aminobenzoic acid with pro-longed release. Microspheres were characterized by FTIR, DSC and XRD. The release of cation of p-aminobenzoic acid was performed in simulated gastric medium at pH 1.2 and 37±0.5°C by UV-VIS analysis to estimate its content. The release data were best fitted to Higuchi model with high correlation coefficient (r² and the obtained values of n from Korsmeyer-Peppas showed that the drug release follows the Fickian diffusion mechanism.

  9. Fluorescent microspheres

    Science.gov (United States)

    Rembaum, A.

    1978-01-01

    Latex particles with attached antibodies have potential biochemical and environmental applications. Human red blood cells and lymphocytes have been labeled with fluorescent microspheres by either direct or indirect immunological technique. Immunolatex spheres can also be used for detecting and localizing specific cell surface receptors. Hormones and toxins may also be bondable.

  10. Evaluation of glibenclamide microspheres for sustained release

    Directory of Open Access Journals (Sweden)

    Kambham Venkateswarlu

    2017-04-01

    Full Text Available Context: Sustained release drug delivery systems are more preferred than the conventional drug delivery systems due to its enhanced bioavailability and patient compliance. Earlier studies reported on glibenclamide (GBCM were not clear and hence, the step has been taken to explore the sustained release drug delivery system of GBCM. Aims: To evaluate the sustained release microspheres obtained of GBCM. Methods: Microspheres were prepared by ionic gelation method using the polymers like Eudragit RS 100 and xanthan gum. Polymers can sustain the drug release from microspheres. The prepared microspheres were subjected to micromeritic studies like Carr’s index, Hausner’s ratio and angle of repose. Results: Micromeritic studies confirmed that the microspheres possessing acceptable flow properties. It was observed from the in vitro release studies, formulations F8 and F9 showed sustained drug release for desired time of 12 h and when compared to F9, formulation F8 showed maximum drug release for 12 h. Conclusions: Results confirmed the formulation F8 consist of the polymers such as Eudragit RS 100 about 150 mg and xanthan gum about 100 mg showed desired sustained release of 12 h with 96.07% and kinetic studies confirmed that the release from microspheres followed non-Fickian diffusion mechanism. Due to its sustained release property, it could enhance the bioavailability of drug thereby improves the patient compliance and expect better treatment than conventional dosage forms.

  11. Hybrid microspheres

    Science.gov (United States)

    Rembaum, Alan (Inventor); Yen, Richard C. K. (Inventor)

    1985-01-01

    Substrates, particularly inert synthetic organic resin beads (10) or sheet (12) such as polystyrene are coated with a covalently bound layer (24) of polyacrolein by irradiation a solution (14) of acrolein or other aldehyde with high intensity radiation. Individual microspheres (22) are formed which attach to the surface to form the aldehyde containing layer (24). The aldehyde groups can be converted to other functional groups by reaction with materials such as hydroxylamine. Adducts of proteins such as antibodies or enzymes can be formed by direct reaction with the surface aldehyde groups.

  12. Rational design on controlled release ion-exchange polymeric microspheres and polymer-lipid hybrid nanoparticles for the delivery of water-soluble drugs through a multidisciplinary approach

    Science.gov (United States)

    Li, Yongqiang

    Sulfopropyl dextran sulfate (SP-DS) microspheres and polymer-lipid hybrid nanoparticles (PLN) for the delivery of water-soluble anticancer drugs and P-glycoprotein inhibitors were developed by our group recently and demonstrated effectiveness in local chemotherapy. To optimize the delivery performance of these particulate systems, particularly PLN, an integrated multidisciplinary approach was developed, based on an in-depth understanding of drug-excipient interactions, internal structure, drug loading and release mechanisms, and application of advanced modeling/optimization techniques. An artificial neural networks (ANN) simulator capable of formulation optimization and drug release prediction was developed. In vitro drug release kinetics of SP-DS microspheres, with various drug loading and in different release media, were predicted by ANN. The effects of independent variables on drug release were evaluated. Good modeling performance suggested that ANN is a useful tool to predict drug release from ion-exchange microspheres. To further improve the performance of PLN, drug-polymer-lipid interactions were characterized theoretically and experimentally using verapamil hydrochloride (VRP) as a model drug and dextran sulfate sodium (DS) as a counter-ion polymer. VRP-DS complexation followed a stoichiometric rule and solid-state transformation of VRP were observed. Dodecanoic acid (DA) was identified as the lead lipid carrier material. Based upon the optimized drug-polymer-lipid interactions, PLN with high drug loading capacity (36%, w/w) and sustained release without initial burst release were achieved. VRP remained amorphous and was molecularly dispersed within PLN. H-bonding contributed to the miscibility between the VRP-DS complex and DA. Drug release from PLN was mainly controlled by diffusion and ion-exchange processes. Drug loading capacity and particle size of PLN depend on the formulation factors of the weight ratio of drug to lipid and concentrations of

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

    Science.gov (United States)

    Deshmukh, Rameshwar K; Naik, Jitendra B

    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 12h. 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(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.

  14. Organic aerogel microspheres and fabrication method therefor

    Science.gov (United States)

    Mayer, Steven T.; Kong, Fung-Ming; Pekala, Richard W.; Kaschmitter, James L.

    1996-01-01

    Organic aerogel microspheres which can be used in capacitors, batteries, thermal insulation, adsorption/filtration media, and chromatographic packings, having diameters ranging from about 1 micron to about 3 mm. The microspheres can be pyrolyzed to form carbon aerogel microspheres. This method involves stirring the aqueous organic phase in mineral oil at elevated temperature until the dispersed organic phase polymerizes and forms nonsticky gel spheres. The size of the microspheres depends on the collision rate of the liquid droplets and the reaction rate of the monomers from which the aqueous solution is formed. The collision rate is governed by the volume ratio of the aqueous solution to the mineral oil and the shear rate, while the reaction rate is governed by the chemical formulation and the curing temperature.

  15. Con-A conjugated mucoadhesive microspheres for the colonic delivery of diloxanide furoate.

    Science.gov (United States)

    Anande, Nalini M; Jain, Sunil K; Jain, Narendra K

    2008-07-01

    The aim of the research work was to develop cyst-targeted novel concanavalin-A (Con-A) conjugated mucoadhesive microspheres of diloxanide furoate (DF) for the effective treatment of amoebiasis. Eudragit microspheres of DF were prepared using emulsification-solvent evaporation method. Formulations were characterized for particle size and size distribution, % drug entrapment, surface morphology and in vitro drug release in simulated gastrointestinal (GI) fluids. Eudragit microspheres of DF were conjugated with Con-A. IR spectroscopy and DSC were used to confirm successful conjugation of Con-A to Eudragit microspheres while Con-A conjugated microspheres were further characterized using the parameters of zeta potential, mucoadhesiveness to colonic mucosa and Con-A conjugation efficiency with microspheres. IR studies confirmed the attachment of Con-A with Eudragit microspheres. All the microsphere formulations showed good % drug entrapment (78+/-5%). Zeta potential of Eudragit microspheres and Con-A conjugated Eudragit microspheres were found to be 3.12+/-0.7mV and 16.12+/-0.5mV, respectively. Attachment of lectin to the Eudragit microspheres significantly increases the mucoadhesiveness and also controls the release of DF in simulated GI fluids. Gamma scintigraphy study suggested that Eudragit S100 coated gelatin capsule retarded the release of Con-A conjugated microspheres at low pH and released microspheres slowly at pH 7.4 in the colon.

  16. DEVELOPMENT AND OPTIMIZATION OF FLOATING MICROSPHERES OF GLICLAZIDE

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    Shardendu Prakash

    2015-05-01

    Full Text Available The objective of the present study was to develop floating microspheres of Gliclazide in order to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The present study involves preparation and evaluation of floating microspheres using Gliclazide as a model drug for prolongation of the gastric retention time. As gliclazide is mainly absorbed from stomach, thus using floating microspheres as a mode of drug delivery helps in increasing its residence time and hence increasing the bioavailability of drug. The microspheres were prepared by the Ionic gelation method. The average diameter and surface morphology of the prepared microspheres were characterized by optical microscope and scanning electron microscopic methods respectively. The prepared microspheres were evaluated for particle size, micromeritic study, drug entrapment efficiency, in vitro buoyancy, swelling index and in vitro release. The effect of various formulation variables on the size and drug release was also investigated. All the formulated microspheres were found to possess good flow properties. Scanning electron microscopy confirmed spherical structure of the prepared microspheres. The best formulation F3 drug release kinetics were evaluated using Zero order, First order, Higuchi model, Korsmeyer - Peppas model. After the interpretation of data that was based on the value of a resulting regression coefficient, it was observed that the Korsmeyer- Peppas model has a highest regression coefficient values indicating that the drug release was based on the erosion of polymeric chain matrix.

  17. Influence of different formulations and process parameters during the preparation of drug-loaded PLGA microspheres evaluated by multivariate data analysis

    Directory of Open Access Journals (Sweden)

    Vysloužil Jakub

    2014-12-01

    Full Text Available The main objective of this study was to evaluate the influence of the formulation and process parameters on PLGA microparticles containing a practically insoluble model drug (ibuprofen prepared by the o/w solvent evaporation method. Multivariate data analysis was used. The effects of altered stirring speed of a mechanical stirrer (600, 1000 rpm, emulsifier concentrations (PVA concentration 0.1 %, 1 % and solvent selection (dichloromethane, ethyl acetate on microparticle characteristics (encapsulation efficiency, drug loading, burst effect were observed. It was found that with increased stirring speed, the PVA concentration or the use of ethyl acetate had a significantly negative effect on encapsulation efficiency. In addition, ethyl acetate had an adverse effect on the burst effect, while increased stirring speed had the opposite effect. Drug load was not affected by any particular variable, but rather by the interactions of evaluated variables.

  18. Coacervate microspheres as carriers of recombinant adenoviruses.

    Science.gov (United States)

    Kalyanasundaram, S; Feinstein, S; Nicholson, J P; Leong, K W; Garver, R I

    1999-01-01

    The therapeutic utility of recombinant adenoviruses (rAds) is limited in part by difficulties in directing the viruses to specific sites and by the requirement for bolus administration, both of which limit the efficiency of target tissue infection. As a first step toward overcoming these limitations, rAds were encapsulated in coacervate microspheres comprised of gelatin and alginate followed by stabilization with calcium ions. Ultrastructural evaluation showed that the microspheres formed in this manner were 0.8-10 microM in diameter, with viruses evenly distributed. The microspheres achieved a sustained release of adenovirus with a nominal loss of bioactivity. The pattern of release and the total amount of virus released was modified by changes in microsphere formulation. Administration of the adenovirus-containing microspheres to human tumor nodules engrafted in mice showed that the viral transgene was transferred to the tumor cells. It is concluded that coacervate microspheres can be used to encapsulate bioactive rAd and release it in a time-dependent manner.

  19. 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

  20. Dextran-modified iron oxide nanoparticles

    Institute of Scientific and Technical Information of China (English)

    Ji(r)í Hradil; Alexander Pisarev; Michal Babi(c); Daniel Horák

    2007-01-01

    Dextran-modified iron oxide nanoparticles were prepared by precipitation of Fe(Ⅱ) and Fe(Ⅲ) salts with ammonium hydroxide by two methods.Iron oxide was precipitated either in the presence of dextran solution, or the dextran solution was added after precipitation. In the second method,the iron oxide particle size and size distribution could be controlled depending on the concentration of dextran in the solution. The nanoparticles were characterized by size-exclusion chromatography, transmission electron microscopy and dynamic light scattering. Optimal conditions for preparation of stable iron oxide colloid particles were determined. The dextran/iron oxide ratio 0-0.16 used in precipitation of iron salts can be recommended for synthesis of nanoparticles suitable for biomedical applications, as the colloid does not contain excess dextran and does not coagulate.

  1. Computational dynamics of acoustically-driven microsphere systems

    CERN Document Server

    Glosser, Connor A; Dault, Daniel L; Piermarocchi, Carlo; Shanker, Balasubramaniam

    2015-01-01

    We propose a computational framework for the self-consistent dynamics of a microsphere system driven by a pulsed acoustic field in an ideal fluid. Our framework combines a molecular dynamics integrator describing the dynamics of the microsphere system with a time-dependent integral equation solver for the acoustic field that makes use of fields represented as surface expansions in spherical harmonic basis functions. The presented approach allows us to describe the inter-particle interaction induced by the field as well as the dynamics of trapping in counter-propagating acoustic pulses. The integral equation formulation leads to equations of motion for the microspheres describing the effect of non-dissipative drag forces. We show (1) that the field-induced interactions between the microspheres give rise to effective dipolar interactions, with effective dipoles defined by their velocities, and (2) that the dominant effect of an ultrasound pulse through a cloud of microspheres gives rise mainly to a translation ...

  2. A review on target drug delivery:magnetic microspheres

    Institute of Scientific and Technical Information of China (English)

    Amit Chandna; Deepa Batra; Satinder Kakar; Ramandeep Singh

    2013-01-01

    Novel drug delivery system aims to deliver the drug at a rate directed by the needs of the body during the period of treatment, and target the active entity to the site of action.A number of novel drug delivery systems have emerged encompassing various routes of administration, to achieve controlled and targeted drug delivery, magnetic micro carriers being one of them. 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.

  3. 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.

  4. Effects of delayed transfer and treatment with oestrogen on the transport of microspheres by the rat oviduct.

    Science.gov (United States)

    Moore, G D; Croxatto, H B

    1988-07-01

    Starch or dextran blue microspheres were transferred microsurgically to the infundibulum of the oviduct on Days 1, 2, or 3 of pregnancy of control and oestradiol-treated rats. The animals were killed a few hours to several days after transfer to assess the number and distribution of ova and microspheres in the tract. After transfer on Day 1 of pregnancy, microspheres and eggs crossed the ampullary-isthmic junction (AIJ) 18 h after ovulation. After transfer on Day 2 of pregnancy, more than 50% of microspheres were retained in the ampulla, indicating that the AIJ changes again 34 h after ovulation. Treatment with oestradiol did not advance the passage of eggs or microspheres across the AIJ but caused accelerated transport through the isthmus as soon as the eggs or microspheres reached this segment. Dextran blue microspheres were seen to move back and forth in the isthmus of control anaesthetized rats at a frequency of 5-6 times/min. Between 7 and 20 h after treatment with oestradiol the frequency of these movements was significantly augmented, indicating that increased frequency of contractions of the smooth muscle of the isthmus precedes and accompanies accelerated transport of ova through this segment.

  5. 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).

  6. Computational dynamics of acoustically driven microsphere systems.

    Science.gov (United States)

    Glosser, Connor; Piermarocchi, Carlo; Li, Jie; Dault, Dan; Shanker, B

    2016-01-01

    We propose a computational framework for the self-consistent dynamics of a microsphere system driven by a pulsed acoustic field in an ideal fluid. Our framework combines a molecular dynamics integrator describing the dynamics of the microsphere system with a time-dependent integral equation solver for the acoustic field that makes use of fields represented as surface expansions in spherical harmonic basis functions. The presented approach allows us to describe the interparticle interaction induced by the field as well as the dynamics of trapping in counter-propagating acoustic pulses. The integral equation formulation leads to equations of motion for the microspheres describing the effect of nondissipative drag forces. We show (1) that the field-induced interactions between the microspheres give rise to effective dipolar interactions, with effective dipoles defined by their velocities and (2) that the dominant effect of an ultrasound pulse through a cloud of microspheres gives rise mainly to a translation of the system, though we also observe both expansion and contraction of the cloud determined by the initial system geometry.

  7. Study of mucoadhesive microsphere of pirfenidone for nasal drug delivery

    Directory of Open Access Journals (Sweden)

    Vrushali Kashikar

    2014-01-01

    Full Text Available The present research work involves formulation development and evaluation of nasal mucoadhesive microsphere in view to, improve bioavailability and reduce dosing regimen. Microspheres were prepared by spray drying and cross-linking method using chitosan and HPMC K4M, using 32 central composite design. Microspheres were evaluated for particle size, drug content, swelling ability, and percentage yield. Compatibility was checked by doing Fourier transform infrared spectroscopy and Differential scanning calorimetry study. The polymorphism and particle shape were studied by X-ray diffraction and scanning electron microscopy. The average particle size of spray-dried and cross-linked formulations were found in the range between 20-50 μm and 30-60 μm with percent mucoadhesion in the range of 80%-90% and 60-70%, respectively. In vitro drug release was found to be proportional to drug to polymer ratio. In vitro drug release for optimized formulation, that is, (F1, for spray-drying method and cross-linking method was found to be 88.73% and 70.93% at the end of 6 h, respectively. Release of drug from microspheres followed non-Fickian diffusion kinetics. Ex vivo studies were performed with sheep nasal mucosa for mucoadhesion, histopathological study, and drug permeation. The histopathological study indicates nonirritant nature of microsphere. The microspheres were found to be stable at accelerated storage conditions for 1 month, as per International Conference of Harmonisation guidelines.

  8. Dextran-modified iron oxide nanoparticles

    Institute of Scientific and Technical Information of China (English)

    Jií; Hradil

    2007-01-01

    [1]Anger,S.,Caldwell,K.,Mehnert,W.,& Muller,R.(1999).Coating of nanoparticles:Analysis of adsorption using sedimentation field-flow fractionation(SdFFF).Proceedings of International Symposium of Controlled Release of Bioactivated Materials,26,599-600.[2]Bonnemain,B.(1998).Superparamagnetic agents in magnetic resonance imaging:Physicochemical characteristics and clinical applications-A review.Journal of Drug Targeting,6(3),167-174.[3]Bootz,A.,Vogel,V.,Schubert,D.,& Kreuter,J.(2004).Comparison of scanning electron microscopy,dynamic light scattering and analytical ultracentrifugation for the sizing of poly(butyl cyanoacrylate) nanoparticles.European Journal of Pharmaceutics and Biopharmaceutics,57(2),369-375.[4]Browarzik,D.(1997).Continuous kinetics of dextran degradation.Journal of Macromolecular Science Pure and Applied Chemistry,34(3),397-404.[5]Cabasso,I.,& Yuan,Y.(1996).Nanoparticles in polymer and polymer dendrimers.In J.Fendler & I.Dekany (Eds.),NATO ASI Series.Part 18Nanoparticles in Solids and Solutions (pp.131-153).[6]Chastellain,M.,Petri,A.,& Hofmann,H.(2004).Particle size investigation of a multistep synthesis of PVA coated superparamagnetic nanoparticles.Journal of Colloid Interface Science,278(2),353-360.[7]Chmela,E.,Tijssen,R.,Blom,M.T.,Gardeniers,H.J.G.E.,& van den Berg,A.(2002).A chip system for size separation of macromolecules and particles by hydrodynamic chromatography.Analytical Chemistry,74(14),3470-3475.[8]Confer,D.R.,& Logan,B.E.(1997).Molecular weight distribution of hydrolysis product during the biodegradation of model macromolecules in suspended and biofilm cultures.Ⅱ:Dextran and dextrin.Water Research,31(9),2137-2145.[9]Griffiths,C.H.,O'Horo,M.P.,& Smith,T.W.(1979).The structure,magnetic characterization and oxidation of colloidal iron dispersions.Journal of Applied Physics,50(11),7108-7115.[10]Gupta,A.K.,& Gupta,M.(2005).Synthesis and surface engineering of iron oxide nanoparticles for biomedical applications.Biomaterials,26

  9. Making Polymeric Microspheres

    Science.gov (United States)

    Rhim, Won-Kyu; Hyson, Michael T.; Chung, Sang-Kun; Colvin, Michael S.; Chang, Manchium

    1989-01-01

    Combination of advanced techniques yields uniform particles for biomedical applications. Process combines ink-jet and irradiation/freeze-polymerization techniques to make polymeric microspheres of uniform size in diameters from 100 to 400 micrometer. Microspheres used in chromatography, cell sorting, cell labeling, and manufacture of pharmaceutical materials.

  10. Polymeric Microspheres for Medical Applications

    Directory of Open Access Journals (Sweden)

    Ketie Saralidze

    2010-06-01

    Full Text Available Synthetic polymeric microspheres find application in a wide range of medical applications. Among other applications, microspheres are being used as bulking agents, embolic- or drug-delivery particles. The exact composition of the spheres varies with the application and therefore a large array of materials has been used to produce microspheres. In this review, the relation between microsphere synthesis and application is discussed for a number of microspheres that are used for different treatment strategies.

  11. Microsphere Insulation Panels

    Science.gov (United States)

    Mohling, R.; Allen, M.; Baumgartner, R.

    2006-01-01

    Microsphere insulation panels (MIPs) have been developed as lightweight, longlasting replacements for the foam and vacuum-jacketed systems heretofore used for thermally insulating cryogenic vessels and transfer ducts. The microsphere core material of a typical MIP consists of hollow glass bubbles, which have a combination of advantageous mechanical, chemical, and thermal-insulation properties heretofore available only separately in different materials. In particular, a core filling of glass microspheres has high crush strength and low density, is noncombustible, and performs well in soft vacuum.

  12. Bilayer Tablet via Microsphere: A Review

    Directory of Open Access Journals (Sweden)

    Piyushkumar Vinubhai Gundaraniya

    2013-01-01

    Full Text Available The aim of the present work is to develop bilayer tablets containing sustained release microspheres as one layer and immediate release as another layer. The proposed dosage form is intended to decrease the dosing frequency and the combined administration of an anti-diabetic agent. Several pharmaceutical companies are currently developing bi-layer tablets, for a variety of reasons: patent extension, therapeutic, marketing to name a few. To reduce capital investment, quite often existing but modified tablet presses are used to develop and produce such tablets. One such approach is using microspheres as carriers for drugs also known as micro particles. It is the reliable means to deliver the drug to the target site with specificity, if modified, and to maintain the desired concentration at the site of interest. Microspheres received much attention not only for prolonged release, but also for targeting of anti-diabetic drugs. Bilayer tablet via microsphere is new era for the successful development of controlled release formulation along with various features to provide a way of successful drug delivery system. Especially when in addition high production output is required. An attempt has been made in this review article to introduce the society to the current technological developments in bilayer and floating drug delivery system.

  13. Evaluation of the Intestinal Colonizing Potential and Immunomodulating Capacity of Lactobacilli Microspheres.

    Science.gov (United States)

    Cotta, Karyn I; Addo, Richard T; D'Souza, Martin J

    2016-05-01

    Lactobacilli species get degraded by acidic conditions in the stomach. Thus, the objective of this study was to (1) formulate and characterize gastro-resistant Lactobacilli microspheres and (2) evaluate the ability of Lactobacilli microspheres to colonize the intestine and their capacity to have an immunomodulating effect in vivo. The product yield and the encapsulation efficiency were 45% and 100%, respectively. The average microsphere particle size was 5 μm. Lactobacilli microspheres were most stable at 4°C and showed a better suspendibility in distilled water. Without encapsulation, the viability of bacteria decreased within 30 min. In the case of Lactobacilli microspheres, no Lactobacilli were released in the first 3 h, and highest release was observed at 4 h, thus, suggesting the significance of encapsulation of Lactobacilli. Lactobacilli microspheres maintained intestinal colonization only during the dosing period, and the serum IgG, serum IgA, fecal, intestinal, nasal IgA, and the serum interleukin-1β levels were higher in the Lactobacilli microsphere group compared with the blank microsphere and the lactobacilli solution group, suggesting that the Lactobacilli microspheres were more gastro-resistant and, hence, showed positive effects compared with the Lactobacilli solution. However, the Lactobacilli microspheres did not have a significant effect on the tumor necrosis factor-α levels.

  14. In vitro-in vivo correlation of parenteral risperidone polymeric microspheres.

    Science.gov (United States)

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

    2015-11-28

    The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal® Consta® was used to prepare risperidone microspheres. Various manufacturing processes were investigated to produce the risperidone microspheres with similar drug loading (approx. 37%) but distinctly different physicochemical properties (e.g. porosity, particle size and particle size distribution). In vitro release of the risperidone microspheres was investigated using different release testing methods (such as sample-and-separate and USP apparatus 4). In vivo pharmacokinetic profiles of the risperidone microsphere formulations following intramuscular administration were determined using a rabbit model. Furthermore, the obtained pharmacokinetic profiles were deconvoluted using the Loo-Riegelman method and the calculated in vivo release was compared with the in vitro release of these microspheres. Level A IVIVCs were established and validated for the compositionally equivalent risperidone microspheres based on the in vitro release data obtained using USP apparatus 4. The developed IVIVCs demonstrated good predictability and were robust. These results showed that the developed USP apparatus 4 method was capable of discriminating PLGA microspheres that are equivalent in formulation composition but with manufacturing differences and predicting their in vivo performance in the investigated animal model.

  15. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    DEFF Research Database (Denmark)

    Guo, Wenjia; Quan, Peng; Fang, Liang

    2015-01-01

    The purpose of this study was to develop a PLGA microspheres-based donepezil (DP) formulation which was expected to sustain release of DP for one week with high encapsulation efficiency (EE). DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion......-solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared...... was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model, which suggested the diffusion governing...

  16. Development of enteric-coated microspheres of embelin for their beneficial pharmacological potential in ulcerative colitis.

    Science.gov (United States)

    Nidhi; Dadwal, Ankita; Hallan, Supandeep Singh; Sharma, Saurabh; Mishra, Neeraj

    2017-09-01

    The aim of the present study is to develop embelin-loaded enteric-coated microspheres and investigate their pharmacological potential in acetic acid induced ulcerative colitis. The optimized formulation of embelin-loaded microspheres has shown significant sustained release of embelin. Further this formulation significantly reduced the ulcer activity score and oxidative stress, and attenuated the inflammatory changes. Thus it may be concluded that embelin-loaded enteric-coated microspheres have shown delayed release capacity than plain embelin and exerts colon ulcer protective effect in rats.

  17. Encapsulation of Liposomes within pH Responsive Microspheres for Oral Colonic Drug Delivery

    Directory of Open Access Journals (Sweden)

    M. J. Barea

    2012-01-01

    Full Text Available A novel liposome-in-microsphere (LIM formulation has been created comprising drug-loaded liposomes within pH responsive Eudragit S100 microspheres. The liposomes contained the model drug 5-ASA and were coated with chitosan in order to protect them during encapsulation within the microspheres and to improve site-specific release characteristics. In vitro drug release studies showed that LIMs prevented drug release within simulated stomach and small intestine conditions with subsequent drug release occurring in large intestine conditions. The formulation therefore has potential for oral colonic drug delivery.

  18. Development and evaluation of sustained-release ibuprofen-wax microspheres. II. In vitro dissolution studies.

    Science.gov (United States)

    Adeyeye, C M; Price, J C

    1994-04-01

    A modified USP paddle method using minibaskets was used to study the effects of various formulations on in vitro dissolution of ibuprofen microspheres. Formulations containing waxes such as paraffin or ceresine wax without modifiers exhibited very slow dissolution profiles and incomplete release, which did not improve with increased drug loading or the preparation of smaller microspheres. The addition of modifiers such as stearyl alcohol and glyceryl monostearate greatly increased the dissolution rate, with 20% (w/w) near the optimum for predictable dissolution. Higher drug loading and decreased microsphere size increased the dissolution rate from microspheres containing modifier. Optimum formulations contained ceresine wax or microcrystalline wax and stearyl alcohol as a modifier, with a drug content of 17%. An increase in the encapsulation dispersant concentration had little effect on the dissolution profiles. The dissolution data from narrow size fractions of microspheres indicated spherical matrix drug release kinetics; the 50% dissolution time decreased with the square of the microsphere diameter. With appropriate modifiers, wax microsphere formulations of drugs with solubility characteristics similar to those of ibuprofen can offer a starting basis for predictable sustained release dosage forms.

  19. Hydrogel microspheres from biodegradable polymers as drug delivery systems

    Science.gov (United States)

    A series of hydrogel microspheres were prepared from pectin, a hydrophilic biopolymer, and zein, a hydrophobic biopolymer, at varying weight ratios. The hydrogel formulation was conducted in the presence of calcium or other divalent metal ions at room temperature under mild conditions. Studies of ...

  20. Melatonin-loaded chitosan/Pluronic® F127 microspheres as in situ forming hydrogel: An innovative antimicrobial wound dressing.

    Science.gov (United States)

    Romić, Marieta Duvnjak; Klarić, Maja Šegvić; Lovrić, Jasmina; Pepić, Ivan; Cetina-Čižmek, Biserka; Filipović-Grčić, Jelena; Hafner, Anita

    2016-10-01

    The aim of this study was to develop melatonin-loaded chitosan based microspheres as dry powder formulation suitable for wound dressing, rapidly forming hydrogel in contact with wound exudate. Microspheres were produced by spray-drying method. Fractional factorial design was employed to elucidate the effect of formulation and process parameters (feed flow rate, inlet air temperature, chitosan concentration, chitosan/melatonin ratio and chitosan/Pluronic® F127 ratio) on the product characteristics related to process applicability (production yield, entrapment efficiency and product moisture content) and microsphere performance in biological environment (microsphere mean diameter and surface charge). Appropriate formulation and process parameters for the establishment of efficient drying process resulting in fine-tuned chitosan and chitosan/Pluronic® F127 microspheres (efficient melatonin encapsulation, small diameter positive surface charge and low moisture content) were identified. Microspheres were characterized by appropriate flowability and high rate and extent of fluid uptake. Incorporation of Pluronic® F127 in microsphere matrix resulted in high melatonin amorphization and consequent higher melatonin release rate. Entrapment of melatonin in chitosan/Pluronic® F127 microspheres has potentiated chitosan antimicrobial activity against Staphylococcus aureus and five clinical isolates S. aureus MRSA strains. Microspheres were shown to be biocompatible with skin keratinocytes and fibroblasts at concentrations relevant for antimicrobial activity against planktonic bacteria.

  1. Development and evaluation of biodegradable microspheres embedded in in situ gel for controlled delivery of hydrophilic drug for treating oral infections: In vitro and in vivo studies

    Directory of Open Access Journals (Sweden)

    Neha Manish Munot

    2014-01-01

    Full Text Available Present investigation was aimed at developing biodegradable polymeric microspheres of Tetracycline hydrochloride to treat oral infections by using Poly (D, L lactic-co-glycolic acid (50:50 as polymer. Microspheres were prepared using oil-in-oil (O/O and water-in-oil-in-water (W/O/W double emulsion solvent evaporation method. Microspheres prepared by W/O/W were spherical in shape compared those prepared with O/O method. Thus, the microspheres formulated by W/O/W method were further evaluated for particle size, morphology, entrapment efficiency, and percent drug release. Effects of salt addition, polymer concentration on the characteristics of microspheres and tetracycline release profile were investigated. An increase in polymer concentration decreased drug release and increased entrapment efficiency of drug. In vitro studies indicated that release of drug from microspheres could be controlled for 10-15 days depending on drug: Polymer concentration. Formulation E released 99.10% of drug from microspheres in 10 days. Addition of sodium chloride to outer aqueous phase produced spherical microspheres with smooth surface and also increased entrapment efficiency. Microspheres were further dispersed in optimized formulation of mucoadhesive in situ gel of Pluronic F127, which acts as carrier for microspheres. In vivo studies were conducted on patients who underwent molar tooth extraction to check efficacy of designed formulation.

  2. 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.

  3. Doppler cooling a microsphere

    CERN Document Server

    Barker, P F

    2010-01-01

    Doppler cooling the center-of-mass motion of an optically levitated microsphere via the velocity dependent scattering force from narrow whispering gallery mode (WGM) resonances is described. Light that is red detuned from the WGM resonance can be used to damp the center-of-mass motion in a process analogous to the Doppler cooling of atoms. Leakage of photons out of the microsphere when the incident field is near resonant with the narrow WGM resonance acts to damp the motion of the sphere. The scattering force is not limited by saturation, but can be controlled by the incident power. Cooling times on the order of seconds are calculated for a 20 micron diameter silica microsphere trapped within optical tweezers, with a Doppler temperature limit in the microKelvin regime.

  4. Factors that Interfere in Dextran Production By Sugarcane Contaminating Microorganisms

    Directory of Open Access Journals (Sweden)

    Maria Celia Oliveira Hauly

    2002-01-01

    Full Text Available Dextrans are polysaccharides produced by microorganisms, specially bacterias from the Leuconostoc genus. Dextrans have a high molecular weigh and most of the glycosidic bonds are a(1®6. For the sugar manufacture, dextran is a problem which changes the quality of sugar and the industry efficiency. Dextrans are synthesized when the sugarcane is spoiled before the harvest period, through the sugarcane fissures, which permit the penetration of microorganisms that deteriorate the sugarcane. This work aims at improving the sugar quality and the industry efficiency by isolating dextran producing microorganisms, comparing the time of burning with the infection index and the dextran concentration in the sugarcane juice. Dextran producing microorganisms were isolated from sugarcane juice during the 97/98; 99/00 and 2001 harvests. The isolated strains were maintained in MRS agar at the temperature of 4°C. The fermentation was carried out in MRS broth for 72 hours at 28°C with 180 rpm. Dextran was analyzed by spectrophotometry at 485 nm. Only three isolated strains showed good dextran production. The average of dextran production in MRS broth was 390 mg%. It was observed that a burning period above 72 hours increases the sugarcane contamination and causes high dextran production, and consequently the reduction of the industry efficiency of the sugar factory.

  5. Doped zinc oxide microspheres

    Science.gov (United States)

    Arnold, Jr., Wesley D.; Bond, Walter D.; Lauf, Robert J.

    1993-01-01

    A new composition and method of making same for a doped zinc oxide microsphere and articles made therefrom for use in an electrical surge arrestor which has increased solid content, uniform grain size and is in the form of a gel.

  6. Polyvinyl pyridine microspheres

    Science.gov (United States)

    Rembaum, Alan (Inventor); Gupta, Amitava (Inventor); Volksen, Willi (Inventor)

    1980-01-01

    Microspheres are produced by cobalt gamma radiation initiated polymerization of a dilute aqueous vinyl pyridine solution. Addition of cross-linking agent provides higher surface area beads. Addition of monomers such as hydroxyethylmethacrylate acrylamide or methacrylamide increases hydrophilic properties and surface area of the beads. High surface area catalytic supports are formed in the presence of controlled pore glass substrate.

  7. Factorial design approach for optimization of floating microspheres of diltiazem hydrochloride

    Directory of Open Access Journals (Sweden)

    Mangal Singh Panwar

    2015-01-01

    Full Text Available The aim of this study was to perform optimization of floating microspheres of diltiazem hydrochloride for the prolongation of gastric residence time. The microspheres were prepared by a nonaqueous solvent evaporation method using polycarbonate. A full factorial design was applied to optimize the formulation. Preliminary studies revealed that the concentration of polymer and stirring speed significantly affected the characteristics of floating microspheres. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 10 h, high entrapment efficiency up to 97% w/w. Scanning electron microscopy confirmed the hollow structure with particle size in the order of 190 μm. The studies revealed that the increase in concentration of polycarbonate increased the drug release from the floating microspheres. The results of two third full factorial design revealed that the concentration of polycarbonate (X1 and stirring speed (X2 significantly affected drug entrapment efficiency, percentage release.

  8. PLGA Microspheres Incorporated Gelatin Scaffold: Microspheres Modulate Scaffold Properties

    OpenAIRE

    Indranil Banerjee; Debasish Mishra; Maiti, Tapas K.

    2009-01-01

    Freeze drying is one of the popular methods of fabrication for poly(lactide-co-glycolide) (PLGA) microspheres incorporated polymer scaffolds. However, the consequence of microspheres incorporation on physical and biological properties of scaffold has not been studied yet. In this study, attempt has been made to characterize the effect of PLGA microsphere incorporation on the physical properties of freeze-dried gelatin scaffold and its influence on cytocompatibility. Scaffolds loaded with va...

  9. Ultrasonic atomization for spray drying: a versatile technique for the preparation of protein loaded biodegradable microspheres.

    Science.gov (United States)

    Bittner, B; Kissel, T

    1999-01-01

    Bovine serum albumin (BDA) loaded microspheres with a spherical shape and smooth surface structure were successfully prepared from poly(lactide-co-glycolide) using an ultrasonic nozzle installed in a Niro laboratory spray dryer. Process and formulation parameters were investigated with respect to their influence on microsphere characteristics, such as particle size, loading capacity, and release properties. Preparation of microspheres in yields of more than 50% was achieved using an ultrasonic atomizer connected to a stream of carrier air. Microsphere characteristics could be modified by changing several technological parameters. An increased polymer concentration of the feed generated larger particles with a significantly reduced initial release of the protein. Moreover, microspheres with a smooth surface structure were obtained from the organic polymer solution with the highest viscosity. Microparticles with a low BSA loading showed a large central cavity surrounded by a thin polymer layer in scanning electron microspheres. A high protein loading led to an enlargement of the shell layer, or even to dense particles without any cavities. A continuous in vitro release pattern of BSA was obtained from the particles with low protein loading. Glass transition temperatures (Tg) of the microspheres before and after lyophilization did not differ from those of the BSA loaded particles prepared by spray drying with a rotary atomizer. Analysis of the polymer by gel permeation chromatography indicated that ultrasonication had no effect on polymer molecular weight. Molecular weight and polydispersity of the pure polymer, placebo microspheres prepared by spray drying, and placebo microspheres prepared using the ultrasonic nozzle were in the same range. In conclusion, ultrasonic atomization represents a versatile and reliable technique for the production of protein loaded biodegradable microspheres without inducing a degradation of the polymer matrix. Particle characteristics

  10. Biodegradable polylactide microspheres enhance specific immune response induced by Hepatitis B surface antigen.

    Science.gov (United States)

    Qiu, Shaohui; Wei, Qiang; Liang, Zhenglun; Ma, Guanghui; Wang, Lianyan; An, Wenqi; Ma, Xiaowei; Fang, Xin; He, Peng; Li, Hemin; Hu, Zhongyu

    2014-01-01

    Hepatitis B (HB) infection caused by Hepatitis B virus (HBV) is the most common liver disease in the world. HB vaccine, when administered in conjunction with alum adjuvants, induces Th2 immunity that confers protection against HBV. However, currently available vaccine formulations and adjuvants do not elicit adequate Th1 and CTL responses that are important for prevention of maternal transmission of the virus. Microspheres synthesized from poly (D, L-lactide-co-glycolide) (PLGA) or poly (D, L-lactide) (PLA) polymers have been considered as promising tools for in vivo delivery of antigens and drugs. Here we describe PLA microspheres synthesized by premix membrane emulsification method and their application in formulating a new microsphere based HB vaccine. To evaluate the immunogenicity of this microsphere vaccine, BALB/c mice were immunized with microsphere vaccine and a series of immunological assays were conducted. Results of Enzyme-linked ImmunoSpot (ELISPOT) assays revealed that the number of interferon-gamma (IFN-γ)-producing splenocytes and CD8(+) T cells increased significantly in the microsphere vaccine group. Microsphere vaccine group showed enhanced specific cell lysis when compared with HB surface antigen (HBsAg) only group in (51)Cr cytotoxicity assays. Moreover, microsphere vaccine elicited a comparable level of antibody production as that of HB vaccine administered with alum adjuvant. We show that phagocytosis of HBsAg by dendritic cells is more pronounced in microsphere vaccine group when compared with other control groups. These results clearly demonstrate the potential of using PLA microspheres as effective HB vaccine adjuvants for an enhanced Th1 immune response.

  11. Protein microspheres as suitable devices for piroxicam release.

    Science.gov (United States)

    Silva, Raquel; Ferreira, Helena; Carvalho, Ana C; Gomes, Andreia C; Cavaco-Paulo, Artur

    2012-04-01

    Bovine serum albumin-piroxicam (BSA-piroxicam) and human serum albumin-piroxicam (HSA-piroxicam) microspheres were sonochemically prepared and characterized. The use of polyvinyl alcohol (PVA) lead to an improvement of formulation characteristics, including smaller size, lower polydispersity index (PDl), higher entrapment efficiency and higher stability. The release kinetics of these proteinaceous microspheres was determined in presence of protease, indicating an anomalous drug transport mechanism (diffusion and polymer degradation). In presence of higher protease concentration, BSA microspheres exhibit Case II transport, leading to zero order release (protein degradation). These proteinaceous devices did not show cytotoxicity against human skin fibroblasts in vitro, for range concentrations below to 300 mg L(-1), greatly supporting their potential application in the treatment of inflammatory diseases.

  12. Dextran: A promising macromolecular drug carrier

    Directory of Open Access Journals (Sweden)

    Dhaneshwar Suneela

    2006-01-01

    Full Text Available Over the past three decades intensive efforts have been made to design novel systems able to deliver the drug more effectively to the target site. The ongoing intense search for novel and innovative drug delivery systems is predominantly a consequence of the well-established fact that the conventional dosage forms are not sufficiently effective in conveying the drug compound to its site of action and once in the target area, in releasing the active agent over a desired period of time. The potential use of macromolecular prodrugs as a means of achieving targeted drug delivery has attracted considerable interest in recent years. Macromolecules such as antibodies, lipoproteins, lectins, proteins, polypeptides, polysaccharides, natural as well as synthetic polymers offer potential applicabilities as high molecular weight carriers for various therapeutically active compounds. Dextrans serve as one of the most promising macromolecular carrier candidates for a wide variety of therapeutic agents due to their excellent physico-chemical properties and physiological acceptance. The present contribution attempts to review various features of the dextran carrier like its source, structural and physico-chemical characteristics, pharmacokinetic fate and its applications as macromolecular carrier with special emphasis on dextran prodrugs.

  13. Chemical, dissolution stability and microscopic evaluation of suspensions of ibuprofen and sustained release ibuprofen-wax microspheres.

    Science.gov (United States)

    Adeyeye, C M; Price, J C

    1997-01-01

    Chemical stability studies of suspensions of ibuprofen powder and ibuprofen-wax microspheres were performed using an accelerated stability protocol with a modified high performance liquid chromatography (HPLC) procedure. The variables considered were pH, suspending agents and temperature. The study showed little or no chemical degradation in the different suspending agents after storage for three months. Dissolution stability was examined in suspensions of ibuprofen microspheres made from an optimized formulation with 17% drug loading. The storage temperature were 23, 37 and 45 degrees C. Other variables for the dissolution stability studies were suspending agents, wax types, suspending medium pH and microsphere size. Suspensions of ceresine wax microspheres stored at 37 degrees C showed faster drug release than room temperature storage, but suspensions stored at 45 degrees C showed an opposite effect. Microspheres suspended in syrup and stored at 37 degrees C had faster dissolution rates than microspheres suspended in methylcellulose at the same temperature, possibly as a result of an interaction between the syrup and the microsphere constituents. Suspensions of microcrystalline wax microspheres had better dissolution stability than microspheres made from ceresine wax. Higher suspending medium pH resulted in faster release of drug from the suspended microspheres, but particle size did not significantly affect the dissolution stability.

  14. Docetaxel-Loaded Chitosan Microspheres as a Lung Targeted Drug Delivery System: In Vitro and in Vivo Evaluation

    Directory of Open Access Journals (Sweden)

    Hao Wang

    2014-02-01

    Full Text Available The aim of this study was to prepare docetaxel-loaded chitosan microspheres and to evaluate their in vitro and in vivo characteristics. Glutaraldehyde crosslinked microspheres were prepared using a water-in-oil emulsification method, and characterized in terms of the morphological examination, particle size distribution, encapsulation ratio, drug-loading coefficient and in vitro release. Pharmacokinetics and biodistribution studies were used to evaluate that microspheres have more advantage than the conventional formulations. The emulsion crosslinking method was simple to prepare microspheres and easy to scale up. The formed microspheres were spherical in shape, with a smooth surface and the size was uniform (9.6 ± 0.8 µm; the encapsulation efficiency and drug loading of prepared microspheres were 88.1% ± 3.5% and 18.7% ± 1.2%, respectively. In vitro release indicated that the DTX microspheres had a well-sustained release efficacy and in vivo studies showed that the microspheres were found to release the drug to a maximum extent in the target tissue (lung. The prepared microspheres were found to possess suitable physico-chemical properties and the particle size range. The sustained release of DTX from microspheres revealed its applicability as drug delivery system to minimize the exposure of healthy tissues while increasing the accumulation of therapeutic drug in target sites.

  15. Efeito da adição de polietilenoglicóis nas formulações de microesferas de acetobutirato de celulose sobre a eficiência de encapsulação da carbamazepina e morfologia das partículas Effect of polyethylene glycols addition in microsphere formulations of cellullose acetate butyrate on efficacy carbamazepine and particles morphology encapsulation

    Directory of Open Access Journals (Sweden)

    Betina Giehl Zanetti

    2002-06-01

    did not affect the drug content in the microspheres. Most porous particles werw observed by SEM when PEG 1500 or 4000 was added to the formulations, however the lost of the spherical shape of the particles was verified when an ABC70:PEG 4000 1:1 mixture was used to prepare the microspheres. The addition of PEGs did not appear to affect the mean diameter of the particles. The decrease of the CBZ content was related to the PEG extraction during the solvent evaporation step and to its ability to dissolve the CBZ in the external phase of the emulsion. The porosity development control, by adjusting the amount or the molecular weight of PEG, can be useful in the drug release from microparticles.

  16. Preparation of Bauxite Ceramic Microsphere

    Institute of Scientific and Technical Information of China (English)

    CHENG Xiaosu; LIU Pingan; LI Xiuyan; SHUI Anze; ZENG Lingke

    2007-01-01

    Ceramic microspheres were prepared by using Chinese bauxite as raw materials through the centrifugal spray drying method. The control technology of microsphere size, degree of sphericity was researched. The ceramic microspheres were sintered by a double sintering process. The microstructure and composition of ceramic microsphere were investigated by X-ray diffraction (XRD), scanning electron microscopy (SEM) and X-ray energy spectroscopy. The results show that the degree of sphericity of the ceramic microsphere was good and the particle size was 10-100 μm. The XRD analysis reveals that the main crystalline phase of the ceramic microsphere was α- Al2O3 and mullite (3Al2O3·2SiO2). The product can be used as reinforced material for composite material, especially for antiskid and hard wearing aluminum alloy coating.

  17. Liraglutide-loaded poly(lactic-co-glycolic acid) microspheres: Preparation and in vivo evaluation.

    Science.gov (United States)

    Wu, Junzi; Williams, Gareth R; Branford-White, Christopher; Li, Heyu; Li, Yan; Zhu, Li-Min

    2016-09-20

    In this work, we sought to generate sustained-release injectable microspheres loaded with the GLP-1 analogue liraglutide. Using water-in-oil-in-water double emulsion methods, poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with liraglutide were prepared. The microspheres gave sustained drug release over 30days, with cumulative release of up to 90% reached in vitro. The microspheres were further studied in a rat model of diabetes, and their performance compared with a group given daily liraglutide injections. Reduced blood sugar levels were seen in the microsphere treatment groups, with the results being similar to those obtained with conventional injections between 10 and 25days after the commencement of treatment. After 5 and 30days of treatment, the microspheres seem a little slower to act than the injections. The pathology of the rats' spleen, heart, kidney and lungs was probed after the 30-day treatment period, and the results indicated that the microspheres were safe and had beneficial effects on the liver, reducing the occurrence of fatty deposits seen in untreated diabetic rats. Moreover, in terms of liver, renal and cardiac functions, and blood lipid and antioxidant levels, the microspheres were as effective as the injections. The expression of several proteases linked to the metabolism of aliphatic acids and homocysteine was promoted by the microsphere formulations. Inflammatory markers in the microsphere treatment groups were somewhat higher than the injection group, however. The liraglutide/PLGA microspheres prepared in this work are overall shown to be efficacious in a rat model of diabetes, and we thus believe they have strong potential for clinical use.

  18. Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine.

    Science.gov (United States)

    Szekalska, Marta; Amelian, Aleksandra; Winnicka, Katarzyna

    2015-03-01

    The present study is aimed at formulation of alginate (ALG) microspheres with ranitidine (RNT) by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers--gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9%. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach.

  19. Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine

    Directory of Open Access Journals (Sweden)

    Szekalska Marta

    2015-03-01

    Full Text Available The present study is aimed at formulation of alginate (ALG microspheres with ranitidine (RNT by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers - gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9 %. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach

  20. Design and Characterization of Colon Targeted Tegaserod Microspheres by Ionotropic Gelation.

    Directory of Open Access Journals (Sweden)

    Nemade M. S.

    2015-11-01

    Full Text Available The aim of study was to develop and evaluate tegaserod maleate (TM microspheres for colonic drug delivery system. Microspheres of TM were prepared by with little modification in the ionotropic gelation method by using polymer tamarind seed polysaccharide (TSP. These microspheres were evaluated for angle of repose, bulk density, tapped density, particle size, percentage drug entrapment, swelling behavior and in-vitro drug release studies. All the micrometric properties of the microsphere were within the range. The mean particle size of prepared microspheres was found to be in a range of 715.66 - 747.00 μm. Percentage drug entrapment observed in all formulations was between 74.03 - 76.69 %. The % water uptake in the pH 1.2 and pH 7.8 was between 69.66 - 73.33 and 181 - 192 respectively. In-vitro drug release studies showed that the release of tegaserod maleate from the microspheres was mainly influenced by the polymer concentration. Among all the formulations, F1 and F3 shows 94.98 and 88.52% better controlled release at the end of 12 hr respectively. The results indicated that a decrease in release of the drug was observed by increasing the polymer concentration. It is concluded from the present investigation that TM loaded microspheres were promising controlled release carriers for colon targeted delivery.

  1. Lectin-conjugated microspheres for eradication of Helicobacter pylori infection and interaction with mucus.

    Science.gov (United States)

    Adebisi, Adeola O; Conway, Barbara R

    2014-08-15

    Using second generation mucoadhesives may enhance targeting antibiotics for eradication of Helicobacter pylori from the stomach for the treatment of peptic ulcer. The aim of this research was to prepare and characterise ethylcellulose/chitosan microspheres containing clarithromycin with their surfaces functionalised with concanavalin A to produce a floating-mucoadhesive formulation. The microspheres were prepared using an emulsification-solvent evaporation method. Particle size, surface morphology, in vitro buoyancy profile, zeta potential, drug entrapment efficiency, in vitro drug release and release kinetics of the particles were determined. Lectin was conjugated to the microsphere surface using two-stage carbodiimide activation and confirmed using FTIR, fluorescence studies and zeta potential measurements. Conjugation ranged from 11 to 15 μg Con A/mg microspheres which represents over 56% efficiency although there was some drug loss during the conjugation process. Conjugation did not have a significant effect on the buoyancy and release of drug from the microspheres using a mucus diffusion model with 53% and 40% of drug released from unconjugated and conjugated microspheres within 12h. Conjugation improved mucoadhesion and interaction with porcine gastric mucin compared to unconjugated microspheres. The buoyancy and improved mucoadhesion of the microspheres provides potential for delivery of clarithromycin and other drugs to the stomach.

  2. Preparation and evaluation of waxes/fat microspheres loaded with lithium carbonate for controlled release

    Directory of Open Access Journals (Sweden)

    Gowda D

    2007-01-01

    Full Text Available To minimize the unwanted toxic effects of anti maniac drug lithium carbonate by kinetic control of drug release, it was entrapped into gastro resistant, biodegradable, waxes and fat such as beeswax, cetostearyl alcohol, spermaceti and cetylalcohol microspheres using meltable emulsified dispersion cooling induced solidification technique utilizing a wetting agent. Solid, discrete, reproducible free flowing microspheres were obtained. The yield of the microspheres was up to 90.0%. More than 98.0% of the isolated microspheres were of particle size range 115 to 855 mm. The microspheres had smooth surfaces, with free flowing and good packing properties. Scanning electron microscope confirmed their spherical structures within a size range of 339-355 mm. The drug loaded in waxes and fat microspheres was stable and compatible, as confirmed by DSC and FTIR studies. The release of drug was controlled for more than 8 hours. Intestinal drug release from waxes/ fat microspheres was studied and compared with the releases behavior of commercially available formulation Intalith CR ®-450. The release kinetics followed different transport mechanisms. The drug release performance was greatly affected by the materials used in microsphere preparations, which allows absorption in the intestinal tract.

  3. In Vitro-In Vivo Correlation of Parenteral Risperidone Polymeric Microspheres

    OpenAIRE

    2015-01-01

    The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal® Consta® was used to prepare risperidone microspheres. Various manufacturing processe...

  4. Functional magnetic microspheres

    Science.gov (United States)

    Yen, Shiao-Ping S. (Inventor); Rembaum, Alan (Inventor); Landel, Robert F. (Inventor)

    1981-01-01

    Functional magnetic particles are formed by dissolving a mucopolysaccharide such as chitosan in acidified aqueous solution containing a mixture of ferrous chloride and ferric chloride. As the pH of the solution is raised magnetite is formed in situ in the solution by raising the pH. The dissolved chitosan is a polyelectrolyte and forms micelles surrounding the granules at pH of 8-9. The chitosan precipitates on the granules to form microspheres containing the magnetic granules. On addition of the microspheres to waste aqueous streams containing dissolved ions, the hydroxyl and amine functionality of the chitosan forms chelates binding heavy metal cations such as lead, copper, and mercury and the chelates in turn bind anions such as nitrate, fluoride, phosphate and borate.

  5. In-vivo evaluation in rats of colon-specific microspheres containing 5-fluorouracil.

    Science.gov (United States)

    Rahman, Ziyaur; Kohli, Kanchan; Zhang, Shuang-Qing; Khar, Roop K; Ali, Mushir; Charoo, Naseem A; Tauseef, Mohammad; Shamsher, Areeg A A; Mohammed, Noorullah N; Repka, Michael A

    2008-05-01

    The aims of this investigation were to determine the distribution in the gastrointestinal (GI) tract of Eudragit S-100 encapsulated colon-specific sodium alginate microspheres containing 5-fluorouracil (5-FU) in rats, and to perform pharmacokinetic and pharmacodynamic studies. Comparisons were with a control immediate-release (IR) formulation of 5-FU. 5-FU was distributed predominantly in the upper GI tract from the IR formulation but was distributed primarily to the lower part of the GI tract from the microsphere formulation. No drug was released in the stomach and intestinal regions from the colon-specific microspheres. Significantly, a high concentration of the active drug was achieved in colonic tissues from the colon-specific microspheres (P IC50 required to halt the growth of and/or kill colon cancer cells. Colon cancer was induced in rats by subcutaneous injection of 1,2-dimethylhydrazine (40 mg kg (-1)) for 10 weeks. The tumours induced were non-invasive adenocarcinomas and were in Duke's stage A. The 5-FU formulations were administered for 4 weeks after tumour induction. Non-significant reductions in tumour volume and multiplicity were observed in animals given the colon-specific microspheres. Enhanced levels of liver enzymes (SGOT, SGPT and alkaline phosphatase) were found in animals given the IR formulation of 5-FU, and values differed significantly (P 5-FU to colonic tissues, with reduced systemic side-effects. A long-term dosing study is required to ascertain the therapeutic benefits.

  6. Mucoadhesive microspheres of propranolol hydrochloride for nasal delivery

    Directory of Open Access Journals (Sweden)

    Dandagi P

    2007-01-01

    Full Text Available Gelatin A microspheres of propranolol hydrochloride for intranasal systemic delivery were developed with the aim to avoid first pass metabolism, to improve the patient compliance, to use an alternative therapy to conventional dosage form, to achieve controlled blood level profiles, and to improve the therapeutic efficacy of propranolol hydrochloride in the treatment of various cardiovascular disorders and as a prophylactic for migraine. Gelatin A microspheres were prepared by emulsion crosslinking method using glutaradehyde as a crosslinking agent. Gelatin and chitosan were used as polymer and co polymer respectively. All the prepared microspheres were evaluated for physical characteristics, such as particle size, incorporation efficiency, swelling index, in vitro bioadhesion using rat jejunum and in vitro drug release in pH 6.6 phosphate buffer. Average particle size of microspheres was found to be in the size range 1-50 mm. Increase in drug and polymer concentration in the formulation increased incorporation efficiency. All the microsphers showed good bioadhesive properties and swelling indices and good sustained release of drug. The data indicates that propranolol hydrochloride release followed Higuchi′s matrix and Peppa′s model. Stability studies showed stability of formulation at all the conditions to which they were subjected.

  7. MICROSPHERIC IN-SITU GEL FOR OCULAR DRUG DELIVERY SYSTEM OF BROMFENAC SODIUM

    Directory of Open Access Journals (Sweden)

    PRERANA VENGURLEKAR

    2014-04-01

    Full Text Available Purpose: The aim of the study was to develop a sustained release microspheric in-situ gel for bromfenac sodium (BNa to be administered through ocular route. It was prepared for the treatment of post-operative cataract surgery. It increases the therapeutic efficiency, reduces dosing frequency and prolonged duration of action. Methods: Albumin microspheres were prepared by protein gelation process and dispersed into in-situ gel, which was prepared by pH triggered method. Result and conclusion: The particle size analysis revealed that all formulations gave particles size in the range of 1-10 μm which is suitable for ocular administration of formulation. The entrapment efficiency of microspheres was found to be 84.2% and drug release from microspheres were found to be 80.558 % at 24 h. The microspheric in-situ gel of optimized formulation shows drug release of 77.989% at the end of 24 hours. Stability studies were conducted. Hence, it can be concluded that microsphere in-situ gels were a viable alternative to conventional eye drops by providing sustained release of medicaments in the eye.

  8. PREPARATION AND IN-VITRO EVALUATION OF BACLOFEN LOADED MICROSPHERES

    Directory of Open Access Journals (Sweden)

    Polepalle Madhulatha

    2012-09-01

    Full Text Available The present study was aimed to prepare Baclofen microspheres for sustained release using various polymers such as ethyl cellulose (hydrophobic, hydroxy propyl methyl cellulose (hydrophilic by employing solvent evaporation technique. Drug and excipients compatibility was studied by Fourier Transform Infrared Spectroscopy and no incompatibility was observed. The obtained microspheres were evaluated for the percent drug content, entrapment efficiency and in-vitro dissolution studies. The entrapment efficiency of the obtained formulations was in between 66-88% and in-vitro release of F7 formulation showed 93% in 24 hrs. Scanning Electron Microscopy, Differential Scanning Calorimetry and X-Ray Diffraction studies were performed for F7 formulation. From the results Scanning Electron Microscopy of reveals that microspheres was found in spherical and porous nature. X-Ray Diffraction studies results showed baclofen was in amorphous form which was further confirmed by Differential Scanning Calorimetry. The curve fitting data revealed that the release of obtained formulations follows mixed order kinetics with non‐fickian type of drug release (anomalous.

  9. pH-sensitive mebeverine microspheres for colon delivery

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    Dandagi P

    2009-01-01

    Full Text Available Mebeverine hydrochloride is known to suffer from extensive first pass effect. In an attempt to improve its oral bioavailability and possibility to restrict its absorption only to the colon, mebeverine microspheres were prepared by emulsion solvent evaporation method. Four formulations were prepared with varying drug and polymer ratio. These formulations were subjected to various evaluation parameters like percent practical yield, entrapment efficiency, particle size, in vitro drug release, in vivo activity. Practical yield of the microspheres was up to 89.59% with encapsulation efficiency up to 79.4%. Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 ΅m. In vitro release of the drug showed biphasic release pattern with non-Fickian diffusion release in 12 h. On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal. Antiirritable bowel syndrome activity was performed in colorectal distention in rat, which is a model for constipation-induced irritable bowel syndrome. The formulations F-2 and F-3 showed significant effect in fecal output when compared to the control as well as the marketed preparation in the constipation-induced irritable bowel syndrome in rats.

  10. Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system

    Science.gov (United States)

    Sayed, Elshaimaa G; Hussein, Amal K; Khaled, Khaled A; Ahmed, Osama AA

    2015-01-01

    The aim of the study was to improve corneal penetration and bioavailability of ofloxacin (OFX) eye preparations. OFX was incorporated in poly (lactide-co-glycolide) as biodegradable microspheres using oil in oil emulsion solvent evaporation technique. The prepared OFX microspheres were then incorporated in Gelrite® in situ gel preparation. In addition, OFX Gelrite-based in situ gel formulations were prepared. OFX formulations were characterized for gelling capacity, viscosity, and rheological properties. Release studies for OFX microspheres, OFX in situ gel, and OFX-loaded microspheres in situ gel formulations were carried out to investigate release characteristics of the drug. The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops. Results showed that the optimum Gelrite concentration was at 0.4%–0.7% w/v; the prepared formulations were viscous liquid transformed into a pourable gel immediately after the addition of simulated tear fluid with a gelling factor of 27–35. Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels and OFX microspheres. In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops. In addition, the longer duration of action of OFX-loaded microspheres in situ gel formula preparations is thought to avoid frequent instillations, which improves patient tolerability and compliance. PMID:25792803

  11. Ringing phenomenon in silica microspheres

    Institute of Scientific and Technical Information of China (English)

    Chunhua Dong; Changling Zou; Jinming Cui; Yong Yang; Zhengfu Han; Guangcan Guo

    2009-01-01

    Whispering gallery modes in silica microspheres are excited by a tunable continuous-wave laser through the fiber taper. Ringing phenomenon can be observed with high frequency sweeping speed. The thermal nonlinearity in the microsphere can enhance this phenomenon. Our measurement results agree very well with the theoretical predictions by the dynamic equation.

  12. Reducing the Oxidation Level of Dextran Aldehyde in a Chitosan/Dextran-Based Surgical Hydrogel Increases Biocompatibility and Decreases Antimicrobial Efficacy.

    Science.gov (United States)

    Chan, Maggie; Brooks, Heather J L; Moratti, Stephen C; Hanton, Lyall R; Cabral, Jaydee D

    2015-06-16

    A highly oxidized form of a chitosan/dextran-based hydrogel (CD-100) containing 80% oxidized dextran aldehyde (DA-100) was developed as a post-operative aid, and found to significantly prevent adhesion formation in endoscopic sinus surgery (ESS). However, the CD-100 hydrogel showed moderate in vitro cytotoxicity to mammalian cell lines, with the DA-100 found to be the cytotoxic component. In order to extend the use of the hydrogel to abdominal surgeries, reformulation using a lower oxidized DA (DA-25) was pursued. The aim of the present study was to compare the antimicrobial efficacy, in vitro biocompatibility and wound healing capacity of the highly oxidized CD-100 hydrogel with the CD-25 hydrogel. Antimicrobial studies were performed against a range of clinically relevant abdominal microorganisms using the micro-broth dilution method. Biocompatibility testing using human dermal fibroblasts was assessed via a tetrazolium reduction assay (MTT) and a wound healing model. In contrast to the original DA-100 formulation, DA-25 was found to be non-cytotoxic, and showed no overall impairment of cell migration, with wound closure occurring at 72 h. However, the lower oxidation level negatively affected the antimicrobial efficacy of the hydrogel (CD-25). Although the CD-25 hydrogel's antimicrobial efficacy and anti-fibroblast activity is decreased when compared to the original CD-100 hydrogel formulation, previous in vivo studies show that the CD-25 hydrogel remains an effective, biocompatible barrier agent in the prevention of postoperative adhesions.

  13. Reducing the Oxidation Level of Dextran Aldehyde in a Chitosan/Dextran-Based Surgical Hydrogel Increases Biocompatibility and Decreases Antimicrobial Efficacy

    Directory of Open Access Journals (Sweden)

    Maggie Chan

    2015-06-01

    Full Text Available A highly oxidized form of a chitosan/dextran-based hydrogel (CD-100 containing 80% oxidized dextran aldehyde (DA-100 was developed as a post-operative aid, and found to significantly prevent adhesion formation in endoscopic sinus surgery (ESS. However, the CD-100 hydrogel showed moderate in vitro cytotoxicity to mammalian cell lines, with the DA-100 found to be the cytotoxic component. In order to extend the use of the hydrogel to abdominal surgeries, reformulation using a lower oxidized DA (DA-25 was pursued. The aim of the present study was to compare the antimicrobial efficacy, in vitro biocompatibility and wound healing capacity of the highly oxidized CD-100 hydrogel with the CD-25 hydrogel. Antimicrobial studies were performed against a range of clinically relevant abdominal microorganisms using the micro-broth dilution method. Biocompatibility testing using human dermal fibroblasts was assessed via a tetrazolium reduction assay (MTT and a wound healing model. In contrast to the original DA-100 formulation, DA-25 was found to be non-cytotoxic, and showed no overall impairment of cell migration, with wound closure occurring at 72 h. However, the lower oxidation level negatively affected the antimicrobial efficacy of the hydrogel (CD-25. Although the CD-25 hydrogel’s antimicrobial efficacy and anti-fibroblast activity is decreased when compared to the original CD-100 hydrogel formulation, previous in vivo studies show that the CD-25 hydrogel remains an effective, biocompatible barrier agent in the prevention of postoperative adhesions.

  14. Influence of excipients on characteristics and release profiles of poly(ε-caprolactone) microspheres containing immunoglobulin G.

    Science.gov (United States)

    Erdemli, Özge; Keskin, Dilek; Tezcaner, Ayşen

    2015-03-01

    Protein instability during microencapsulation has been one of the major drawbacks of protein delivery systems. In this study, the effects of various excipients (poly vinyl alcohol, glucose, starch, heparin) on the stability of encapsulated human immunoglobulin G (IgG) in poly(ε-caprolactone) (PCL) microspheres and on microsphere characteristics were investigated before and after γ-sterilization. Microspheres formulated without any excipients and with glucose had a mean particle size around 3-4μm whereas the mean particle sizes of other microspheres were around 5-6μm. Use of PVA significantly increased the IgG-loading and encapsulation efficiency of microspheres. After γ-irradiation, IgG stability was mostly maintained in the microspheres with excipients compared to microspheres without any excipients. According to the μBCA results, microspheres without any excipient showed a high initial burst release as well as a fast release profile among all groups. Presence of PVA decreased the loss in the activity of IgG released before (completely retained after 6h and 15.69% loss after 7days) and after γ-irradiation (26.04% loss and 52.39% loss after 6h and 7days, respectively). The stabilization effect of PVA on the retention of the activity of released IgG was found more efficient compared to other groups formulated with carbohydrates.

  15. Stomach-specific anti-H. pylori therapy. II. Gastric residence studies of tetracycline-loaded chitosan microspheres in gerbils.

    Science.gov (United States)

    Hejazi, Radi; Amiji, Mansoor

    2003-08-01

    This study examines the gastric residence of chitosan microspheres and the local tetracycline concentrations following oral administration in gerbils. Chitosan microspheres were prepared by ionic cross-linking and precipitation with sodium sulfate. Gastric retention studies were performed by administering radioiodinated [125I] chitosan microsphere suspension in the nonacid-suppressed and acid-suppressed states. At different time points, animals were sacrificed, and the radioactivity in tissues and fluids was measured with a gamma counter. Local tetracycline concentrations were measured using chitosan microspheres loaded with tritiated-[3H]-tetracycline. The radioactivity, measured with a liquid scintillation analyzer, was used to determine the microg of drug per gram of tissues or fluids under nonacid-suppressed and acid-suppressed states. Microspheres with a spherical shape and an average diameter of 2.0-3.0 microm were formed. After 2 hr in the fasted stomach, approximately 10% of the administered dose remained. The microspheres were predominantly found in the colon after 6 hr of administration. There was no detectable radioactivity in the small intestine, plasma, urine, liver, and kidneys. Additionally, acid suppression with ranitidine did not influence the gastric residence time of chitosan microspheres. To our disappointment, tetracycline concentration profile in the stomach from microsphere formulation was similar to the aqueous solution. Also, there was no significant difference between the stomach tetracycline concentrations in the nonacid-suppressed and acid-suppressed states. The drug was predominantly found in the colon and urine samples after 6 hr. Tetracycline could not be detected in the plasma, small intestine, liver, or kidneys. Results of this study show that chitosan microspheres prepared by ionic cross-linking do not provide a longer residence time in the fasted gerbil stomach. The tetracycline concentration profile in the stomach, following

  16. Encapsulation of azithromycin into polymeric microspheres by reduced pressure-solvent evaporation method.

    Science.gov (United States)

    Li, Xiujuan; Chang, Si; Du, Guangsheng; Li, Yi; Gong, Junbo; Yang, Mingshi; Wei, Zhenping

    2012-08-20

    Azithromycin loaded microspheres with blends of poly-l-lactide and ploy-D,L-lactide-co-glycolide as matrices were prepared by the atmosphere-solvent evaporation (ASE) and reduced pressure-solvent evaporation (RSE) method. Both the X-ray diffraction spectra and DSC thermographs demonstrated that poly-L-lactide existed in a crystalline form in the ASE microspheres, while an amorphous form was present in the RSE formulations. Besides, solvent removal at atmosphere gave microspheres of porous and rough surfaces, but smooth surfaces appeared in the RSE microspheres. The incorporation efficiency as well as the burst release (cumulative release in the first 24h) in the ASE formulations was 39.94 ± 1.18% and 23.96 ± 2.01% respectively, yet the encapsulation efficiency of the microspheres fabricated under 385 mmHg was high up to 57.19 ± 3.81% and the burst release was 4.12 ± 0.15%. The in vitro drug release studies indicated that the ASE microspheres presented a zero-order profile; while the RSE formulations followed first-order kinetics. Other factors including solidification time, temperature, drug to polymer ratio and pH value of the continuous phase could also influence the physicochemical characteristics and release profiles of microspheres. In conclusion, the overall improvement of microspheres in appearance, encapsulation efficiency and controlled drug release through the RSE method could be easily fulfilled under optimal preparation conditions. Copyright © 2012 Elsevier B.V. All rights reserved.

  17. Thermo-sensitive gels containing lorazepam microspheres for intranasal brain targeting.

    Science.gov (United States)

    Jose, S; Ansa, C R; Cinu, T A; Chacko, A J; Aleykutty, N A; Ferreira, S V; Souto, E B

    2013-01-30

    Thermo-sensitive gels containing lorazepam microspheres were developed and characterized for intranasal brain targeting. Pluronics (PF-127 and PF-68) have been selected since they are thermo-reversible polymers with the property of forming a solution at low temperatures (4-5 °C), and a gel at body temperature (37 °C). This property makes them an interesting material to work with, especially in case of controlled release formulations. The present study focuses on the development of an intranasal formulation for lorazepam, as an alternative route of drug delivery to the brain. Direct transport of drugs to the brain circumventing the brain barrier, following intranasal administration, provides a unique feature and better option to target brain. The presence of mucoadhesive microspheres in the gel vehicle via nasal route can achieve a dual purpose of prolonged drug release and enhanced bioavailability. To optimise the microsphere formulation, Box Behnken design was employed by investigating the effect of three factors, polymer concentration (chitosan), emulsifier concentration (Span 80) and cross-linking agent (glutaraldehyde) on the response variable which is the mean particle size. The concentration of 21% PF-127 and 1% PF-68 were found to be promising gel vehicles. The results showed that the release rate followed a prolonged profile dispersion of the microspheres in the viscous media, in comparison to the microspheres alone. Histopathological studies proved that the optimised formulation does not produce any toxic effect on the microscopic structure of nasal mucosa.

  18. Preparation of Functional Polymeric Microspheres

    Institute of Scientific and Technical Information of China (English)

    Changchun Wang; Yonghui Deng; Wuli Yang; Shoukuang Fu

    2005-01-01

    @@ 1Introduction Because of the wide applications in the area of biomedical and biotechnological fields, a great efforts have been done to fabricate different kinds of microspheres with tailored structural and surface properties over the last decade[1]. Among them, stimuli responsive microspheres are microspheres that show ability to change their physical-chemical properties and colloidal properties in response to environmental stimuli such as changes of temperature, pH, chemicals, light, electrical field, magnetic field or mechanic stress, etc. These microspheres have been under intensive study for their high potential applications in biomedical and biotechnological fields such as controlled drug delivery[2], biosensor[3], chemical isolation[4], cell culture substrates[5], enzyme immobilization[6], bioelectrocatalysis[7], and magnetically controlled electrochemical reaction[8]. However,most of the reported stimuli responsive microspheres only show response to one specific stimulus. Up to now,to the best of our knowledge, only a few works have been directed to the fabrication of microspheres which show response to more than one stimulus[9]. In this paper, a system synthesis method for stimuli responsive microspheres with more useful properties was reported, and the simple application in biomedical area have been mentioned.

  19. Preparation of novel pirfenidone microspheres for lung-targeted delivery: in vitro and in vivo study

    Directory of Open Access Journals (Sweden)

    Li DB

    2016-09-01

    Full Text Available Dianbo Li, Liping Gong Department of Thoracic Surgery, Linyi Tumor Hospital, Linyi, Shandong, People’s Republic of China Abstract: The aim of this study was to develop and characterize pirfenidone (PF-loaded chitosan microspheres for lung targeting. The microspheres were prepared using the emulsion-solvent evaporation method and characterized by assessing morphology, particle size, and zeta potential. The microspheres had a spherical nature with highly smooth and integrated surfaces. The particle size of microspheres was 4.6±0.3 µm, and the zeta potential was 20.3±1.4 mV. The in vitro release results indicated that the obtained formulation of PF could reach the state of sustained release with a biphasic drug release pattern. It was observed that there was no significant difference in both the percentage of entrapment efficiency and that of drug release before and after the stability study. In vivo, the calculated relative bioavailability indicated greater pulmonary absorption of PF when it was encapsulated in microspheres. According to histopathological studies, no histological change occurred to the rat lung after the administration of PF-loaded chitosan microspheres. Keywords: pirfenidone, chitosan, microspheres, in vitro release

  20. Sophoridine-loaded PLGA microspheres for lung targeting: preparation, in vitro, and in vivo evaluation.

    Science.gov (United States)

    Wang, Wenping; Cai, Yaqin; Zhang, Guangxing; Liu, Yanhua; Sui, Hong; Park, Kinam; Wang, Hong

    2016-11-01

    Lung-targeting sophoridine-loaded poly(lactide-co-glycolide) (PLGA) microspheres were constructed by a simple oil-in-oil emulsion-solvent evaporation method. The obtained microspheres were systematically studied on their morphology, size distribution, drug loading, encapsulation efficiency, in vitro release profile, and biodistribution in rats. The drug-loaded microparticles showed as tiny spheres under SEM and had an average size of 17 μm with 90% of the microspheres ranging from 12 to 24 μm. The drug loading and encapsulation efficiency were 65% and 6.5%, respectively. The in vitro drug release behavior of microspheres exhibited an initial burst of 16.6% at 4 h and a sustained-release period of 14 days. Drug concentration in lung tissue of rats was 220.10 μg/g for microspheres and 6.77 μg/g for solution after intraveneous injection for 30 min, respectively. And the microsphere formulation showed a significantly higher drug level in lung tissue than in other major organs and blood samples for 12 days. These results demonstrated that the obtained PLGA microspheres could potentially improve the treatment efficacy of sophoridine against lung cancer.

  1. The potential of using biodegradable microspheres in retinal diseases and other intraocular pathologies.

    Science.gov (United States)

    Herrero-Vanrell, Rocío; Bravo-Osuna, Irene; Andrés-Guerrero, Vanessa; Vicario-de-la-Torre, Marta; Molina-Martínez, Irene Teresa

    2014-09-01

    Pathologies affecting the posterior segment of the eye are one of the major causes of blindness in developed countries and are becoming more prevalent due to the increase in society longevity. Successful therapy of diseases affecting the back of the eye requires effective concentrations of the active substance maintained during a long period of time in the intraocular target site. Treatment of vitreoretinal diseases often include repeated intravitreous injections that are associated with adverse effects. Local administration of biodegradable microspheres offers an excellent alternative to multiple administrations, as they are able to deliver the therapeutic molecule in a controlled fashion. Furthermore, injection of microparticles is performed without the need for surgical procedures. As most of the retinal diseases are multifactorial, microspheres result especially promising because they can be loaded with more than one active substance and complemented with the inclusion of additives with pharmacological properties. Personalized therapy can be easily achieved by changing the amount of administered microspheres. Contrary to non-biodegradable devices, biodegradable PLA and PLGA microspheres disappear from the site of administration after delivering the drug. Furthermore, microspheres prepared from these mentioned biomaterials are well tolerated after periocular and intravitreal injections in animals and humans. After injection, PLA and PLGA microspheres suffer aggregation behaving like an implant. Biodegradable microspheres are potential tools in regenerative medicine for retinal repair. According to the reported results, presumably a variety of microparticulate formulations for different ophthalmic therapeutic uses will be available in the clinical practice in the near future.

  2. Comparative assessment of in vitro release kinetics of calcitonin polypeptide from biodegradable microspheres.

    Science.gov (United States)

    Prabhu, Sunil; Sullivan, Jennifer L; Betageri, Guru V

    2002-01-01

    The objective of our study was to compare the in vitro release kinetics of a sustained-release injectable microsphere formulation of the polypeptide drug, calcitonin (CT), to optimize the characteristics of drug release from poly-(lactide-co-glycolide) (PLGA) copolymer biodegradable microspheres. A modified solvent evaporation and double emulsion technique was used to prepare the microspheres. Release kinetic studies were carried out in silanized tubes and dialysis bags, whereby microspheres were suspended and incubated in phosphate buffered saline, sampled at fixed intervals, and analyzed for drug content using a modified Lowry protein assay procedure. An initial burst was observed whereby about 50% of the total dose of the drug was released from the microspheres within 24 hr and 75% within 3 days. This was followed by a period of slow release over a period of 3 weeks in which another 10-15% of drug was released. Drug release from the dialysis bags was more gradual, and 50% CT was released only after 4 days and 75% after 12 days of release. Scanning electron micrographs revealed spherical particles with channel-like structures and a porous surface after being suspended in an aqueous solution for 5 days. Differential scanning calorimetric studies revealed that CT was present as a mix of amorphous and crystalline forms within the microspheres. Overall, these studies demonstrated that sustained release of CT from PLGA microspheres over a 3-week period is feasible and that release of drug from dialysis bags was more predictable than from tubes.

  3. Ammonolysis-induced solvent removal: a facile approach for solidifying emulsion droplets into PLGA microspheres.

    Science.gov (United States)

    Kim, Jayoung; Hong, Dasom; Chung, Younglim; Sah, Hongkee

    2007-12-01

    An ammonolysis-based microencapsulation technique useful for the preparation of biodegradable microspheres was described in this study. A dispersed phase consisting of poly- d, l-lactide- co-glycolide, progesterone, and methyl chloroacetate was emulsified in an aqueous phase. Upon addition of ammonia solution, the emulsion droplets were quickly transformed into poly- d, l-lactide- co-glycolide microspheres laden with progesterone. Rapid solvent removal was accompanied by ammonolysis. The chemical reaction converted water-immiscible methyl chloroacetate to water-miscible chloroacetamide and methanol. Chloroacetamide formation was proved by (1)H NMR and ESI-MS studies. Thermogravimetric analysis showed that the microspheres contained only small amounts of residual methyl chloroacetate. Incorporation efficiencies of progesterone ranged from 64.3 +/- 1.1 to 72.8 +/- 0.3%, depending upon microsphere formulations. X-ray powder diffractometry analysis substantiated that no polymorphic transition of progesterone occurred during microencapsulation. To evaluate the feasibility of this new method against the commonly used microencapsulation method, microspheres were also prepared by a typical dichloromethane-based solvent evaporation process. The important attributes of microspheres prepared from both methods were characterized for comparison. The new ammonolysis-based microencapsulation process showed interesting features distinct from those of the solvent evaporation process. The microencapsulation process reported in this study might be applicable in loading pharmaceuticals into various polymeric microspheres.

  4. Three dimensional distribution of surfactant in microspheres revealed by synchrotron radiation X-ray microcomputed tomography

    Directory of Open Access Journals (Sweden)

    Li Wu

    2017-07-01

    Full Text Available This study investigated the formulation mechanism of microspheres via internal surfactant distribution. Eudragit L100 based microspheres loaded with bovine serum albumin were prepared by solid in oil in oil emulsion solvent evaporation method using acetone and liquid paraffin system containing sucrose stearate as a surfactant. The fabricated microspheres were evaluated for encapsulation efficiency, particle size, production yield, and in vitro release characteristics. The internal structures of microspheres were characterized using synchrotron radiation X-ray microcomputed tomography (SR-µCT. The enhanced contrast made the sucrose stearate distinguished from Eudragit to have its three dimensional (3D distribution. Results indicated that the content and concentration determined the state of sucrose stearate and had significant influences on the release kinetics of protein. The dispersity of sucrose stearate was the primary factor that controlled the structure of the microspheres and further affected the encapsulation efficiency, effective drug loading, as well as in vitro release behavior. In conclusion, the 3D internal distribution of surfactant in microspheres and its effects on protein release behaviors have been revealed for the first time. The highly resolved 3D architecture provides new evidence for the deep understanding of the microsphere formation mechanism.

  5. In vitro and In vivo assessment of lawsone microsphere loaded chitosan scaffolds

    Directory of Open Access Journals (Sweden)

    Jamal Basha D

    2016-09-01

    Full Text Available Objective: To prepare, assess the lawsone loaded chitosan scaffolds for antibacterial and wound healing activity.Methods: The work was focused is to develop a topical formulation preferably, natural biodegradable scaffolds of lawsone drug for treating skin wounds and bacterial infections. Here, lawsone loaded chitosan microspheres were impregnated into chitosan scaffolds. The lawsone microspheres prepared by emulsification and cross linking method. Incorporation of lawsone loaded chitosan microspheres into chitosan scaffolds by emulsification and freeze drying technique. The lawsone a microspheres characterized by FT-IR, SEM, evaluated through entrapment efficiency, percentage yield, in vitro drug release studies. Lawsone scaffolds was assessed for wound healing ability using albino rats and anti bacterial activity by agar disc diffusion method.Results: the FT-IR spectra showing almost similar peaks within the same wave length range indicating the there is no possible interaction between the drug and polymer. The SEM of Lawsone microspheres and prepared scaffolds showing oval shape, slightly rough, porous surface, slightly aggregated and interconnected porous structure of the scaffolds was slightly reddish brown in colour. The lawsone loaded chitosan scaffolds had exhibited antibacterial activity against different bacrial strains and wound healing potential in albino rats.Conclusion:  The schematic process of lawsone loaded chitosan microspheres imparts quality in the in the topical formulation and obtained results were judicious.

  6. Mucoadhesive Microsphere - Review

    Directory of Open Access Journals (Sweden)

    Ratnaparkhi M P

    2014-06-01

    Full Text Available Several approaches have been immerged to prolong the residence time of the dosage forms at the absorption site and one of them is the development of oral controlled release mucoadhesive system. Mucoadhesive drug delivery systems are used to enhance drug absorption in a site-specific manner. Bioadhesion has been defined as the attachment of synthetic or biological macromolecules to a biological tissue. The biological surface can be epithelial tissue or the mucous coat on the surface of a tissue. If adhesive attachment is to a mucous coat, the phenomenon is referred to as mucoadhesion. Mucus is a thin blanket covering all epithelia that are in contact with the external environment in the gastrointestinal, respiratory, and urogenital tracts. This approach involves the use of mucoadhesive polymers, which can adhere to the epithelial surface in the stomach. Carrier technology offers an intelligent approach for drug delivery by coupling the drug to a carrier particle such as microspheres, nanospheres, liposomes, nanoparticles, etc., which modulates the release and absorption of the drug. Microspheres constitute an important part of these particulate drug delivery systems by virtue of their small size and efficient carrier capacity.

  7. Chitosan-Montmorillonite microspheres: A sustainable fertilizer delivery system.

    Science.gov (United States)

    dos Santos, Bruna Rodrigues; Bacalhau, Fabiana Britti; Pereira, Tamires dos Santos; Souza, Claudinei Fonseca; Faez, Roselena

    2015-08-20

    Controlled release fertilizers are efficient tools that increase the sustainability of agricultural practices. However, the biodegradability of the matrices and the determination of the release into soil still require some investigation. This paper describes the preparation of potassium-containing microspheres based on chitosan and montmorillonite clay and the in situ soil release. The chitosan-montmorillonite microspheres were prepared using a coagulation method and different proportions of montmorillonite. The structural, thermal and morphological properties as well the water swelling and fertilizer sorption capacity were evaluated. The best formulations were applied in soil, and the fertilizer release was monitored using time-domain reflectometry (TDR). Montmorillonite clay provides better sorption properties than the chitosan microspheres because of the rough and porous surface. Due to these properties, high levels of fertilizer were sorbed onto the material. ChMMT33-containing potassium shows two specific periods of fertilizer release: the first one lasted approximately three days and was assigned to the external fertilizer on the microspheres. The second was assigned to the internal fertilizer. TDR is an important and fast tool and was used to determine the fertilizer release and the ion movement in the soil.

  8. Nanoparticles of hydrophobically modified dextrans as potential drug carrier systems.

    Science.gov (United States)

    Aumelas, A; Serrero, A; Durand, A; Dellacherie, E; Leonard, M

    2007-09-01

    Nanoparticles combining a hydrophobically modified dextran core and a polysaccharide surface coverage were elaborated. Their suitability for applications like drug delivery was evaluated. The selected polysaccharide, dextran, was chemically modified by the covalent attachment of hydrocarbon groups (aliphatic or aromatic) via the formation of ether links. According to the extent of modification, either water-soluble or water-insoluble dextran derivatives were obtained. The latter exhibited solubility in organic solvents like tetrahydrofuran or dichloromethane saturated with water. Water-soluble dextran derivatives were used as polymeric surfactants for the control of nanoparticles surface characteristics. Nanoparticles were prepared either by o/w emulsion or solvent-diffusion methods. The size and surface properties of dextran nanoparticles were correlated to processing conditions. The stability of colloidal suspensions was examined as a function of ionic strength and related to the particle surface characteristics. The redispersability of freeze-dried suspensions without the addition of cryoprotectant was demonstrated. Finally, the degradability of modified dextrans was compared to that of starting dextran, after enzymatic hydrolysis in the presence of dextranase.

  9. Glass microsphere lubrication

    Science.gov (United States)

    Geiger, Michelle; Goode, Henry; Ohanlon, Sean; Pieloch, Stuart; Sorrells, Cindy; Willette, Chris

    1991-01-01

    The harsh lunar environment eliminated the consideration of most lubricants used on earth. Considering that the majority of the surface of the moon consists of sand, the elements that make up this mixture were analyzed. According to previous space missions, a large portion of the moon's surface is made up of fine grained crystalline rock, about 0.02 to 0.05 mm in size. These fine grained particles can be divided into four groups: lunar rock fragments, glasses, agglutinates (rock particles, crystals, or glasses), and fragments of meteorite material (rare). Analysis of the soil obtained from the missions has given chemical compositions of its materials. It is about 53 to 63 percent oxygen, 16 to 22 percent silicon, 10 to 16 percent sulfur, 5 to 9 percent aluminum, and has lesser amounts of magnesium, carbon, and sodium. To be self-supporting, the lubricant must utilize one or more of the above elements. Considering that the element must be easy to extract and readily manipulated, silicon or glass was the most logical choice. Being a ceramic, glass has a high strength and excellent resistance to temperature. The glass would also not contaminate the environment as it comes directly from it. If sand entered a bearing lubricated with grease, the lubricant would eventually fail and the shaft would bind, causing damage to the system. In a bearing lubricated with a solid glass lubricant, sand would be ground up and have little effect on the system. The next issue was what shape to form the glass in. Solid glass spheres was the only logical choice. The strength of the glass and its endurance would be optimal in this form. To behave as an effective lubricant, the diameter of the spheres would have to be very small, on the order of hundreds of microns or less. This would allow smaller clearances between the bearing and the shaft, and less material would be needed. The production of glass microspheres was divided into two parts, production and sorting. Production includes the

  10. In vitro properties of surface-modified solid lipid microspheres containing an antimalarial drug:halofantrine

    Institute of Scientific and Technical Information of China (English)

    Anthony A Attama; Collins N Igbonekwu

    2011-01-01

    Objective:To formulate and evaluatein vitro, surface-modified solid lipid microspheres containing halofantrine using lipid matrix formed from goat fat and a phospholipid (P90H). Methods: The model drug, halofantrine in an increasing concentration of1%, 2%, 3%, 4% and5% w/w was incorporated into surface-modified solid lipid microspheres formulated by hot homogenization. Effect of drug concentration on the encapsulation efficiency was studied. The dispersion was evaluated using particle size, particle morphology, pH and encapsulation efficiency. The drug formulation with highest encapsulation efficiency was selected and used for the release studies and compared with the release from a commercial dosage form (Halfan® 250 mg tablet, Glaxo-Smithkline, Mayenne France) using simulated gastric fluid (SGF pH1.2), simulated intestinal fluid (SIF pH7.2) and phosphate buffer (pH6.8) as biorelevant media. Results were analyzed statistically and the level of significance was taken to beP<0.05). Results:Discrete and spherical solid lipid microspheres were produced. The particle size of the dispersion was low (32.48-33.87 μm) with minimal particle growth and high encapsulation efficiencies(86.8%-91.0%) after3 months. The pH of the microspheres dispersion changed appreciably after3 months.In vitro release result obtained revealed sustained and controlled drug release from the lipid microspheres compared with the tablet dosage form.Conclusions:Formulation of halofantrine as solid lipid microspheres presents a better alternative to the conventional tablet formulation as thein vitro dissolution of the highly lipophilic halofantrine was highly improved.

  11. Formulations of Amlodipine: A Review

    Directory of Open Access Journals (Sweden)

    Muhammad Ali Sheraz

    2016-01-01

    Full Text Available Amlodipine (AD is a calcium channel blocker that is mainly used in the treatment of hypertension and angina. However, latest findings have revealed that its efficacy is not only limited to the treatment of cardiovascular diseases as it has shown to possess antioxidant activity and plays an important role in apoptosis. Therefore, it is also employed in the treatment of cerebrovascular stroke, neurodegenerative diseases, leukemia, breast cancer, and so forth either alone or in combination with other drugs. AD is a photosensitive drug and requires protection from light. A number of workers have tried to formulate various conventional and nonconventional dosage forms of AD. This review highlights all the formulations that have been developed to achieve maximum stability with the desired therapeutic action for the delivery of AD such as fast dissolving tablets, floating tablets, layered tablets, single-pill combinations, capsules, oral and transdermal films, suspensions, emulsions, mucoadhesive microspheres, gels, transdermal patches, and liposomal formulations.

  12. Biodegradable nanoparticles made from polylactide-grafted dextran copolymers.

    Science.gov (United States)

    Nouvel, C; Raynaud, J; Marie, E; Dellacherie, E; Six, J-L; Durand, A

    2009-02-15

    Polysaccharide-covered polyester nanoparticles were prepared using the emulsion/solvent evaporation process. The core of the nanoparticles was made either of PLA or of a blend of polylactide and polylactide-grafted dextran copolymer in various proportions. The surface of the nanoparticles was covered by dextran chains via the use of water-soluble polylactide-grafted dextrans as polymeric stabilizers during the emulsification step. The characteristics of the nanoparticles (size, surface coverage, thickness of superficial layer, colloidal stability) were correlated to the structural parameters (length and number of polylactide grafts) of the copolymers as well as to their surface active properties. The complete biodegradability of the nanoparticles was evaluated by considering the rate of hydrolysis of polylactide grafts in phosphate buffer and the rate of enzymatic degradation of dextran backbone by dextranase.

  13. Assessment of Dextran Antigenicity of Intravenous Iron Preparations with Enzyme-Linked Immunosorbent Assay (ELISA)

    OpenAIRE

    Susann Neiser; Koskenkorva, Taija S.; Katrin Schwarz; Maria Wilhelm; Susanna Burckhardt

    2016-01-01

    Intravenous iron preparations are typically classified as non-dextran-based or dextran/dextran-based complexes. The carbohydrate shell for each of these preparations is unique and is key in determining the various physicochemical properties, the metabolic pathway, and the immunogenicity of the iron-carbohydrate complex. As intravenous dextran can cause severe, antibody-mediated dextran-induced anaphylactic reactions (DIAR), the purpose of this study was to explore the potential of various int...

  14. Dextran sulfate inhibits acute Toxoplama gondii infection in pigs

    OpenAIRE

    2016-01-01

    Background Toxoplasma gondii is a highly prevalent protozoan that can infect all warm-blooded animals, including humans. Its definitive hosts are Felidae and its intermediate hosts include various other mammals and birds, including pigs. It is found in the meat of livestock which is a major source of human infection. Hence the control of toxoplasmosis in pigs is important for public health. We previously showed that dextran sulfate (DS), especially DS10 (dextran sulfate MW 10 kDa), is effecti...

  15. Mitoxantrone-loaded albumin microspheres for localized intratumoral chemotherapy of breast cancer

    Science.gov (United States)

    Almond, Brett Anthony

    /or microsphere-loaded mitoxantrone significantly improved survival time compared to controls. Cure rates as high as 80% were achieved after a single treatment with some microsphere formulations compared to 0% for untreated controls. The combination of mitoxantrone-loaded microspheres followed by the surgical excision of the tumor produced the most promising results with up to 100% survival in some treatment groups. Based on results of these studies, the initiation of a Phase-I clinical trial in human breast cancer patients may be warranted.

  16. Preparation of polystyrene microspheres for laser velocimetry in wind tunnels

    Science.gov (United States)

    Nichols, Cecil E., Jr.

    1987-01-01

    Laser Velocimetry (L/V) had made great strides in replacing intrusive devices for wind tunnel flow measurements. The weakness of the L/V has not been the L/V itself, but proper size seeding particles having known drag characteristics. For many Langley Wind Tunnel applications commercial polystyrene latex microspheres suspended in ethanol, injected through a fluid nozzle provides excellent seeding but was not used due to the high cost. This paper provides the instructions, procedures, and formulations for producing polystyrene latex monodisperse microspheres of 0.6, 1.0, 1.7, 2.0, and 2.7 micron diameters. These are presently being used at Langley Research Center as L/V seeding particles.

  17. Microspheres and their methods of preparation

    Science.gov (United States)

    Bose, Anima B; Yang, Junbing

    2015-03-24

    Carbon microspheres are doped with boron to enhance the electrical and physical properties of the microspheres. The boron-doped carbon microspheres are formed by a CVD process in which a catalyst, carbon source and boron source are evaporated, heated and deposited onto an inert substrate.

  18. Floating microspheres: a review

    Directory of Open Access Journals (Sweden)

    Jagtap Yogesh Mukund

    2012-03-01

    Full Text Available Gastric emptying is a complex process, one that is highly variable and that makes in vivo performance of drug delivery systems uncertain. A controlled drug delivery system with prolonged residence time in the stomach can be of great practical importance for drugs with an absorption window in the upper small intestine. The main limitations are attributed to the inter- and intra-subject variability of gastro-intestinal (GI transit time and to the non-uniformity of drug absorption throughout the alimentary canal. Floating or hydrodynamically controlled drug delivery systems are useful in such applications. Various gastroretentive dosage forms are available, including tablets, capsules, pills, laminated films, floating microspheres, granules and powders. Floating microspheres have been gaining attention due to the uniform distribution of these multiple-unit dosage forms in the stomach, which results in more reproducible drug absorption and reduced risk of local irritation. Such systems have more advantages over the single-unit dosage forms. The present review briefly addresses the physiology of the gastric emptying process with respect to floating drug delivery systems. The purpose of this review is to bring together the recent literature with respect to the method of preparation, and various parameters affecting the performance and characterization of floating microspheres.O esvaziamento gástrico é um processo complexo, com elevada variabilidade e responsável pela incerteza do desempenho dos medicamentos in vivo. Dessa forma, os sistemas de liberação modificada de fármacos, com tempo de residência prolongado no estômago, em especial, considerando aqueles fármacos com janela de absorção na porção superior do intestino delgado, apresentam fundamental importância. As principais limitações relativas à absorção do fármaco são, no geral, atribuídas à variabilidade inter e intra-paciente do tempo de trânsito gastro-intestinal (GI e

  19. Immobilized carboxymethylated dextran coatings for enhanced ELISA.

    Science.gov (United States)

    Liberelle, Benoît; Merzouki, Abderrazzak; De Crescenzo, Gregory

    2013-03-29

    We here report the development of a new generation of enzyme-linked immunosorbent assay (ELISA) that takes advantage of a low-fouling carboxymethylated dextran (CMD) layer chemically grafted on ELISA wells. In our approach, the overnight capture antibody adsorption step found in classical ELISA was replaced by a covalent attachment step to the CMD layer completed in 15 min. As a model, the potential of our approach was highlighted using commercially available anti-human epidermal growth factor (EGF) antibodies to quantify EGF present in various samples. Of interest, the grafted CMD layer was found to be as efficient as the commonly used bovine serum albumine (BSA) to reduce non-specific adsorption, thus eliminating the need of a time-consuming BSA blocking step normally required in classical ELISA. Our results demonstrated similar specificity, affinity, and intra- and inter-assay variations regardless of the diluent used in the assay (BSA-based diluent or protein-free buffer solution) when compared to standard ELISA. Finally, accuracy and precision of the CMD-based ELISA were verified by a spike and recovery test. Dilutions of recombinant human EGF in serum from healthy human volunteers showed almost-perfect linearity and mean recovery rates ranging between 90 and 110%.

  20. Paromomycin-loaded albumin microspheres: efficacy and stability studies.

    Science.gov (United States)

    Khan, Wahid; Kumar, Rajendra; Singh, Sukhvinder; Arora, Sunil Kumar; Kumar, Neeraj

    2013-06-01

    In the present work, paromomycin-loaded albumin microspheres (PM-MS) have been formulated for passive targeting of paromomycin (PM) to macrophages, for the treatment of visceral leishmaniasis (VL). PM-MS were prepared by spray-drying method with a mean particle size of ≈ 3 µm. Thermal and chemical cross-linking methods were used for controlling drug release from the prepared microspheres (MS). PM-MS were then tested for efficacy and stability studies. In efficacy study, in vitro promastigote assay was carried out to assess the susceptibility of promastigote to PM in the concentration range of 5.0-150 µg/ml; cytotoxicity assay was performed to determine possible toxicity of PM for the host cells (peritoneal macrophages) and intracellular amastigote assay was carried out to determine the efficacy of free PM (PM solution) and encapsulated PM (PM-MS). Results obtained indicated a significant increase in efficacy of PM-MS in comparison to PM solution at equivalent concentration. Subsequently, stability studies of prepared formulation was carried out at various temperature and humidity conditions, these studies provided stability of formulation at all tested conditions including accelerated conditions. Thus, it can be concluded that present work provides an optimized formulation with stability and enhanced efficacy.

  1. Mesoporous phenylalanine ammonia lyase microspheres with improved stability through calcium carbonate templating.

    Science.gov (United States)

    Cui, Jiandong; Zhao, Yamin; Tan, Zhilei; Zhong, Cheng; Han, Peipei; Jia, Shiru

    2017-05-01

    Cross-linked enzyme aggregates (CLEAs) have recently emerged as a promising method for enzyme immobilization due to its simplicity and low cost. However, a lack of good size and morphological control over the as-prepared CLEAs has limited their practical applications in some cases. Here, monodisperse spherical CLEAs of phenylalanine ammonia lyase (PAL microspheres) were prepared based on CaCO3 microtemplates. The preparation procedure involves filling porous CaCO3 microtemplates with the protein by salt precipitation, glutaraldehyde crosslinking, and dissolution of the microtemplates. The formulation of CaCO3 templates with controlled size was studied in detail. Characterization of the prepared PAL microspheres was investigated. The results showed that the PAL microspheres with high immobilization efficiency (79%) exhibited excellent stability, including increased tolerance to proteolysis, low pH, and denaturants, and excellent mechanical properties. For example, free PAL almost lost all activity after they were incubated in the presence of trypsin for 2min, whereas PAL microspheres still retained 95% of their initial activity. Moreover, scanning electron microscope, transmission electron microscope, and N2 adsorption-desorption isotherms revealed that the resultant PAL microspheres possessed good monodispersity and mesoporous structure instead of the amorphous clusters of conventional CLEAs with few pores. Compared with conventional CLEAs, the monodisperse PAL microspheres with mesoporous make them more potentially useful for biomedical and biotechnological applications.

  2. Penetration profile of microspheres in follicular targeting of terminal hair follicles.

    Science.gov (United States)

    Toll, R; Jacobi, U; Richter, H; Lademann, J; Schaefer, H; Blume-Peytavi, U

    2004-07-01

    The transfollicular administration of pharmacologically active molecules is of current therapeutic interest, mainly with regard to delivery to specific sites of the hair follicle (HF) and the reduction of hepatic metabolism and systemic toxicity. HF are privileged pathways for specific molecules depending on formulations, which enter faster into these shunts than through the stratum corneum. The aim was to optimize the delivery of fluorescent microspheres into the HF, thereby, developing a standardized protocol for follicular targeting with microspheres. The number of HF showing penetration, as well as the depth of penetration, was determined. Freshly excised skin samples with terminal HF were divided into groups, with or without prior treatment with cyanoacrylate skin surface stripping-technique (CSSS). Thereafter microspheres at a size of 0.75-6.0 microm were applied according to the developed standardized protocol. Skin biopsies were obtained, shock-frozen, and sectioned in 5 microm slices. We demonstrated a selective penetration route of the microspheres into the HF. Optimal microsphere size proved to be approximately 1.5 microm, with a 55% rate of all HF, and with a maximum penetration depth of >2300 microm. Without previous CSSS treatment of the skin, the transfollicular microsphere penetration was below 27% with a maximum penetration depth of 1000 microm. Thus, the basis for follicular targeting of essential structures containing stem cells for keratinocytes, melanocytes, and mast cells has been laid.

  3. Study on encapsulation of chlorine dioxide in gelatin microsphere for reducing release rate.

    Science.gov (United States)

    Ci, Ying; Wang, Lin; Guo, Yanchuan; Sun, Ruixue; Wang, Xijie; Li, Jinyou

    2015-01-01

    This study aims to explore the effects of encapsulation of chlorine dioxide in a hydrophilic biodegradable polymer gelatin to reduce its release rate. An emulsification-coacervation method was adopted. The characterizations of chlorine dioxide-gelatin microspheres were described. Using UV-vis spectrophotometer the λmax of chlorine dioxide was observed at 358 nm. The particle size and distribution of chlorine oxide-gelatin microspheres was measured by a dynamic light scattering (DLS) method, the diameter was (1400~1900) nm. The entrapment of chlorine dioxide-gelatin microspheres was confirmed by IR. The surface morphology, size, and shape of chlorine dioxide-gelatin microspheres were analyzed using Scanning electron microscope (SEM). It showed that the encapsulated microspheres size was around 2000 nm with uniform distribution. The percentage entrapment of chlorine dioxide in the encapsulated samples was about 80~85%. A slow release study of chlorine dioxide from the encapsulated biopolymer (gelatin) in air was also carried out, which showed continuous release up to ten days. It can be concluded that it is possible to make a slow release formulation of ClO2 by entrapped in a hydrophilic biodegradable polymer gelatin. ClO2-gelatin microspheres can stable release low concentration ClO2 gas over an extended period.

  4. Advances in Microsphere Insulation Systems

    Science.gov (United States)

    Allen, M. S.; Baumgartner, R. G.; Fesmire, J. E.; Augustynowicz, S. D.

    2004-06-01

    Microsphere insulation, typically consisting of hollow glass bubbles, combines in a single material the desirable properties that other insulations only have individually. The material has high crush strength, low density, is noncombustible, and performs well in soft vacuum. Microspheres provide robust, low-maintenance insulation systems for cryogenic transfer lines and dewars. They also do not suffer from compaction problems typical of perlite that result in the necessity to reinsulate dewars because of degraded thermal performance and potential damage to its support system. Since microspheres are load bearing, autonomous insulation panels enveloped with lightweight vacuum-barrier materials can be created. Comprehensive testing performed at the Cryogenics Test Laboratory located at the NASA Kennedy Space Center demonstrated competitive thermal performance with other bulk materials. Test conditions were representative of actual-use conditions and included cold vacuum pressure ranging from high vacuum to no vacuum and compression loads from 0 to 20 psi. While microspheres have been recognized as a legitimate insulation material for decades, actual implementation has not been pursued. Innovative microsphere insulation system configurations and applications are evaluated.

  5. Optical trapping of coated microspheres.

    Science.gov (United States)

    Bormuth, Volker; Jannasch, Anita; Ander, Marcel; van Kats, Carlos M; van Blaaderen, Alfons; Howard, Jonathon; Schäffer, Erik

    2008-09-01

    In an optical trap, micron-sized dielectric particles are held by a tightly focused laser beam. The optical force on the particle is composed of an attractive gradient force and a destabilizing scattering force. We hypothesized that using anti-reflection-coated microspheres would reduce scattering and lead to stronger trapping. We found that homogeneous silica and polystyrene microspheres had a sharp maximum trap stiffness at a diameter of around 800 nm--the trapping laser wavelength in water--and that a silica coating on a polystyrene microsphere was a substantial improvement for larger diameters. In addition, we noticed that homogeneous spheres of a correct size demonstrated anti-reflective properties. Our results quantitatively agreed with Mie scattering calculations and serve as a proof of principle. We used a DNA stretching experiment to confirm the large linear range in detection and force of the coated microspheres and performed a high-force motor protein assay. These measurements show that the surfaces of the coated microspheres are compatible with biophysical assays.

  6. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    Directory of Open Access Journals (Sweden)

    Wenjia Guo

    2015-10-01

    Full Text Available The purpose of this study was to develop a PLGA microspheres-based donepezil (DP formulation which was expected to sustain release of DP for one week with high encapsulation efficiency (EE. DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared successfully with average diameter of 30 µm, drug loading of 15.92 ± 0.31% and EE up to 78.79 ± 2.56%. Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface. Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model, which suggested the diffusion governing release mechanism. After single-dose administration of DP microspheres via subcutaneous injection in rats, the plasma concentration of DP reached peak concentration at 0.50 d, and then declined gradually, but was still detectable at 15 d. A good correlation between in vitro and in vivo data was obtained. The results suggest the potential use of DP microspheres for treatment of Alzheimer's disease over long periods.

  7. Design and evaluation of controlled release mucoadhesive microspheres of amoxicillin for anti Helicobacter pylori therapy

    Directory of Open Access Journals (Sweden)

    N Venkateswaramurthy

    2011-01-01

    Full Text Available The aim of this study was to develop controlled release mucoadhesive microspheres of amoxicillin trihydrate for the treatment of peptic ulcer disease caused by Helicobacter pylori (H. pylori. Microspheres were prepared by solvent evaporation technique using carbopol 974P, hydroxypropyl methyl cellulose K4M (HPMC K4M and Eudragit RS 100. The prepared microspheres were subjected to evaluation for particle size, incorporation efficiency, in vitro mucoadhesion and in vitro drug release characteristics. Absence of drug-polymer interaction was confirmed using differential scanning calorimetry analysis and fourier transform infrared spectrophotometry. The prepared microspheres showed a strong mucoadhesive property. The polymer concentration influenced the in vitro drug release significantly in 0.1N HCl. The particle sizes of systems ranged between 123±8.35 μm and 524±11.54 μm. Percent drug entrapment and release profiles of amoxicillin trihydrate in 0.1 N HCl were determined using high-performance liquid chromatography. The percentage drug entrapment and percentage yield of formulations were about 56.71±1.66% to 88.32±0.65% and 39.20±1.62% to 92.40±1.32%, respectively. The stability of the drugs was assessed in 0.1 N HCl. The results further substantiated that mucoadhesive microspheres improved the gastric stability of amoxicillin trihydrate (due to entrapment within the microsphere. From the above results, it was concluded that the mucoadhesive microspheres of amoxicillin trihydrate has feasibility for eradicating H. pylori from the stomach more effectively because of the prolonged gastrointestinal residence time and controlled release of drug from the formulation.

  8. Encapsulation of azithromycin into polymeric microspheres by reduced pressure-solvent evaporation method

    DEFF Research Database (Denmark)

    Li, Xiujuan; Chang, Si; Du, Guangsheng

    2012-01-01

    Azithromycin loaded microspheres with blends of poly-l-lactide and ploy-D,L-lactide-co-glycolide as matrices were prepared by the atmosphere-solvent evaporation (ASE) and reduced pressure-solvent evaporation (RSE) method. Both the X-ray diffraction spectra and DSC thermographs demonstrated...... that poly-L-lactide existed in a crystalline form in the ASE microspheres, while an amorphous form was present in the RSE formulations. Besides, solvent removal at atmosphere gave microspheres of porous and rough surfaces, but smooth surfaces appeared in the RSE microspheres. The incorporation efficiency...... as well as the burst release (cumulative release in the first 24h) in the ASE formulations was 39.94 ± 1.18% and 23.96 ± 2.01% respectively, yet the encapsulation efficiency of the microspheres fabricated under 385 mmHg was high up to 57.19 ± 3.81% and the burst release was 4.12 ± 0.15%. The in vitro drug...

  9. Spectroscopic study of copper(II) complexes with carboxymethyl dextran and dextran sulfate

    Science.gov (United States)

    Glišić, S.; Nikolić, G.; Cakić, M.; Trutić, N.

    2015-07-01

    The copper(II) ion complexes with carboxymethyl dextran (CMD) and dextran sulfate (DS) were studied by different methods. Content of copper was determined by atomic absorption spectroscopy. It was found that copper : ligand mole ratio (Cu : CMD) is 1 : 2, and Cu : DS is 1 : 1 by mole ratio method. Spectrophotometric parameters of synthesized compounds are characteristic for Cu(II) ion in octahedral ( O h ) coordination. Analyzing of FTIR spectra in ν(C=O) vibration region has showed that -COOH group acts as bidentate ligand, while the compounds of Cu(II) with DS copper ions are in the region of four oxygen atoms of two adjacent sulfo groups. The presence of crystalline water was determined by isotopic substitution of H2O molecules with D2O molecules. Comparison of spectra recorded at room (RT) and liquid nitrogen temperature (LNT) has enabled detection bands of water molecules libration indicating that they are coordinated complementing coordination sphere of Cu(II) ions to six. The complexes are of Cu(II) · (CMD)2 · (H2O)2 or Cu(II) · DS · (H2O)2 type. The similarities of the γ(C-H) range in a part of FTIR spectra indicate that there is no difference in the conformation of the 4 C 1 glucopyranose (Glc) unit CMD and DS synthesized Cu(II) complexes.

  10. Development of lovastatin-loaded poly(lactic acid microspheres for sustained oral delivery: in vitro and ex vivo evaluation

    Directory of Open Access Journals (Sweden)

    Guan QG

    2015-02-01

    Full Text Available Qigang Guan,1 Wei Chen,2 Xianming Hu2 1Department of Cardiology, The First Affiliated Hospital of China Medical University, Shenyang, People’s Republic of China; 2Department of Pharmaceutical, Shenyang Institute of Pharmaceutical Industry, Shenyang, People’s Republic of China Background: A novel lovastatin (LVT-loaded poly(lactic acid microsphere suitable for oral administration was developed in this study, and in vitro and in vivo characteristics were evaluated. Methods: The designed microspheres were obtained by an improved emulsion-solvent evaporation method. The morphological examination, particle size, encapsulation ratio, drug loading, and in vitro release were characterized. Pharmacokinetics studies were used to show that microspheres possess more advantages than the conventional formulations. Results: By using the emulsion-solvent evaporation method, it was simple to prepare microspheres and easy to scale up production. The morphology of formed microspheres showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the microspheres was 2.65±0.69 µm; the encapsulation efficiency was 92.5%±3.6%, and drug loading was 16.7%±2.1%. In vitro release indicated that the LVT microspheres had a well-sustained release efficacy, and ex vivo studies showed that after LVT was loaded to microspheres, the area under the plasma concentration-time curve from zero to the last measurable plasma concentration point and the extrapolation to time infinity increased significantly, which represented 2.63-fold and 2.49-fold increases, respectively, compared to suspensions. The rate of ex vivo clearance was significantly reduced. Conclusion: This research proved that poly(lactic acid microspheres can significantly prolong the drug circulation time in vivo and can also significantly increase the relative bioavailability of the drug. Keywords: lovastatin, microspheres, PLA, in vitro release, pharmacokinetics 

  11. Polarization Dependent Whispering Gallery Modes in Microspheres

    Science.gov (United States)

    Adamovsky, Grigory (Inventor); Wrbanek, Susan Y. (Inventor)

    2016-01-01

    A tunable resonant system is provided and includes a microsphere that receives an incident portion of a light beam generated via a light source, the light beam having a fundamental mode, a waveguide medium that transmits the light beam from the light source to the microsphere, and a polarizer disposed in a path of the waveguide between the light source and the microsphere. The incident portion of the light beam creates a fundamental resonance inside the microsphere. A change in a normalized frequency of the wavelength creates a secondary mode in the waveguide and the secondary mode creates a secondary resonance inside the microsphere.

  12. Porous microsphere and its applications

    Directory of Open Access Journals (Sweden)

    Cai Y

    2013-03-01

    Full Text Available Yunpeng Cai,1,2* Yinghui Chen,3* Xiaoyun Hong,2 Zhenguo Liu,1 Weien Yuan2 1Department of Neurology, Xinhua Hospital affiliated to Shanghai Jiaotong University School of Medicine, 2School of Pharmacy, Shanghai JiaoTong University, 3Department of Neurology Jinshan Hospital, Fudan University, Shanghai, People's Republic of China *These authors contributed equally to this workAbstract: Porous microspheres have drawn great attention in the last two decades for their potential applications in many fields, such as carriers for drugs, absorption and desorption of substances, pulmonary drug delivery, and tissue regeneration. The application of porous microspheres has become a feasible way to address existing problems. In this essay, we give a brief introduction of the porous microsphere, its characteristics, preparation methods, applications, and a brief summary of existing problems and research tendencies.Keywords: pore, porosity, porogen, suspension polymerization, seed swelling, pulmonary drug delivery, tissue regeneration

  13. Microsphere Super-resolution Imaging

    CERN Document Server

    Wang, Zengbo

    2015-01-01

    Recently, it was discovered that microsphere can generate super-resolution focusing beyond diffraction limit. This has led to the development of an exciting super-resolution imaging technique -microsphere nanoscopy- that features a record resolution of 50 nm under white lights. Different samples have been directly imaged in high resolution and real time without labelling, including both non-biological (nano devices, structures and materials) and biological (subcellular details, viruses) samples. This chapter reviews the technique, which covers its background, fundamentals, experiments, mechanisms as well as the future outlook.

  14. Dextran coated bismuth-iron oxide nanohybrid contrast agents for computed tomography and magnetic resonance imaging.

    Science.gov (United States)

    Naha, Pratap C; Zaki, Ajlan Al; Hecht, Elizabeth; Chorny, Michael; Chhour, Peter; Blankemeyer, Eric; Yates, Douglas M; Witschey, Walter R T; Litt, Harold I; Tsourkas, Andrew; Cormode, David P

    2014-12-14

    Bismuth nanoparticles have been proposed as a novel CT contrast agent, however few syntheses of biocompatible bismuth nanoparticles have been achieved. We herein report the synthesis of composite bismuth-iron oxide nanoparticles (BION) that are based on a clinically approved, dextran-coated iron oxide formulation; the particles have the advantage of acting as contrast agents for both CT and MRI. BION were synthesized and characterized using various analytical methods. BION CT phantom images revealed that the X-ray attenuation of the different formulations was dependent upon the amount of bismuth present in the nanoparticle, while T2-weighted MRI contrast decreased with increasing bismuth content. No cytotoxicity was observed in Hep G2 and BJ5ta cells after 24 hours incubation with BION. The above properties, as well as the yield of synthesis and bismuth inclusion efficiency, led us to select the Bi-30 formulation for in vivo experiments, performed in mice using a micro-CT and a 9.4 T MRI system. X-ray contrast was observed in the heart and blood vessels over a 2 hour period, indicating that Bi-30 has a prolonged circulation half-life. Considerable signal loss in T2-weighted MR images was observed in the liver compared to pre-injection scans. Evaluation of the biodistribution of Bi-30 revealed that bismuth is excreted via the urine, with significant concentrations found in the kidneys and urine. In vitro experiments confirmed the degradability of Bi-30. In summary, dextran coated BION are biocompatible, biodegradable, possess strong X-ray attenuation properties and also can be used as T2-weighted MR contrast agents.

  15. Formulation and Physicochemical Characterization of Buccoadhesive Microspheres Containing Diclofenac Sodium

    Directory of Open Access Journals (Sweden)

    Mitra Jelvehgari

    2014-05-01

    Full Text Available Purpose: The present study involves preparation and evaluation of diclofenac buccal-mucoadhesive microparticles for prolongation of buccal residence time. Methods: The microparticles were prepared by modified double-emulsion dehydration method (O1/W/O2 using sodium carboxymethylcellulose (CMC-Na as mucoadhesive polymer. Calcium chloride was used as a cross-linking agent. Buccal-mucoadhesive microparticles with different drug to polymers ratios were prepared and characterized by encapsulation efficiency, particle size, DSC (Differential Scanning Calormetric, flowability, degree of swelling, surface pH, mucoadhesive property and drug release studies. Results: The best drug to polymer ratio in microparticles was 1:5 (F3 with CMC-Na. F1 microparticles showed loading efficiency 51.43% and mean particle size 1013.92 μm. The DSC showed stable character of drug in microparticles and revealed amorphous form. Microparticles had slower release than the commercial tablet (p50 min. Histopathological studies revealed no buccal mucosal damage. Conclusion: It may be concluded that drug loaded buccal-mucoadhesive microparticles are a suitable delivery system for DS.

  16. Controlled-release and preserved bioactivity of proteins from (self-assembled core-shell double-walled microspheres

    Directory of Open Access Journals (Sweden)

    Yuan W

    2012-01-01

    Full Text Available Weien Yuan1,2, Zhenguo Liu11Department of Neurology, Xinhua Hospital, affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, 2School of Pharmacy, Shanghai Jiao Tong University, Shanghai, People’s Republic of ChinaAbstract: In order to address preserved protein bioactivities and protein sustained-release problems, a method for preparing double-walled microspheres with a core (protein-loaded nanoparticles with a polymer-suspended granule system-formed core and a second shell (a polymer-formed shell for controlled drug release and preserved protein bioactivities has been developed using (solid-in-oil phase-in-hydrophilic oil-in-water (S/O/Oh/W phases. The method, based on our previous microsphere preparation method (solid-in-oil phase-in-hydrophilic oil-in-water (S/O/Oh/W, employs different concentric poly(D,L-lactide-co-glycolide, poly(D,L-lactide, and protein-loaded nanoparticles to produce a suspended liquid which then self-assembles to form shell-core microspheres in the hydrophilic oil phase, which are then solidified in the water phase. Variations in the preparation parameters allowed complete encapsulation by the shell phase, including the efficient formation of a poly(D,L-lactide shell encapsulating a protein-loaded nanoparticle-based poly(D,L-lactide-co-glycolide core. This method produces core-shell double-walled microspheres that show controlled protein release and preserved protein bioactivities for 60 days. Based upon these results, we concluded that the core-shell double-walled microspheres might be applied for tissue engineering and therapy for chronic diseases, etc.Keywords: protein delivery, protein stability, core-shell microspheres, dextran nanoparticles

  17. Novel preparation method for sustained-release PLGA microspheres using water-in-oil-in-hydrophilic-oil-in-water emulsion

    Directory of Open Access Journals (Sweden)

    Hong X

    2013-07-01

    Full Text Available Xiaoyun Hong,1,2,* Liangming Wei,3,* Liuqing Ma,2 Yinghui Chen,4 Zhenguo Liu,1 Weien Yuan2,* 1Department of Neurology, Xinhua Hospital affiliated to Shanghai JiaoTong University, School of Medicine, Shanghai, People's Republic of China; 2School of Pharmacy, Shanghai JiaoTong University, 3Key Laboratory for Thin Film and Microfabrication Technology, Ministry of Education, Research Institute of Micro/Nanometer Science and Technology, Shanghai JiaoTong University, Shanghai, People's Republic of China; 4Department of Neurology, Jinshan Hospital, Fudan University, Shanghai, People's Republic of China *These authors contributed equally to this work Abstract: An increasing number of drugs are needing improved formulations to optimize patient compliance because of their short half-lives in blood. Sustained-release formulations of drugs are often required for long-term efficacy, and microspheres are among the most popular ones. When drugs are encapsulated into microsphere formulations, different methods of preparation need to be used according to specific clinical requirements and the differing physicochemical characteristics of individual drugs. In this work, we developed a novel method for sustained-release drug delivery using a water-in-oil-in-hydrophilic oil-in-water (w/o/oh/w emulsion to encapsulate a drug into poly(lactic-co-glycolic acid (PLGA microspheres. Different effects were achieved by varying the proportions and concentrations of hydrophilic oil and PLGA. Scanning electron and optical microscopic images showed the surfaces of the microspheres to be smooth and that their morphology was spherical. Microspheres prepared using the w/o/oh/w emulsion were able to load protein efficiently and had sustained-release properties. These results indicate that the above-mentioned method might be useful for developing sustained-release microsphere formulations in the future. Keywords: protein, microspheres, water-in-oil-in-hydrophilic oil

  18. Development and characterization of sustain release gastro retentive floating microsphere of diltiazem hydrochloride for the treatment of hypertension

    Directory of Open Access Journals (Sweden)

    Mangal S Panwar

    2015-01-01

    Full Text Available Gastroretentive drug delivery systems are the systems, which are retained in the stomach for a longer period and thereby improve the bio-availability of drugs. Diltiazem hydrochloride (DTZ HCl, is a calcium channel blocker, an antihypertension and antianginal drug, DTZ HCl undergoes an extensive biotransformation, mainly through cytochrome P-450 CYP3A, which results in <4% of its oral dose being excreted unchanged in urine. Suffers from poor bio-availability (~30-40% owing to an important first pass metabolism. It has an elimination half-life of 3.5 h and an absorption zone from the upper intestinal tract. Thus, the present work is aimed to formulate sustain release floating microsphere of DTZ HCl for gastroretentive drug delivery system. Floating microsphere were prepared using nonaqueous solvent evaporation method using polycarbonate, chitosan, ethyl cellulose, hydroxypropyl methycellulose and acrycoat as materials in various quantities, in varying ratio to formulate 20 formulations of the floating microsphere. Observations of all formulations for physical characterization had shown that, all of them comply with the specification of official pharmacopoeias and/or standard reference. It was observed that microsphere of batch F3 followed the results obtained, it was concluded that the formulation 98.72% F3 is the best formulations as the extent of drug release was found to be around 99.81% at the desired time 12 h.

  19. Sunitinib microspheres based on [PDLLA-PEG-PDLLA]-b-PLLA multi-block copolymers for ocular drug delivery.

    Science.gov (United States)

    Ramazani, F; Hiemstra, C; Steendam, R; Kazazi-Hyseni, F; Van Nostrum, C F; Storm, G; Kiessling, F; Lammers, T; Hennink, W E; Kok, R J

    2015-09-01

    Sunitinib is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that blocks several angiogenesis related pathways. The aim of this study was to develop sunitinib-loaded polymeric microspheres that can be used as intravitreal formulation for the treatment of ocular diseases. A series of novel multi-block copolymers composed of amorphous blocks of poly-(D,L-lactide) (PDLLA) and polyethylene glycol (PEG) and of semi-crystalline poly-(L-lactide) (PLLA) blocks were synthesized. Sunitinib-loaded microspheres were prepared by a single emulsion method using dichloromethane as volatile solvent and DMSO as co-solvent. SEM images showed that the prepared microspheres (∼ 30 μm) were spherical with a non-porous surface. Sunitinib-loaded microspheres were studied for their degradation and in-vitro release behavior. It was found that increasing the percentage of amorphous soft blocks from 10% to 30% accelerated the degradation of the multi-block copolymers. Sunitinib microspheres released their cargo for a period of at least 210 days by a combination of diffusion and polymer erosion. The initial burst (release in 24h) and release rate could be tailored by controlling the PEG-content of the multi-block copolymers. Sunitinib-loaded microspheres suppressed angiogenesis in a chicken chorioallantoic membrane (CAM) assay. These microspheres therefore hold promise for long-term suppression of ocular neovascularization.

  20. Budesonide-Loaded Guar Gum Microspheres for Colon Delivery: Preparation, Characterization and in Vitro/in Vivo Evaluation

    Directory of Open Access Journals (Sweden)

    Ye Liu

    2015-01-01

    Full Text Available A novel budesonide (BUD colon delivery release system was developed by using a natural polysaccharide, guar gum. The rigidity of the microspheres was induced by a chemical cross-linking method utilizing glutaraldehyde as the cross-linker. The mean particle size of the microspheres prepared was found to be 15.21 ± 1.32 µm. The drug loading and entrapment efficiency of the formulation were 17.78% ± 2.31% and 81.6% ± 5.42%, respectively. The microspheres were spherical in shape with a smooth surface, and the size was uniform. The in vitro release profiles indicated that the release of BUD from the microspheres exhibited a sustained release behavior. The model that fitted best for BUD released from the microspheres was the Higuchi kinetic model with a correlation coefficient r = 0.9993. A similar phenomenon was also observed in a pharmacokinetic study. The prolongation of the half-life (t1/2, enhanced residence time (mean residence time, MRT and decreased total clearance (CL indicated that BUD microspheres could prolong the acting time of BUD in vivo. In addition, BUD guar gum microspheres are thought to have the potential to maintain BUD concentration within target ranges for a long time, decreasing the side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency. None of the severe signs, like the appearance of epithelial necrosis and the sloughing of epithelial cells, were detected.

  1. Assessment of Dextran Antigenicity of Intravenous Iron Preparations with Enzyme-Linked Immunosorbent Assay (ELISA).

    Science.gov (United States)

    Neiser, Susann; Koskenkorva, Taija S; Schwarz, Katrin; Wilhelm, Maria; Burckhardt, Susanna

    2016-07-21

    Intravenous iron preparations are typically classified as non-dextran-based or dextran/dextran-based complexes. The carbohydrate shell for each of these preparations is unique and is key in determining the various physicochemical properties, the metabolic pathway, and the immunogenicity of the iron-carbohydrate complex. As intravenous dextran can cause severe, antibody-mediated dextran-induced anaphylactic reactions (DIAR), the purpose of this study was to explore the potential of various intravenous iron preparations, non-dextran-based or dextran/dextran-based, to induce these reactions. An IgG-isotype mouse monoclonal anti-dextran antibody (5E7H3) and an enzyme-linked immunosorbent assay (ELISA) were developed to investigate the dextran antigenicity of low molecular weight iron dextran, ferumoxytol, iron isomaltoside 1000, ferric gluconate, iron sucrose and ferric carboxymaltose, as well as isomaltoside 1000, the isolated carbohydrate component of iron isomaltoside 1000. Low molecular weight iron dextran, as well as dextran-based ferumoxytol and iron isomaltoside 1000, reacted with 5E7H3, whereas ferric carboxymaltose, iron sucrose, sodium ferric gluconate, and isolated isomaltoside 1000 did not. Consistent results were obtained with reverse single radial immunodiffusion assay. The results strongly support the hypothesis that, while the carbohydrate alone (isomaltoside 1000) does not form immune complexes with anti-dextran antibodies, iron isomaltoside 1000 complex reacts with anti-dextran antibodies by forming multivalent immune complexes. Moreover, non-dextran based preparations, such as iron sucrose and ferric carboxymaltose, do not react with anti-dextran antibodies. This assay allows to assess the theoretical possibility of a substance to induce antibody-mediated DIARs. Nevertheless, as this is only one possible mechanism that may cause a hypersensitivity reaction, a broader set of assays will be required to get an understanding of the mechanisms that may

  2. Assessment of Dextran Antigenicity of Intravenous Iron Preparations with Enzyme-Linked Immunosorbent Assay (ELISA

    Directory of Open Access Journals (Sweden)

    Susann Neiser

    2016-07-01

    Full Text Available Intravenous iron preparations are typically classified as non-dextran-based or dextran/dextran-based complexes. The carbohydrate shell for each of these preparations is unique and is key in determining the various physicochemical properties, the metabolic pathway, and the immunogenicity of the iron-carbohydrate complex. As intravenous dextran can cause severe, antibody-mediated dextran-induced anaphylactic reactions (DIAR, the purpose of this study was to explore the potential of various intravenous iron preparations, non-dextran-based or dextran/dextran-based, to induce these reactions. An IgG-isotype mouse monoclonal anti-dextran antibody (5E7H3 and an enzyme-linked immunosorbent assay (ELISA were developed to investigate the dextran antigenicity of low molecular weight iron dextran, ferumoxytol, iron isomaltoside 1000, ferric gluconate, iron sucrose and ferric carboxymaltose, as well as isomaltoside 1000, the isolated carbohydrate component of iron isomaltoside 1000. Low molecular weight iron dextran, as well as dextran-based ferumoxytol and iron isomaltoside 1000, reacted with 5E7H3, whereas ferric carboxymaltose, iron sucrose, sodium ferric gluconate, and isolated isomaltoside 1000 did not. Consistent results were obtained with reverse single radial immunodiffusion assay. The results strongly support the hypothesis that, while the carbohydrate alone (isomaltoside 1000 does not form immune complexes with anti-dextran antibodies, iron isomaltoside 1000 complex reacts with anti-dextran antibodies by forming multivalent immune complexes. Moreover, non-dextran based preparations, such as iron sucrose and ferric carboxymaltose, do not react with anti-dextran antibodies. This assay allows to assess the theoretical possibility of a substance to induce antibody-mediated DIARs. Nevertheless, as this is only one possible mechanism that may cause a hypersensitivity reaction, a broader set of assays will be required to get an understanding of the

  3. Polymer microspheres with structured surfaces

    NARCIS (Netherlands)

    Wagdare, N.A.; Baggerman, J.; Marcelis, A.T.M.; Boom, R.M.; Rijn, van C.J.M.

    2011-01-01

    Microspheres from polymethyl methacrylate (PMMA) and Eudragit FS 30D (a commercial copolymer of poly(methyl acrylate-co-methyl methacrylate-co-methacrylic acid) 7:3:1) were prepared using microsieve emulsification. A mixture of these polymers in dichloromethane (DCM) was dispersed into water, leadin

  4. Optical trapping of coated microspheres

    NARCIS (Netherlands)

    Bormuth, V.; Jannasch, A.; Ander, M.; van Kats, C.M.; van Blaaderen, A.; Howard, J.; Schäffer, E.

    2008-01-01

    In an optical trap, micron-sized dielectric particles are held by a tightly focused laser beam. The optical force on the particle is composed of an attractive gradient force and a destabilizing scattering force. We hypothesized that using anti-reflection-coated microspheres would reduce scattering a

  5. Power output and efficiency of beta-emitting microspheres

    Science.gov (United States)

    Cheneler, David; Ward, Michael

    2015-01-01

    Current standard methods to calculate the dose of radiation emitted during medical applications by beta-minus emitting microspheres rely on an over-simplistic formalism. This formalism is a function of the average activity of the radioisotope used and the physiological dimensions of the patient only. It neglects the variation in energy of the emitted beta particle due to self-attenuation, or self-absorption, effects related to the finite size of the sphere. Here it is assumed the sphere is comprised of a pure radioisotope with beta particles being emitted isotropically throughout the material. The full initial possible kinetic energy distribution of a beta particle is taken into account as well as the energy losses due to scattering by other atoms in the microsphere and bremsstrahlung radiation. By combining Longmire's theory of the mean forward range of charged particles and the Rayleigh distribution to take into account the statistical nature of scattering and energy straggling, the linear attenuation, or self-absorption, coefficient for beta-emitting radioisotopes has been deduced. By analogy with gamma radiation transport in spheres, this result was used to calculate the rate of energy emitted by a beta-emitting microsphere and its efficiency. Comparisons to standard point dose kernel formulations generated using Monte Carlo data show the efficacy of the proposed method. Yttrium-90 is used as a specific example throughout, as a medically significant radioisotope, frequently used in radiation therapy for treating cancer.

  6. New Collagen-Dextran-Zinc Oxide Composites for Wound Dressing

    Directory of Open Access Journals (Sweden)

    Georgeta Păunica-Panea

    2016-01-01

    Full Text Available The goal of this paper was the design, development, and characterization of some new composites, based on collagen and dextran as natural polymers and zinc oxide as antimicrobial, to be used in wound healing. Collagen hydrogels with various concentrations of dextran and zinc oxide were investigated in terms of rheological analysis. The spongious composites, obtained by freeze-drying of hydrogels, were evaluated by morphology (SEM, water uptake, and biological (enzymatic biodegradation analysis. All the results were strongly influenced by the nature and concentration of composite components. Based on the performances of the hydrogels, stationary rheometry, porous structure, morphology, and biological behavior, the antimicrobial spongious composite based on collagen and dextran with 50% ZnO were the most promising for future applications in wound dressing and a biomaterial with high potential in skin regeneration.

  7. Safety and Efficacy of Dextran-Rosmarinic Acid Conjugates as Innovative Polymeric Antioxidants in Skin Whitening: What Is the Evidence?

    Directory of Open Access Journals (Sweden)

    Ortensia I. Parisi

    2017-08-01

    Full Text Available Background: Melanins are high molecular weight pigments responsible for the mammalian skin and hair colour and play a key role in skin protection from UV radiation; however, their overproduction and excessive accumulation lead to pigmentation problems including melasma, freckles, uneven colouring, and age spots. Therefore, the modulation of melanin synthesis represents a critical issue in medicine and cosmetology. In the present study, an innovative polymeric antioxidant to be used as skin whitening agent is developed by the conjugation of dextran with rosmarinic acid. Methods: Dextran-rosmarinic acid conjugates (DEX-RA were synthesized in a one-pot method starting from Origanum vulgare aqueous leaf extract and dextran. The total polyphenol content and the antioxidant activity were assessed by Folin-Ciocalteau assay and 2,2-diphenyl-1-picrylhydrazyl radical (DPPH and bleaching tests, respectively. The efficacy of DEX-RA was evaluated by inhibition of tyrosinase activity, in vitro diffusion and stability studies and in vivo studies. The biocompatibility of the conjugates was investigated by 3-[4,5-Dimethylthiaoly]-2,5-diphenyltetrazoliumbromide (MTT and EPISKIN™ model. Results: Efficacy and safety studies confirmed the antioxidant and tyrosinase inhibitory activities and the biocompatibility of the synthesized conjugates. Conclusion: The polymeric conjugates, comparing to the free antioxidant, show a long-lasting efficacy combined to an enhanced stability resulting in an improved performance of the cosmetic formulations prepared using this innovative whitening agent as a bioactive ingredient.

  8. A comparison of analytic procedures for measurement of fractional dextran clearances

    NARCIS (Netherlands)

    Hemmelder, MH; de Jong, PE; de Zeeuw, D

    1998-01-01

    Fractional dextran clearances have been extensively used to study glomerular size selectivity. We report on an analysis of different laboratory procedures involved in measuring fractional dextran clearances. The deproteinization of plasma samples by 20% trichloroacetic acid (TCA) revealed a protein

  9. Biodistribution of ~(99)Tc~m Labelled Dextran Conjugates for Sentinel Lymph Node Detection

    Institute of Scientific and Technical Information of China (English)

    2011-01-01

    Mannosylated dextran conjugates showed high receptor affinity to the receptors on the surface of macrophages in the lymph node. 99Tcm labelled mannosylated dextran conjugates could be used for sentinel lymph node (SLN) detection. In this paper,

  10. A comparison of analytic procedures for measurement of fractional dextran clearances

    NARCIS (Netherlands)

    Hemmelder, MH; de Jong, PE; de Zeeuw, D

    1998-01-01

    Fractional dextran clearances have been extensively used to study glomerular size selectivity. We report on an analysis of different laboratory procedures involved in measuring fractional dextran clearances. The deproteinization of plasma samples by 20% trichloroacetic acid (TCA) revealed a protein

  11. Structural and biocompatibility properties of dextran from Weissella cibaria JAG8 as food additive.

    Science.gov (United States)

    Tingirikari, Jagan Mohan Rao; Kothari, Damini; Shukla, Rishikesh; Goyal, Arun

    2014-09-01

    Dextran produced from Weissella cibaria JAG8 was purified and characterized. The molecular mass of dextran as determined by the gel filtration and copper bicinchoninate method was approximately, 800 kDa. Monosaccharide analysis revealed that the polysaccharide comprised only glucose units. Dynamic light scattering study confirmed the mono-disperse nature of dextran with hydrodynamic radius of 900 nm. Surface morphology study of dextran by scanning electron microscopy showed the porous web like structure. Cytotoxicity studies on human cervical cancer (HeLa) cell line showed non-toxic and biocompatible nature of dextran. The relative browning for dextran from W. cibaria JAG8 was similar to commercial prebiotic Nutraflora P-95 and 3-fold lower than Raftilose P-95. Synthesis of dextran by dextransucrase treated, sucrose-supplemented skimmed milk revealed the promising potential of dextran as a food additive.

  12. 5-Fluorouracil loaded guar gum microspheres for colon delivery:preparation, characterization and in vitro release

    Institute of Scientific and Technical Information of China (English)

    KAUSHIK Dinesh; SARDANA Satish; MISHRA DN

    2009-01-01

    The present investigation is aimed to develop a new formulation containing chemically cross-linked guar gum microspheres loaded with 5-fluorouracil for targeting colorectal cancer. The emulsification polymerization method involving the dispersion of aqueous phase of guar gum in castor oil was used to prepare spherical microspheres. Various processing parameters were studied in order to optimize the formulation. Particle size and surface morphology of the microspheres were determined using optical microscopy and scanning electron microscopy. The in vitro drug release studies performed in simulated gastric fluid (SGF) for 2 h followed by intestinal fluid for 3 h, revealed the retention of the drug inside the microspheres from which only (15.27±0.56)% of the drug was released in 5 h. In vitro release rate studies were also carried out in simulated colonic fluid (SCF) in the presence of rat caecal contents, which showed improved drug release. The drug release from the formulation was found to be (41.6±3.5) % with 2% (w/v) caecal matter in 24 h as compared to control study where (25.2±3.5) % of drug was released. The drug release from the formulation with 2% and 4% rat caecal contents medium after 2 days of enzyme induction was found to be (56.3±4.1) % and (78.9±2.8) % in 24 h respectively. Similarly, (61.3±5.4) % and (90.2±2.9) % drug was released respectively with 2% and 4% rat caecal matter after 4 days of enzyme induction and (72.1±2.9) % and (90.2±3.2) % after 6 days of enzyme induction. In this way, 5-fluorouracil loaded guar gum microspheres have shown promising results in the management of colorectal cancer, warranting thorough in vivo study for scale up technology.

  13. Influence of excipients on characteristics and release profiles of poly(ε-caprolactone) microspheres containing immunoglobulin G

    Energy Technology Data Exchange (ETDEWEB)

    Erdemli, Özge [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Keskin, Dilek [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara (Turkey); Tezcaner, Ayşen, E-mail: tezcaner@metu.edu.tr [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara (Turkey)

    2015-03-01

    Protein instability during microencapsulation has been one of the major drawbacks of protein delivery systems. In this study, the effects of various excipients (poly vinyl alcohol, glucose, starch, heparin) on the stability of encapsulated human immunoglobulin G (IgG) in poly(ε-caprolactone) (PCL) microspheres and on microsphere characteristics were investigated before and after γ-sterilization. Microspheres formulated without any excipients and with glucose had a mean particle size around 3–4 μm whereas the mean particle sizes of other microspheres were around 5–6 μm. Use of PVA significantly increased the IgG-loading and encapsulation efficiency of microspheres. After γ-irradiation, IgG stability was mostly maintained in the microspheres with excipients compared to microspheres without any excipients. According to the μBCA results, microspheres without any excipient showed a high initial burst release as well as a fast release profile among all groups. Presence of PVA decreased the loss in the activity of IgG released before (completely retained after 6 h and 15.69% loss after 7 days) and after γ-irradiation (26.04% loss and 52.39% loss after 6 h and 7 days, respectively). The stabilization effect of PVA on the retention of the activity of released IgG was found more efficient compared to other groups formulated with carbohydrates. - Highlights: • Good excipient provides retention of protein stability during microencapsulation. • PVA was more effective on retention of the IgG stability compared to carbohydrates. • Starch was not an appropriate excipient for the retention of IgG stability.

  14. Bioavailability of ketoprofen from orally administered ketoprofen-dextran ester prodrugs in the pig

    DEFF Research Database (Denmark)

    Larsen, C.; Jensen, Bodil Hamborg; Olesen, H. P.

    1991-01-01

    The bioavailability of ketoprofen after oral administration of aqueous solutions of various ketoprofen-dextran ester prodrugs in pigs was assessed. Conjugates derived from dextran fractions in the molecular weight range 10,000-500,000 were employed. Compared to the administration of an oral......-dextran esters. Thus, the present study adds support to a more versatile application of the dextran ester prodrug approach to providing selective colon delivery of drugs possessing a carboxylic acid functional group....

  15. ERYTHROMYCIN POLYLACTIC ACID MICROSPHERES FOR LUNG TARGETING

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    AIM: To prepare polylactic acid microspheres of Erythromycin for Lung targeting.METHEDS: The orthogonal test design was used to optimize the technology,of preparation. Thecharacter of the microspheres, drug release in vitro, stability and tissue distribution were examinedRESULTS: The Erythromycin polylactic acid microspheres was regular in its morphology. Drugwas enveloped in microspheres but not physically mixed with PDLLA. The average particle size was11.65μn with over 94% of the microspheres being in the range of 5~20trn; The drug loading andthe incorporation efciency were 18% and 60% respectively. The microspheres were stable for threemonth at 4 ℃ and room temperature. The in vitro release properties could be expressed by theHiguchi's equation: y = 28.067 + 3.8515t11/2 (r = 0.9834). Comparing with injection, the drug inmicrospheres was more concentrated in lung tissue. CONCLUSION: Erythromycin polylactic acidmicrospheres showed significant sustained release and lung targeting.

  16. Facile fabrication of biocompatible PLGA drug-carrying microspheres by O/W pickering emulsions.

    Science.gov (United States)

    Wei, Zengjiang; Wang, Chaoyang; Liu, Hao; Zou, Shengwen; Tong, Zhen

    2012-03-01

    This study is focused on the preparation of Ibuprofen (IBU) loaded micrometer-sized poly(lactic-co-glycolic acid) (PLGA) microspheres and process variables on the size, drug loading and release during preparation of formulation. Silicon dioxide (SiO(2)) nanoparticle-coated PLGA microspheres were fabricated via a combined system of "Pickering-type" emulsion route and solvent volatilization method in the absence of any molecular surfactants. Stable oil-in-water emulsions were prepared using SiO(2) nanoparticles as a particulate emulsifier and a dichloromethane (CH(2)Cl(2)) solution of PLGA as an oil phase. The SiO(2) nanoparticle-coated PLGA microspheres were fabricated by the evaporation of CH(2)Cl(2) in situ, and then bare-PLGA microspheres were prepared by removal of the SiO(2) nanoparticles using HF aqueous solution. The two types of microspheres were characterized in terms of size, component and morphology using scanning electronic microscope (SEM), Fourier-transform infrared, optical microscope, and so on. Moreover, IBU was encapsulated into the hybrid beads by dispersing them in the CH(2)Cl(2) solution of PLGA in the fabrication process. The sustained release could be obtained due to the barrier of the polymeric matrix (PLGA). More over, the release curves were nicely fitted by the Weibull equation and the release followed Fickian diffusion. The combined system of Pickering emulsion and solvent volatilization opens up a new route to fabricate a variety of microspheres. The resulting microspheres may find applications as delivery vehicles for biomolecules, drugs, cosmetics and living cells. Copyright © 2011 Elsevier B.V. All rights reserved.

  17. POE-PEG-POE triblock copolymeric microspheres containing protein. II. Polymer erosion and protein release mechanism.

    Science.gov (United States)

    Wan, J P; Yang, Y Y; Chung, T S; Tan, D; Ng, S; Heller, J

    2001-07-10

    The first paper of this series presented the fabrication and characterization of POE-PEG-POE triblock copolymeric microspheres containing protein. In this paper, we focus on the polymer erosion and the mechanism of protein release. Fourteen-week in vitro behaviors of POE-PEG-POE microspheres loaded with bovine serum albumin (BSA) have been monitored. SEM micrographs reveal that after 14-week incubation in PBS buffer, pH 7.4, 37 degrees C, the polymeric particles remain spherical despite mass loss of almost 90%. On the other hand, molecular weight undergoes a high initial loss of 38% and 44% during the first 2-week incubation for POE-PEG(5%)-POE and POE-PEG(10%)-POE, respectively. Then, it keeps relatively unchanged over 12 weeks. However, POE-PEG(20%)-POE copolymer provides a better compatibility between the POE and PEG blocks. Hydrolysis is homogeneous through the polymer backbone. Thus, its molecular weight remains relatively constant and mass loss shows quite sustained over the 14-week in vitro release. The similar phenomena are observed in the polydispersity index of the degrading copolymers. SDS-PAGE of the encapsulated BSA within the POE-PEG(5%)-POE microspheres displays that the structural integrity of BSA is intact for at least 8 weeks due to a mild environment provided by the copolymer. In addition, XPS and FTIR are utilized to investigate protein behaviors in the degrading microspheres. Protein release from the POE-PEG-POE microspheres shows a biphasic pattern, characterized by an initial stage followed by a non-detectable release. The non-release phase is dominated by either slow polymer degradation or dense microsphere matrix structures. The microsphere formulation is optimized and a sustained protein release over 2 weeks is achieved by using POE-PEG(20%)-POE at a high protein loading.

  18. Adult respiratory distress syndrome complicating intravenous infusion of low-molecular weight dextran.

    Science.gov (United States)

    Taylor, M A; DiBlasi, S L; Bender, R M; Santoian, E C; Cha, S D; Dennis, C A

    1994-07-01

    Respiratory failure is one of the most uncommon and serious adverse drug reactions. Low-molecular-weight-dextran (Dextran-40) is a useful adjunctive anti-platelet agent in the setting of coronary angioplasty and intracoronary stent placement. We report the occurrence of the adult respiratory distress syndrome following intravenous infusion of Dextran-40.

  19. More complications in patients with septic shock treated with dextran compared with crystalloids

    DEFF Research Database (Denmark)

    Rasmussen, Anders Mølgaard; Jakobsen, Rasmus; Strøm, Thomas;

    2015-01-01

    of patients admitted to our intensive care unit with septic shock and treated with dextran-70 in the period from 1 January 2009 to 31 December 2009. The controls were included from 1 March 2012 to 28 February 2013 when dextran-70 was replaced with crystalloids. RESULTS: There were 91 patients in the dextran...

  20. Removal of methyl violet dye by adsorption onto N-benzyltriazole derivatized dextran

    DEFF Research Database (Denmark)

    Cho, Eunae; Tahir, Muhammad Nazir; Kim, Hwanhee

    2015-01-01

    In this work, N-benzyltriazole derivatized dextran was evaluated for its potential as a novel carbohydrate-based adsorbent for the removal of methyl violet dye from water. The modified dextran was synthesized by a click reaction of pentynyl dextran and benzyl azide, and the structure...

  1. Preparation and Determination of Drug-Polymer Interaction and In-vitro Release of Mefenamic Acid Microspheres Made of CelluloseAcetate Phthalate and/or Ethylcellulose Polymers

    Science.gov (United States)

    Jelvehgari, Mitra; Hassanzadeh, Davoud; Kiafar, Farhad; Delf Loveym, Badir; Amiri, Sara

    2011-01-01

    The objective of this study was to formulate and evaluate the drug-polymer interaction of mefenamic acid (MA) using two polymers with different characteristics as ethylcellulose (EC) and/or cellulose acetate phthalate (CAP). Microspheres were prepared by the modified emulsion solvent evaporation (MESE). The effect of drug-polymer interaction was studied for each of microspheres. Important parameters in the evaluation of a microencapsulation technique are encapsulation efficiency, yield production, particle size, surface characteristics of microspheres, scanning electronic microscopy (SEM), powder X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). The in-vitro release studies are performed in Tris buffer (pH 9) with Sodium lauryl sulfate (SLS). Microspheres containing CAP and EC showed 68-97% and 63-76% of entrapment efficiency, respectively. The thermogram X-ray and DSC showed stable character of MA in the microspheres and revealed an absence of drug polymer interaction. The prepared microspheres were spherical in shape and had a size range of 235-436 μm for CAP-microspheres and 358-442 μm for EC-microspheres. The results suggest that MA was successfully and efficiently encapsulated; the release rates of matrix microspheres are related to the type of polymer, only when polymers (EC and CAP combine with 1 : 1 ratio) were used to get prolonged drug release with reducing the polymers content in the microspheres. Data obtained from in-vitro release for microspheres and commercial capsule were fitted to various kinetic models and the high correlation was obtained in the peppas model. Mefenamic acid, Ethylcellulose, Cellulose acetate phthalate, Microparticles, Modified emulsion-solvent evaporation. PMID:24250377

  2. Magnetoresponsive Photonic Microspheres with Structural Color Gradient.

    Science.gov (United States)

    Lee, Seung Yeol; Choi, Jongkook; Jeong, Jong-Ryul; Shin, Jung H; Kim, Shin-Hyun

    2017-02-06

    Photonic Janus particles are created by alternately sputtering silica and titania on microspheres in order to obtain a structural color gradient. In addition, the microspheres are rendered magnetoresponsive. The Janus microspheres with optical and magnetic anisotropy enable on-demand control over orientation and structural color through manipulation of an external magnetic field, thereby being useful as active color pigments for reflection-mode displays.

  3. Synthesis of biodegradable polymer-mesoporous silica composite microspheres for DNA prime-protein boost vaccination.

    Science.gov (United States)

    Ho, Jenny; Huang, Yi; Danquah, Michael K; Wang, Huanting; Forde, Gareth M

    2010-03-18

    DNA vaccines or proteins are capable of inducing specific immunity; however, the translation to the clinic has generally been problematic, primarily due to the reduced magnitude of immune response and poor pharmacokinetics. Herein we demonstrate a composite microsphere formulation, composed of mesoporous silica spheres (MPS) and poly(D,L-lactide-co-glycolide) (PLGA), enables the controlled delivery of a prime-boost vaccine via the encapsulation of plasmid DNA (pDNA) and protein in different compartments. Method with modified dual-concentric-feeding needles attached to a 40 kHz ultrasonic atomizer was studied. These needles focus the flow of two different solutions, which passed through the ultrasonic atomizer. The process synthesis parameters, which are important to the scale-up of composite microspheres, were also studied. These parameters include polymer concentration, feed flowrate, and volumetric ratio of polymer and pDNA-PEI/MPS-BSA. This fabrication technique produced composite microspheres with mean D[4,3] ranging from 6 to 34 microm, depending upon the microsphere preparation. The resultant physical morphology of composite microspheres was largely influenced by the volumetric ratio of pDNA-PEI/MPS-BSA to polymer, and this was due to the precipitation of MPS at the surface of the microspheres. The encapsulation efficiencies were predominantly in the range of 93-98% for pDNA and 46-68% for MPS. In the in vitro studies, the pDNA and protein showed different release kinetics in a 40 day time frame. The dual-concentric-feeding in ultrasonic atomization was shown to have excellent reproducibility. It was concluded that this fabrication technique is an effective method to prepare formulations containing a heterologous prime-boost vaccine in a single delivery system.

  4. Prediction of dexamethasone release from PLGA microspheres prepared with polymer blends using a design of experiment approach.

    Science.gov (United States)

    Gu, Bing; Burgess, Diane J

    2015-11-10

    Hydrophobic drug release from poly (lactic-co-glycolic acid) (PLGA) microspheres typically exhibits a tri-phasic profile with a burst release phase followed by a lag phase and a secondary release phase. High burst release can be associated with adverse effects and the efficacy of the formulation cannot be ensured during a long lag phase. Accordingly, the development of a long-acting microsphere product requires optimization of all drug release phases. The purpose of the current study was to investigate whether a blend of low and high molecular weight polymers can be used to reduce the burst release and eliminate/minimize the lag phase. A single emulsion solvent evaporation method was used to prepare microspheres using blends of two PLGA polymers (PLGA5050 (25 kDa) and PLGA9010 (113 kDa)). A central composite design approach was applied to investigate the effect of formulation composition on dexamethasone release from these microspheres. Mathematical models obtained from this design of experiments study were utilized to generate a design space with maximized microsphere drug loading and reduced burst release. Specifically, a drug loading close to 15% can be achieved and a burst release less than 10% when a composition of 80% PLGA9010 and 90 mg of dexamethasone is used. In order to better describe the lag phase, a heat map was generated based on dexamethasone release from the PLGA microsphere/PVA hydrogel composite coatings. Using the heat map an optimized formulation with minimum lag phase was selected. The microspheres were also characterized for particle size/size distribution, thermal properties and morphology. The particle size was demonstrated to be related to the polymer concentration and the ratio of the two polymers but not to the dexamethasone concentration.

  5. Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs.

    Science.gov (United States)

    El-Say, Khalid M; El-Helw, Abdel-Rahim M; Ahmed, Osama A A; Hosny, Khaled M; Ahmed, Tarek A; Kharshoum, Rasha M; Fahmy, Usama A; Alsawahli, Majed

    2015-01-01

    The purpose was to improve the encapsulation efficiency of cetirizine hydrochloride (CTZ) microspheres as a model for water soluble drugs and control its release by applying response surface methodology. A 3(3) Box-Behnken design was used to determine the effect of drug/polymer ratio (X1), surfactant concentration (X2) and stirring speed (X3), on the mean particle size (Y1), percentage encapsulation efficiency (Y2) and cumulative percent drug released for 12 h (Y3). Emulsion solvent evaporation (ESE) technique was applied utilizing Eudragit RS100 as coating polymer and span 80 as surfactant. All formulations were evaluated for micromeritic properties and morphologically characterized by scanning electron microscopy (SEM). The relative bioavailability of the optimized microspheres was compared with CTZ marketed product after oral administration on healthy human volunteers using a double blind, randomized, cross-over design. The results revealed that the mean particle sizes of the microspheres ranged from 62 to 348 µm and the efficiency of entrapment ranged from 36.3% to 70.1%. The optimized CTZ microspheres exhibited a slow and controlled release over 12 h. The pharmacokinetic data of optimized CTZ microspheres showed prolonged tmax, decreased Cmax and AUC0-∞ value of 3309 ± 211 ng h/ml indicating improved relative bioavailability by 169.4% compared with marketed tablets.

  6. Microbial dextran-hydrolyzing enzymes: fundamentals and applications.

    Science.gov (United States)

    Khalikova, Elvira; Susi, Petri; Korpela, Timo

    2005-06-01

    Dextran is a chemically and physically complex polymer, breakdown of which is carried out by a variety of endo- and exodextranases. Enzymes in many groups can be classified as dextranases according to function: such enzymes include dextranhydrolases, glucodextranases, exoisomaltohydrolases, exoisomaltotriohydrases, and branched-dextran exo-1,2-alpha-glucosidases. Cycloisomalto-oligosaccharide glucanotransferase does not formally belong to the dextranases even though its side reaction produces hydrolyzed dextrans. A new classification system for glycosylhydrolases and glycosyltransferases, which is based on amino acid sequence similarities, divides the dextranases into five families. However, this classification is still incomplete since sequence information is missing for many of the enzymes that have been biochemically characterized as dextranases. Dextran-degrading enzymes have been isolated from a wide range of microorganisms. The major characteristics of these enzymes, the methods for analyzing their activities and biological roles, analysis of primary sequence data, and three-dimensional structures of dextranases have been dealt with in this review. Dextranases are promising for future use in various scientific and biotechnological applications.

  7. 21 CFR 520.1182 - Iron dextran suspension.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Iron dextran suspension. 520.1182 Section 520.1182 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... dose dispenser. (2) Indications for use. For the prevention of iron deficiency anemia in baby pigs. (3...

  8. The investigation of Co(II-dextran complexes

    Directory of Open Access Journals (Sweden)

    Mitić Žarko J.

    2007-01-01

    Full Text Available Co(II ion complex compounds were synthesized with reduced dextran (RD in alkali solutions using CoCl2, 6H2O and isolated in the solid state. UV-VIS spectrophotometric investigations of Co(II complexes with reduced dextran showed that the complexation of Co(II ions begins at pH over 7. The formation of Co(II ion complexes with dextran monomer units was observed at pH 7-13. With increase in solution pH the light absorption maximum of complex solutions shifts to longer wavelengths (bat-hochromic shift compared with [Co(H2O6]2+ ion. Dextran complexes with Co(II ion are formed by the displacement of water molecules from the coordination sphere of cobalt by the OH ligand groups. The spectrophotometric parameters of the investigated complexes are characteristic of a Co(II ion in octahedral or distorted octahedral coordination with O ligand atoms.

  9. Preparation and Determination of Drug-Polymer Interaction and In-vitro Release of Didanosine Microspheres made of Cellulose Acetate Phthalate or Ethyl cellulose Polymers

    OpenAIRE

    Sethi R. K; Barik B. B.; Sahoo S. K.

    2013-01-01

    The objective of this study was to formulate and evaluate the drug-polymer interaction of Didanosine using two polymers with different characteristics as Ethyl cellulose or Cellulose acetate phthalate. Microspheres were prepared by the emulsion solvent evaporation. The effect of drug-polymer interaction was studied for each of microspheres. Important parameters in the evaluation of a microencapsulation technique are encapsulation efficiency, yield production, particle size, surface characteri...

  10. Compression molding of aerogel microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Pekala, Richard W. (Pleasant Hill, CA); Hrubesh, Lawrence W. (Pleasanton, CA)

    1998-03-24

    An aerogel composite material produced by compression molding of aerogel microspheres (powders) mixed together with a small percentage of polymer binder to form monolithic shapes in a cost-effective manner. The aerogel composites are formed by mixing aerogel microspheres with a polymer binder, placing the mixture in a mold and heating under pressure, which results in a composite with a density of 50-800 kg/m.sup.3 (0.05-0.80 g/cc). The thermal conductivity of the thus formed aerogel composite is below that of air, but higher than the thermal conductivity of monolithic aerogels. The resulting aerogel composites are attractive for applications such as thermal insulation since fabrication thereof does not require large and expensive processing equipment. In addition to thermal insulation, the aerogel composites may be utilized for filtration, ICF target, double layer capacitors, and capacitive deionization.

  11. Compression molding of aerogel microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Pekala, R.W.; Hrubesh, L.W.

    1998-03-24

    An aerogel composite material produced by compression molding of aerogel microspheres (powders) mixed together with a small percentage of polymer binder to form monolithic shapes in a cost-effective manner is disclosed. The aerogel composites are formed by mixing aerogel microspheres with a polymer binder, placing the mixture in a mold and heating under pressure, which results in a composite with a density of 50--800 kg/m{sup 3} (0.05--0.80 g/cc). The thermal conductivity of the thus formed aerogel composite is below that of air, but higher than the thermal conductivity of monolithic aerogels. The resulting aerogel composites are attractive for applications such as thermal insulation since fabrication thereof does not require large and expensive processing equipment. In addition to thermal insulation, the aerogel composites may be utilized for filtration, ICF target, double layer capacitors, and capacitive deionization. 4 figs.

  12. Surface-assembled poly(I:C) on PEGylated PLGA microspheres as vaccine adjuvant: APC activation and bystander cell stimulation.

    Science.gov (United States)

    Hafner, Annina M; Corthésy, Blaise; Textor, Marcus; Merkle, Hans P

    2016-11-30

    Biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres are potential vehicles to deliver antigens for vaccination. Because they lack the full capacity to activate professional antigen presenting cells (APCs), combination with an immunostimulatory adjuvant may be considered. A candidate is the synthetic TLR3 ligand polyriboinosinic acid-polyribocytidylic acid, poly(I:C), which drives cell-mediated immunity. However, poly(I:C) has also been linked to the pathogenesis of autoimmunity, as affected by widespread stimulation of non-hematopoietic bystander cells. To address this aspect, we propose to minimize the poly(I:C) dose as well as to control the stimulation of non-immune bystander cells by poly(I:C). To facilitate the maturation of APCs with minimal poly(I:C) doses, we surface-assembled poly(I:C) onto PLGA microspheres. The microspheres' surface was further modified by poly(ethylene glycol) (PEG) coronas with varying PEG-densities. PLGA microspheres loaded with tetanus toxoid (tt) as model antigen were manufactured by microextrusion-based solvent extraction. The negatively charged PLGA(tt) microspheres were coated with polycationic poly(l-lysine) (PLL) polymers, either PLL itself or PEG-grafted PLL (PLL-g-PEG) with varying grafting ratios (g=2.2 and g=10.1). Stable surface assembly of poly(I:C) was achieved by subsequent incubation of polymer-coated PLGA microspheres with aqueous poly(I:C) solutions. We evaluated the immunostimulatory potential of such PLGA(tt) microsphere formulations on monocyte-derived dendritic cells (MoDCs) as well as human foreskin fibroblasts (HFFs) as model for non-hematopoietic bystander cells. Formulations with surface-assembled poly(I:C) readily activated MoDCs with respect to the expression of maturation-related surface markers, proinflammatory cytokine secretion and directed migration. When surface-assembled, poly(I:C) enhanced its immunostimulatory activity by more than one order of magnitude as compared to free poly

  13. Dextran fractional clearance studies in acute dengue infection.

    Directory of Open Access Journals (Sweden)

    Julie Nguyen-Pouplin

    2011-08-01

    Full Text Available BACKGROUND: Although increased capillary permeability is the major clinical feature associated with severe dengue infections the mechanisms underlying this phenomenon remain unclear. Dextran clearance methodology has been used to investigate the molecular sieving properties of the microvasculature in clinical situations associated with altered permeability, including during pregnancy and in various renal disorders. In order to better understand the characteristics of the vascular leak associated with dengue we undertook formal dextran clearance studies in Vietnamese dengue patients and healthy volunteers. METHODOLOGY/PRINCIPAL FINDINGS: We carried out serial clearance studies in 15 young adult males with acute dengue and evidence of vascular leakage a during the phase of maximal leakage and b one and three months later, as well as in 16 healthy control subjects. Interestingly we found no difference in the clearance profiles of neutral dextran solutions among the dengue patients at any time-point or in comparison to the healthy volunteers. CONCLUSIONS/SIGNIFICANCE: The surface glycocalyx layer, a fibre-matrix of proteoglycans, glycosaminoglycans, and plasma proteins, forms a complex with the underlying endothelial cells to regulate plasma volume within circumscribed limits. It is likely that during dengue infections loss of plasma proteins from this layer alters the permeability characteristics of the complex; physical and/or electrostatic interactions between the dextran molecules and the glycocalyx structure may temporarily restore normal function, rendering the technique unsuitable for assessing permeability in these patients. The implications for resuscitation of patients with dengue shock syndrome (DSS are potentially important. It is possible that continuous low-dose infusions of dextran may help to stabilize the permeability barrier in patients with profound or refractory shock, reducing the need for repeated boluses, limiting the total

  14. Microspheres in Plasma Display Panels

    Science.gov (United States)

    2006-01-01

    Filling small bubbles of molten glass with gases is just as difficult as it sounds, but the technical staff at NASA is not known to shy away from a difficult task. When Microsphere Systems, Inc. (MSI), of Ypsilanti, Michigan, and Imaging Systems Technology, Inc. (IST), of Toledo, Ohio, were trying to push the limits of plasma displays but were having difficulty with the designs, NASA s Glenn Garrett Morgan Commercialization Initiative (GMCI) assembled key personnel at Glenn Research Center and Ohio State University for a brainstorming session to come up with a solution for the companies. They needed a system that could produce hollow, glass micro-sized spheres (microspheres) that could be filled with a variety of gasses. But the extremely high temperature required to force the micro-sized glass bubbles to form at the tip of a metal nozzle resulted in severe discoloration of the microspheres. After countless experiments on various glass-metal combinations, they had turned to the GMCI for help. NASA experts in advanced metals, ceramics, and glass concluded that a new design approach was necessary. The team determined that what was needed was a phosphate glass composition that would remain transparent, and they went to work on a solution. Six weeks later, using the design tips from the NASA team, Tim Henderson, president of MSI, had designed a new system in which all surfaces in contact with the molten glass would be ceramic instead of metal. Meanwhile, IST was able to complete a Phase I Small Business Innovation Research (SBIR) grant supported by the National Science Foundation (NSF) and supply a potential customer with samples of the microspheres for evaluation as filler materials for high-performance insulations.

  15. Manufacture of poly(methyl methacrylate) microspheres using membrane emulsification.

    Science.gov (United States)

    Bux, Jaiyana; Manga, Mohamed S; Hunter, Timothy N; Biggs, Simon

    2016-07-28

    Accurate control of particle size at relatively narrow polydispersity remains a key challenge in the production of synthetic polymer particles at scale. A cross-flow membrane emulsification (XME) technique was used here in the preparation of poly(methyl methacrylate) microspheres at a 1-10 l h(-1) scale, to demonstrate its application for such a manufacturing challenge. XME technology has previously been shown to provide good control over emulsion droplet sizes with careful choice of the operating conditions. We demonstrate here that, for an appropriate formulation, equivalent control can be gained for a precursor emulsion in a batch suspension polymerization process. We report here the influence of key parameters on the emulsification process; we also demonstrate the close correlation in size between the precursor emulsion and the final polymer particles. Two types of polymer particle were produced in this work: a solid microsphere and an oil-filled matrix microcapsule.This article is part of the themed issue 'Soft interfacial materials: from fundamentals to formulation'.

  16. Preparation and in vitro characterization of mucoadhesive hydroxypropyl guar microspheres containing amlodipine besylate for nasal administration.

    Science.gov (United States)

    Swamy, N G N; Abbas, Z

    2011-11-01

    Amlodipine besylate microspheres for intranasal administration were prepared with an aim to avoid first-pass metabolism, to achieve controlled blood level profiles and to improve therapeutic efficacy. Hydroxypropyl Guar, a biodegradable polymer, was used in the preparation of microspheres by employing water in oil emulsification solvent evaporation technique. The formulation variables were drug concentration, emulsifier concentration, temperature, agitation speed and polymer concentration. All the formulations were evaluated for particle size, particle shape and surface morphology by scanning electron microscopy, percentage yield, drug entrapment efficiency, in vitro mucoadhesion test, degree of swelling and in vitro drug diffusion through sheep nasal mucosa. The microspheres obtained were free flowing, spherical and the particles ranged in size from 13.4±2.38 μm to 43.4±1.92 μm very much suitable for nasal delivery. Increasing polymer concentration resulted in increased drug entrapment efficiency and increased particle size. Amlodipine besylate was entrapped into the microspheres with an efficiency of 67.2±1.18 % to 81.8±0.64 %. The prepared microspheres showed good mucoadhesion properties, swellability and sustained the release of the drug over a period of 8 h. The data obtained were analysed by fitment into various kinetic models; it was observed that the drug release was matrix diffusion controlled and the release mechanism was found to be non-Fickian. Stability studies were carried out on selected formulations at 5±3°, 25±2°/60±5% RH and 40±2°/75±5% RH for 90 days. The drug content was observed to be within permissible limits and there were no significant deviations in the in vitro mucoadhesion and in vitro drug diffusion characteristics.

  17. Preparation and in vitro characterization of mucoadhesive hydroxypropyl guar microspheres containing amlodipine besylate for nasal administration

    Directory of Open Access Journals (Sweden)

    N. G. N. Swamy

    2011-01-01

    Full Text Available Amlodipine besylate microspheres for intranasal administration were prepared with an aim to avoid first-pass metabolism, to achieve controlled blood level profiles and to improve therapeutic efficacy. Hydroxypropyl Guar, a biodegradable polymer, was used in the preparation of microspheres by employing water in oil emulsification solvent evaporation technique. The formulation variables were drug concentration, emulsifier concentration, temperature, agitation speed and polymer concentration. All the formulations were evaluated for particle size, particle shape and surface morphology by scanning electron microscopy, percentage yield, drug entrapment efficiency, in vitro mucoadhesion test, degree of swelling and in vitro drug diffusion through sheep nasal mucosa. The microspheres obtained were free flowing, spherical and the particles ranged in size from 13.4±2.38 μm to 43.4±1.92 μm very much suitable for nasal delivery. Increasing polymer concentration resulted in increased drug entrapment efficiency and increased particle size. Amlodipine besylate was entrapped into the microspheres with an efficiency of 67.2±1.18 % to 81.8±0.64 %. The prepared microspheres showed good mucoadhesion properties, swellability and sustained the release of the drug over a period of 8 h. The data obtained were analysed by fitment into various kinetic models; it was observed that the drug release was matrix diffusion controlled and the release mechanism was found to be non-Fickian. Stability studies were carried out on selected formulations at 5±3° , 25±2° /60±5% RH and 40±2° /75±5% RH for 90 days. The drug content was observed to be within permissible limits and there were no significant deviations in the in vitro mucoadhesion and in vitro drug diffusion characteristics.

  18. Enhanced in vitro dissolution of Iloperidone using Caesalpinia Pulcherrima mucoadhesive microspheres

    Directory of Open Access Journals (Sweden)

    Pradum Pundlikrao Ige

    2015-03-01

    Full Text Available The aim of the present investigation was to improve the solubility and dissolution rate of Iloperidone. Microspheres containing Iloperidone were prepared by spray drying using mucilage extracted from seeds of Caesalpinia pulcherrima. The novelty of this work is that, the extraction of mucilage and its usage for preparation of drug loaded microspheres. The prepared microspheres were characterized by SEM, DSC, XRPD, FTIR, 1H-NMR, particle size, drug content, entrapment efficiency, in vitro dissolution and ex vivo mucoadhesion. Based on particle size, drug content, ex vivo mucoadhesive strength and in vitro drug release, the best formulation was optimized. Percent entrapment efficiency and mean particle size for optimized formulation was found to be 73.49 and 3.27 ± 1.23 μm, respectively. More precisely, mucilage of C. pulcherrima could be significant carrier of (drug and polymer ratio 1:5 microspheres for the development of oral drug delivery.

  19. 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

  20. POROUS WALL, HOLLOW GLASS MICROSPHERES

    Energy Technology Data Exchange (ETDEWEB)

    Sexton, W.

    2012-06-30

    Hollow Glass Microspheres (HGM) is not a new technology. All one has to do is go to the internet and Google{trademark} HGM. Anyone can buy HGM and they have a wide variety of uses. HGM are usually between 1 to 100 microns in diameter, although their size can range from 100 nanometers to 5 millimeters in diameter. HGM are used as lightweight filler in composite materials such as syntactic foam and lightweight concrete. In 1968 a patent was issued to W. Beck of the 3M{trademark} Company for 'Glass Bubbles Prepared by Reheating Solid Glass Particles'. In 1983 P. Howell was issued a patent for 'Glass Bubbles of Increased Collapse Strength' and in 1988 H. Marshall was issued a patent for 'Glass Microbubbles'. Now Google{trademark}, Porous Wall, Hollow Glass Microspheres (PW-HGMs), the key words here are Porous Wall. Almost every article has its beginning with the research done at the Savannah River National Laboratory (SRNL). The Savannah River Site (SRS) where SRNL is located has a long and successful history of working with hydrogen and its isotopes for national security, energy, waste management and environmental remediation applications. This includes more than 30 years of experience developing, processing, and implementing special ceramics, including glasses for a variety of Department of Energy (DOE) missions. In the case of glasses, SRS and SRNL have been involved in both the science and engineering of vitreous or glass based systems. As a part of this glass experience and expertise, SRNL has developed a number of niches in the glass arena, one of which is the development of porous glass systems for a variety of applications. These porous glass systems include sol gel glasses, which include both xerogels and aerogels, as well as phase separated glass compositions, that can be subsequently treated to produce another unique type of porosity within the glass forms. The porous glasses can increase the surface area compared to &apos

  1. Mucoadhesive, triclosan-loaded polymer microspheres for application to the oral cavity: preparation and controlled release characteristics.

    Science.gov (United States)

    Kockisch, Sandra; Rees, Gareth D; Tsibouklis, John; Smart, John D

    2005-01-01

    The aim of this study was to develop mucoadhesive microspheres that can be utilised for the controlled release of triclosan in oral-care formulations, specifically dental pastes. Using a double-emulsion solvent evaporation technique, triclosan was incorporated into microspheres that were prepared from Gantreztrade mark MS-955, Carbopol 974P, polycarbophil or chitosan and the profiles for its release were established under simulated 'in use' conditions. Triclosan was rapidly released into a sodium lauryl sulphate containing buffer from all but the chitosan microspheres. The release of triclosan from microspheres suspended in a non-aqueous paste, was found to be sustained over considerable time-periods, which were influenced strongly by the nature of the polymeric carrier. For microspheres that were fabricated from Gantrez, Carbopol or polycarbophil, the release appeared to obey zero-order kinetics whereas in the case of chitosan-derived vehicles, the release profile fitted the Baker and Lonsdale model. The work has demonstrated that these polymeric microspheres, particularly those of chitosan, are promising candidates for the sustained release of triclosan in the oral cavity.

  2. ERYTHROMYCIN POLYLACTIC ACID MICROSPHERES FOR LUNG TARGETING

    Institute of Scientific and Technical Information of China (English)

    YANGFan; YANBing; 等

    2002-01-01

    AIM:To prepare polylactiv acid microspheres of Erythromycin for Lung targeting.METHEDS:The orthogonal test design was used to optimize the technology of preparation.The character of the microspheres,drug release in vitro,stabiligy and tissue distribution were examined. RESULTS:The Erythromycin polylatic acid microspheres was regular in its morphology.Drug was enveloped in microspheres but not physically mixed with PDLLA.The average particle size was 11.65μm with over 94% of the microspheres being in the range of 5-20μm;The drug loading and the incorporation efficiency were 18% and 60% respectively.The microspheres were stable for three month at 4℃ and room temperature.The in vitro release properties could be expressed by the Higuchi′s equation:y=28.067+3.8515t1/2(r=0.9834).Comparing with injection,the drug in microspheres was more concentrated in lung tissue.CONLUSION:Erythromycin polylactic acid microspheres showed significant sustained release and lung targeting.

  3. Assembly of ordered magnetic microsphere arrays

    Science.gov (United States)

    Xu, Wanling; Ketterson, John

    2008-08-01

    We have developed a straightforward technique to assemble ordered arrays of magnetic microspheres on patterned thin Permalloy (Py) films deposited on the surface of a silicon wafer. Droplets containing micrometer-sized carboxyl paramagnetic microspheres are placed on a horizontally oriented wafer. The field produced by a permanent magnet placed under the wafer is rendered inhomogeneous by the patterned Py features and the resulting field gradients attract and hold the paramagnetic microspheres to these features. While the magnetic microspheres are being attracted to and secured on the pattered Permalloy features, a horizontal flow is created by a pipette, which also removes loose (unsecured) microspheres. By applying this technique to a cocktail of individually functionalized microspheres, a sensor could be realized, which will screen, in parallel, for a large number of targets per unit area. The ability to resolve individual microspheres is close to 100%. A desirable feature is that the substrate is reusable; removing the magnet allows an existing batch of microspheres, which may have lost sensitivity due to environmental exposure, to be flushed from the substrate and replaced with a new batch. The technique complements existing approaches in the field of microarrays widely used in immunoassay, DNA fragment detection, pathogen detection, and other applications in functional genomics and diagnostics.

  4. 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 impermeab

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

    National Research Council Canada - National Science Library

    Szekalska, Marta; Wróblewska, Magdalena; Sosnowska, Katarzyna; Winnicka, Katarzyna

    2016-01-01

      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...

  6. Sunitinib microspheres based on [PDLLA-PEG-PDLLA]-b-PLLA multi-block copolymers for ocular drug delivery

    NARCIS (Netherlands)

    Ramazani, F.; Hiemstra, C.; Steendam, R.; Kazazi-Hyseni, F.; Van Nostrum, C. F.; Storm, G.; Kiessling, F.; Lammers, T.; Hennink, W. E.; Kok, R. J.

    2015-01-01

    Sunitinib is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that blocks several angiogenesis related pathways. The aim of this study was to develop sunitinib-loaded polymeric microspheres that can be used as intravitreal formulation for the treatment of ocular diseases. A series of novel

  7. Phase separation behavior of fusidic acid and rifampicin in PLGA microspheres.

    Science.gov (United States)

    Gilchrist, Samuel E; Rickard, Deborah L; Letchford, Kevin; Needham, David; Burt, Helen M

    2012-05-01

    The purpose of this study was to characterize the phase separation behavior of fusidic acid (FA) and rifampicin (RIF) in poly(d,l-lactic acid-co-glycolic acid) (PLGA) using a model microsphere formulation. To accomplish this, microspheres containing 20% FA with 0%, 5%, 10%, 20%, and 30% RIF and 20% RIF with 30%, 20% 10%, 5%, and 0% FA were prepared by solvent evaporation. Drug-polymer and drug-drug compatibility and miscibility were characterized using laser confocal microscopy, Raman spectroscopy, XRPD, DSC, and real-time video recordings of single-microsphere formation. The encapsulation of FA and RIF alone, or in combination, results in a liquid-liquid phase separation of solvent-and-drug-rich microdomains that are excluded from the polymer bulk during microsphere hardening, resulting in amorphous spherical drug-rich domains within the polymer bulk and on the microsphere surface. FA and RIF phase separate from PLGA at relative droplet volumes of 0.311 ± 0.014 and 0.194 ± 0.000, respectively, predictive of the incompatibility of each drug and PLGA. When coloaded, FA and RIF phase separate in a single event at the relative droplet volume 0.251 ± 0.002, intermediate between each of the monoloaded formulations and dependent on the relative contribution of FA or RIF. The release of FA and RIF from phase-separated microspheres was characterized exclusively by a burst release and was dependent on the phase exclusion of surface drug-rich domains. Phase separation results in coalescence of drug-rich microdroplets and polymer phase exclusion, and it is dependent on the compatibility between FA and RIF and PLGA. FA and RIF are mutually miscible in all proportions as an amorphous glass, and they phase separate from the polymer as such. These drug-rich domains were excluded to the surface of the microspheres, and subsequent release of both drugs from the microspheres was rapid and reflected this surface location.

  8. Holmium-lipiodol-alginate microspheres for fluoroscopy-guided embolotherapy and multimodality imaging.

    Science.gov (United States)

    Oerlemans, Chris; Seevinck, Peter R; Smits, Maarten L; Hennink, Wim E; Bakker, Chris J G; van den Bosch, Maurice A A J; Nijsen, J Frank W

    2015-03-30

    Embolotherapy is a minimally invasive transcatheter technique aiming at reduction or complete obstruction of the blood flow by infusion of micro-sized particles in order to induce tumor regression. A major drawback of the current commercially available and clinically used microspheres is that they cannot be detected in vivo with medical imaging techniques, impeding intra- and post-procedural feedback. It can be expected that real-time monitoring of microsphere infusion and post-procedural imaging will result in better predictability and higher efficacy of the treatment. In this study, a novel microsphere formulation has been developed that can be visualized with fluoroscopy, X-ray computed tomography (CT) and magnetic resonance imaging (MRI). The microspheres were prepared with the JetCutter technique and consist of alginate (matrix-forming polymer), holmium (cross-linking and MRI contrast agent), lipiodol (radiopaque contrast agent) and Pluronic F-68 (surfactant). The mean size (±SEM) of the hydrated holmium-lipiodol-alginate microspheres (Ho-lip-ams) was 570±12 μm with a holmium content of 0.38±0.01% (w/w). Stability studies showed that the microspheres remained intact during incubation for two weeks in fetal calf serum (FCS) at 37 °C. The inclusion of lipiodol in the microspheres rendered excellent visualization capabilities for fluoroscopy and CT, whereas the holmium ions, which keep the alginate network together, also allow MR imaging. In this study it was shown that single sphere detection was possible by fluoroscopy, CT and MRI. The Ho-lip-ams were visualized in real-time, during infusion in a porcine kidney using fluoroscopy, and post-procedural, the deposition of the microspheres was examined with fluoroscopy, (cone beam rotational) CT and MRI. The different imaging modalities showed similar deposition patterns of the microspheres within the organ. The combination of intra-procedural visualization, multimodality imaging for patient follow-up and the

  9. Spectrally resolved resonant propulsion of dielectric microspheres

    CERN Document Server

    Li, Yangcheng; Limberopoulos, Nicholaos I; Urbas, Augustine M; Astratov, Vasily N

    2015-01-01

    Use of resonant light forces opens up a unique approach to high-volume sorting of microspherical resonators with much higher uniformity of resonances compared to that in coupled-cavity structures obtained by the best semiconductor technologies. In this work, the spectral response of the propulsion forces exerted on polystyrene microspheres near tapered microfibers is directly observed. The measurements are based on the control of the detuning between the tunable laser and internal resonances in each sphere with accuracy higher than the width of the resonances. The measured spectral shape of the propulsion forces correlates well with the whispering-gallery mode resonances in the microspheres. The existence of a stable radial trap for the microspheres propelled along the taper is demonstrated. The giant force peaks observed for 20-{\\mu}m spheres are found to be in a good agreement with a model calculation demonstrating an efficient use of the light momentum for propelling the microspheres.

  10. Hydroxyapatite nanocrystal coating on biodegradable microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Okada, Masahiro [Department of Bioengineering, Advanced Medical Engineering Center, National Cardiovascular Center Research Institute, 5-7-1 Fujishirodai, Suita, Osaka 565-8565 (Japan); Furuzono, Tsutomu, E-mail: furuzono@ri.ncvc.go.jp [Department of Bioengineering, Advanced Medical Engineering Center, National Cardiovascular Center Research Institute, 5-7-1 Fujishirodai, Suita, Osaka 565-8565 (Japan)

    2010-10-15

    Nano-sized single crystals of calcined hydroxyapatite (HAp) were uniformly coated on poly(L-lactic acid) (PLLA) microspheres through the ionic interaction between calcium ions on the HAp nanocrystal and carboxyl groups on the PLLA microsphere. In order to coat the substrate with HAp nanocrystals through ionic interaction, the surfaces of the PLLA microspheres were hydrolyzed in an alkaline aqueous solution at pH 11.0 for 1 h at room temperature. The interaction between the HAp nanocrystals and the carboxyl groups originating from PLLA end groups was estimated by Fourier transform infrared spectroscopy. The alkali-treated PLLA microspheres were coated with HAp nanocrystals by immersing the microspheres in an ethanol dispersion of HAp nanocrystals followed by washing in an ultrasonic bath.

  11. Novel tamarind seed polysaccharide-alginate mucoadhesive microspheres for oral gliclazide delivery: in vitro-in vivo evaluation.

    Science.gov (United States)

    Pal, Dilipkumar; Nayak, Amit Kumar

    2012-04-01

    Novel tamarind seed polysaccharide (TSP)-alginate mucoadhesive microspheres were prepared using TSP and alginate as blend in different ratios with different calcium chloride (CaCl(2)) concentration as a cross linker by ionotropic gelation. The prepared microspheres were of spherical shape having rough surfaces, and average particle sizes within the range of 752.12 ± 6.42 to 948.49 ± 20.92 µm. The drug entrapment efficiency of these microspheres were within the range between 58.12 ± 2.42 to 82.78 ± 3.43% w/w. Fourier transform infrared (FTIR) studies indicated that there were no reactions between gliclazide, and polymers (TSP, and sodium alginate) used. Different formulations of gliclazide loaded TSP-alginate microspheres showed prolonged in vitro release profiles of gliclazide over 12 hours in both stomach pH (pH 1.2), and intestinal pH (pH 7.4). It was found that the gliclazide release in gastric pH was comparatively slow and sustained than intestinal pH. These TSP-alginate microspheres also exhibited good mucoadhesivity. The in vivo studies on alloxan-induced diabetic rats (Animal Ethical Committee registration number: IFTM/837ac/0160) demonstrated the significant hypoglycemic effect of selected formulation of TSP-alginate mucoadhesive microspheres containing gliclazide on oral administration. This developed gliclazide loaded new TSP-alginate mucoadhesive microspheres may be very much useful for prolonged systemic absorption of gliclazide for proper maintaining blood glucose level and advanced patient compliance.

  12. Biofunctionalization of silica microspheres for protein separation

    Energy Technology Data Exchange (ETDEWEB)

    Li, Binjie [Institute of Immunology, Henan University, Kaifeng 475004 (China); Key Laboratory of Ministry of Education for Special Functional Materials, Henan University, Kaifeng 475004 (China); Zou, Xueyan [Key Laboratory of Ministry of Education for Special Functional Materials, Henan University, Kaifeng 475004 (China); Zhao, Yanbao, E-mail: yanbaozhao@126.com [Key Laboratory of Ministry of Education for Special Functional Materials, Henan University, Kaifeng 475004 (China); Sun, Lei [Institute of Immunology, Henan University, Kaifeng 475004 (China); Key Laboratory of Ministry of Education for Special Functional Materials, Henan University, Kaifeng 475004 (China); Li, Shulian [Institute of Immunology, Henan University, Kaifeng 475004 (China)

    2013-07-01

    Mercapto-silica (SiO{sub 2}–SH) microspheres were prepared via direct hydrolysis of 3-mercaptopropyltrimethoxysilane (MPS) in a basic aqueous solution. The content of surface thiol group (-SH) of SiO{sub 2}–SH microspheres was measured by Ellman's reagent method and X-ray photoelectron spectroscopy (XPS) and the content of surface thiol group of SiO{sub 2}–SH microspheres is strongly dependent on the reaction conditions. The thermal stability of SiO{sub 2}–SH microspheres was evaluated by thermogravimetric (TG) analysis, which tended to reduce with the increase of content of surface thiol groups. SiO{sub 2}–SH microspheres can be easily modified with reduced glutathione (GSH) to generate SiO{sub 2}–GSH microspheres for the affinity separation of Glutathione S-transferase (GST). Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was performed to examine the validity of the separation procedure. The results showed that SiO{sub 2}–GSH microspheres were efficient in GST affinity separation from mixed proteins. - Graphical abstract: The prepared SiO{sub 2}–SH microsphere binding reduced glutathione (SiO{sub 2}–GSH) as affinity precipitation support can capture selectively Glutathione S-transferase (GST) from mixed protein solution. Highlights: ► SiO{sub 2}–SH microspheres were prepared in water using one-pot synthesis. ► The content of surface -SH was investigated by Ellman method and XPS spectra. ► The ratio of -SH to mass strongly depends on the reaction conditions. ► SiO{sub 2}–SH microspheres were biofunctionalized by glutathione. ► SiO{sub 2}–GSH can be used to capture selectively Glutathione S-transferase.

  13. Porous microspheres as promising vehicles for the topical delivery of poorly soluble asiaticoside accelerate wound healing and inhibit scar formation in vitro &in vivo.

    Science.gov (United States)

    Zhang, Chen-Zhen; Niu, Jie; Chong, Yee-Song; Huang, Yan-Fen; Chu, Yang; Xie, Sheng-Yang; Jiang, Zhi-Hong; Peng, Li-Hua

    2016-12-01

    Asiaticoside is a natural compound possessing diverse pharmacological effects with great potential for clinical use. However, the low solubility and oil-water partition coefficient of asiaticoside lead to reduced effect and limited application. This study aims to construct a porous microsphere for the sustained release of asiaticoside to improve its absorption and enhance the therapeutic effects. Parameters of the formulations, including the drug to polymer ratio, solvent amounts of the inner and external phases, the stirring speed for preparation, and the drug entrapment efficiency were investigated and optimized. Particle size, morphology, pores structure, and Fourier transform infrared spectrum of the microsphere were characterized. The release kinetics and cellular uptake profiles of the asiaticoside-microspheres were examined. The therapeutic effects of asiaticoside-microspheres on wound healing and skin appendages regeneration were investigated in vitro & in vivo. Results showed that the optimized asiaticoside-microspheres possess spherical spongy structure with cylindrical holes. Asiaticoside can be loaded in the microsphere with high efficiency and released with sustained manner. The cellular uptake of asiaticoside from the microspheres was increased with 9.1 folds higher than that of free solution. Asiaticoside-microspheres expressed the strong promotion in the proliferation, migration of keratinocytes and wound scratching healing in vitro. More importantly, they significantly accelerated the re-epithelization, collagen synthesis and pro-angiogenesis in the rat full-skin wound healing. Porous microsphere was shown a novel carrier for the sustained delivery of poorly soluble asiaticoside, with absorption and therapeutic effects improved. Asiaticoside-microsphere is a promising topical preparation with excellent regenerative effects for the wound therapy.

  14. Injectable PLGA microsphere/calcium phosphate cements: physical properties and degradation characteristics.

    Science.gov (United States)

    Habraken, W J E M; Wolke, J G C; Mikos, A G; Jansen, J A

    2006-01-01

    Calcium phosphate (CaP) cements show an excellent biocompatibility and often have a high mechanical strength, but in general degrade relatively slow. To increase degradation rates, macropores can be introduced into the cement, e.g., by the inclusion of biodegradable microspheres into the cement. The aim of this research is to develop an injectable PLGA microsphere/CaP cement with sufficient setting/cohesive properties and good mechanical and physical properties. PLGA microspheres were prepared using a water-in-oil-in-water double-emulsion technique. The CaP-cement used was Calcibon, a commercially available hydroxyapatite-based cement. 10:90 and 20:80 dry wt% PLGA microsphere/CaP cylindrical scaffolds were prepared as well as microporous cement (reference material). Injectability, setting time, cohesive properties and porosity were determined. Also, a 12-week degradation study in PBS (37 degree C) was performed. Results showed that injectability decreased with an increase in PLGA microsphere content. Initial and final setting time of the PLGA/CaP samples was higher than the microporous sample. Porosity of the different formulations was 40.8% (microporous), 60.2% (10:90) and 69.3% (20:80). The degradation study showed distinct mass loss and a pH decrease of the surrounding medium starting from week 6 with the 10:90 and 20:80 formulations, indicating PLGA erosion. Compression strength of the PLGA microsphere/CaP samples decreased siginificantly in time, the microporous sample remained constant. After 12 weeks both PLGA/CaP samples showed a structure of spherical micropores and had a compressive strength of 12.2 MPa (10:90) and 4.3 MPa (20:80). Signs of cement degradation were also found with the 20:80 formulation. In conclusion, all physical parameters were well within workable ranges with both 10:90 and 20:80 PLGA microsphere/CaP cements. After 12 weeks the PLGA was totally degraded and a highly porous, but strong scaffold remained.

  15. The influence of gellan gum on the transfer of fluorescein dextran across rat nasal epithelium in vivo.

    Science.gov (United States)

    Jansson, Björn; Hägerström, Helene; Fransén, Nelly; Edsman, Katarina; Björk, Erik

    2005-04-01

    The nasal uptake of a 3000 Da fluorescein dextran (FD3) was investigated in rats, using fluorescence microscopy. The uptake from a formulation containing deacetylated gellan gum, an in situ gelling agent, was compared to that from a mannitol solution. Additionally, the rheological behavior of the gellan gum in water and saline was studied. It was shown that the gellan gum solution was easily administered owing to its low viscosity, and upon contact with the mucosa, a gel was formed. The epithelial uptake and transfer of FD3 appeared to be increased and prolonged using the gellan gum formulation. This increase was not accompanied by qualitative changes of the epithelial FD3 distribution or any visible harmful effects.

  16. Size-controlled nanoassemblies based on cyclodextrin-modified dextrans.

    Science.gov (United States)

    Wintgens, Véronique; Nielsen, Thorbjørn Terndrup; Larsen, Kim Lambertsen; Amiel, Catherine

    2011-09-09

    Nanoassemblies formed by host/guest interactions between two polymers in aqueous media are studied. Two types of polymers with the same dextran backbone are modified with adamantyl or βCD groups. The sizes of the spontaneously formed nanoassemblies depend on the βCD:Ada ratio and on the total concentration and composition of the mixtures. The results can be rationalized by assuming a core/shell structure of the nanoassemblies, the core resulting from associative phase separation of the two polymers and being stabilized by an external shell made of Ada-grafted dextran and containing ions adsorbed from the solution. Hydrophobic compounds such as benzophenone can be incorporated efficiently without inducing changes in properties of the nanoassemblies.

  17. Effect of Molecular Weight and Molar Ratio of Dextran on Self-Assembly of Dextran Stearate Polymeric Micelles as Nanocarriers for Etoposide

    Directory of Open Access Journals (Sweden)

    Jaleh Varshosaz

    2012-01-01

    Full Text Available Amphiphilic polymer surfactants are composed of hydrophilic and hydrophobic polymers and are widely used in targeted drug delivery. The purpose of this study was the evaluation of the effect of molecular weight and molar ratio of dextran on physicochemical properties of dextran stearate polymeric micelles. Dextran stearate was synthesized by acylation of dextran with stearoyl chloride. Etoposide loaded polymeric micelles were prepared by dialysis method. The resulting micelles were evaluated for particle size, zeta potential, critical micelle concentration (CMC, drug loading capacity, and release efficiency. Cytotoxicity and cellular uptake of micelles were studied in CT-26 colorectal carcinoma cell line. Molecular weight and molar ratio of dextran-stearate were impressive on zeta potential, CMC, drug loading capacity, and release efficiency. Unlike polymer molecular weight, molar ratio of stearate had a significant effect on cytotoxicity and particle size of etoposide loaded micelles. Although molecular weight of dextran had no significant effect on cytotoxicity of micelles on CT-26 cells, it had drastic attributes for stability of polymeric micelles. Consequently, both variables of molecular weight of dextran and molar ratio of stearate should be taken into account to have a stable and effective micelle of dextran-stearate.

  18. Assessment of active pharmaceutical ingredient particle size in tablets by Raman chemical imaging validated using polystyrene microsphere size standards.

    Science.gov (United States)

    Kuriyama, Atsushi; Ozaki, Yukihiro

    2014-04-01

    Particle size is a critical parameter for controlling pharmaceutical quality. The aim of this study was to assess the size of the micrometer-scale active pharmaceutical ingredients (API) in tablets using Raman chemical imaging and to understand the effects of formulation on particle size. Model tablets containing National Institute of Standards and Technology traceable polystyrene microsphere size standards were developed to determine the binarization threshold value of Raman chemical images for API particle sizing in specific formulations and processes. Three sets of model tablets containing 5, 10, and 15 μm polystyrene microspheres, used to mimic API, were prepared using a commercial tablet formulation (Ebastel tablets, mean API particle size was about 5 μm). Raman mapping with a 50× objective (NA, 0.75) was applied to tablet cross-sections, and particle size of polystyrene microspheres was estimated from binary images using several binarization thresholds. Mean particle size for three sets of polystyrene microspheres showed good agreement between pre- and postformulation (the slope = 1.024, R = 1.000) at the specific threshold value ((mean + 0.5σ) of the polystyrene-specific peak intensity histogram), regardless of particle agglomeration, tablet surface roughness, and laser penetration depth. The binarization threshold value showed good applicability to Ebastel tablets, where the API-specific peak intensity histogram showed a pattern similar to that of polystyrene microspheres in model tablets. The model tablets enabled determination of an appropriate binarization threshold for assessing the mean particle size of micrometer-scale API in tablets by utilizing the unique physicochemical properties of polystyrene microspheres.

  19. Acetalated dextran encapsulated AR-12 as a host-directed therapy to control Salmonella infection.

    Science.gov (United States)

    Hoang, Ky V; Borteh, Hassan M; Rajaram, Murugesan V S; Peine, Kevin J; Curry, Heather; Collier, Michael A; Homsy, Michael L; Bachelder, Eric M; Gunn, John S; Schlesinger, Larry S; Ainslie, Kristy M

    2014-12-30

    AR-12 has been evaluated in clinical trials as an anti-cancer agent but also has demonstrated host-directed, broad-spectrum clearance of bacteria. We have previously shown that AR-12 has activity in vitro against Salmonella enterica serovar Typhimurium and Francisella species by inducing autophagy and other host immune pathways. AR-12 treatment of S. Typhimurium-infected mice resulted in a 10-fold reduction in bacterial load in the liver and spleen and an increased survival time. However, AR-12 treatment did not protect mice from death, likely due poor formulation. In the current study, AR-12 was encapsulated in a microparticulate carrier formulated from the novel degradable biopolymer acetalated dextran (Ace-DEX) and subsequently evaluated for its activity in human monocyte-derived macrophages (hMDMs). Our results show that hMDMs efficiently internalized Ace-DEX microparticles (MPs), and that encapsulation significantly reduced host cell cytotoxicity compared to unencapsulated AR-12. Efficient macrophage internalization of AR-12 loaded MPs (AR-12/MPs) was further demonstrated by autophagosome formation that was comparable to free AR-12 and resulted in enhanced clearance of intracellular Salmonella. Taken together, these studies provide support that Ace-DEX encapsulated AR-12 may be a promising new therapeutic agent to control intracellular bacterial pathogens of macrophages by targeting delivery and reducing drug toxicity.

  20. Preparation of polyvinylpyrrodione microspheres by dispersion polymerization

    Institute of Scientific and Technical Information of China (English)

    Linfeng ZHAI; Tiejun SHI; Hualin WANG

    2009-01-01

    The preparation of polyvinylpyrrolidone (PVP) microspheres in ethyl acetate by dispersion polymerization with N-vinylpyrrolidone (NVP) as initial monomer, poly(N-vinylpyrrolidone-co-vinyl acetate) (P (NVP-co-VAc)) as dispersant, and 2, 2'-azobisisobutyr-onitrile(AIBN) as initiator is reported. The influences of monomer concentration, dispersant concentration and initiator concentration on the size of PVP microspheres as well as the monomer conversion were studied. The structure and properties of PVP microspheres were analyzed. The results show that the prepared PVP micro-spheres have a mean diameter of 3-4 μm. With an increase in NVP concentration, the size and the molecular weight of the PVP microspheres as well as the monomer conversion all increase. With increasing P(NVP-co-VAc) concentra-tions, the PVP molecular weight and monomer conversion both increase while the size of the microspheres becomes smaller. As the concentration of AIBN increases, the microsphere size and monomer conversion increase whereas the PVP molecular weight decreases. The PVP prepared by dispersion polymerization has a crystal structure, and its molecular weight is lower compared to that prepared by solution polymerization.

  1. Release of a Wound-Healing Agent from PLGA Microspheres in a Thermosensitive Gel

    Directory of Open Access Journals (Sweden)

    H. A. Machado

    2013-01-01

    Full Text Available The purpose of this research was to develop a topical microsphere delivery system in a thermosensitive 20% poloxamer 407 gel (Pluronic F127 to control release of KSL-W, a cationic antimicrobial decapeptide, for a period of 4–7 days for potential application in combat related injuries. KSL-W loaded microsphere formulations were prepared by a solvent extraction-evaporation method (water-oil-water, with poly (D,L-lactic-co-glycolic acid (PLGA (50 : 50, low-weight, and hydrophilic end as the polymeric system. After optimization of the process, three formulations (A, B, and C were prepared with different organic to water ratio of the primary emulsion while maintaining other components and manufacturing parameters constant. Formulations were characterized for surface morphology, porous nature, drug loading, in vitro drug release, and antimicrobial activity. Microspheres containing 20% peptide with porous surfaces and internal structure were prepared in satisfactory yields and in sizes varying from 25 to 50 μm. Gels of 20% Pluronic F127, which were liquid at or below 24.6°C and formed transparent films at body temperature, were used as carriers for the microspheres. Rheological studies showed a gelation temperature of 24.6°C for the 20% Pluronic F127 gel alone. Gelation temperature and viscosity of formulations A, B, and C as a function of temperature were very close to those of the carrier. A Franz diffusion cell system was used to study the release of peptide from the microspheres suspended in both, phosphate-buffered saline (PBS and a 20% Pluronic F127 gel. In vitro release of greater than 50% peptide was found in all formulations in both PBS and the gel, and in one formulation there was a release of 75% in both PBS and the gel. Fractions collected from the release process were also tested for bactericidal activity against Staphylococcus epidermidis using the broth microdilution method and found to provide effective antimicrobial activity

  2. Amphotericin B formulations and drug targeting.

    Science.gov (United States)

    Torrado, J J; Espada, R; Ballesteros, M P; Torrado-Santiago, S

    2008-07-01

    Amphotericin B is a low-soluble polyene antibiotic which is able to self-aggregate. The aggregation state can modify its activity and pharmacokinetical characteristics. In spite of its high toxicity it is still widely employed for the treatment of systemic fungal infections and parasitic disease and different formulations are marketed. Some of these formulations, such as liposomal formulations, can be considered as classical examples of drug targeting. The pharmacokinetics, toxicity and activity are clearly dependent on the type of amphotericin B formulation. New drug delivery systems such as liposomes, nanospheres and microspheres can result in higher concentrations of AMB in the liver and spleen, but lower concentrations in kidney and lungs, so decreasing its toxicity. Moreover, the administration of these drug delivery systems can enhance the drug accessibility to organs and tissues (e.g., bone marrow) otherwise inaccessible to the free drug. During the last few years, new AMB formulations (AmBisome, Abelcet, and Amphotec) with an improved efficacy/toxicity ratio have been marketed. This review compares the different formulations of amphotericin B in terms of pharmacokinetics, toxicity and activity and discusses the possible drug targeting effect of some of these new formulations.

  3. Characterization of a Polyamine Microsphere and Its Adsorption for Protein

    Directory of Open Access Journals (Sweden)

    Huixian Wei

    2012-12-01

    Full Text Available A novel polyamine microsphere, prepared from the water-in-oil emulsion of polyethylenimine, was characterized. The investigation of scanning electron microscopy showed that the polyamine microsphere is a regular ball with a smooth surface. The diameter distribution of the microsphere is 0.37–4.29 μm. The isoelectric point of the microsphere is 10.6. The microsphere can adsorb proteins through the co-effect of electrostatic and hydrophobic interactions. Among the proteins tested, the highest value of adsorption of microsphere, 127.8 mg·g−1 microsphere, was obtained with lipase. In comparison with other proteins, the hydrophobic force is more important in promoting the adsorption of lipase. The microsphere can preferentially adsorb lipase from an even mixture of proteins. The optimum temperature and pH for the selective adsorption of lipase by the microsphere was 35 °C and pH 7.0.

  4. A method for synthesis and functionalization of ultrasmall superparamagnetic covalent carriers based on maghemite and dextran

    Energy Technology Data Exchange (ETDEWEB)

    Mornet, Stephane [Institut de Chimie de la Matiere Condensee de Bordeaux, CNRS UPR 9048, Universite Bordeaux-1, 87 avenue du Dr Albert Schweitzer, F-33608 Pessac, Cedex (France); Portier, Josik [Institut de Chimie de la Matiere Condensee de Bordeaux, CNRS UPR 9048, Universite Bordeaux-1, 87 avenue du Dr Albert Schweitzer, F-33608 Pessac, Cedex (France); Duguet, Etienne [Institut de Chimie de la Matiere Condensee de Bordeaux, CNRS UPR 9048, Universite Bordeaux-1, 87 avenue du Dr Albert Schweitzer, F-33608 Pessac, Cedex (France)]. E-mail: duguet@icmcb.u-bordeaux1.fr

    2005-05-15

    A new generation of susceptibility contrast agents for MRI and based on maghemite cores covalently bonded to dextran stabilizing macromolecules was investigated. The multistep preparation of these versatile ultrasmall superparamagnetic iron oxides (VUSPIO) consisted of colloidal maghemite synthesis, surface modification by aminopropylsilane groups, and coupling of partially oxidized dextran via Schiff's bases and secondary amine bonds. The dextran corona might be easily derivatized, e.g. by PEGylation.

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

    NARCIS (Netherlands)

    Manen, van Henk-Jan; Apeldoorn, van Aart A.; Verrijk, Ruud; Blitterswijk, van 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 par

  6. 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.

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

    Science.gov (United States)

    Sarabia-Sainz, Andre-i; Sarabia-Sainz, Hector Manuel; Ramos-Clamont Montfort, Gabriela; Mata-Haro, Veronica; Guzman-Partida, Ana María; Guzman, Roberto; Garcia-Soto, Mariano; Vazquez-Moreno, Luz

    2015-01-01

    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. PMID:26389896

  8. Synthesis of polycaprolactone/nano hydroxyapatite microspheres; Sintese de microesferas de policaprolactona/nanohidroxiapatita

    Energy Technology Data Exchange (ETDEWEB)

    Sampaio, Greyce Y.H.; Souza, Mairly K. da S.; Melo, Rafaela Q. da C.; Carrodeguas, Raul G.; Fook, Marcus V.L., E-mail: greycesampaio@gmail.com [Universidade Federal de Campina Grande (UFCG), Campina Grande, PB (Brazil)

    2013-07-01

    Polycaprolactone(PCL)/nano hydroxyapatite(nHA) microspheres are advantageous material for manufacturing tridimensional scaffolds and formulating drug delivery systems for bone regeneration. The work was aimed to study the effect of processing variables on the properties of PCL/nHA microspheres. nHA was produced by precipitation method and was obtained calcium deficient nanoparticles consisted of nanorods (∼47 nm x ∼8 nm), according to the results of XRD, FTIR and TEM. PCL/nHA microspheres was produced by solid-in-oil-in-water emulsion solvent evaporation method. The variables studied were concentration of PCL (5,7.5 and 10 % w/v), nHA addition (17, 23 and 28.5% m/m) and surface treatment of nHA with stearic acid (AE). PCL/nHA microspheres were characterized by XRD, FTIR, SEM and TGA. The best result was obtained with a PCL concentration of 10% (w/v) and 23 % (m/m) of modified nHA. Solid PCL/nHA particles ranging 30-70 μm and containing 14 % of nHA dispersed in the polymer matrix were obtained, with agglomerates of nHA raging 5 -15 μm. These results suggest the promising use of this material in bone regeneration devices. (author)

  9. Cellular interactions of lauric acid and dextran-coated magnetite nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Pradhan, Pallab [School of Biosciences and Bioengineering, Indian Institute of Technology, Mumbai 400076 (India); Giri, Jyotsnendu [Department of Metallurgical Engineering and Materials Science, Indian Institute of Technology, Mumbai 400076 (India); Banerjee, Rinti [School of Biosciences and Bioengineering, Indian Institute of Technology, Mumbai 400076 (India); Bellare, Jayesh [School of Biosciences and Bioengineering, Indian Institute of Technology, Mumbai 400076 (India); Bahadur, Dhirendra [Department of Metallurgical Engineering and Materials Science, Indian Institute of Technology, Mumbai 400076 (India)]. E-mail: dhirenb@iitb.ac.in

    2007-04-15

    In vitro cytocompatibility and cellular interactions of lauric acid and dextran-coated magnetite nanoparticles were evaluated with two different cell lines (mouse fibroblast and human cervical carcinoma). Lauric acid-coated magnetite nanoparticles were less cytocompatible than dextran-coated magnetite nanoparticles and cellular uptake of lauric acid-coated magnetic nanoparticles was more than that of dextran-coated magnetite nanoparticles. Lesser cytocompatibility and higher uptake of lauric acid-coated magnetite nanoparticles as compared to dextran-coated magnetic nanoparticles may be due to different cellular interactions by coating material. Thus, coating plays an important role in modulation of biocompatibility and cellular interaction of magnetic nanoparticles.

  10. Cellular interactions of lauric acid and dextran-coated magnetite nanoparticles

    Science.gov (United States)

    Pradhan, Pallab; Giri, Jyotsnendu; Banerjee, Rinti; Bellare, Jayesh; Bahadur, Dhirendra

    2007-04-01

    In vitro cytocompatibility and cellular interactions of lauric acid and dextran-coated magnetite nanoparticles were evaluated with two different cell lines (mouse fibroblast and human cervical carcinoma). Lauric acid-coated magnetite nanoparticles were less cytocompatible than dextran-coated magnetite nanoparticles and cellular uptake of lauric acid-coated magnetic nanoparticles was more than that of dextran-coated magnetite nanoparticles. Lesser cytocompatibility and higher uptake of lauric acid-coated magnetite nanoparticles as compared to dextran-coated magnetic nanoparticles may be due to different cellular interactions by coating material. Thus, coating plays an important role in modulation of biocompatibility and cellular interaction of magnetic nanoparticles.

  11. Preparation of dextran immunological magnetic nanoparticles and their application to combined targeting carrier

    Institute of Scientific and Technical Information of China (English)

    李民勤; 徐慧显; 左榘; 姬昂; 何炳林; 庞雁; 黄建英; 牛瑞芳

    1996-01-01

    Superparamagnetic dextran nanoparticles were prepared by coprecipitation. Effects of concentration of dextran, amount of ironic salts, stirring speed, concentration of ammonium hydroxide and mole ratio of Fe3+/Fe2+ on the effective diameter of dextran magnetic nanopartides (DMNP) were studied. Dextran immunological magnetic nanoparticles (DIMNP) were formed by the reaction of the monoclonal anti-human mammary cancer antibody with DMNP oxidized by sodium periodate, and the properties of magnetic susceptibility, shape and retention of antibody activity were investigated. The in vitro cancer antigen binding ability of DIMNP was demonstrated by radioimmunoassay, and the in vivo magnetic localization and antibody targeting ability of radiolabeled DIMNP were studied.

  12. Aerosolized antimicrobial agents based on degradable dextran nanoparticles loaded with silver carbene complexes

    KAUST Repository

    Ornelas-Megiatto, Cátia

    2012-11-05

    Degradable acetalated dextran (Ac-DEX) nanoparticles were prepared and loaded with a hydrophobic silver carbene complex (SCC) by a single-emulsion process. The resulting particles were characterized for morphology and size distribution using scanning electron microscopy (SEM), transmission electron microscopy (TEM), and dynamic light scattering (DLS). The average particle size and particle size distribution were found to be a function of the ratio of the organic phase to the surfactant containing aqueous phase with a 1:5 volume ratio of Ac-DEX CH2Cl2 (organic):PBS (aqueous) being optimal for the formulation of nanoparticles with an average size of 100 ± 40 nm and a low polydispersity. The SCC loading was found to increase with an increase in the SCC quantity in the initial feed used during particle formulation up to 30% (w/w); however, the encapsulation efficiency was observed to be the best at a feed ratio of 20% (w/w). In vitro efficacy testing of the SCC loaded Ac-DEX nanoparticles demonstrated their activity against both Gram-negative and Gram-positive bacteria; the nanoparticles inhibited the growth of every bacterial species tested. As expected, a higher concentration of drug was required to inhibit bacterial growth when the drug was encapsulated within the nanoparticle formulations compared with the free drug illustrating the desired depot release. Compared with free drug, the Ac-DEX nanoparticles were much more readily suspended in an aqueous phase and subsequently aerosolized, thus providing an effective method of pulmonary drug delivery. © 2012 American Chemical Society.

  13. Controlled Release of Chitosan and Sericin from the Microspheres-Embedded Wound Dressing for the Prolonged Anti-microbial and Wound Healing Efficacy.

    Science.gov (United States)

    Aramwit, Pornanong; Yamdech, Rungnapha; Ampawong, Sumate

    2016-05-01

    One approach in wound dressing development is to incorporate active molecules or drugs in the dressing. In order to reduce the frequency of dressing changes as well as to prolong wound healing efficacy, wound dressings that can sustain the release of the active molecules should be developed. In our previous work, we developed chitosan/sericin (CH/SS) microspheres that released sericin in a controlled rate. However, the difficulty of applying the microspheres that easily diffuse and quickly degrade onto the wound was its limitations. In this study, we aimed to develop wound dressing materials which are easier to apply and to provide extended release of sericin. Different amounts of CH/SS microspheres were embedded into various compositions of polyvinyl alcohol/gelatin (PVA/G) scaffolds and fabricated using freeze-drying and glutaraldehyde crosslinking techniques. The obtained CH/SS microspheres-embedded scaffolds with appropriate design and formulation were introduced as a wound dressing material. Sericin was released from the microspheres and the scaffolds in a sustained manner. Furthermore, an optimized formation of the microspheres-embedded scaffolds (2PVA2G+2CHSS) was shown to possess an effective antimicrobial activity against both gram-positive and gram-negative bacteria. These microspheres-embedded scaffolds were not toxic to L929 mouse fibroblast cells, and they did not irritate the tissue when applied to the wound. Finally, probably by the sustained release of sericin, these microspheres-embedded scaffolds could promote wound healing as well as or slightly better than a clinically used wound dressing (Allevyn®) in a mouse model. The antimicrobial CH/SS microspheres-embedded PVA/G scaffolds with sustained release of sericin would appear to be a promising candidate for wound dressing application.

  14. Hydrogen transport and storage in engineered microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G. [Lawrence Livermore National Lab., CA (United States); Hendricks, C. [W.J. Schafer Associates, Livermore, CA (United States)

    1996-10-01

    This project is a collaboration between Lawrence Livermore National Laboratory (LLNL) and W.J. Schafer Associates (WJSA). The authors plan to experimentally verify the performance characteristics of engineered glass microspheres that are relevant to the storage and transport of hydrogen for energy applications. They will identify the specific advantages of hydrogen transport by microspheres, analyze the infrastructure implications and requirements, and experimentally measure their performance characteristics in realistic, bulk storage situations.

  15. Development and evaluation of chitosan microspheres for tetanus, diphtheria and divalent vaccines: a comparative study of subcutaneous and intranasal administration in mice.

    Science.gov (United States)

    Hashem, Fahima M; Fahmy, Sahar A; El-Sayed, Aly M; Al-Sawahli, Majid M

    2013-01-01

    There is a need to use the new technologies to induce immunity with minimum number of vaccination sessions to ensure compliance with reducing cost. To develop single shot vaccines of tetanus, diphtheria and divalent toxoids microsphere's formulations and to induce their immune response after intranasal and subcutaneous administration in mice. The microspheres were prepared using different concentrations of chitosan. Microsphere's morphology, particle size analysis, encapsulation efficiency and antigen integrity were performed and the best formulations were selected for in vitro and in vivo testing in mice. The developed microspheres have a yield percent of 70.3-91.5%. In vitro release of antigens indicated that tetanus release was increased up to 75 and 81% post T5 and TD5 formulations respectively, whereas diphtheria cumulative release increased up to 74 and 69% post D3 and TD5, respectively. Antibody levels produced were lower than that obtained from alum adsorbed vaccine but higher than the minimum level required to induce immunogenicity (>0.01 IU/mL). The subcutaneous route of administration was superior over the intranasal route in producing higher antibody levels. Chitosan microspheres were developed successfully and prove that chitosan represents a good candidate for vaccines delivery.

  16. A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice

    Directory of Open Access Journals (Sweden)

    Huang Y

    2016-03-01

    Full Text Available Yu Huang,1,* Yumeng Wei,1,* Hongru Yang,2 Chao Pi,1 Hao Liu,1 Yun Ye,1,3 Ling Zhao1 1Department of Pharmaceutical Sciences, College of Pharmacy, Sichuan Medical University, 2Department of Oncology, 3Department of Pharmacy, The First Affiliated Hospital of Sichuan Medical University, Luzhou, People’s Republic of China *These authors contributed equally to this work Abstract: 5-Fluorouracil (5-FU was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diffusion–evaporation method. The effect of Span 80 concentration, ether/ethanol volume ratio, and polyvinyl pyrrolidone/ethyl cellulose weight ratio on physicochemical characteristics, floating, and in vitro release behaviors of 5-FU hollow microspheres was investigated and optimized. The formulation and technology composed of Span 80 (1.5%, w/v, ether/ethanol (1.0:10.0, v/v, and polyvinyl pyrrolidone/ethyl cellulose (1.0:10.0, w/w were employed to develop three batch samples, which showed an excellent reproducibility. The microspheres were spherical with a hollow structure with high drug loading amount (28.4%±0.5% and production yield (74.2%±0.6%; they exhibited excellent floating and sustained release characteristics in simulated gastric and intestinal fluid. Pharmacokinetic studies demonstrated that 5-FU hollow microspheres significantly enhanced oral bioavailability (area under curve, [AUC](0-t: 12.53±1.65 mg/L*h vs 7.80±0.83 and 5.82±0.83 mg/L*h with longer elimination half-life (t1/2 (15.43±2.12 hours vs 2.25±0.22 and 1.43±0.18 hours and mean residence time (7.65±0.97 hours vs 3.61±0.41 and 2.34±0.35 hours, in comparison with its solid microspheres and powder. In vivo distribution results from tumor-bearing nude mice demonstrated that the animals administered with 5-FU hollow microspheres had much higher drug content in tumor, plasma, and stomach at 1 and 8 hours except for 0.5 hours sample collection time

  17. Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres.

    Science.gov (United States)

    Momoh, Mumuni A; Kenechukwu, Franklin C; Nnamani, Petra O; Umetiti, Jennifer C

    2015-01-01

    Effective oral insulin delivery has remained a challenge to the pharmaceutical industry. This study was designed to evaluate the effect of magnesium stearate on the properties of insulin-loaded Eudragit® RL 100 entrapped mucoadhesive microspheres. Microspheres containing Eudragit® RL 100, insulin, and varying concentrations of magnesium stearate (agglomeration-preventing agent) were prepared by emulsification-coacervation method and characterized with respect to differential scanning calorimetry (DSC), morphology, particle size, loading efficiency, mucoadhesive and micromeritics properties. The in vitro release of insulin from the microspheres was performed in simulated intestinal fluid (SIF, pH 7.2) while the in vivo hypoglycemic effect was investigated by monitoring the plasma glucose level of the alloxan-induced diabetic rats after oral administration. Stable, spherical, brownish, mucoadhesive, discrete and free flowing insulin-loaded microspheres were formed. While the average particle size and mucoadhesiveness of the microspheres increased with an increase in the proportion of magnesium stearate, loading efficiency generally decreased. After 12 h, microspheres prepared with Eudragit® RL 100: magnesium stearate ratios of 15:1, 15:2, 15:3 and 15:4 released 68.20 ± 1.57, 79.40 ± 1.52, 76.60 ± 1.93 and 70.00 ± 1.00 (%) of insulin, respectively. Reduction in the blood glucose level for the subcutaneously (sc) administered insulin was significantly (p ≤ 0.05) higher than for most of the formulations. However, the blood glucose reduction effect produced by the orally administered insulin-loaded microspheres prepared with four parts of magnesium stearate and fifteen parts of Eudragit® RL 100 after 12 h was equal to that produced by subcutaneously administered insulin solution. The results of this study can suggest that this carrier system could be an alternative for the delivery of insulin.

  18. Demonstration of Microsphere Insulation in Cryogenic Vessels

    Science.gov (United States)

    Baumgartner, R. G.; Myers, E. A.; Fesmire, J. E.; Morris, D. L.; Sokalski, E. R.

    2006-04-01

    While microspheres have been recognized as a legitimate insulation material for decades, actual use in full-scale cryogenic storage tanks has not been demonstrated until now. The performance and life-cycle-cost advantages previously predicted have now been proven. Most bulk cryogenic storage tanks are insulated with either multilayer insulation (MLI) or perlite. Microsphere insulation, consisting of hollow glass bubbles, combines in a single material the desirable properties that other insulations only have individually. The material has high crush strength, low density, is noncombustible, and performs well in soft vacuum. These properties were proven during recent field testing of two 22,700-L (6,000-gallon) liquid nitrogen tanks, one insulated with microsphere insulation and the other with perlite. Normal evaporation rates (NER) for both tanks were monitored with precision test equipment and insulation levels within the tanks were observed through view ports as an indication of insulation compaction. Specific industrial applications were evaluated based on the test results and beneficial properties of microsphere insulation. Over-the-road trailers previously insulated with perlite will benefit not only from the reduced heat leak, but also the reduced mass of microsphere insulation. Economic assessments for microsphere-insulated cryogenic vessels including life-cycle cost are also presented.

  19. Immobilization of Lipase by Covalent Binding on Crosslinked Ally Dextran

    Institute of Scientific and Technical Information of China (English)

    WangChen; SongGuoqiang; 等

    1998-01-01

    Lipase was immobilized by covalent binding on crosslinked allyl dextran using SESA as coupling agent.It is shown that this immobilization approach is an efficient one for lipase.The activity of the immobilized lipase can reach to 300-450U/g(dry weight).It exhibits good temperature stability,can retain 88% activity after being incubated at 70℃ for 2h.Special effects will be expected from our immobilized lipase in its applications in organic media due to the nature of the support.

  20. POE/PLGA composite microspheres: formation and in vitro behavior of double walled microspheres.

    Science.gov (United States)

    Yang, Yi-Yan; Shi, Meng; Goh, Suat-Hong; Moochhala, Shabbir M; Ng, Steve; Heller, Jorge

    2003-03-07

    The poly(ortho ester) (POE) and poly(D,L-lactide-co-glycolide) 50:50 (PLGA) composite microspheres were fabricated by a water-in-oil-in-water (w/o/w) double emulsion process. The morphology of the composite microspheres varied depending on POE content. When the POE content was 50, 60 or 70% in weight, the double walled microspheres with a dense core of POE and a porous shell of PLGA were formed. The formation of the double walled POE/PLGA microspheres was analysed. Their in vitro degradation behavior was characterized by scanning electron microscopy, gel permeation chromatography, Fourier-transform infrared microscopy and nuclear magnetic resonance spectroscopy (NMR). It was found that compared to the neat POE or PLGA microspheres, distinct degradation mechanism was achieved in the double walled POE/PLGA microspheres system. The degradation of the POE core was accelerated due to the acidic microenvironment produced by the hydrolysis of the outer PLGA layer. The formation of hollow microspheres became pronounced after the first week in vitro. 1H NMR spectra showed that the POE core was completely degraded after 4 weeks. On the other hand, the outer PLGA layer experienced slightly retarded degradation after the POE core disappeared. PLGA in the double walled microspheres kept more than 32% of its initial molecular weight over a period of 7 weeks.

  1. 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.

  2. Designing improved poly lactic-co-glycolic acid microspheres for a malarial vaccine: incorporation of alginate and polyinosinic-polycytidilic acid.

    Science.gov (United States)

    Salvador, Aiala; Igartua, Manoli; Hernández, Rosa María; Pedraz, José Luis

    2014-01-01

    Vaccination using proteins and peptides is currently gaining importance. One of the major drawbacks of this approach is the lack of an efficient immune response when the antigens are administered without adjuvants. In this study, we have taken the advantage of a combined adjuvant system in order to improve the immunogenicity of the SPf66 malarial antigen. For that purpose, we have combined poly (lactic-co-glycolic) acid microspheres, alginate, and polyinosinic polycytidilic acid. Our results show that microspheres can enhance the IgG production obtained with Freund's complete adjuvant. We have attributed this improvement to the presence of polyinosinic polycytidilic acid, since formulations comprising this adjuvant overcame the immune response from the others. In addition, our microspheres produced both IgG1 and IgG2a, leading to mixed Th1/Th2 activation, optimal for malaria vaccination. In conclusion, we have designed a preliminary formulation with a high potential for the treatment of malaria.

  3. Hierarchical bismuth phosphate microspheres with high photocatalytic performance

    Energy Technology Data Exchange (ETDEWEB)

    Pei, Lizhai; Wei, Tian; Lin, Nan; Yu, Haiyun [Anhui University of Technology, Ma' anshan (China). Key Laboratory of Materials Science and Processing of Anhui Province

    2016-05-15

    Hierarchical bismuth phosphate microspheres have been prepared by a simple hydrothermal process with polyvinyl pyrrolidone. Scanning electron microscopy observations show that the hierarchical bismuth phosphate microspheres consist of nanosheets with a thickness of about 30 nm. The diameter of the microspheres is about 1 - 3 μm. X-ray diffraction analysis shows that the microspheres are comprised of triclinic Bi{sub 23}P{sub 4}O{sub 44.5} phase. The formation of the hierarchical microspheres depends on polyvinyl pyrrolidone concentration, hydrothermal temperature and reaction time. Gentian violet acts as the pollutant model for investigating the photocatalytic activity of the hierarchical bismuth phosphate microspheres under ultraviolet-visible light irradiation. Irradiation time, dosage of the hierarchical microspheres and initial gentian violet concentration on the photocatalytic efficiency are also discussed. The hierarchical bismuth phosphate microspheres show good photocatalytic performance for gentian violet removal in aqueous solution.

  4. [Cardiovascular effect of solcoseryl with low molecular dextran in normal late pregnancy].

    Science.gov (United States)

    Schwarz, R; Retzke, U; Wilken, H P

    1977-01-01

    By means of quantitative sphygmometry and the unbloody recording of arterial blood pressure the hemodynamic effect of an infusion of Solcoseryl in combination with low molecular dextrane on the maternal cardiovascular system in 9 normotensive healthy late pregnant women is examined. Solcoseryl causes no improvement of the cardiovascular effects known for low molecular dextrane.

  5. Development of monoclonal antibody-based sandwich ELISA for detection of dextran.

    Science.gov (United States)

    Wang, Sheng-Yu; Li, Zhe; Wang, Xian-Jiang; Lv, Sha; Yang, Yun; Zeng, Lian-Qiang; Luo, Fang-Hong; Yan, Jiang-Hua; Liang, Da-Feng

    2014-10-01

    Dextran as anti-nutritional factor is usually a result of bacteria activity and has associated serial problems during the process stream in the sugar industry and in medical therapy. A sensitive method is expected to detect dextran quantitatively. Here we generated four monoclonal antibodies (MAbs) against dextran using dextran T40 conjugated with bovine serum albumin (BSA) as immunogen in our lab following hybridoma protocol. Through pairwise, an MAb named D24 was determined to be conjugated with horseradish peroxidase (HRP) and was used in the establishment of a sensitive sandwich enzyme-linked immunosorbent assay (ELISA) method for determination of dextran, in which MAb D9 was chosen as a capture antibody. The detection limit and working scope of the developed sandwich ELISA method were 3.9 ng/mL and 7.8-500 ng/mL with a correlation coefficient of 0.9909. In addition, the cross-reaction assay demonstrated that the method possessed high specificity with no significant cross-reaction with dextran-related substances, and the recovery rate ranged from 96.35 to 102.00%, with coefficient of variation ranging from 1.58 to 6.94%. These results indicated that we developed a detection system of MAb-based sandwich ELISA to measure dextran and this system should be a potential tool to determine dextran levels.

  6. Mechanisms of the ultrasound-mediated intracellular delivery of liposomes and dextrans.

    Science.gov (United States)

    Afadzi, Mercy; Strand, Sabina P; Nilssen, Esben A; Måsøy, Svein-Erik; Johansen, Tonni F; Hansen, Rune; Angelsen, Bjørn A; de L Davies, Catharina

    2013-01-01

    The mechanism involved in the ultrasoundenhanced intracellular delivery of fluorescein-isothiocyanate (FITC)-dextran (molecular weight 4 to 2000 kDa) and liposomes containing doxorubicin (Dox) was studied using HeLa cells and an ultrasound transducer at 300 kHz, varying the acoustic power. The cellular uptake and cell viability were measured using flow cytometry and confocal microscopy. The role of endocytosis was investigated by inhibiting clathrin- and caveolae-mediated endocytosis, as well as macropinocytosis. Microbubbles were found to be required during ultrasound treatment to obtain enhanced cellular uptake. The percentage of cells internalizing Dox and dextran increased with increasing mechanical index. Confocal images and flow cytometric analysis indicated that the liposomes were disrupted extracellularly and that released Dox was taken up by the cells. The percentage of cells internalizing dextran was independent of the molecular weight of dextrans, but the amount of the small 4-kDa dextran molecules internalized per cell was higher than for the other dextrans. The inhibition of endocytosis during ultrasound exposure resulted in a significant decrease in cellular uptake of dextrans. Therefore, the improved uptake of Dox and dextrans may be a result of both sonoporation and endocytosis.

  7. Mussel-inspired modification of dextran for protein-resistant coatings of titanium oxide.

    Science.gov (United States)

    Park, Jae Yoon; Kim, Jee Seon; Nam, Yoon Sung

    2013-09-12

    Surface modification of inorganic materials to prevent non-specific protein adsorption is critically important for developing a biocompatible materials' platform for medical implantation, diagnostics, and therapeutics. Here we report mussel-inspired chemical modification of dextran for anti-fouling coatings of metal oxide. Catechols are conjugated to dextran via a carbamate ester linkage, producing catechol-grafted dextran with a grafting density of 7.3 mol.%. Titanium dioxide (TiO₂) is coated with the catechol-grafted dextran, and the anti-fouling effect of dextran coatings is examined by using the adsorption of human serum albumin. The mussel-inspired dextran coatings show excellent resistance to non-specific protein adsorption: the adsorption equilibrium constant (K) is 0.69 Lg(-1) for dextran-coated TiO₂ while that for pristine TiO₂ surface is 3.53 Lg(-1). This study suggests that catechol-grafted dextran is a promising material for effective anti-fouling coatings of implantable inorganic materials. Copyright © 2013 Elsevier Ltd. All rights reserved.

  8. The effect of hypertonic saline dextran solutions on hypoxic pulmonary vasoconstriction in anaesthetised piglets.

    Science.gov (United States)

    Bellezza, M; Kerbaul, F; Roussel, L; Imbert, M; Guidon, C

    2002-10-01

    Hypoxic pulmonary vasoconstriction (HPV) is a regulatory mechanism by which blood is diverted from poorly ventilated to better ventilated areas of the lung. The aim of the present study was to assess the extent to which hypertonic saline dextran and dextran solutions modify the magnitude of HPV during isovolumic haemodilution in intact acutely instrumented piglets. Eighteen large white piglets were anesthetised and assigned to two groups. Mean pulmonary arterial pressure (PAP) and cardiac output (Q), systemic arterial pressure and left arterial pressure (LAP) were measured. A decrease in Q was obtained by reducing venous return. This enabled measurement of transpulmonary pressures (mean PAP minus LAP) at four levels of Q in hyperoxia (inspiratory oxygen fraction (FiO2)=0.4) then in hypoxia (Fi,O2=0.1) in the two groups before blood soustraction (10 mL x kg(-1)) and after loading with sodium chloride (NaCl) 7.5% and dextran 6% or with dextran 6% alone. Dextran alone led to a decrease in mean PAP-LAP/Q values, and NaCl with dextran was associated with a significant shift of mean PAP-LAP/Q plots to higher pressures in hypoxia. Hypertonic saline dextran solution, as replacement fluid in isovolaemic haemodilution increased the magnitude of hypoxic pulmonary vasoconstriction, whereas dextran solution reduced it.

  9. In situ production and analysis of Weissella confusa dextran in wheat sourdough.

    Science.gov (United States)

    Katina, Kati; Maina, Ndegwa Henry; Juvonen, Riikka; Flander, Laura; Johansson, Liisa; Virkki, Liisa; Tenkanen, Maija; Laitila, Arja

    2009-10-01

    Several lactic acid bacteria belonging to the genera Leuconostoc, Lactobacillus, and Weissella have been introduced to wheat sourdough baking for in situ production of exopolysaccharides. This is considered a novel method for improving the shelf-life, volume and nutritional value of bread without additives. However, in situ production of exopolysaccharides during sourdough fermentation is challenged by simultaneous acidification due to metabolic activities of the bacteria, which may significantly diminish the positive technological impact of exopolysaccharides. In this study, the growth, activity and in situ production of dextran by Weissella confusa VTT E-90392 in wheat sourdoughs were investigated. Furthermore, the influence of dextran-enriched sourdoughs, at the addition level of 43%, on the subsequent bread quality was established. W. confusa efficiently produced dextran from the added sucrose in wheat sourdough without strong acid production. A new specific enzyme-assisted method for in situ analysis of dextran in sourdoughs was developed. With this method, we could for the first time proof significant (11-16 g/kg DW) production of polymeric dextran in sourdoughs. Concomitant formation of shorter isomaltooligosaccharides by W. confusa was also detected. The produced dextran significantly increased the viscosity of the sourdoughs. Application of dextran-enriched sourdoughs in bread baking provided mildly acidic wheat bread with improved volume (up to 10%) and crumb softness (25-40%) during 6 days of storage. Hence, W. confusa is a promising new strain for efficient in situ production of dextrans and isomaltooligosaccharides in sourdoughs without strong acidification.

  10. Dextran vesicular carriers for dual encapsulation of hydrophilic and hydrophobic molecules and delivery into cells.

    Science.gov (United States)

    Pramod, P S; Takamura, Kathryn; Chaphekar, Sonali; Balasubramanian, Nagaraj; Jayakannan, M

    2012-11-12

    Dextran vesicular nanoscaffolds were developed based on polysaccharide and renewable resource alkyl tail for dual encapsulation of hydrophilic and hydrophobic molecules (or drugs) and delivery into cells. The roles of the hydrophobic segments on the molecular self-organization of dextran backbone into vesicles or nanoparticles were investigated in detail. Dextran vesicles were found to be a unique dual carrier in which water-soluble molecules (like Rhodamine-B, Rh-B) and polyaromatic anticancer drug (camptothecin, CPT) were selectively encapsulated in the hydrophilic core and hydrophobic layer, respectively. The dextran vesicles were capable of protecting the plasma-sensitive CPT lactone pharmacophore against the hydrolysis by 10× better than the CPT alone in PBS. The aliphatic ester linkage connecting the hydrophobic tail with dextran was found to be cleaved by esterase under physiological conditions for fast releasing of CPT or Rh-B. Cytotoxicity of the dextran vesicle and its drug conjugate were tested on mouse embryonic fibroblast cells (MEFs) using MTT assay. The dextran vesicular scaffold was found to be nontoxic to living cells. CPT loaded vesicles were found to be 2.5-fold more effective in killing fibroblasts compared to that of CPT alone in PBS. Confocal microscopic images confirmed that both Rh-B and CPT loaded vesicles to be taken up by fibroblasts compared to CPT alone, showing a distinctly perinuclear localization in cells. The custom designed dextran vesicular provides new research opportunities for dual loading and delivering of hydrophilic and hydrophobic drug molecules.

  11. Injectable dextran hydrogels fabricated by metal-free click chemistry for cartilage tissue engineering.

    Science.gov (United States)

    Wang, Xiaoyu; Li, Zihan; Shi, Ting; Zhao, Peng; An, Kangkang; Lin, Chao; Liu, Hongwei

    2017-04-01

    Injectable dextran-based hydrogels were prepared for the first time by bioorthogonal click chemistry for cartilage tissue engineering. Click-crosslinked injectable hydrogels based on cyto-compatible dextran (Mw=10kDa) were successfully fabricated under physiological conditions by metal-free alkyne-azide cycloaddition (click) reaction between azadibenzocyclooctyne-modified dextran (Dex-ADIBO) and azide-modified dextran (Dex-N3). Gelation time of these dextran hydrogels could be regulated in the range of approximately 1.1 to 10.2min, depending on the polymer concentrations (5% or 10%) and ADIBO substitution degree (DS, 5 or 10) of Dex-ADIBO. Rheological analysis indicated that the dextran hydrogels were elastic and had storage moduli from 2.1 to 6.0kPa with increasing DS of ADIBO from 5 to 10. The in vitro tests revealed that the dextran hydrogel crosslinked from Dex-ADIBO DS 10 and Dex-N3 DS 10 at a polymer concentration of 10% could support high viability of individual rabbit chondrocytes and the chondrocyte spheroids encapsulated in the hydrogel over 21days. Individual chondrocytes and chondrocyte spheroids in the hydrogel could produce cartilage matrices such as collagen and glycosaminoglycans. However, the chondrocyte spheroids produced a higher content of matrices than individual chondrocytes. This study indicates that metal-free click chemistry is effective to produce injectable dextran hydrogels for cartilage tissue engineering. Copyright © 2016 Elsevier B.V. All rights reserved.

  12. In-vivo evaluation of clindamycin release from glyceryl monooleate-alginate microspheres by NIR spectroscopy.

    Science.gov (United States)

    Mohamed, Amir Ibrahim; Ahmed, Osama A A; Amin, Suzan; Elkadi, Omar Anwar; Kassem, Mohamed A

    2015-10-15

    The purpose of this study was to use near-infrared (NIR) transmission spectroscopic technique to determine clindamycin plasma concentration after oral administration of clindamycin loaded GMO-alginate microspheres using rabbits as animal models. Lyophilized clindamycin-plasma standard samples at a concentration range of 0.001-10 μg/ml were prepared and analyzed by NIR and HPLC as a reference method. NIR calibration model was developed with partial least square (PLS) regression analysis. Then, a single dose in-vivo evaluation was carried out and clindamycin-plasma concentration was estimated by NIR. Over 24 h time period, the pharmacokinetic parameters of clindamycin were calculated for the clindamycin loaded GMO-alginate microspheres (F3) and alginate microspheres (F2), and compared with the plain drug (F1). PLS calibration model with 7-principal components (PC), and 8000-9200 cm(-1) spectral range shows a good correlation between HPLC and NIR values with root mean square error of cross validation (RMSECV), root mean square error of prediction (RMSEP), and calibration coefficient (R(2)) values of 0.245, 1.164, and 0.9753, respectively, which suggests that NIR transmission technique can be used for drug-plasma analysis without any extraction procedure. F3 microspheres exhibited controlled and prolonged absorption Tmax of 4.0 vs. 1.0 and 0.5 h; Cmax of 2.37±0.3 vs. 3.81±0.8 and 5.43±0.7 μg/ml for F2 and F1, respectively. These results suggest that the combination of GMO and alginate (1:4 w/w) could be successfully employed for once daily clindamycin microspheres formulation which confirmed by low Cmax and high Tmax values.

  13. Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper-Lin small composite design.

    Science.gov (United States)

    El-Say, Khalid Mohamed

    2016-01-01

    This study was aimed at developing a controlled-release cetirizine hydrochloride (CTZ)-loaded polymethacrylate microsphere by optimization technique using software-based response surface methodology. The emulsion solvent evaporation method was utilized in the preparation of microspheres. Four process variables were selected, namely, Eudragit RLPO loading percentage in total polymer, the emulsifier hydrophilic lipophilic balance (HLB), the antitacking percentage, and the dispersed phase volume. The desired responses were particle size, angle of repose, production yield, encapsulation efficiency, loading capacity, initial drug release, and the time for 85% of drug release from the microspheres. Optimization was carried out by fitting the experimental data to the software program (Statgraphics Centurion XV). Moreover, 18 batches were subjected to various characterization tests required for the production of dosage form. The pharmacokinetic parameters were evaluated after the oral administration of 10 mg CTZ in both optimized formulation and commercial product on healthy human volunteers using a double-blind, randomized, cross-over design. The optimized formulation showed satisfactory yield (84.43%) and drug encapsulation efficiency (87.1%). Microspheres were of spherical shape, smooth surface, and good flowability with an average size of 142.3 μm. The developed optimized batch of microspheres ensured 28.87% initial release after 2 hours, and the release of CTZ extended for >12 hours. In addition, the relative bioavailability of the optimized formulation was 165.5% with respect to the marketed CTZ tablets indicating a significant enhancement of CTZ bioavailability. Thus, there is an expectation to decrease the administered dose and the frequency of administration, and subsequently minimize the adverse effects that are faced by the patient during the treatment.

  14. Dextran-protamine coated nanostructured lipid carriers as mucus-penetrating nanoparticles for lipophilic drugs.

    Science.gov (United States)

    Beloqui, Ana; Solinís, María Ángeles; des Rieux, Anne; Préat, Véronique; Rodríguez-Gascón, Alicia

    2014-07-01

    The main objectives of the present study were (i) to evaluate the effect of the mucus layer on saquinavir-loaded nanostructured lipid carriers (SQV-NLCs) uptake and (ii) to evaluate the mucopenetrating properties of dextran-protamine (Dex-Prot) coating on NLCs as per SQV permeability enhancement. Three different NLC formulations differing on particle size and surfactant content were obtained and coated with Dex-Prot complexes. SQV permeability was then evaluated across Caco-2 cell monolayers (enterocyte-like model) and Caco-2/HT29-MTX cell monolayers (mucus model). In the Caco-2 monolayers, Dex-Prot-NLCs increased up to 9-fold SQV permeability in comparison to uncoated nanoparticles. In the Caco-2/HT29-MTX monolayers, Dex-Prot-NLCs presenting a surface charge close to neutrality significantly increased SQV permeability. Hence, Dex-Prot complex coating is a promising strategy to ensure successful nanoparticle mucus-penetration, and thus, an efficient nanoparticle oral delivery. To our knowledge, this is the first time that Dex-Prot coating has been described as a nanoparticle muco-penetration enhancer across the intestinal mucus barrier. Copyright © 2014 Elsevier B.V. All rights reserved.

  15. Optimization of preparation method for ketoprofen-loaded microspheres consisting polymeric blends using simplex lattice mixture design.

    Science.gov (United States)

    Das, Sanjoy Kumar; Khanam, Jasmina; Nanda, Arunabha

    2016-12-01

    In the present investigation, simplex lattice mixture design was applied for formulation development and optimization of a controlled release dosage form of ketoprofen microspheres consisting polymers like ethylcellulose and Eudragit(®)RL 100; when those were formed by oil-in-oil emulsion solvent evaporation method. The investigation was carried out to observe the effects of polymer amount, stirring speed and emulsifier concentration (% w/w) on percentage yield, average particle size, drug entrapment efficiency and in vitro drug release in 8h from the microspheres. Analysis of variance (ANOVA) was used to estimate the significance of the models. Based on the desirability function approach numerical optimization was carried out. Optimized formulation (KTF-O) showed close match between actual and predicted responses with desirability factor 0.811. No adverse reaction between drug and polymers were observed on the basis of Fourier transform infrared (FTIR) spectroscopy and Differential scanning calorimetric (DSC) analysis. Scanning electron microscopy (SEM) was carried out to show discreteness of microspheres (149.2±1.25μm) and their surface conditions during pre and post dissolution operations. The drug release pattern from KTF-O was best explained by Korsmeyer-Peppas and Higuchi models. The batch of optimized microspheres were found with maximum entrapment (~90%), minimum loss (~10%) and prolonged drug release for 8h (91.25%) which may be considered as favourable criteria of controlled release dosage form.

  16. Terpene and dextran renewable resources for the synthesis of amphiphilic biopolymers.

    Science.gov (United States)

    Alvès, Marie-Hélène; Sfeir, Huda; Tranchant, Jean-François; Gombart, Emilie; Sagorin, Gilles; Caillol, Sylvain; Billon, Laurent; Save, Maud

    2014-01-13

    The present work shows the synthesis of amphiphilic polymers based on the hydrophilic dextran and the hydrophobic terpenes as renewable resources. The first step concerns the synthesis of functional terpene molecules by thiol-ene addition chemistry involving amino or carboxylic acid thiols and dihydromyrcenol terpene. The terpene-modified polysaccharides were subsequently synthesized by coupling the functional terpenes with dextran. A reductive amination step produced terpene end-modified dextran with 94% of functionalization, while the esterification step produced three terpene-grafted dextrans with a number of terpene units per dextran of 1, 5, and 10. The amphiphilic renewable grafted polymers were tested as emulsifiers for the stabilization of liquid miniemulsion of terpene droplets dispersed in an aqueous phase. The average hydrodynamic diameter of the stable droplets was observed at about 330 nm.

  17. Electrospray formation of gelled nano-aluminum microspheres with superior reactivity.

    Science.gov (United States)

    Wang, Haiyang; Jian, Guoqiang; Yan, Shi; DeLisio, Jeffery B; Huang, Chuan; Zachariah, Michael R

    2013-08-14

    Nanometallic fuels with high combustion enthalpy, such as aluminum, have been proposed as a potential fuel replacement for conventional metallic fuel to improve propellant performance in a variety of propulsive systems. Nevertheless, nanometallic fuels suffer from the processing challenges in polymer formulations such as increased viscosity and large agglomeration, which hinder their implementation. In this letter, we employ electrospray as a means to create a gel within a droplet, via a rapid, solvent evaporation-induced aggregation of aluminum nanoparticles, containing a small mass fraction of an energetic binder. The gelled aluminum microspheres were characterized and tested for their burning behavior by rapid wire heating ignition experiments. The gelled aluminum microspheres show enhanced combustion behavior compared to nanoaluminum, which possibly benefits from the nitrocellulose coating and the gelled microstructure, and is far superior to the corresponding dense micrometer-sized aluminum.

  18. Release of macromolecules from albumin-heparin microspheres

    NARCIS (Netherlands)

    Kwon, Glen S.; Bae, You Han; Cremers, Harry; Feijen, Jan; Kim, Sung Wan

    1992-01-01

    Hydrophilic microspheres based on albumin-heparin conjugates have been prepared as a macromolecular delivery system. The soluble albumin-heparin conjugate was synthesized and crosslinked in a water-in-oil emulsion with glutaraldehyde to form microspheres in the same manner as for albumin microsphere

  19. Preparation of microstructured hydroxyapatite microspheres using oil in water emulsions

    Indian Academy of Sciences (India)

    T S Pradeesh; M C Sunny; H K Varma; P Ramesh

    2005-08-01

    Hydroxyapatite (HAP) microspheres with peculiar spheres-in-sphere morphology were prepared by using oil-in-water emulsions and solvent evaporation technique. Ethylene vinyl acetate co-polymer (EVA) was used as the binder material. Preparation of HAP/EVA microspheres was followed by the thermal debinding and sintering at 1150°C for 3 h to obtain HAP microspheres. Each microsphere of 100–1000 m was in turn composed of spherical hydroxyapatite granules of 2–15 m size which were obtained by spray drying the precipitated HAP. The parameters such as percentage of initial HAP loading, type of stabilizer, concentration of stabilizer, stirring speed and temperature of microsphere preparation were varied to study their effect on the particle size and geometry of the microspheres obtained. It was observed that these parameters do have an effect on the size and shape of the microspheres obtained, which in turn will affect the sintered HAP microstructure. Of the three stabilizers used viz. polyoxyethylene(20) sorbitan monopalmitate (Tween-40), sodium laurate and polyvinyl alcohol (PVA), only PVA with a concentration not less than 0.1 wt% showed controlled stabilization of HAP granules resulting in spherical microspheres of required size. Morphologically better spherical microspheres were obtained at 20°C. Increasing the stirring speed produced smaller microspheres. Smaller microspheres having size < 50 m were obtained at a stirring speed of 1500 ± 50 rpm. A gradual decrease in pore size was observed in the sintered microspheres with increase in HAP loading.

  20. Preparation of Biodegradable Microspheres of Testosterone with Poly(D,L-lactide-co-glycolide) and Test of Drug Release in vitro

    Institute of Scientific and Technical Information of China (English)

    ShenZheng-rong; ZhuJia-hui; MaZhen; WangFang; WangZun-yuan

    2005-01-01

    Biodegradable microspheres formulation of testosterone (T)can be used as a new physiological approach for androgen replacement in hypogonadal men.In this study, poly(D, L-lactide-co-glycolide)(PLGA)microspheres containing T were prepared by a solvent-evaporation/solvent-diffusion process and the drug release tests of the microspheres were carried out in vitro.T/PLGA microspheres with good yield,desired size and satisfied drug loading were obtained.A significant testosterone sustained release was shown in the drug release tests in vitro.Since PLGA microspheres preparations are normally sterilized by colbat-60 irradiation.the effects of 25 kGy colbat-60 irradiation on physicochemical properties and in vitro drug release profile of T/PLGA microsphere were investigatedphysicochemical propertiesd. The results showed that the irradiation didn't have any effects on the of T.Though about one-third decrease in molcoulaar weight of PLGA was caused by the irradiation, no significant changes were observed on the drug release profile in vitro.

  1. Dextran-coated superparamagnetic nanoparticles as potential cancer drug carriers in vivo

    Science.gov (United States)

    Peng, Mingli; Li, Houli; Luo, Zhiyi; Kong, Jian; Wan, Yinsheng; Zheng, Lemin; Zhang, Qinlu; Niu, Hongxin; Vermorken, Alphons; van de Ven, Wim; Chen, Chao; Zhang, Xikun; Li, Fuqiang; Guo, Lili; Cui, Yali

    2015-06-01

    Dextran-coated superparamagnetic iron oxide nanoparticles (DSPIONs) have gained considerable interest, because of their biocompatibility and biosafety in clinics. Doxorubicin (Dox), a widely used chemotherapeutic drug, always has limited applications in clinical therapy due to its serious side effects of dose-limiting irreversible cardiotoxicity and myelo suppression. Herein, DSPIONs were synthesized and developed as magnetic carriers for doxorubicin. The Dox-DSPION conjugates were evaluated in the in vitro test of Dox release, which showed pH-dependence with the highest release percentage of 50.3% at pH 5.0 and the lowest release percentage of 11.8% in a physiological environment. The cytotoxicity of DSPIONs and Dox-DSPIONs evaluated by the MTT assay indicated that DSPIONs had no cytotoxicity and the conjugates had significantly reduced the toxicity (IC50 = 1.36 μg mL-1) compared to free Dox (IC50 = 0.533 μg mL-1). Furthermore, confocal microscopic data of cell uptake suggest that less cytotoxicity of Dox-DSPIONs may be attributed to the cellular internalization of the conjugates and sustainable release of Dox from the formulation in the cytoplasm. More importantly, the results from the rabbit VX2 liver tumor model test under an external magnetic field showed that the conjugates had approximately twice the anti-tumor activity and two and a half times the animal survival rate, respectively, compared to free Dox. Collectively, our data have demonstrated that Dox-DSPIONs have less toxicity with better antitumor effectiveness in in vitro and in vivo applications, suggesting that the conjugates have potential to be developed into chemo-therapeutic formulations.

  2. Preparation and characterization of isoniazid and lamivudine co-loaded polymeric microspheres.

    Science.gov (United States)

    Pandey, Gitu; Yadav, Sarita Kumari; Mishra, Brahmeshwar

    2016-12-01

    Context The rate of co-infection of HIV/Tuberculosis is increasing alarmingly. This calls for a drug delivery approach targeting both diseases. Objective The study aims to investigate co-loading of isoniazid, an antitubercular drug and lamivudine an antiretroviral drug, into polymeric microspheres for simultaneous treatment of both diseases. Materials and methods Microspheres were prepared by o/o emulsion solvent evaporation method by employing ethylcellulose and eudragit RS 100 as polymers. The prepared formulation was suitably characterized for FTIR, DSC, percent yield, loose surface crystals, entrapment efficiency, and in vitro studies. The surface morphology of microspheres was observed using digital microscope and scanning electron microscope. Cell viability study was done on Caco-2 cells. Results and discussion FTIR and DSC studies demonstrated compatibility and stability of excipients. Microscopy studies revealed that particles were spherical in shape and distributed over a range of 120-270 μm. Percent yield, LSC and %EE have shown promising results. In vitro release showed biphasic release pattern with sustained release up to 12 h. Mechanism of drug release followed Higuchi Kinetics and non-fickian release behaviour. The formulation containing drug/polymer ratio 1:2 and EU/EC of 1:1 showed optimum response in context to achievement of controlled release. The cell viability studies showed that the prepared system had no toxic effect on intestinal epithelial Caco-2 cells. Conclusion Polymeric microspheres were prepared and suitably characterized for simultaneous delivery of two drugs. This matrix system could be used for better therapeutic outcome in this deadly co-infection.

  3. A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice.

    Science.gov (United States)

    Huang, Yu; Wei, Yumeng; Yang, Hongru; Pi, Chao; Liu, Hao; Ye, Yun; Zhao, Ling

    2016-01-01

    5-Fluorouracil (5-FU) was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diffusion-evaporation method. The effect of Span 80 concentration, ether/ethanol volume ratio, and polyvinyl pyrrolidone/ethyl cellulose weight ratio on physicochemical characteristics, floating, and in vitro release behaviors of 5-FU hollow microspheres was investigated and optimized. The formulation and technology composed of Span 80 (1.5%, w/v), ether/ethanol (1.0:10.0, v/v), and polyvinyl pyrrolidone/ethyl cellulose (1.0:10.0, w/w) were employed to develop three batch samples, which showed an excellent reproducibility. The microspheres were spherical with a hollow structure with high drug loading amount (28.4%±0.5%) and production yield (74.2%±0.6%); they exhibited excellent floating and sustained release characteristics in simulated gastric and intestinal fluid. Pharmacokinetic studies demonstrated that 5-FU hollow microspheres significantly enhanced oral bioavailability (area under curve, [AUC](0-t): 12.53±1.65 mg/L(*)h vs 7.80±0.83 and 5.82±0.83 mg/L(*)h) with longer elimination half-life (t1/2) (15.43±2.12 hours vs 2.25±0.22 and 1.43±0.18 hours) and mean residence time (7.65±0.97 hours vs 3.61±0.41 and 2.34±0.35 hours), in comparison with its solid microspheres and powder. In vivo distribution results from tumor-bearing nude mice demonstrated that the animals administered with 5-FU hollow microspheres had much higher drug content in tumor, plasma, and stomach at 1 and 8 hours except for 0.5 hours sample collection time point in comparison with those administered with 5-FU solid microspheres and its powder. These results suggested that the hollow microspheres would be a promising controlled drug delivery system for an oral chemotherapy agent like 5-FU.

  4. Biosensing by WGM Microspherical Resonators

    Directory of Open Access Journals (Sweden)

    Giancarlo C. Righini

    2016-06-01

    Full Text Available Whispering gallery mode (WGM microresonators, thanks to their unique properties, have allowed researchers to achieve important results in both fundamental research and engineering applications. Among the various geometries, microspheres are the simplest 3D WGM resonators; the total optical loss in such resonators can be extremely low, and the resulting extraordinarily high Q values of 108–109 lead to high energy density, narrow resonant-wavelength lines and a lengthy cavity ringdown. They can also be coated in order to better control their properties or to increase their functionality. Their very high sensitivity to changes in the surrounding medium has been exploited for several sensing applications: protein adsorption, trace gas detection, impurity detection in liquids, structural health monitoring of composite materials, detection of electric fields, pressure sensing, and so on. In the present paper, after a general introduction to WGM resonators, attention is focused on spherical microresonators, either in bulk or in bubble format, to their fabrication, characterization and functionalization. The state of the art in the area of biosensing is presented, and the perspectives of further developments are discussed.

  5. Biosensing by WGM Microspherical Resonators

    Science.gov (United States)

    Righini, Giancarlo C.; Soria, Silvia

    2016-01-01

    Whispering gallery mode (WGM) microresonators, thanks to their unique properties, have allowed researchers to achieve important results in both fundamental research and engineering applications. Among the various geometries, microspheres are the simplest 3D WGM resonators; the total optical loss in such resonators can be extremely low, and the resulting extraordinarily high Q values of 108–109 lead to high energy density, narrow resonant-wavelength lines and a lengthy cavity ringdown. They can also be coated in order to better control their properties or to increase their functionality. Their very high sensitivity to changes in the surrounding medium has been exploited for several sensing applications: protein adsorption, trace gas detection, impurity detection in liquids, structural health monitoring of composite materials, detection of electric fields, pressure sensing, and so on. In the present paper, after a general introduction to WGM resonators, attention is focused on spherical microresonators, either in bulk or in bubble format, to their fabrication, characterization and functionalization. The state of the art in the area of biosensing is presented, and the perspectives of further developments are discussed. PMID:27322282

  6. Development of novel solid-phase protein formulations

    Science.gov (United States)

    Montalvo Ortiz, Brenda Liz

    Proteins are the next-generation drugs for the treatment of several diseases. However, the number of protein drugs is still limited due to the physical or chemical instability of proteins during processing, formulation, storage, and delivery. The formulation of proteins at the solid state has advantages over liquid state, such as improved stability during long-term storage and delivery and decreases transportation costs. In this dissertation, we developed new solid-phase protein formulations in which the integrity of the protein was not compromised. The long term goal of this research was to use these protein formulations to improve protein stability in drug delivery devices, such as poly(lactic-co-glycolic) acid (PLGA). The first solid-phase protein formulation developed in this investigation was named "glassification". We proposed glassification as an alternative protein dehydration technique to the common used one, lyophilization, because this last method involves a series of steps which are detrimental to protein structure and stability. The glassification method consisted on protein dehydration by the use of organic solvents. As a result of the glassification process a small (micrometer size range) protein solid bead was obtained. The proteins used to study the glassification process were lysozyme (LYS), alpha-chymotrypsin (CHYMO) and horseradish peroxidase (HRP). These studies revealed that the glassification process itself did not alter protein structure and the activity was preserved. Ethyl acetate was the most effective organic solvent for protein glassification because it led to the highest protein residual activity, no insoluble aggregate formation and is a relatively non-toxic solvent, which allow the incorporation of these protein microparticles in PLGA microspheres. The incorporation of spherical HRP microparticles into PLGA microspheres resulted in superior properties when compared with encapsulated lyophilized HRP powder, such as improved release

  7. Acrolein Microspheres Are Bonded To Large-Area Substrates

    Science.gov (United States)

    Rembaum, Alan; Yen, Richard C. K.

    1988-01-01

    Reactive cross-linked microspheres produced under influence of ionizing radiation in aqueous solutions of unsaturated aldehydes, such as acrolein, with sodium dodecyl sulfate. Diameters of spheres depend on concentrations of ingredients. If polystyrene, polymethylmethacrylate, or polypropylene object immersed in solution during irradiation, microspheres become attached to surface. Resulting modified surface has grainy coating with reactivity similar to free microspheres. Aldehyde-substituted-functional microspheres react under mild conditions with number of organic reagents and with most proteins. Microsphere-coated macrospheres or films used to immobilize high concentrations of proteins, enzymes, hormones, viruses, cells, and large number of organic compounds. Applications include separation techniques, clinical diagnostic tests, catalytic processes, and battery separators.

  8. Improving photoprotection: 4-methylbenzylidene camphor microspheres.

    Science.gov (United States)

    Centini, Marisanna; Miraglia, Giovanna; Quaranta, Valeria; Buonocore, Anna; Anselmi, Cecilia

    2014-05-22

    Abstract We propose a new approach for photoprotection. 4-Methylbenzylidene camphor (4-MBC), one of the most widely used UV filters, was encapsulated in microspheres, with a view to overcoming problems (percutaneous absorption, photodegradation and lack of lasting effect) arising with organic sunscreens, and to achieve safe photoprotection. We focused on this filter in the light of the Cosmetics Europe opinion concerning its possible effects on the thyroid gland. Microspheres were prepared by emulsification-solvent evaporation, using different amounts of 4-MBC and characterized for morphology, encapsulation efficiency and particle size. The particles were then mixed in O/W emulsions. The in vitro sun protection factors, in vitro release and photostability were investigated and compared with emulsions containing the free sunscreen. The new microspheres offer good morphology and loading (up to 40%), and the same photoprotection as the free filter while at the same time protecting it from photodegradation. The systems also give a slower release from the emulsions.

  9. Removal of radioactive contaminants by polymeric microspheres.

    Science.gov (United States)

    Osmanlioglu, Ahmet Erdal

    2016-11-01

    Radionuclide removal from radioactive liquid waste by adsorption on polymeric microspheres is the latest application of polymers in waste management. Polymeric microspheres have significant immobilization capacity for ionic substances. A laboratory study was carried out by using poly(N-isopropylacrylamide) for encapsulation of radionuclide in the liquid radioactive waste. There are numbers of advantages to use an encapsulation technology in radioactive waste management. Results show that polymerization step of radionuclide increases integrity of solidified waste form. Test results showed that adding the appropriate polymer into the liquid waste at an appropriate pH and temperature level, radionuclide was encapsulated into polymer. This technology may provide barriers between hazardous radioactive ions and the environment. By this method, solidification techniques became easier and safer in nuclear waste management. By using polymer microspheres as dust form, contamination risks were decreased in the nuclear industry and radioactive waste operations.

  10. 3-hydroxyflavone-bovine serum albumin interaction in Dextran medium

    Directory of Open Access Journals (Sweden)

    Voicescu Mariana

    2015-01-01

    Full Text Available Spectroscopic analysis of a bioactive flavonol, 3-Hydroxyflavone (3-HF, in systems based on Dextran 70 (Dx70 (an important bio-relevant polysacharide and Bovine Serum Albumin (BSA (a carrier protein, have been studied by fluorescence and circular dichroism. Changes produced by different concentrations of Dx70 on the fluorescent characteristics of 3-HF, and on the excited - state intramolecular proton transfer (ESIPT process were studied. The influence of 3-HF binding and of Dx70 on the secondary structure of BSA were investigated by circular dichroism spectroscopy. The influence of temperature (30-80°C range on the intrinsic Tryptophan fluorescence in 3-HF/BSA/Dx70 systems, was investigated. The results are discussed with relevance to 3-HF as a sensitive fluorescence probe for exploring flavone-protein interaction in plasma expander media and also for its biological evaluation.

  11. Dextran sulfate sodium (DSS)-induced colitis in mice.

    Science.gov (United States)

    Chassaing, Benoit; Aitken, Jesse D; Malleshappa, Madhu; Vijay-Kumar, Matam

    2014-02-04

    Inflammatory bowel diseases (IBD), mainly comprising ulcerative colitis and Crohn's Disease, are complex and multifactorial diseases with unknown etiology. For the past 20 years, to study human IBD mechanistically, a number of murine models of colitis have been developed. These models are indispensable tools to decipher underlying mechanisms of IBD pathogenesis as well as to evaluate a number of potential therapeutics. Among various chemically induced colitis models, the dextran sulfate sodium (DSS)-induced colitis model is widely used because of its simplicity and many similarities with human ulcerative colitis. This model has both advantages and disadvantages that must be considered when employed. This protocol describes the DSS-induced colitis model, focusing on details and factors that could affect DSS-induced pathology.

  12. Chitosan/dextran multilayer microcapsules for polyphenol co-delivery

    Energy Technology Data Exchange (ETDEWEB)

    Paini, Marco, E-mail: marco.paini@unige.it [Department of Civil, Chemical and Environmental Engineering, University of Genoa, via Opera Pia 15, 16145 Genoa (Italy); Research Center for Biologically Inspired Engineering in Vascular Medicine and Longevity (BELONG), Via Montallegro 1, 16145 Genoa (Italy); Aliakbarian, Bahar; Casazza, Alessandro A.; Perego, Patrizia [Department of Civil, Chemical and Environmental Engineering, University of Genoa, via Opera Pia 15, 16145 Genoa (Italy); Research Center for Biologically Inspired Engineering in Vascular Medicine and Longevity (BELONG), Via Montallegro 1, 16145 Genoa (Italy); Ruggiero, Carmelina; Pastorino, Laura [Department of Informatics, Bioengineering, Robotics and Systems Engineering, University of Genoa, Via Opera Pia 13, 16145 Genoa (Italy)

    2015-01-01

    Polysaccharide-based nanostructured polymeric microcapsules were fabricated by the electrostatic layer-by-layer self-assembly technique and used to encapsulate mixtures of four different polyphenols in order to achieve their controlled release. The real-time fabrication of the dextran/chitosan multilayer was monitored by quartz crystal microbalance with dissipation monitoring, and the morphology of the nanostructured polymeric capsules was characterized by scanning electron microscopy. The polyphenol encapsulation was obtained by reversible permeability variation of the capsule shell in ethanol:water mixtures. The loading efficiency in different water:ethanol mixtures and the release rate in acidic conditions were characterized by UV spectroscopy and HPLC. The higher loading efficiency was obtained with an ethanol:water 35:65 phenolic solution, equal to 42.0 ± 0.6%, with a total release of 11.5 ± 0.7 mg of total polyphenols per 11.3 μL of microcapsules after 240 min of incubation in acidic environment. The results suggest that polysaccharide-based capsules can be successfully used to encapsulate and release low water-soluble molecules, such as polyphenols. - Highlights: • Chitosan/dextran nanocapsules were made by layer-by-layer self-assembly technique. • Different ethanol:water mixtures of four polyphenols were encapsulated. • An encapsulation efficiency of 42.0 ± 0.6% was obtained using ethanol:water 35:65. • Release profiles in acidic environment were monitored by UV spectroscopy and HPLC. • Nanocapsules had shown a complete release after 60 min in acidic environment.

  13. Functional food applications of dextran from Weissella cibaria RBA12 from pummelo (Citrus maxima).

    Science.gov (United States)

    Baruah, Rwivoo; Maina, Ndegwa H; Katina, Kati; Juvonen, Riikka; Goyal, Arun

    2017-02-02

    Weissella cibaria RBA12 isolated from pummelo from Northeast India produces a dextran composed of 97% α-(1→6) linkages in the main chain and 3% α-(1→3) branched linkages. The in vitro prebiotic activity of dextran-RBA12 was explored. Dextran-RBA12 displayed enhanced growth of probiotic Bifidobacterium and Lactobacillus spp., and controlled growth of non-probiotic enteric bacteria. Dextran-RBA12 showed superior resistance to physiological barriers with a maximum hydrolysis of 0.51%, 0.31% and 0.24% by artificial gastric juice, α-amylase and intestinal fluid, respectively, whereas compared to maximum hydrolysis of 25.23%, 19.13% and 6%, respectively after 5h of incubation shown by commercial prebiotic inulin. The production of dextran from Weissella cibaria RBA12 in sourdough prepared from whole wheat flour, wheat bran and rye bran showed the highest dextran of 3.26±0.12% d.w. in rye bran. The overall study summarized that dextran-RBA12 can be used as a prebiotic and also can be easily produced in sourdough. Copyright © 2016 Elsevier B.V. All rights reserved.

  14. Quantum Magnetomechanics with Levitating Superconducting Microspheres

    CERN Document Server

    Romero-Isart, O; Navau, C; Sanchez, A; Cirac, J I

    2011-01-01

    We show that by magnetically trapping a superconducting microsphere close to a quantum circuit, it is experimentally feasible to perform ground state cooling and to prepare quantum superpositions of the center-of-mass motion of the microsphere. Due to the absence of clamping losses and time dependent electromagnetic fields, the mechanical motion of micrometer-sized metallic spheres in the Meissner state is predicted to be extremely well isolated from the environment. Hence, we propose to combine the technology of magnetic mictrotraps and superconducting qubits to bring relatively large objects to the quantum regime.

  15. 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.

  16. High Resolutions Obtained by Microspheres, and Phase Contrast Microscope with a Microsphere

    CERN Document Server

    Ben-Aryeh, Y

    2015-01-01

    High resolutions obtained in optical systems with microspheres are studied by Helmholtz equation and boundary conditions for the EM fields. The large lateral spatial wave vectors of the evanescent waves, which include information on the fine structures of the object, are converted at the microsphere surface to smaller spatial wave vectors. Due to reduction in the magnitudes of these spatial wave vectors a part of the EM waves propagate in the microsphere without decay, but preserve the fine structures which can be recovered in the image plane. A new method for measuring phase objects, like those of semi-transparent biological tissues, with high resolutions is described by an optical system composed of a combination of the microsphere with an interferometer.

  17. Preparation of Micron-size Functional Fluorescent Microspheres

    Institute of Scientific and Technical Information of China (English)

    WANG Di-qiang; LIU Bai-ling; LI He; HU Jie

    2004-01-01

    As a kind of special functional microspheres, fluorescent polymer microspheres could be used in cell label and separation, blood flow assay, flow cytometer marking, chemical reaction assay,and in analyst of the transform and diffusion of particles in soil 1. However, one of the most important applications of fluorescent microspheres is in the high-throughput screening of drugs (HTS) 2. Through affinity interaction, radioactive ligands (latent drugs) are bound to fluorescent microspheres covered by receptor, and luminescence is produced by radioactivity, so ligands can be assayed and screened.In this study, we developed a technique for preparing micron-size fluorescent microspheres with different functional groups. The methods included the synthesis of micron-size polystyrene microspheres through the dispersion polymerization of styrene in different media such as ethanol,ethanol-water, and isopropanol; the functional polystyrene microspheres were prepared by introduction of functional monomers into the reaction system of styrene; the functional fluorescent microspheres were obtained by the way of dying functional microspheres in the fluorescent material's ethanol solvent.The average diameter of microspheres was in the range of 1~10 μm, and the distribution was normal distribution. The functional groups included -OH, -CHO, -COOH, -CONH2, and SO3H. The absorbing spectrum and exciting spectrum were tested, the results showed that the maximal absorbance of fluorescent microsphere was near 306.5 nm, and its maximal excitation was near 362 nm. The excitation spectrum of fluorescent material (DPO) and fluorescent microspheres were shown in figure 1, and it indicated that the developed fluorescent microspheres showed the same excitation behavior like DPO, which related to the fluorescent microspheres had stable luminescence property.

  18. Preparation of biodegradable porous poly(butylene succinate microspheres

    Directory of Open Access Journals (Sweden)

    Pepić Dragana

    2008-01-01

    Full Text Available The aim of this study was to determine the optimal conditions for the fabrication of porous microspheres based on poly(butylene succinate, PBS. The biodegradable non-porous PBS microspheres were prepared by the oil-in-water (o/w emulsion solvent evaporation method using poly(vinyl alcohol, PVA, as the surfactant. Fabrication conditions, such as stirring rate, organic/aqueous ratio, PBS concentration and surfactant (PVA concentration, which have an important influence on both the particle size and the morphology of the microspheres, were varied. Scanning electron microscopy, SEM, observations confirmed the size, size distribution and surface morphology of the microspheres. The optimal conditions for the preparation of the non-porous microspheres were found to be: concentration the PBS solution, 10 mass%; PVA concentration, 1 mass%; the organic/ aqueous ratio CHCl3/H2O = 1/20 and stirring rate 800 rpm. Porous PBS microspheres were fabricated under the optimal conditions using various amounts of hexane and poly(ethylene oxide, PEO, as porogens. The influence of the amount of porogen on the pore size and the particle size was investigated using SEM and the apparent density. The microspheres exhibited various porosities and the pore sizes. The average particle size of the microspheres with PEO as the porogen was from 100 to 122μm and that of the microspheres with hexane as the porogen was from 87 to 97μm. The apparent density of the porous microspheres with PEO as the porogen, from 0.16 to 0.23 g/cm3, was much smaller than the non-porous microspheres, 0.40 g/cm3. In the in vitro degradation experiments, the porous microspheres were incubated in phosphate buffer solution (pH 7 at 37°C. After incubating for one month, the microspheres showed significant extent of the hydrolytic degradation of the porous PBS microspheres.

  19. Uncertainties in the use of periodate oxidation for determination of dextran structure.

    Science.gov (United States)

    Leonard, G J

    1975-05-01

    A glucan of high molecular weight isolated from stale sugar-cane, and previously shown to have a marked effect on sucrose crystallisation processes-1, is a relatively linear dextran. Approximately 96-97% of its D-glucose residues are involved in (1 yields 6)-alpha-D linkages and constitute the linear backbone of the polymer. The remaining 3-4% of D-glucose residues form branch-points by (1 yields 3)-alpha-D linkages. The periodate-oxidation technique, which has been extensively used by other workers to determine dextran structure, gave erroneous results when applied to the dextran from stale sugar-cane.

  20. Beat-Frequency/Microsphere Medical Ultrasonic Imaging

    Science.gov (United States)

    Yost, William T.; Cantrell, John H.; Pretlow, Robert A., III

    1995-01-01

    Medical ultrasonic imaging system designed to provide quantitative data on various flows of blood in chambers, blood vessels, muscles, and tissues of heart. Sensitive enough to yield readings on flows of blood in heart even when microspheres used as ultrasonic contrast agents injected far from heart and diluted by circulation of blood elsewhere in body.

  1. Tumor Vaccination With Cytokine-Loaded Microspheres

    Science.gov (United States)

    2005-12-01

    buffer (1% hydroxypropylmethylcellulose [DOW Co., Midlands, MI, USA] and 1% Pluronic F127 [Sigma] in phosphate-buffered saline [PBS], pH 7.2). Control mice...hydration buffer (1% hydroxypropylmethylcellulose (Dow) and 1% Pluronic F-127 (Sigma- Aldrich) in PBS, pH 7.2). Control mice received blank microspheres

  2. Arabinoxylan Microspheres: Structural and Textural Characteristics

    Directory of Open Access Journals (Sweden)

    Yolanda López-Franco

    2013-04-01

    Full Text Available The aim of this research was to study the structural and textural characteristics of maize bran arabinoxylan (MBAX microspheres. The laccase-induced cross-linking process was monitored by storage (G' and loss (G'' moduli changes in a 4% (w/v MBAX solution. The G' and G'' values at the plateau region were 215 and 4 Pa, respectively. After gelation, the content of ferulic acid dimers decreased from 0.135 to 0.03 µg/mg MBAX, suggesting the formation of ferulated structures unreleased by mild alkaline hydrolysis. MBAX microspheres presented an average diameter of 531 µm and a swelling ratio value (q of 18 g water/g MBAX. The structural parameters of MBAX microspheres were calculated from equilibrium swelling experiments, presenting an average mesh size of 52 nm. Microstructure and textural properties of dried MBAX microspheres were studied by scanning electron microscopy and nitrogen adsorption/desorption isotherms, respectively, showing a heterogeneous mesoporous and macroporous structure throughout the network.

  3. Encapsulated PDMS microspheres with reactive handles

    DEFF Research Database (Denmark)

    Gonzalez, Lidia; Ma, Baoguang; Li, Li

    2014-01-01

    Cured poly(dimethyl siloxane) microspheres are prepared by an emulsion polymerization reaction of silicone droplets in a continuous aqueous phase. The commonly used PDMS elastomer, Sylgard 184 from Dow Corning, is used as the dispersed phase. PDMS is polymerized and cross-linked by reacting vinyl...

  4. Optimization and evaluation of gastroretentive ranitidine HCl microspheres by using design expert software.

    Science.gov (United States)

    Hooda, Aashima; Nanda, Arun; Jain, Manish; Kumar, Vikash; Rathee, Permender

    2012-12-01

    The current study involves the development and optimization of their drug entrapment and ex vivo bioadhesion of multiunit chitosan based floating system containing Ranitidine HCl by ionotropic gelation method for gastroretentive delivery. Chitosan being cationic, non-toxic, biocompatible, biodegradable and bioadhesive is frequently used as a material for drug delivery systems and used to transport a drug to an acidic environment where it enhances the transport of polar drugs across epithelial surfaces. The effect of various process variables like drug polymer ratio, concentration of sodium tripolyphosphate and stirring speed on various physiochemical properties like drug entrapment efficiency, particle size and bioadhesion was optimized using central composite design and analyzed using response surface methodology. The observed responses were coincided well with the predicted values given by the optimization technique. The optimized microspheres showed drug entrapment efficiency of 74.73%, particle size 707.26 μm and bioadhesion 71.68% in simulated gastric fluid (pH 1.2) after 8 h with floating lag time 40s. The average size of all the dried microspheres ranged from 608.24 to 720.80 μm. The drug entrapment efficiency of microspheres ranged from 41.67% to 87.58% and bioadhesion ranged from 62% to 86%. Accelerated stability study was performed on optimized formulation as per ICH guidelines and no significant change was found in drug content on storage.

  5. Composition and structure of calcium aluminosilicate microspheres

    Science.gov (United States)

    Sharonova, O. M.; Oreshkina, N. A.; Zhizhaev, A. M.

    2017-06-01

    The composition was studied of calcium aluminosilicate microspheres of three morphological types in high-calcium fly ash from combustion of brown coal from the Kansk-Achinsk basin in slag-tap boilers at temperatures from 1400 to 1500°C and sampled in the first field of electrostatic precipitators at the Krasnoyarsk Cogeneration Power Station no. 2 (TETs-2). Gross compositions and the composition of local areas were determined using a scanning electron microscopy technique and an energy-dispersive analysis with full mapping of globules. With a high content of basic oxides O ox (68 to 79 wt %) and a low content of acid oxides K ox (21 to 31 wt %), type 1 microspheres are formed. They consist of heterogeneous areas having a porous structure and crystalline components in which the content of CaO, SiO2, or Al2O3 differs by two to three times and the content of MgO differs by seven times. With a lower content of O ox (55 to 63 wt %) and an elevated content of K ox (37 to 45 wt %), type 2 microspheres are formed. They are more homogeneous in the composition and structure and consist of similar crystalline components. Having a close content of O ox (46 to 53 wt %) and K ox (47 to 54 wt %), type 3 microspheres, which are a dense matter consisting of amorphous substance with submicron- and nanostructure of crystalline components, are formed. The basic precursor in formation of high-calcium aluminosilicate microspheres is calcium from the organomineral matter of coals with various contribution of Mg, Fe, S, or Na from the coal organic matter and Al, Fe, S, or Si in the form of single mineral inclusions in a coal particle. On the basis of the available data, the effect was analyzed of the composition of a CaO-MgO-Al2O3-SiO2-FeO system on the melting and viscous properties of the matter in microspheres and formation of globules of different morphology. The results of this analysis will help to find a correlation with properties of microspheres in their use as functional

  6. Preparation of Hollow Porous HAP Microspheres as Drug Delivery Vehicles

    Institute of Scientific and Technical Information of China (English)

    WANG Qing; HUANG Wenhai; WANG Deping

    2007-01-01

    Hollow HAP microspheres in sub-millimeter size were prepared and investigated as a drug delivery vehicle. The LCB (lithium-calcium borate) glass microspheres, which were made through flame spray process, were chosen as precursor for hollow HAP microspheres. The LCB glass microspheres reacted with phosphate buffer (K2HPO4) solution for 5 days at 37 ℃. During the reaction the Ca-P-OH compound precipitated on the surface of LCB glass microspheres and formed porous shells. Then the microspheres turned to be hollow ones with the same diameter as the glass microspheres after LCB glass run out in the chemical reaction. After heat-treated at 600 ℃ for 4 h, the Ca-P-OH compound became HAP, thus the hollow HAP microspheres were produced. The mechanism of forming hollow HAP microspheres through the chemical reaction between phosphate buffer and LCB glass was confirmed by the XRD analysis. The microstructure characteristics of the hollow, porous microspheres were observed by SEM.

  7. PLGA/alginate composite microspheres for hydrophilic protein delivery.

    Science.gov (United States)

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

    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.

  8. Phase-transition and aggregation characteristics of a thermoresponsive dextran derivative in aqueous solutions.

    Science.gov (United States)

    Shi, Huan-Ying; Zhang, Li-Ming

    2006-10-16

    Grafting of poly(N-vinylcaprolactam) side chains onto a hydrophilic dextran backbone was found to provide the dextran with new, thermoresponsive properties in aqueous solutions. Depending on its solution concentration, the resulting dextran derivative could exhibit a temperature-induced phase-transition and critical transition temperature (T(c)). Different anions and cations of added salts, including five potassium salts and five alkali-metal chlorides, were observed to influence the T(c) value of its aqueous solution. Except for potassium iodide, all added salts were found to lower the T(c) value. The addition of the surfactant, cationic cetyltrimethylammonium bromide or anionic sodium dodecyl sulfate, resulted in an increase of the T(c) value. With the help of the Coomassie Brilliant Blue dye as a polarity probe, the formation of hydrophobic aggregates above the T(c) was revealed for this new dextran derivative in aqueous solution.

  9. Crystallization and preliminary X-ray analysis of Streptococcus mutans dextran glucosidase

    Energy Technology Data Exchange (ETDEWEB)

    Saburi, Wataru; Hondoh, Hironori, E-mail: hondoh@abs.agr.hokudai.ac.jp [Research Faculty of Agriculture, Hokkaido University, Sapporo, Hokkaido 060-8589 (Japan); Unno, Hideaki [Faculty of Engineering, Nagasaki University, Bunkyo-machi, Nagasaki 852-8521 (Japan); Okuyama, Masayuki; Mori, Haruhide [Research Faculty of Agriculture, Hokkaido University, Sapporo, Hokkaido 060-8589 (Japan); Nakada, Toshitaka [Faculty of Science and Engineering, Ritsumeikan University, Kusatsu, Shiga 525-8577 (Japan); Matsuura, Yoshiki [Institute for Protein Research, Osaka University, Suita, Osaka 565-0871 (Japan); Kimura, Atsuo [Research Faculty of Agriculture, Hokkaido University, Sapporo, Hokkaido 060-8589 (Japan)

    2007-09-01

    Dextran glucosidase from S. mutans was crystallized using the hanging-drop vapour-diffusion method. The crystals diffracted to 2.2 Å resolution. Dextran glucosidase from Streptococcus mutans is an exo-hydrolase that acts on the nonreducing terminal α-1,6-glucosidic linkage of oligosaccharides and dextran with a high degree of transglucosylation. Based on amino-acid sequence similarity, this enzyme is classified into glycoside hydrolase family 13. Recombinant dextran glucosidase was purified and crystallized by the hanging-drop vapour-diffusion technique using polyethylene glycol 6000 as a precipitant. The crystals belong to the orthorhombic space group P2{sub 1}2{sub 1}2{sub 1}, with unit-cell parameters a = 72.72, b = 86.47, c = 104.30 Å. A native data set was collected to 2.2 Å resolution from a single crystal.

  10. Inhibitory effect of substituted dextrans on MCF7 human breast cancer cell growth in vitro.

    Science.gov (United States)

    Morere, J F; Letourneur, D; Planchon, P; Avramoglou, T; Jozefonvicz, J; Israel, L; Crepin, M

    1992-12-01

    Substituted dextrans can reproduce some of the properties of heparin and can thus be used to alter cellular growth. We studied the effect of heparin (H108), dextran (D), carboxymethylbenzylamide dextran (CMDB) and carboxymethylbenzylamide sulfonate dextran (CMDBS) on the growth of human mammary cells of the MCF7 tumor line. The cells were cultured in minimum Eagle's medium containing 2% fetal calf serum without biopolymer, or with increasing concentrations of H108, D, CMDB or CMDBS. Growth curves were accurately based on cell counting using a Coulter counter. Cell distribution in the various phases of the cycle was analyzed by flow cytometry. Dose-dependent growth inhibitory effects (400-4000 micrograms/ml) were observed. The effect on MCF7 tumor cells was most apparent with CMDBS. The percentage of cells in the S phase decreased with preferential blocking in the G0/G1 phase. Pre-clinical studies can be anticipated as there is an absence of in vivo toxicity.

  11. Probing Conformational Change of Bovine Serum Albumin–Dextran Conjugates under Controlled Dry Heating

    Energy Technology Data Exchange (ETDEWEB)

    Xia, Shuqin; Li, Yunqi; Zhao, Qin; Li, Ji; Xia, Qiuyang; Zhang, Xiaoming; Huang, Qingrong (Rutgers); (Chinese Aca. Sci.); (Jiangnan)

    2015-04-29

    The time-dependent conformational change of bovine serum album (BSA) during Maillard reaction with dextran under controlled dry heating has been studied by small-angle X-ray scattering, fluorescence spectroscopy, dynamic light scattering, and circular dichroism analysis. Through the research on the radii of gyration (Rg), intrinsic fluorescence, and secondary structure, conjugates with dextran coating were found to inhibit BSA aggregation and preserve the secondary structure of native BSA against long-time heat treatment during Maillard reaction. The results suggested that the hydrophilic dextran was conjugated to the compact protein surface and enclosed it and more dextran chains were attached to BSA with the increase of the heating time. The study presented here will be beneficial to the understanding of the conformational evolution of BSA molecules during the dry-heating Maillard reaction and to the control of the protein–polysaccharide conjugate structure.

  12. PLGA microspheres encapsulating siRNA.

    Science.gov (United States)

    De Rosa, Giuseppe; Salzano, Giuseppina

    2015-01-01

    The therapeutic use of small interfering RNA (siRNA) represents a new and powerful approach to suppress the expression of pathologically genes. However, biopharmaceutical drawbacks, such as short half-life, poor cellular uptake, and unspecific distribution into the body, hamper the development of siRNA-based therapeutics. Poly(lactide-co-glycolide), (PLGA) microspheres can be a useful tool to overcome these issues. siRNA can be encapsulated into the PLGA microspheres, which protects the loaded nucleic acid against the enzymatic degradation. Moreover, PLGA microspheres can be injected directly into the action site, where the siRNA can be released in controlled manner, thus avoiding the need of frequent invasive administrations. The complete biodegradability of PLGA to monomers easily metabolized by the body, and its approval by FDA and EMA for parenteral administration, assure the safety of this copolymer and do not require the removal of the device after the complete drug release. In chapter, a basic protocol for the preparation of PLGA microspheres encapsulating siRNA is described. This protocol is based on a double emulsion/solvent evaporation technique, a well known and easy to reproduce method. This specific protocol has been developed to encapsulate a siRNA anti-TNFα in PLGA microspheres, and it has been designed and optimized to achieve high siRNA encapsulation efficiency and slow siRNA release in vitro. However, it can be extended also to other siRNA as well as other RNA or DNA-based oligonucleotides (miRNA, antisense, decoy, etc.). Depending on the applications, chemical modifications of the backbone and site-specific modification within the siRNA sequences could be required.

  13. Subcritical CO{sub 2} sintering of microspheres of different polymeric materials to fabricate scaffolds for tissue engineering

    Energy Technology Data Exchange (ETDEWEB)

    Bhamidipati, Manjari; Sridharan, BanuPriya [Bioengineering Graduate Program, University of Kansas, Lawrence, KS (United States); Scurto, Aaron M. [Bioengineering Graduate Program, University of Kansas, Lawrence, KS (United States); Department of Chemical and Petroleum Engineering, University of Kansas, Lawrence, KS (United States); Detamore, Michael S., E-mail: detamore@ku.edu [Bioengineering Graduate Program, University of Kansas, Lawrence, KS (United States); Department of Chemical and Petroleum Engineering, University of Kansas, Lawrence, KS (United States)

    2013-12-01

    The aim of this study was to use CO{sub 2} at sub-critical pressures as a tool to sinter 3D, macroporous, microsphere-based scaffolds for bone and cartilage tissue engineering. Porous scaffolds composed of ∼ 200 μm microspheres of either poly(lactic-co-glycolic acid) (PLGA) or polycaprolactone (PCL) were prepared using dense phase CO{sub 2} sintering, which were seeded with rat bone marrow mesenchymal stromal cells (rBMSCs), and exposed to either osteogenic (PLGA, PCL) or chondrogenic (PLGA) conditions for 6 weeks. Under osteogenic conditions, the PLGA constructs produced over an order of magnitude more calcium than the PCL constructs, whereas the PCL constructs had far superior mechanical and structural integrity (125 times stiffer than PLGA constructs) at week 6, along with twice the cell content of the PLGA constructs. Chondrogenic cell performance was limited in PLGA constructs, perhaps as a result of the polymer degradation rate being too high. The current study represents the first long-term culture of CO{sub 2}-sintered microsphere-based scaffolds, and has established important thermodynamic differences in sintering between the selected formulations of PLGA and PCL, with the former requiring adjustment of pressure only, and the latter requiring the adjustment of both pressure and temperature. Based on more straightforward sintering conditions and more favorable cell performance, PLGA may be the material of choice for microspheres in a CO{sub 2} sintering application, although a different PLGA formulation with the encapsulation of growth factors, extracellular matrix-derived nanoparticles, and/or buffers in the microspheres may be advantageous for achieving a more superior cell performance than observed here. - Highlights: • The first long-term culture of CO{sub 2}-sintered microsphere-based scaffolds. • Established important thermodynamic differences between sintering PLGA and PCL. • PCL sintering with CO{sub 2} required manipulation of both

  14. Dextran and 5-aminosalicylic acid (5-ASA) conjugates: synthesis, characterisation and enzymic hydrolysis.

    Science.gov (United States)

    Ahmad, Shavej; Tester, Richard F; Corbett, Alistair; Karkalas, John

    2006-11-27

    Mesalamine (5-aminosalicylic acid) is the drug of choice for the treatment of Crohn's disease. A scheme for the synthesis of 5-aminosalicylic acid (5-ASA) conjugates of dextrans was developed with a focus on Crohn's disease applications. Dextrans were oxidised using sodium periodate (NaIO(4)), where the aldehyde groups formed were coupled with the alpha-amino (-NH(2)) group of 5-ASA. The resulting imine bonds were unstable in water and were consequently reduced to secondary amine groups. The effects of different aspects of the conjugation reaction were studied. These included the following: the molecular weight of the dextrans, the molar proportion of NaIO(4) to the dextrans (for periodate oxidation), the pH of the conjugation solutions, the ratio 5-ASA to oxidised polysaccharide and the relationship between the degree of conjugation and the amount of enzyme hydrolysis. Conjugates incubated in HCl were stable in 0.5 and 1.0M HCl, but they underwent degradation in 2.0 and 4.0M HCl. Dextrans (MW 20,000) with various degrees of oxidation (12%, 26%, 46%, 65%, 90% and 93%) were also prepared. Each oxidised dextran sample was conjugated with 5-ASA, and the product was quantified by high-performance liquid chromatography (HPLC). Dextrans with a maximum degree of oxidation (93%) unsurprisingly gave maximum conjugation of 5-ASA (49.1mg per 100mg of product) but were resistant to dextranase hydrolysis. Less oxidised dextrans (12%) conjugated proportionally less 5-ASA (15.1mg per 100mg of product) but were successfully hydrolysed by dextranase, suggesting their potential applications for the treatment of Crohn's disease in the distal ileum and proximal colon.

  15. Formulation development and evaluation of orally disintegrating tablets of doxazosin mesylate

    Directory of Open Access Journals (Sweden)

    Shilpa P Chaudhari

    2012-01-01

    Full Text Available Doxazosin mesylate has some of the ideal characteristics required for an orally disintegrating tablet. There were some challenges faced during this formulation development. The aims of the present research were to mask the bitter taste of Doxazosin mesylate and to formulate orally disintegrating tablets of taste masked drug. Taste masking was performed by coating Doxazosin Mesylate with suitable polymer Eudragit powdered E-100 using spray drying technique. The resultant microspheres were then evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentration of super-disintegrants and granulated Mannitol was selected as diluent and compressed using direct compression method. The tablets prepared were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release and compared with marketed IR tablet of Doxazosin mesylate.

  16. Crystallization Formulation Lab

    Data.gov (United States)

    Federal Laboratory Consortium — The Crystallization Formulation Lab fills a critical need in the process development and optimization of current and new explosives and energetic formulations. The...

  17. Cell-repellant dextran coatings of porous titania using mussel adhesion chemistry.

    Science.gov (United States)

    Park, Jae Yoon; Yeom, Jihyeon; Kim, Jee Seon; Lee, Mihyun; Lee, Haeshin; Nam, Yoon Sung

    2013-11-01

    The resistance of bioceramics against non-specific adsorption of serum proteins is critical for a wide range of biomedical applications. Some polysaccharides serve as natural protein-resistant molecules in extracellular matrices; however, the stable adhesion of polysaccharides to ceramic biomaterials in an aqueous solution is very challenging because chemical linkages at organic/inorganic interfaces are susceptible to hydrolytic degradation. Here, a catechol-grafted dextran, which strongly binds to titania (TiO2 ) in an aqueous milieu to effectively suppress cell adhesion through anti-fouling activity against non-specific protein adsorption, is introduced. Catechol is conjugated approximately to 6.7 mol% of glucose units of dextran via a carbamate ester linkage, corresponding to roughly three catechols per dextran chain having an average molecular weight of 6 kDa. Multivalent interactions of catechols with a titanium atom, enabled by the graft-type structure, provide a very stable coating of dextran on this inorganic surface. The adhesion of HeLa cells on the dextran-coated titania surface is reduced by 2.4-fold compared to that on a pristine titania surface. These results suggest that the graft-type incorporation of a small number of catechol moieties along a dextran backbone is an effective means of producing a stable anti-fouling interface on inorganic biomaterials in an aqueous environment.

  18. An efficient acetylation of dextran using in situ activated acetic anhydride with iodine

    Directory of Open Access Journals (Sweden)

    MUHAMMAD A. HUSSAIN

    2010-02-01

    Full Text Available A facile, efficient, cost-effective and solvent-free acetylation method has been developed for the acetylation of dextran. Dextran acetates were successfully synthesized using different molar ratios of acetic anhydride in the presence of iodine as a catalyst without the use of any solvent. The reactions were realized at 50 °C for 3 h under stirring and nitrogen. This efficient method yielded highly pure and organosoluble dextran esters. The reaction appears highly effective for obtaining higher degrees of substitution (DS with great efficiency. Under solvent-free conditions, dextran triacetates were efficiently synthesized. It was also observed that the molar ratio can easily control the DS of pendant groups onto the polymer backbone. Hence, a range of products with varying DS were successfully designed, purified and characterized. Covalent attachment of the pendant groups onto the polymer backbone was verified by spectroscopic techniques. Thermogravimetric analysis indicated that the obtained dextran esters were thermally as stable as dextran. The DS of the pendant groups onto the polymer backbone was calculated using standard acid base titration after saponification. Furthermore, all products were thoroughly characterized by thermal analysis (TG and DTG, and FTIR and 1H-NMR spectroscopic analysis.

  19. Water Kefir grain as a source of potent dextran producing lactic acid bacteria

    Directory of Open Access Journals (Sweden)

    Davidović Slađana Z.

    2015-01-01

    Full Text Available Water kefir is abeverage fermented by a microbial consortium captured in kefir grains. The kefir grains matrix is composed of polysaccharide, primarily dextran, whichis produced by members of the microbial consortium. In this study, we have isolated lactic acid bacteria (LAB from non-commercial water kefir grains (from Belgrade, Serbia and screened for dextran production. Among twelve Lisolates threeproduced slime colonies on modified MRS (mMRS agar containing sucrose instead of glucoseand were presumed to produce dextran. Three LABwere identified based on morphological, physiological and biochemical characteristics and 16S rRNA sequencing as Leuconostoc mesenteroides(strains T1 and T3 and Lactobacillus hilgardii (strain T5. The isolated strains were able to synthesize a substantial amount of dextran in mMRS broth containing 5% sucrose. Maximal yields (11.56, 18.00 and 18.46 g/l were obtained after 16h, 20h and 32h for T1, T3 and T5, respectively. Optimal temperature for dextran production was 23oC for two Leuconostoc mesenteroides strains and 30oC for Lactobacillus hilgardii strain. The produced dextrans were identified based on paper chromatography while the main structure characteristics of purified dextranwere observed by FT-IR spectroscopy. Our study shows that water kefir grains are a natural source of potent dextranproducing LAB. [Projekat Ministarstva nauke Republike Srbije, br. TR 31035

  20. The molecular mass of dextran used to modify magnetite nanoparticles affects insulin amyloid aggregation

    Science.gov (United States)

    Siposova, Katarina; Pospiskova, Kristyna; Bednarikova, Zuzana; Safarik, Ivo; Safarikova, Mirka; Kubovcikova, Martina; Kopcansky, Peter; Gazova, Zuzana

    2017-04-01

    Protein transformation from its soluble state into amyloid aggregates is associated with amyloid-related diseases. Amyloid deposits of insulin fibrils have been found in the sites of subcutaneous insulin application in patients with prolonged diabetes. Using atomic force microscopy and ThT fluorescence assay we have investigated the interference of insulin amyloid aggregation with superparamagnetic Fe3O4-based nanoparticles (SPIONs) coated with dextran (DEX); molecular mass of dextran was equal to 15-20, 40 or 70 kDa. The obtained data indicate that all three types of dextran coated nanoparticles (NP-FeDEXs) are able to inhibit insulin fibrillization and to destroy amyloid fibrils. The extent of anti-amyloid activities depends on the properties of NP-FeDEXs, mainly on the size of nanoparticles which is determined by molecular mass of dextran molecules. The most effective inhibiting activity was observed for the smallest nanoparticles coated with 15-20 kDa dextran. Contrary, the highest destroying activity was observed for the largest NP-FeDEX (70 kDa dextran).

  1. Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery

    Science.gov (United States)

    Shahi, Priya; Kumari, Neeraj; Pathak, Kamla

    2015-01-01

    The objective of the present work was to develop a novel delivery system of ketorolac tromethamine (KT) for dual pulse release based on microspheres and tablet in capsule system (MATICS) as a treatment modality for rheumatoid arthritis. The design consisted of an impermeable hard gelatin capsule body, in which a core tablet was (second pulse) placed in the bottom and sealed with a hydrogel plug (HP2). The body was locked with enteric coated cap filled with KT microspheres (first pulse). The microspheres for first pulse were selected by screening the formulations (M1–M6), and M1 with least particle size of 96.38 ± 0.05 μm, highest drug loading of 25.10% ± 0.28% and maximum CDR of 89.32% ± 0.21% was adjudged as the best formulation. The HP2 tablet was selected based on its capability for maintaining a lag period of 6 h. The selection criterion of the second pulse (core tablet: T3) was its disintegration time of 4.02 ± 0.53 min and CDR of 99.10% ± 0.32% in 30 min. All the optimized formulations were assembled in accordance with the proposed design to form pulsatile MATICS and evaluated for in vitro release. MATICS displayed delayed sustained CDR of 80.15% in 8 h from the first pulse (microspheres) after a lag time of 2 h, followed by 97.05% KT release from second pulse (core tablet) in simulated colonic fluid within 10 h. Conclusively, in vitro pulsatile release was a rational combination of delayed sustained and immediate release of KT that has the potential to combat the pain at night and morning stiffness. Incorporation of two pulses in one system offers a reduction in dose frequency and better pain management. PMID:26258058

  2. New nasal nanocomplex self-assembled from charged biomacromolecules: N,N,N-Trimethyl chitosan and dextran sulfate.

    Science.gov (United States)

    Kulkarni, Abhijeet D; Vanjari, Yogesh H; Sancheti, Karan H; Patel, Harun M; Belgamwar, Veena S; Surana, Sanjay J; Pardeshi, Chandrakantsing V

    2016-07-01

    Although chitosan (CHT, a linear cationic polysaccharide) is biodegradable, biocompatible, non-toxic, and mucoadhesive in nature, the low solubility of CHT in aqueous and alkaline media limits its applicability in pharmaceutical and biomedical field. This necessitate the introduction of new chemically-modified derivatives of CHT those can surmount the solubility barrier. Herein, N,N,N-trimethyl chitosan (TMC), a quaternized hydrophilic derivative of CHT, was synthesized by two-step reductive methylation of CHT and characterized for (1)H NMR and zeta potential measurements. Polyelectrolyte complexes (PECs) based on TMC and dextran sulfate (DS) were prepared via ionic interactions between charged functional groups of former polysaccharides at different pH conditions (pH 5, 8, 10, and 12) and characterized for physicochemical (particle size and zeta potential) and solid- state characterizations (HR-TEM, SEM, FTIR, TGA and XRD). At alkaline pH conditions, the participant polymer chains (TMC and DS) are sufficiently close to form more stable PECs. The release efficiency was assessed after loading a model drug into optimized PEC formulation. Data indicated that the PECs fabricated at alkaline pH presents a reliable formulation for pharmaceutical and biomedical applications.

  3. Pluronic F127/chitosan blend microspheres for mucoadhesive drug delivery

    Science.gov (United States)

    Gu, W. Z.; Hu, X. F.

    2017-01-01

    Pluronic F127/chitosan blend microspheres were prepared via emulsification and cross-linking process using glutaraldehyde as a cross-linker. Compared with chitosan microspheres fabricated under the same experimental conditions, blend microspheres exhibited better physical stability and higher swelling capacity. Puerarin, a traditional Chinese medicine, was incorporated into microparticlesas the model drug. The in vitro release of puerarin from blend microspheres was reduced because of the improved compatibility of the drug with the matrices. According to the results from in vitro adhesion experiments, mucoadhesive behavior of blend microspheres on a mucosa-like surface was similar to that of chitosan microspheres, despite their good ability of anti-protein absorption in solution.

  4. Method of detecting luminescent target ions with modified magnetic microspheres

    Science.gov (United States)

    Shkrob, Ilya A; Kaminski, Michael D

    2014-05-13

    This invention provides methods of using modified magnetic microspheres to extract target ions from a sample in order to detect their presence in a microfluidic environment. In one or more embodiments, the microspheres are modified with molecules on the surface that allow the target ions in the sample to form complexes with specific ligand molecules on the microsphere surface. In one or more embodiments, the microspheres are modified with molecules that sequester the target ions from the sample, but specific ligand molecules in solution subsequently re-extract the target ions from the microspheres into the solution, where the complexes form independent of the microsphere surface. Once the complexes form, they are exposed to an excitation wavelength light source suitable for exciting the target ion to emit a luminescent signal pattern. Detection of the luminescent signal pattern allows for determination of the presence of the target ions in the sample.

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

    Science.gov (United States)

    Hnatowich, D J; Schlegel, P

    1981-07-01

    Albumin microspheres have been synthesized eith 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 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 hr. Since labeling is by chelation, the microspheres may also be tagged with other metallic radionuclides

  6. Laser-assisted fabrication of highly viscous alginate microsphere

    Science.gov (United States)

    Lin, Yafu; Huang, Yong

    2011-04-01

    Encapsulated microspheres have been widely used in various biomedical applications. However, fabrication of encapsulated microspheres from highly viscous materials has always been a manufacturing challenge. The objective of this study is to explore a novel metallic foil-assisted laser-induced forward transfer (LIFT), a laser-assisted fabrication technique, to make encapsulated microspheres using high sodium alginate concentration solutions. The proposed four-layer approach includes a quartz disk, a sacrificial and adhesive layer, a metallic foil, and a transferred suspension layer. It is found that the proposed four-layer modified LIFT approach provides a promising fabrication technology for making of bead-encapsulated microspheres from highly viscous solutions. During the process, the microsphere only can be formed if the direct-writing height is larger than the critical direct-writing height; otherwise, tail structured droplets are formed; and the encapsulated microsphere diameter linearly increases with the laser fluence and decreases with the sodium alginate concentration.

  7. Bioreducible carboxymethyl dextran nanoparticles for tumor-targeted drug delivery.

    Science.gov (United States)

    Thambi, Thavasyappan; You, Dong Gil; Han, Hwa Seung; Deepagan, V G; Jeon, Sang Min; Suh, Yung Doug; Choi, Ki Young; Kim, Kwangmeyung; Kwon, Ick Chan; Yi, Gi-Ra; Lee, Jun Young; Lee, Doo Sung; Park, Jae Hyung

    2014-11-01

    Bioreducible carboxymethyl dextran (CMD) derivatives are synthesized by the chemical modification of CMD with lithocholic acid (LCA) through a disulfide linkage. The hydrophobic nature of LCA allows the conjugates (CMD-SS-LCAs) to form self-assembled nanoparticles in aqueous conditions. Depending on the degree of LCA substitution, the particle diameters range from 163 to 242 nm. Doxorubicin (DOX), chosen as a model anticancer drug, is effectively encapsulated into the nanoparticles with high loading efficiency (>70%). In vitro optical imaging tests reveal that the fluorescence signal of DOX quenched in the bioreducible nanoparticles is highly recovered in the presence of glutathione (GSH), a tripeptide capable of reducing disulfide bonds in the intracellular compartments. Bioreducible nanoparticles rapidly release DOX when they are incubated with 10 mm GSH, whereas the drug release is greatly retarded in physiological buffer (pH 7.4). DOX-loaded bioreducible nanoparticles exhibit higher toxicity to SCC7 cancer cells than DOX-loaded nanoparticles without the disulfide bond. Confocal laser scanning microscopy observation demonstrate that bioreducible nanoparticles can effectively deliver DOX into the nuclei of SCC7 cells. In vivo biodistribution study indicates that Cy5.5-labeled CMD-SS-LCAs selectively accumulate at tumor sites after systemic administration into tumor-bearing mice. Notably, DOX-loaded bioreducible nanoparticles exhibit higher antitumor efficacy than reduction-insensitive control nanoparticles. Overall, it is evident that bioreducible CMD-SS-LCA nanoparticles are useful as a drug carrier for cancer therapy.

  8. Covalent immobilization of Enterococcus faecalis Esawy dextransucrase and dextran synthesis.

    Science.gov (United States)

    Hashem, Amal M; Gamal, Amira A; Hassan, Mohamed E; Hassanein, Naziha M; Esawy, Mona A

    2016-01-01

    Enterococcus faecalis Esawy dextransucrase was immobilized in Fe(3+)-cross-linked alginate/carboxymethyl cellulose (AC) beads. The gel beads were modified with polyethylenimine (PEI) followed by glutaraldehyde (GA) to form Fe(3+) (ACPG) beads. Fe(3+) (ACPG) was characterized using FTIR and DSC techniques. GA activated beads showed new two peaks. The first was at 1,717 cm(-1) which refers to (CO) group of a free aldehyde end of glutaraldehyde, and another peak was at 1,660 cm(-1) referring to (CN) group. The immobilization process improved the optimum temperature from 35 to 45°C. The immobilized enzyme showed its optimum activity in wide pH range (4.5-5.4) compared to pH 5.4 in case of free form. Also, the immobilization process improved the thermal and pH enzyme stability to great extent. Reusability test proved that the enzyme activity retained 60% after 15 batch reactions. Immobilized enzyme was applied successfully in the synthesis of oligosaccharides and different molecular weights of dextran.

  9. Biotinylated dextran amine anterograde tracing of the canine corticospinal tract

    Institute of Scientific and Technical Information of China (English)

    Xiao Han; Guangming Lv; Huiqun Wu; Dafeng Ji; Zhou Sun; Yaofu Li; Lemin Tang

    2012-01-01

    In this study, biotinylated dextran amine (BDA) was microinjected into the left cortical motor area of the canine brain. Fluorescence microscopy results showed that a large amount of BDA-labeled pyramidal cells were visible in the left cortical motor area after injection. In the left medulla oblongata, the BDA-labeled corticospinal tract was evenly distributed, with green fluorescence that had a clear boundary with the surrounding tissue. The BDA-positive corticospinal tract entered into the right lateral funiculus of the spinal cord and descended into the posterior part of the right lateral funiculus, close to the posterior horn, from cervical to sacral segments. There was a small amount of green fluorescence in the sacral segment. The distribution of BDA labeling in the canine central nervous system was consistent with the course of the corticospinal tract. Fluorescence labeling for BDA gradually diminished with time after injection. Our findings indicate that the BDA anterograde tracing technique can be used to visualize the localization and trajectory of the corticospinal tract in the canine central nervous system.

  10. Agaricus bisporus attenuates dextran sulfate sodium-induced colitis.

    Science.gov (United States)

    Um, Min Young; Park, Jae Ho; Gwon, So Young; Ahn, Jiyun; Jung, Chang Hwa; Ha, Tae Youl

    2014-12-01

    Agaricus bisporus (white button mushroom, WBM) is widely consumed in most countries and is reported to have anti-inflammatory and antioxidant activities. However, little is known regarding its effects in dextran sulfate sodium (DSS)-induced colitis, which are related to dysfunction of intestinal immunity. The aim of the present study was to investigate the effects of WBMs in an animal model of DSS-induced colitis. Male, 4-week-old ICR mice (n=10 per group) were fed a normal diet with or without 10% WBM for 4 weeks, and colitis was induced by 3% DSS in drinking water for 7 days. WBMs prevented DSS-induced shortening of colon length (P=.033) and diminished diarrhea (P=.049) and gross bleeding (P=.001), resulting in a decreased disease activity index. Results of histological analysis showed that WBMs suppressed mucosal damage. In addition, WBMs attenuated the DSS-induced increase in myeloperoxidase activity (P=.012) and upregulation of proinflammatory cytokine tumor necrosis factor-α (P=.020) in the colon segment. Taken together, these findings suggest a possible role for the WBM as an immunomodulator that can prevent and/or treat ulcerative colitis.

  11. MULTIMODE THEORY OF WHISPERING GALLERY-MODE MICROSPHERE LASER

    Institute of Scientific and Technical Information of China (English)

    CHAI JIN-HUA; LU YI-QUN; LEUNG PUI-TANG

    2000-01-01

    A multimode theory of whispering-gallery-mode microsphere laser is developed based on the linear and nonlinear semiclassical theory of the microsphere laser. The average photon-number of each lasing mode and the pumping level requirement for multimode coexistence are derived. The comparison between the theory and experimental results shows that the theory can be used to treat the practical problems on microsphere laser.

  12. Preparation and characterization of immobilized lipase on magnetic hydrophobic microspheres

    DEFF Research Database (Denmark)

    Guo, Zheng; Bai, Shu; Sun, Yan

    2003-01-01

    A novel magnetic poly(vinyl acetate (VAc)–divinyl benzene (DVB)) material (8–34 μm) was synthesized by copolymerization of vinyl acetate and divinyl benzene using oleic acid-stabilized magnetic colloids as magnetic cores. The magnetic colloids and the copolymer microspheres were characterized...... with transmission and scanning electron microscopes, respectively. Magnetization of the microspheres could be described by the Langevin function. All the observations indicated that the microspheres were superparamagnetic. Magnetic sedimentation of the microspheres was achieved within 3 min, over 300 times faster...

  13. Controlled Delivery of Gentamicin Using Poly(3-hydroxybutyrate Microspheres

    Directory of Open Access Journals (Sweden)

    Ipsita Roy

    2011-07-01

    Full Text Available Poly(3-hydroxybutyrate, P(3HB, produced from Bacillus cereus SPV using a simple glucose feeding strategy was used to fabricate P(3HB microspheres using a solid-in-oil-water (s/o/w technique. For this study, several parameters such as polymer concentration, surfactant and stirring rates were varied in order to determine their effect on microsphere characteristics. The average size of the microspheres was in the range of 2 µm to 1.54 µm with specific surface areas varying between 9.60 m2/g and 6.05 m2/g. Low stirring speed of 300 rpm produced slightly larger microspheres when compared to the smaller microspheres produced when the stirring velocity was increased to 800 rpm. The surface morphology of the microspheres after solvent evaporation appeared smooth when observed under SEM. Gentamicin was encapsulated within these P(3HB microspheres and the release kinetics from the microspheres exhibiting the highest encapsulation efficiency, which was 48%, was investigated. The in vitro release of gentamicin was bimodal, an initial burst release was observed followed by a diffusion mediated sustained release. Biodegradable P(3HB microspheres developed in this research has shown high potential to be used in various biomedical applications.

  14. Poly(styrene-acrylic acid) magnetic polymer microspheres

    Institute of Scientific and Technical Information of China (English)

    Yanling CHENG; Liuqiang MA; Ruohui LI

    2008-01-01

    Magnetic polymer microspheres have been considered as a kind of new biopolymer materials with great advantages in bioseparation engineering and biome-dicine engineering because they have not only polymer functional groups but also magnetic characteristics. Styrene-acrylic acid copolymer (p(S-AA)) magnetic microspheres were synthesized by dispersion polymeriza-tion with Fe3O4 as core and p(S-AA) as shell. The micro-spheres were characterized by SEM, size analysis, molecular weight and solid content measurement. All of them indicate that the microspheres are small in size, nar-row in distribution, stable in chemistry and rich in func-tional groups on their surface.

  15. Preparation and Characterization of Albumin Microspheres Encapsulated with Propranolol HCl

    Directory of Open Access Journals (Sweden)

    Sayyed Abolghassem Sajadi Tabassi

    2003-10-01

    Full Text Available Albumin microspheres (AMS have found many applications in the diagnosis and treatment in recent years and more than 100 diagnostic agents and drugs have been incorporated into AMS. In the present study Bovine Serum Albumin (BSA based microspheres bearing propranolol hydrochloride were prepared by an emulsion-internal phase stabilization technique. The prepared microspheres were studied for particle size distribution, drug loading, release characteristics, bioadhesion and in-vitro controlled diffusion across the rat intestine. The microspheres had mean diameters between 1-25 mm of which more than 50 percent were below 5 mm. The encapsulated drug was found to be about 9% w/w of that initially added to microspheres and the superficial drug was 25% of the total amount of the encapsulated drug. Also AMS were noted to possess good bioadhesion in such a way that about 70% of microspheres remained adherent on the surface mucosa of rat jejunum.The drug release from albumin microspheres was mainly controlled by diffusion and showed a biphasic pattern with a high initial release (burst effect, followed by a more gradual terminal release. The total amount of drug released from microspheres after 12h was 70%. In vitro experiments on the rat intestinal segments revealed that the microspheres could effectively pass their content through intestinal membrane.

  16. Chitosan microspheres in PLG films as devices for cytarabine release.

    Science.gov (United States)

    Blanco, M D; Gómez, C; Olmo, R; Muñiz, E; Teijón, J M

    2000-07-20

    Cytarabine was included in chitosan microspheres and several of these microspheres were embedded in a poly(lactide-co-glycolide) (PLG) film to constitute a comatrix system, to develop a prolonged release form. Chitosan microspheres, in the range of 92+/-65 microm, having good spherical geometry and a smooth surface incorporating cytarabine, were prepared. The cytarabine amount included in chitosan microspheres was 43.7 microg of ara-C per milligram microsphere. The incorporation efficiency of the cytarabine in microspheres was 70.6%. Total cytarabine release from microspheres in vitro was detected at 48 h. Inclusion of cytarabine-loaded microspheres in poly(lactide-co-glycolide) film initiated a slower release of the drug and, in this way, the maximum of cytarabine released (80%) took place in vitro at 94.5 h. Comatrices, with 8.7 mg of cytarabine, signifying a dose of 34.5 microg/kg, were subcutaneously implanted in the back of rats. Maximum plasma cytarabine concentration was 18.5+/-1.5 microg/ml, 48 h after the device implantation and the drug was detected in plasma for 13 days. The histological studies show a slow degradative process. After 6 months of implantation, most of the microspheres of the matrix seemed to be intact, the comatrix appeared surrounded by conjunctive tissue and small blood vessels and nerve packets were detected in the periphery of the implant.

  17. Synthesis of raspberry-like magnetic polystyrene microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Xu Zhizhong [Key Laboratory of Molecular Engineering of Polymers (Ministry of Education), Department of Macromolecular Science, Fudan University, Shanghai 200433 (China); Xia Ao [Key Laboratory of Molecular Engineering of Polymers (Ministry of Education), Department of Macromolecular Science, Fudan University, Shanghai 200433 (China); Wang Changchun [Key Laboratory of Molecular Engineering of Polymers (Ministry of Education), Department of Macromolecular Science, Fudan University, Shanghai 200433 (China)]. E-mail: ccwang@fudan.edu.cn; Yang Wuli [Key Laboratory of Molecular Engineering of Polymers (Ministry of Education), Department of Macromolecular Science, Fudan University, Shanghai 200433 (China); Fu Shoukuang [Key Laboratory of Molecular Engineering of Polymers (Ministry of Education), Department of Macromolecular Science, Fudan University, Shanghai 200433 (China)

    2007-06-15

    Raspberry-like magnetic polystyrene microspheres were prepared via soap-free emulsion polymerization using 2,2'-azobis(2-methylpropionamidine) dihydrochloride (V50) as initiator. The effect of polymerization parameters, such as initiator type, initiator content and the feeding sequence on the particle size and morphology of magnetic polystyrene microspheres, were examined. The final magnetic polystyrene microspheres were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), vibrating sample magnetometer (VSM) and thermogravimetric analysis (TGA). The experimental results showed that V50 was a suitable initiator for preparation of raspberry-like magnetic polystyrene microspheres.

  18. Osteogenic differentiation of human mesenchymal stem cells through alginate-graft-poly(ethylene glycol) microsphere-mediated intracellular growth factor delivery.

    Science.gov (United States)

    Miao, Tianxin; Rao, Krithika S; Spees, Jeffrey L; Oldinski, Rachael A

    2014-10-28

    The intracellular delivery of growth factors increases opportunities for controlling cell behavior and maintaining tissue homeostasis. Recently, VEGFA was reported to enhance osteogenic differentiation of mesenchymal stem cells (MSCs) through an intracrine mechanism, suggesting a new strategy to promote bone tissue formation in osteoporotic patients. The goal of this study was to design and fabricate ligand-conjugated alginate-graft-poly(ethylene glycol) microspheres for intracellular delivery and release of VEGFA in primary human MSCs to enhance osteogenic differentiation as a potential therapeutic. Three types of microspheres were synthesized and characterized by scanning electron microscopy, in vitro drug release kinetics, MSC uptake and internalization: alginate alone (Alg), alginate-graft-poly(ethylene glycol) (Alg-g-PEG) and alginate-graft-poly(ethylene glycol)-S-S-arginine-glycine-aspartic acid (Alg-g-RGD). Each of the different microsphere formulations successfully transported bioactive VEGFA into primary human MSCs within 48h of culture, and significantly enhanced osteogenic differentiation compared to control treatments with empty microspheres (intracellular control) or non-encapsulated VEGFA (extracellular control). Adipogenic differentiation was not affected by the presence of VEGFA intracellularly or extracellularly. These results demonstrating the internalization of alginate-based microspheres and intracellular delivery of VEGFA support the efficacy of using this drug delivery and intracrine mechanism to control the fate of human MSCs and enhance osteogenic differentiation. Copyright © 2014 Elsevier B.V. All rights reserved.

  19. Activation of Human Complement System by Dextran-Coated Iron Oxide Nanoparticles Is Not Affected by Dextran/Fe Ratio, Hydroxyl Modifications, and Crosslinking

    DEFF Research Database (Denmark)

    Wang, Guankui; Chen, Fangfang; Banda, Nirmal K

    2016-01-01

    , whereas opsonization with C3 fragments promotes rapid recognition and clearance of nanomaterials by mononuclear phagocytes. We used dextran-coated superparamagnetic iron oxide nanoparticles (SPIO), which are potent activators of the complement system, to study the role of nanoparticle surface chemistry...

  20. Neutron transmission measurements on hydrogen filled microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Dyrnjaja, Eva, E-mail: dyrnjaja@ati.ac.at [Vienna University of Technology, Institute of Atomic and Subatomic Physics, Stadionallee 2, Vienna (Austria); Hummel, Stefan, E-mail: hummel@fotec.at [FOTEC GmbH, Viktor Kaplan-Straße 2, 2700 Wiener Neustadt (Austria); Keding, Marcus, E-mail: keding@fotec.at [FOTEC GmbH, Viktor Kaplan-Straße 2, 2700 Wiener Neustadt (Austria); Smolle, Marie-Theres, E-mail: marie-theres.smolle@tuwien.ac.at [Vienna University of Technology, Institute of Atomic and Subatomic Physics, Stadionallee 2, Vienna (Austria); Gerger, Joachim, E-mail: gerger@fotec.at [FOTEC GmbH, Viktor Kaplan-Straße 2, 2700 Wiener Neustadt (Austria); Zawisky, Michael, E-mail: zawisky@ati.ac.at [Vienna University of Technology, Institute of Atomic and Subatomic Physics, Stadionallee 2, Vienna (Austria)

    2014-01-01

    Hollow microspheres are promising candidates for future hydrogen storage technologies. Although the physical process for hydrogen diffusion through glass is well understood, measurements of static quantities (e.q. hydrogen pressure inside the spheres) as well as dynamic properties (e.g. diffusion rate of hydrogen through glass) are still difficult to handle due to the small size of the spheres (d≈15μm). For diffusion rate measurements, the long-term stability of the experiment is also mandatory due to the relatively slow diffusion rate. In this work, we present an accurate and long-term stable measurement technique for static and dynamic properties, using neutron radiography. Furthermore, possible applications for hydrogen filled microspheres within the scope of radiation issues are discussed.

  1. Optical Microspherical Resonators for Biomedical Sensing

    Directory of Open Access Journals (Sweden)

    Giancarlo C. Righini

    2011-01-01

    Full Text Available Optical resonators play an ubiquitous role in modern optics. A particular class of optical resonators is constituted by spherical dielectric structures, where optical rays are total internal reflected. Due to minimal reflection losses and to potentially very low material absorption, these guided modes, known as whispering gallery modes, can confer the resonator an exceptionally high quality factor Q, leading to high energy density, narrow resonant-wavelength lines and a lengthy cavity ringdown. These attractive characteristics make these miniaturized optical resonators especially suited as laser cavities and resonant filters, but also as very sensitive sensors. First, a brief analysis is presented of the characteristics of microspherical resonators, of their fabrication methods, and of the light coupling techniques. Then, we attempt to overview some of the recent advances in the development of microspherical biosensors, underlining a number of important applications in the biomedical field.

  2. 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.

  3. Dextran: Influence of Molecular Weight in Antioxidant Properties and Immunomodulatory Potential

    Directory of Open Access Journals (Sweden)

    Vinicius C. Soeiro

    2016-08-01

    Full Text Available Dextrans (α-d-glucans extracted from Leuconostoc mesenteroides, with molecular weights (MW of 10 (D10, 40 (D40 and 147 (D147 kDa, were evaluated as antioxidant, anticoagulant and immunomodulatory drugs for the first time. None presented anticoagulant activity. As for the antioxidant and immunomodulatory tests, a specific test showed an increase in the dextran activity that was proportional to the increase in molecular weight. In a different assay, however, activity decreased or showed no correlation to the MW. As an example, the reducing power assay showed that D147 was twice as potent as other dextrans. On the other hand, all three samples showed similar activity (50% when it came to scavenging the OH radical, whereas only the D10 sample showed sharp activity (50% when it came to scavenging the superoxide ion. D40 was the single dextran that presented with immunomodulatory features since it stimulated the proliferation (~50% of murine macrophages (RAW 264.7 and decreased the release of nitric oxide (~40% by the cells, both in the absence and presence of lipopolysaccharides (LPS. In addition, D40 showed a greater scavenging activity (50% for the hydrogen peroxide, which caused it to also be the more potent dextran when it came to inhibiting lipid peroxidation (70%. These points toward dextrans with a 40 kDa weight as being ideal for antioxidant and immunomodulatory use. However, future studies with the D40 and other similarly 40 kDa dextrans are underway to confirm this hypothesis.

  4. Sputter coating of microspherical substrates by levitation

    Science.gov (United States)

    Lowe, A.T.; Hosford, C.D.

    Microspheres are substantially uniformly coated with metals or nonmetals by simltaneously levitating them and sputter coating them at total chamber pressures less than 1 torr. A collimated hole structure comprising a parallel array of upwardly projecting individual gas outlets is machined out to form a dimple. Glass microballoons,, which are particularly useful in laser fusion applications, can be substantially uniformly coated using the coating method and apparatus.

  5. Growth inhibition of human melanoma tumor cells by the combination of sodium phenylacetate (NaPA) and substituted dextrans and one NaPA-dextran conjugate.

    Science.gov (United States)

    Gervelas, C; Avramoglou, T; Crépin, M; Jozefonvicz, J

    2002-01-01

    We have studied the cytostatic effects of sodium phenylacetate (NaPA) in association with several substituted dextrans on human tumor melanoma 1205LU cells. We show that NaPA alone inhibits the growth of these cells (IC50 = 3.9 mM) while a weak inhibitory effect appears at a concentration of 37 microM (10 microg/ml) for a dextran methyl carboxylate benzylamide (LS17-DMCB). The precursors of LS17-DMCB [T40 Dextran and carboxymethyl dextran (LS17-DMC)] did not affect the growth of 1205LU cells. To potentiate the inhibitory activity of NaPA at low concentrations (below 5.6 mM), we have tested NaPA and LS17-DMCB in physical mixture (association) or linked together covalently (this conjugate is termed 'LS17-NaPaC'). We have observed an increase of the 1205LU cell growth inhibition effect with NaPA in association (IC50 1.8 mM). For a concentration of 5 mM of NaPA (free in the case of association or linked in the case of conjugate), the association with dextran derivative exhibits a 4.6-fold higher efficacy than with NaPA alone (9 versus 41% surviving fraction), while the conjugate is 1.3-fold smaller (52% growth inhibition). By performing isobologram analysis of the IC50 data, we have shown a synergistic effect for a particular molar ratio of NaPA and LS17-DMCB (NaPA:LS17-DMCB = 0.35).

  6. Correlation between UV-VIS spectra and the structure of Cu(II) complexes with hydrogenated dextran in alkaline solutions

    OpenAIRE

    Nikolić Goran S.; Cakić Milorad D.; Mitić Žarko J.; Nikolić Ružica S.; Ilić Ljubomir A.

    2005-01-01

    UV-VIS spectrophotometric investigations of Cu(II) complexes with hydroge-nated dextran showed that the complexation of Cu(II)-ions began at pH > 7. The formation of Cu(II) complexes with dextran monomer units was observed at pH 7-12. With further increase in solution pH > 12, the Cu(II)-dextran complex decomposed to Cu(OH)42~-ions and dextran. With increasing solution pH the absorption maximum of complex solutions increased and shifted to shorter wavelength (hypsochromic shift) compare...

  7. Mechanistic analysis of triamcinolone acetonide release from PLGA microspheres as a function of varying in vitro release conditions.

    Science.gov (United States)

    Doty, Amy C; Zhang, Ying; Weinstein, David G; Wang, Yan; Choi, Stephanie; Qu, Wen; Mittal, Sachin; Schwendeman, Steven P

    2017-04-01

    In vitro tests for controlled release PLGA microspheres in their current state often do not accurately predict in vivo performance of these products during formulation development. Here, we introduce a new mechanistic and multi-phase approach to more clearly understand in vitro-in vivo relationships, and describe the first "in vitro phase" with the model drug, triamcinolone acetonide (Tr-A). Two microsphere formulations encapsulating Tr-A were prepared from PLGAs of different molecular weights and end-capping (18kDa acid-capped and 54kDa ester-capped). In vitro release kinetics and the evidence for controlling mechanisms (i.e., erosion, diffusion, and water-mediated processes) were studied in four release media: PBST pH 7.4 (standard condition), PBST pH 6.5, PBS+1.0% triethyl citrate (TC), and HBST pH 7.4. The release mechanism in PBST was primarily polymer erosion-controlled as indicated by the similarity of release and mass loss kinetics. Release from the low MW PLGA was accelerated at low pH due to increased rate of hydrolysis and in the presence of the plasticizer TC due to slightly increased hydrolysis and much higher diffusion in the polymer matrix. TC also increased release from the high MW PLGA due to increased hydrolysis, erosion, and diffusion. This work demonstrates how in vitro conditions can be manipulated to change not only rates of drug release from PLGA microspheres but also the mechanism(s) by which release occurs. Follow-on studies in the next phases of this approach will utilize these results to compare the mechanistic data of the Tr-A/PLGA microsphere formulations developed here after recovery of microspheres in vivo. This new approach based on measuring mechanistic indicators of release in vitro and in vivo has the potential to design better, more predictive in vitro release tests for these formulations and potentially lead to mechanism-based in vitro-in vivo correlations. Copyright © 2016. Published by Elsevier B.V.

  8. Yttrium-90 microsphere induced gastrointestinal tract ulceration

    Directory of Open Access Journals (Sweden)

    Rikabi Ali A

    2008-09-01

    Full Text Available Abstract Background Radiomicrosphere therapy (RT utilizing yttrium-90 (90Y microspheres has been shown to be an effective regional treatment for primary and secondary hepatic malignancies. We sought to determine a large academic institution's experience regarding the extent and frequency of gastrointestinal complications. Methods Between 2004 and 2007, 27 patients underwent RT for primary or secondary hepatic malignancies. Charts were subsequently reviewed to determine the incidence and severity of GI ulceration. Results Three patients presented with gastrointestinal bleeding and underwent upper endoscopy. Review of the pretreatment angiograms showed normal vascular anatomy in one patient, sclerosed hepatic vasculature in a patient who had undergone prior chemoembolization in a second, and an aberrant left hepatic artery in a third. None had undergone prophylactic gastroduodenal artery embolization. Endoscopic findings included erythema, mucosal erosions, and large gastric ulcers. Microspheres were visible on endoscopic biopsy. In two patients, gastric ulcers were persistent at the time of repeat endoscopy 1–4 months later despite proton pump inhibitor therapy. One elderly patient who refused surgical intervention died from recurrent hemorrhage. Conclusion Gastrointestinal ulceration is a known yet rarely reported complication of 90Y microsphere embolization with potentially life-threatening consequences. Once diagnosed, refractory ulcers should be considered for aggressive surgical management.

  9. Unstirred Water Layer Effects on Biodegradable Microspheres

    Directory of Open Access Journals (Sweden)

    Susan D’Souza

    2015-01-01

    Full Text Available This study explores the mechanistic aspects of in vitro release from biodegradable microspheres with the objective of understanding the effect of the unstirred water layer on polymer degradation and drug release. In vitro drug release experiments on Leuprolide PLGA microspheres were performed under “static” and “continuous” agitation conditions using the “sample and separate” method. At specified time intervals, polymer degradation, mass loss, and drug release were assessed. While molecular weight and molecular number profiles for “static” and “continuous” samples were indistinct, mass loss occurred at a faster rate in “continuous” samples than under “static” conditions. In vitro results describe a fourfold difference in drug release rates between the “continuous” and “static” samples, ascribed to the acceleration of various processes governing release, including elimination of the boundary layer. The findings were confirmed by the fourfold increase in drug release rate when “static” samples were subjected to “continuous” agitation after 11 days. A schema was proposed to describe the complex in vitro release process from biodegradable polymer-drug dosage forms. These experiments highlight the manner in which the unstirred water layer influences drug release from biodegradable microspheres and stress the importance of selecting appropriate conditions for agitation during an in vitro release study.

  10. 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.

  11. STUDIES AND EVALUATION OF COMPRESSED MICROSPHERES

    Directory of Open Access Journals (Sweden)

    Idris Mohamed El-Mahdi

    2016-05-01

    Full Text Available This work was aimed at the use of dissolution testing and similarity factor to assess the level of damage taken by active drug microspheres during compression in tablet dosage form. To achieve that, combinations of suitable excipients were used to protect drug microspheres during compression. The excipients were used in the form of powders, granules or placebo pellets prepared by extrusion-spheronization technology. The excipients were evaluated alone, in combinations and post-compression into compacts.  Preliminary experiments included density, hardness, friability and disintegration on all of the selected excipients. Based on such experiments it was found that the flowability of combination powders was more acceptable than individual excipients. Two combinations of microcrystalline -starch and microcrystalline cellulose -calcium carbonate granules were selected to be compressed with active ketoprofen pellets. In all the combinations used there was a significant amount of damage to drug pellets.  The kinetics of drug release appears to follow the zero-order rate and the rate remained unchanged even when a significant degree of damage to pellets occur. It was found that a high level of excipients is required in order to prepare microspheres as a rapid disintegrating tablet. Citation DOI: 10.21502/limuj.002.01.2016  LIMUJ is licensed under a Creative Commons Attribution 4.0 International License

  12. Custom-Made Microspheres for Optical Tweezers.

    Science.gov (United States)

    Jannasch, Anita; Abdosamadi, Mohammad K; Ramaiya, Avin; De, Suman; Ferro, Valentina; Sonnberger, Aaron; Schäffer, Erik

    2017-01-01

    Due to their high position and force sensitivity and the ability to remotely apply forces and torques, optical tweezers are widely used in diverse fields, such as biology, material science, and physics. Often, small dielectric particles are trapped and used as probes, which for experimental convenience are mostly spherical and composed of silica or polystyrene. The optical properties of these materials together with the microsphere size determine the trapping efficiency, and the position and force resolution. However, using only a single, homogeneous, isotropic, and unstructured material limits the range of trapping properties and thereby the applications of optical tweezers. Here, we show how custom-made microspheres composed of coated high-refractive-index materials-titania and nanodiamonds-and birefringent, liquid crystals extend the range and combination of desired trapping properties. These custom-made microspheres either enable the generation of high forces, a high force or time resolution, or the applications of torques. Custom-made probes expand the range of possible experiments and approaches broadening the scope and applicability of optical tweezers.

  13. ROSIN MICROSPHERES AS TASTE MASKING AGENT IN ORAL DRUG DELIVERY SYSTEM

    Directory of Open Access Journals (Sweden)

    Shery Jacob

    2012-09-01

    Full Text Available Natural resources in general and plant materials in particular are receiving more attention due to their safety as pharmaceutical excipients. Present work assessed the combination potential of natural hydrophobic resin, rosin, and synthetic polymer ethyl cellulose to mask the abhorrent inherent taste of ambroxol hydrochloride, by microencapsulation technique, and its possibility to formulate as a fast dissolving dosage form. Being of natural origin, rosin and its derivatives are biodegradable and biocompatible. Although It has excellent film forming property the native rosin films are brittle and break easily upon handling. The film forming properties of rosin was modified by substituting a part with ethyl cellulose.The prepared rosin-ethyl cellulose composite microspheres by emulsion solvent evaporation technique possessed good sphericity, smooth surface morphology, uniform and narrow size distribution (1090 µm, when analyzed by scanning electron microscopy. PEG 400 was used as plasticizer because of its hydrophilicity, biocompatibility and their excellent plasticizing activity. Method of preparation has influenced the particle size and drug loading efficiency. Drug-polymer compatibility was confirmed by Fourier transform infrared spectroscopy and thin layer chromatography. DSC studies revealed that the drug was molecularly dispersed inside the microspheres in the form of solid solution. Sensory studies in healthy human volunteers indicated that the taste and palatability were significantly improved by microencapsulation. This study demonstrated that rosin could be a right choice in developing patient favored formulations for bitter drugs and can be utilized in fast disintegrating dosage forms as well.

  14. Sustained reduction of intraocular pressure by supraciliary delivery of brimonidine-loaded poly(lactic acid) microspheres for the treatment of glaucoma.

    Science.gov (United States)

    Chiang, B; Kim, Y C; Doty, A C; Grossniklaus, H E; Schwendeman, S P; Prausnitz, M R

    2016-04-28

    Although effective drugs that lower intraocular pressure (IOP) in the management of glaucoma exist, their efficacy is limited by poor patient adherence to the prescribed eye drop regimen. To replace the need for eye drops, in this study we tested the hypothesis that IOP can be reduced for one month after a single targeted injection using a microneedle for administration of a glaucoma medication (i.e., brimonidine) formulated for sustained release in the supraciliary space of the eye adjacent to the drug's site of action at the ciliary body. To test this hypothesis, brimonidine-loaded microspheres were formulated using poly(lactic acid) (PLA) to release brimonidine at a constant rate for 35 days and microneedles were designed to penetrate through the sclera, without penetrating into the choroid/retina, in order to target injection into the supraciliary space. A single administration of these microspheres using a hollow microneedle was performed in the eye of New Zealand White rabbits and was found to reduce IOP initially by 6 mmHg and then by progressively smaller amounts for more than one month. All administrations were well tolerated without significant adverse events, although histological examination showed a foreign-body reaction to the microspheres. This study demonstrates, for the first time, that the highly-targeted delivery of brimonidine-loaded microspheres into the supraciliary space using a microneedle is able to reduce IOP for one month as an alternative to daily eye drops.

  15. Metformin HCl loaded mucoadhesive agar microspheres for sustained release

    Directory of Open Access Journals (Sweden)

    Khokan Bera

    2013-01-01

    Full Text Available In the recent past, a major interest in the control of blood sugar had been targeted to develop plenty of new formulations. The present work aims at the development of a low cost sustained release system of metformin hydrochloride embedded in microspheres of agar (Gelidium cartilagineum to overcome the frequent dosing of the drug. Models were developed with respect to controlling variables (X 1 , drug: Polymer, X 2 , surfactant concentration, and X 3 , pH of phosphate buffer. The most effective levels of parameters were found as X 1 (1 : 2, X 2 (1.25%, X 3 (phosphate buffer pH 7.4. Instrumental analysis (Fourier transforms infra-red spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy, mucoadhesion study, toxicity test and in vivo study were performed with the optimized product. The best batch (A2 exhibited a high drug entrapment efficiency of 84.82 ± 1.23%, swelling index of 3.84 ± 0.38 and 86% of mucoadhesion after 12 h. The in vitro release was also sustained for more than 12 h.

  16. Validation of a cage implant system for assessing in vivo performance of long-acting release microspheres.

    Science.gov (United States)

    Doty, Amy C; Hirota, Keiji; Olsen, Karl F; Sakamoto, Naoya; Ackermann, Rose; Feng, Meihua R; Wang, Yan; Choi, Stephanie; Qu, Wen; Schwendeman, Anna; Schwendeman, Steven P

    2016-12-01

    Here we describe development of a silicone rubber/stainless steel mesh cage implant system, much like that used to assess biocompatibility of biomaterials [1], for easy removal of injectable polymer microspheres in vivo. The sterile cage has a type 316 stainless steel mesh size (38 μm) large enough for cell penetration and free fluid flow in vivo but small enough for microsphere retention, and a silicone rubber shell for injection of the microspheres. Two model drugs, the poorly soluble steroid, triamcinolone acetonide, and the highly water-soluble luteinizing hormone-releasing hormone (LHRH) peptide superagonist, leuprolide, were encapsulated in PLGA microspheres large enough (63-90 μm) to be restrained by the cage implant in vivo. The in vitro release from both formulations was followed by ultra-performance liquid chromatography (UPLC) with and without the cage in a standard release media, PBS pH 7.4 + 0.02% Tween 80 + 0.05% sodium azide, at 37 °C. Pharmacokinetics (PK) in rats was assessed after SC injection or SC in-cage implantation of microspheres with plasma analysis by LC-MS/MS or EIA. Tr-A and leuprolide in vitro release was largely unaffected after the initial burst irrespective of the cage or test tube incubation vessel and release was much slower than observed in vivo for both drugs. Moreover, Tr-A and leuprolide pharmacokinetics with and without the cage were highly similar during the 2-3 week release duration before a significant inflammatory response was caused by the cage implant. Hence, the PK-validated cage implant provides a simple means to recover and evaluate the microsphere drug carriers in vivo during a time window of at least a few weeks in order to characterize the polymer microsphere release and erosion behavior in vivo. This approach may facilitate development of mechanism-based in vitro/in vivo correlations and enable development of more accurate and useful in vitro release tests. Copyright © 2016 Elsevier Ltd. All

  17. Antiviral activity of derivatized dextrans on HIV-1 infection of primary macrophages and blood lymphocytes.

    Science.gov (United States)

    Seddiki, N; Mbemba, E; Letourneur, D; Ylisastigui, L; Benjouad, A; Saffar, L; Gluckman, J C; Jozefonvicz, J; Gattegno, L

    1997-11-28

    The present study demonstrates at the molecular level that dextran derivatives carboxymethyl dextran benzylamine (CMDB) and carboxymethyl dextran benzylamine sulfonate (CMDBS), characterized by a statistical distribution of anionic carboxylic groups, hydrophobic benzylamide units, and/or sulfonate moieties, interact with HIV-1 LAI gp120 and V3 consensus clades B domain. Only limited interaction was observed with carboxy-methyl dextran (CMD) or dextran (D) under the same conditions. CMDBS and CMDB (1 microM) strongly inhibited HIV-1 infection of primary macrophages and primary CD4+ lymphocytes by macrophage-tropic and T lymphocyte-tropic strains, respectively, while D or CMD had more limited effects on M-tropic infection of primary macrophages and exert no inhibitory effect on M- or T-tropic infection of primary lymphocytes. CMDBS and CMDB (1 microM) had limited but significant effect on oligomerized soluble recombinant gp120 binding to primary macrophages while they clearly inhibit (> 50%) such binding to primary lymphocytes. In conclusion, the inhibitory effect of CMDB and the CMDBS, is observed for HIV M- and T-tropic strain infections of primary lymphocytes and macrophages which indicates that these compounds interfere with steps of HIV replicative cycle which neither depend on the virus nor on the cell.

  18. Induction heating studies of dextran coated MgFe2O4 nanoparticles for magnetic hyperthermia.

    Science.gov (United States)

    Khot, V M; Salunkhe, A B; Thorat, N D; Ningthoujam, R S; Pawar, S H

    2013-01-28

    MgFe(2)O(4) nanoparticles with sizes around 20 nm have been prepared by a combustion method and functionalized with dextran for their possible applications in magnetic particle hyperthermia. The induction heating study of these nanoparticles at different magnetic field amplitudes, from 6.7 kA m(-1) to 26.7 kA m(-1), showed self-heating temperature rise up to 50.25 °C and 73.32 °C (at 5 mg mL(-1) and 10 mg mL(-1) concentrations in water respectively) which was primarily thought to be due to hysteresis losses activated by an AC magnetic field. The dextran coated nanoparticles showed a maximum specific absorption rate (SAR) of about 85.57 W g(-1) at 26.7 kA m(-1) (265 kHz). Dextran coated nanoparticles at concentrations below 1.8 mg mL(-1) exhibit good viability above 86% on mice fibroblast L929 cells. The results suggest that combustion synthesized MgFe(2)O(4) nanoparticles coated with dextran can be used as potential heating agents in magnetic particle hyperthermia. Uncoated and dextran coated samples were characterized by X-ray diffraction (XRD), transmission electron microscopy (TEM) and vibrating sample magnetometry (VSM), Fourier transform infrared spectroscopy (FTIR), thermogravimetric-differential thermal analysis (TG-DTA) and zeta potential-DLS studies.

  19. Effect of dextran 500 on radial migration of erythrocytes in postcapillary venules at low flow rates.

    Science.gov (United States)

    Kim, Sangho; Ong, Peng Kai; Johnson, Paul C

    2009-06-01

    Recently, we reported that collision efficiency (fraction of total collisions that result in the formation of aggregates) between red blood cells was an important factor in the formation of aggregates in postcapillary venules. In the present study, we focus on how high molecular weight dextran influences the overall radial migration trend of red blood cells in the postcapillary venule along a longitudinal distance of 50 microm from the bifurcation which would in turn affect collision behavior of these cells. A radial migration index, which defines the extent of radial migration of individual cells relative to the vessel center, was found to have a larger magnitude after infusion of dextran (1.9 +/- 2.73) compared to that before dextran infusion (1.48 +/- 3.89). This implied that dextran-induced aggregation might provide an external force to actively move cells towards the centerline of the vessel, which could contribute to the greater number of red blood cells participating in collision (16% increase) and aggregate formation. Further analysis of the collision behavior of individual red blood cells revealed that collision frequencies of individual cells decreased from a wide range (1 to 14) to a narrow range (1 to 5) after dextran treatment, indicating the alteration of collision behavior of red blood cells by the presence of aggregates along the flow stream.

  20. Fusion and infection of influenza and Sendai viruses as modulated by dextran sulfate: a comparative study.

    Science.gov (United States)

    Ramalho-Santos, J; de Lima, M C

    2001-06-01

    We have directly compared the effect of two types of dextran sulfate with distinct molecular weights (500 kDa and 5 kDa) on the fusion activity and infectivity of both Sendai and influenza viruses, two lipid-enveloped viruses that differ in their routes of entry into target cells. To correlate membrane merging and infectivity MDCK cells were used as targets for the viruses in both approaches. In either case pronounced inhibition of virus-cell interactions by dextran sulfate was only observed at low pH, even though Sendai virus fuses maximally at pH 7.4. Although membrane merging could not be fully abolished, the inhibitory effect was always greater when the higher molecular weight dextran sulfate was used. The presence of this residual fusion activity, that could not be reduced even with high concentrations of agent, suggests that a limited number of binding sites for dextran sulfate may exist on the viral envelopes. The compounds also inhibited fusion of bound virions, and all results could be reproduced using erythrocyte ghosts as target membranes in the fusion assay, instead of MDCK cells. In agreement with these observations only the infectivity of influenza virus (which requires a low pH-dependent step to enter target cells) was affected by dextran sulfate, again the higher molecular weight compound showing a more pronounced inhibitory effect.

  1. Effect of dextran and dextran sulfate on the structural and rheological properties of model acid milk gels.

    Science.gov (United States)

    Pachekrepapol, U; Horne, D S; Lucey, J A

    2015-05-01

    Various types of polysaccharides are widely used in cultured dairy products. However, the interaction mechanisms, between milk proteins and these polysaccharides, are not entirely clear. To explore the interactions between uncharged and charged polysaccharides and the caseins, we used a model acid-milk-gel system, which allowed acidification to occur separately from gelation. The effect of adding uncharged dextran (DX; molecular weight ~2.0×10(6) Da) and negatively charged dextran sulfate (DS; molecular weight ~1.4×10(6) Da) to model acid milk gels was studied. Two concentrations (0.075 and 0.5%, wt/wt) of DX or DS were added to cold milk (~0°C) that had been acidified to pH values 4.4, 4.6, 4.8, or 4.9. Acidified milks containing DX or DS were then quiescently heated at the rate of 0.5°C/min to 30°C, which induced gelation, and gels were then held at 30°C for 17 h to facilitate gel development. Dynamic small-amplitude-oscillation rheology and large-deformation (shear) tests were performed. Microstructure of gels was examined by fluorescence microscopy. Gels made with a high concentration of DX gelled at a lower temperature, but after 17 h at 30°C, these gels exhibited lower storage moduli and lower yield-stress values. At pH 4.8 or 4.9 (pH values greater than the isoelectric point of caseins), addition of 0.5% DS to acidified milk resulted in lower gelation temperature. At pH 4.4 (pH values less than the isoelectric point of caseins), addition of 0.5% DS to acidified milk resulted in gels with very high stiffness values. Gels made at pH 4.8 or 4.9 with both concentrations of DS had much lower stiffness and yield-stress values than control gels. Microstructural analysis indicated that gels made at pH 4.4 with the addition of 0.5% DX exhibited large protein strands and pores, whereas gels made with 0.075% DX or the control gels had a finer protein matrix. At higher pH values (>4.4), gels made with 0.5% DX had a finer structure. At all pH values, gels made

  2. Performance Evaluation of Mucoadhesive Potential of Sodium Alginate on Microspheres Containing an Anti-Diabetic Drug: Glipizide

    Directory of Open Access Journals (Sweden)

    Yaswanth Allamneni

    2012-04-01

    Full Text Available The objective of the present investigation was to design mucoadhesive microspheres to achieve a substantial increase in length of stay of the drug in the GI tract of glipizide for treatment of type 2 diabetes mellitus. Glipizide is a second-generation sulfonylurea derivative used for the treatment of type II diabetes. Its short biological half-life (0.3 ± 0.7 h necessitates the need to be administered in two or three doses of 2.5-10 mg per day. Mucoadhesive microsphere exhibit a prolonged residence time at the site of application and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved or better therapeutic performance of drug. It would, therefore be advantageous to have means for providing an intimate contact of the drug delivery system with the absorbing membranes. In the present study, alginate based mucoadhesive microspheres of were prepared by ionotropic external gelation technique utilizing calcium chloride (CaCl2 as a cross linking agent, to take the advantage of swelling and mucoadhesive property of alginate beads for improving the oral delivery of glipizide. Interaction studies performed using FTIR spectroscopy and DSC revealed that there was no drug to polymer interactions. The prepared microspheres are discrete, spherical and free flowing which was characterized by entrapment efficiency, particle size, micromeritic properties, in-vitro release behavior, scanning electron microscopy (SEM, in-vitro wash off test etc. Depending upon the variability in the concentration of sodium alginate, time of cross linking agent, the factors like particle size, and incorporation efficiency and release rate and mucoadhesion properties of microspheres varies. It was observed that increasing the polymer concentration along with the cross-linking time given the better affect on microspheres characteristic and percentage release of drug. Formulation F8 containing 5% w/v sodium alginate was selected as best

  3. MAGNETIC MICROSPHERES: A LATEST APPROACH IN NOVEL DRUG DELIVERY SYSTEM

    Directory of Open Access Journals (Sweden)

    Mukherjee S

    2012-10-01

    Full Text Available Magnetic microspheres are at the forefront of the rapidly developing field of pharmaceutical technology with several potential applications in drug delivery, clinical medicine and research as well as in other varied sciences. Due to their unique size-dependent properties, magnetic microspheres offer the possibility to develop new therapeutics. The ability to incorporate drugs into carriers offers a new prototype in drug delivery that could be used for secondary and tertiary levels of drug targeting. Hence, magnetic microspheres hold great promise for reaching the goal of controlled and site specific drug delivery and hence have attracted wide attention of researchers. This review presents a broad treatment of magnetic microspheres discussing their advantages, limitations and their possible remedies. Different production methods which are suitable for large scale production and applications of magnetic microspheres are described. Appropriate analytical techniques for characterization of magnetic microspheres like Photon correlation spectroscopy, scanning electron microscopy, differential scanning calorimetry are highlighted. Aspects of magnetic microspheres route of administration and their biodistribution are also incorporated. If appropriately investigated, magnetic microspheres may open new vistas in therapy of complex diseases.

  4. 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

  5. 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

    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

  6. Preparation and characterization of albumin-heparin microspheres

    NARCIS (Netherlands)

    Cremers, H.F.M.; Kwon, G.; Bae, Y.H.; Kim, S.W.; Verrijk, R.; Noteborn, H.P.J.M.; Feijen, J.

    1994-01-01

    Albumin-heparin microspheres were prepared by a two-step process which involved the preparation of a soluble albumin-heparin conjugate, followed by formation of microspheres from this conjugate or by a double cross-linking technique involving both coupling of soluble albumin and heparin and microsph

  7. Pectin/zein microspheres as a sustained drug delivery system

    Science.gov (United States)

    A series of microspheres were prepared from pectins and corn proteins from various sources in the presence of the divalent ions calcium or zinc. The results showed that the yield of microsphere and the efficiency of drug incorporation were dependent on the type and ratio of biopolymers, the size of ...

  8. 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.

  9. Design and Fabrication of Superparamaganitic Hybrid Microspheres for Protein Immobilization

    Institute of Scientific and Technical Information of China (English)

    REN Qi; CHU Hong; CHEN Mingqing; NI Zhongbin; CHEN Qiuyun

    2011-01-01

    Superparamagnetic poly(styrene)-co-poly(2-acrylanmido-2-methyl propanesulfonic acid) (PStco-PAMPS) and poly(methylmethacrylate)-co-poly(glycidyl methacrylate) (PMMA-co-PGMA) microspheres with mean size of 170 nm were prepared by emulsion polymerization in the presence of oleic acid-coated Fe3O4 nanoparticles.The structures,morphologies,diameter and diameter distribution of the as-prepared microspheres were identified by Fourier transform infrared spectroscopy (FT-IR) and transmission electron microscopy (TEM).The saturation magnetizations of PSt-co-PAMPS and PMMA-co-PGMA microspheres are 21.94 and 25.07emu/g,respectively.The as-synthesized magnetic microspheres were used for immobilization of Bovine serum albumin (BSA) by physical interaction and covalent interaction respectively.The equilibrium amount of BSA immobilized onto PMMA-co-PGMA microspheres was 86.48 mg/g microspheres in 90 min,while on PSt-coPAMPS microspheres was 59.62 mg/g microspheres in 120 min.

  10. 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.

  11. Coacervate droplets, proteinoid microspheres, and the genetic apparatus

    Science.gov (United States)

    Fox, S. W.

    1974-01-01

    Differences between typical coacervate droplets and typical proteinoid microspheres are examined. It is pointed out that coacervate droplets are produced from polymers obtained from contemporary organisms. The microspheres considered are aggregates of proteinoid formed from monomeric amino acids under geologically relevant conditions. Aspects regarding the primordial sequence are discussed along with the origin of the genetic apparatus and the genetic code.

  12. Surface wrinkling on polydimethylsiloxane microspheres via wet surface chemical oxidation.

    Science.gov (United States)

    Yin, Jian; Han, Xue; Cao, Yanping; Lu, Conghua

    2014-07-16

    Here we introduce a simple low-cost yet robust method to realize spontaneously wrinkled morphologies on spherical surfaces. It is based on surface chemical oxidation of aqueous-phase-synthesized polydimethylsiloxane (PDMS) microspheres in the mixed H2SO4/HNO3/H2O solution. Consequently, curvature and overstress-sensitive wrinkles including dimples and labyrinth patterns are successfully induced on the resulting oxidized PDMS microspheres. A power-law dependence of the wrinkling wavelength on the microsphere radius exists. The effects of experimental parameters on these tunable spherical wrinkles have been systematically investigated, when the microspheres are pre-deposited on a substrate. These parameters include the radius and modulus of microspheres, the mixed acid solution composition, the oxidation duration, and the water washing post-treatment. Meanwhile, the complicated chemical oxidation process has also been well studied by in-situ optical observation via the microsphere system, which represents an intractable issue in a planar system. Furthermore, we realize surface wrinkled topographies on the whole microspheres at a large scale, when microspheres are directly dispersed in the mixed acid solution for surface oxidation. These results indicate that the introduced wet surface chemical oxidation has the great potential to apply to other complicated curved surfaces for large-scale generation of well-defined wrinkling patterns, which endow the solids with desired physical properties.

  13. 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.

  14. 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.

  15. Resolution enhancement phase-contrast imaging by microsphere digital holography

    Science.gov (United States)

    Wang, Yunxin; Guo, Sha; Wang, Dayong; Lin, Qiaowen; Rong, Lu; Zhao, Jie

    2016-05-01

    Microsphere has shown the superiority of super-resolution imaging in the traditional 2D intensity microscope. Here a microsphere digital holography approach is presented to realize the resolution enhancement phase-contrast imaging. The system is designed by combining the microsphere with the image-plane digital holography. A microsphere very close to the object can increase the resolution by transforming the object wave from the higher frequency to the lower one. The resolution enhancement amplitude and phase images can be retrieved from a single hologram. The experiments are carried on the 1D and 2D gratings, and the results demonstrate that the observed resolution has been improved, meanwhile, the phase-contrast image is obtained. The proposed method can improve the transverse resolution in all directions based on a single exposure. Furthermore, this system has extended the application of the microsphere from the conventional 2D microscopic imaging to 3D phase-contrast microscopic imaging.

  16. 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.

  17. IT Supporting Strategy Formulation

    NARCIS (Netherlands)

    Achterbergh, J.M.I.M.

    2005-01-01

    This overview approaches information and communication technology (ICT) for competitive intelligence from the perspective of strategy formulation. It provides an ICT architecture for supporting the knowledge processes producing relevant knowledge for strategy formulation. To determine what this arch

  18. IT Supporting Strategy Formulation

    NARCIS (Netherlands)

    Achterbergh, J.M.I.M.

    2005-01-01

    This overview approaches information and communication technology (ICT) for competitive intelligence from the perspective of strategy formulation. It provides an ICT architecture for supporting the knowledge processes producing relevant knowledge for strategy formulation. To determine what this arch

  19. Labelling of silica microspheres with fluorescent lanthanide-doped LaF{sub 3} nanocrystals

    Energy Technology Data Exchange (ETDEWEB)

    Zhang Yong [Division of Bioengineering, Faculty of Engineering, National University of Singapore, 117576, Singapore (Singapore); Lu Meihua [Division of Bioengineering, Faculty of Engineering, National University of Singapore, 117576, Singapore (Singapore)

    2007-07-11

    Fluorescent microspheres have been demonstrated to be useful in a variety of biological applications. Fluorescent silica or polymer microspheres have been produced by incorporation of chromophores into the microspheres, which usually produces microspheres with nonuniform sizes and reduced fluorescence. Here we present a simple and straightforward method to produce silica microspheres with fluorescent lanthanide-doped LaF{sub 3} nanocrystals grown on the surface. LaF{sub 3} nanocrystals are in situ grown on silica microspheres of different sizes to form a raspberry-like structure. The microspheres exhibit strong fluorescence and the colour could be altered by changing the lanthanide ions doped in LaF{sub 3} nanocrystals.

  20. Hypertonic Saline Dextran Ameliorates Organ Damage in Beagle Hemorrhagic Shock.

    Directory of Open Access Journals (Sweden)

    Jing-xiang Zhao

    Full Text Available The goal of this study was to investigate the effect of hypertonic saline with 6% Dextran-70 (HSD resuscitation on organ damage and the resuscitation efficiency of the combination of HSD and lactated ringers (LR in a model of hemorrhage shock in dogs.Beagles were bled to hold their mean arterial pressure (MAP at 50 ± 5 mmHg for 1 h. After hemorrhage, beagles were divided into three groups (n = 7 to receive pre-hospital resuscitation for 1 h (R1: HSD (4 ml/kg, LR (40 ml/kg, and HSD+LR (a combination of 4 ml/kg HSD and 40 ml/kg LR. Next, LR was transfused into all groups as in-hospital resuscitation (R2. After two hours of observation (R3, autologous blood was transfused. Hemodynamic responses and systemic oxygenation were measured at predetermined phases. Three days after resuscitation, the animals were sacrificed and tissues including kidney, lung, liver and intestinal were obtained for pathological analysis.Although the initial resuscitation with HSD was shown to be faster than LR with regard to an ascending MAP, the HSD group showed a similar hemodynamic performance compared to the LR group throughout the experiment. Compared with the LR group, the systemic oxygenation performance in the HSD group was similar but showed a lower venous-to-arterial CO2 gradient (Pv-aCO2 at R3 (p < 0.05. Additionally, the histology score of the kidneys, lungs and liver were significantly lower in the HSD group than in the LR group (p < 0.05. The HSD+LR group showed a superior hemodynamic response but higher extravascular lung water (EVLW and lower arterial oxygen tension (PaO2 than the other groups (p < 0.05. The HSD+LR group showed a marginally improved systemic oxygenation performance and lower histology score than other groups.Resuscitation after hemorrhagic shock with a bolus of HSD showed a similar hemodynamic response compared with LR at ten times the volume of HSD, but HSD showed superior efficacy in organ protection. Our findings suggest that

  1. Coagulation competence for predicting perioperative hemorrhage in patients treated with lactated Ringer's vs. Dextran

    DEFF Research Database (Denmark)

    Rasmussen, Kirsten C; Højskov, Michael; Johansson, Per Ingemar

    2015-01-01

    BACKGROUND: Perioperative hemorrhage may depend on coagulation competence and this study evaluated the influence of coagulation competence on blood loss during cystectomy due to bladder cancer. METHODS: Forty patients undergoing radical cystectomy were included in a randomized controlled trial...... to receive either lactated Ringer's solution or Dextran 70 (Macrodex ®) that affects coagulation competence. RESULTS: By thrombelastography evaluated coagulation competence, Dextran 70 reduced "maximal amplitude" (MA) by 25 % versus a 1 % reduction with the administration of lactated Ringer's solution (P ....001). Blinded evaluation of the blood loss was similar in the two groups of patients - 2339 ml with the use of Dextran 70 and 1822 ml in the lactated Ringer's group (P = 0.27). Yet, the blood loss was related to the reduction in MA (r = -0.427, P = 0.008) and by multiple regression analysis independently...

  2. Microwire formation based on dielectrophoresis of electroless gold plated polystyrene microspheres

    Institute of Scientific and Technical Information of China (English)

    Jiang Hong-Yuan; Ren Yu-Kun; Tao Ye

    2011-01-01

    Microspheres coated with a perfectly conductive surface have many advantages in the applications of biosensors and micro-electromechanical systems. Polystyrene microspheres with the diameter of 10 μm were coated with a 50 nmthick gold layer using an electroless gold plating approach. Dielectrophoresis (DEP) for bare microspheres and shelled microspheres was theoretically analysed and the real part of the Clausius-Mossotti factor was calculated for the two kinds of microspheres. The experiments on the dielectrophoretic characterisation of the uncoated polystyrene microspheres and gold coated polystyrene microspheres (GCPMs) were carried out. Experimental results showed that the gold coated polystyrene microspheres were only acted by a positive dielectrophoretic force when the frequency was below 40M Hz,while the uncoated polystyrene microspheres were governed by a negative dielectrophoretic force in this frequency range.The gold coated polystyrene microspheres were exploited to form the microwire automatically according to their stable dielectrophoretic and electric characterisations.

  3. Torsion formulation of gravity

    Energy Technology Data Exchange (ETDEWEB)

    Lledo, M A; Sommovigo, L, E-mail: Maria.Lledo@ific.uv.e, E-mail: Luca.Sommovigo@mfn.unipmn.i [Departament de Fisica Teorica, Universitat de Valencia, and IFIC (Centro mixto CSIC-UVEG) C/Dr Moliner, 50, E-46100 Burjassot (Valencia) (Spain)

    2010-03-21

    We explain precisely what it means to have a connection with torsion as a solution of the Einstein equations. While locally the theory remains the same, the new formulation allows for topologies that would have been excluded in the standard formulation of gravity. In this formulation it is possible to couple arbitrary torsion to gauge fields without breaking the gauge invariance.

  4. Morphological alterations of exogenous surfactant inhibited by meconium can be prevented by dextran

    Directory of Open Access Journals (Sweden)

    Stichtenoth Guido

    2006-06-01

    Full Text Available Abstract Background Surfactant dysfunction due to inhibition is involved in the pathophysiology of meconium aspiration syndrome. Dextran addition has been shown to reverse exogenous surfactant inactivation by meconium, but the precise mechanisms and the morphological correlate of this effect are yet unknown. Morphological surfactant analysis by transmission electron microscopy (TEM and stereology allows the differentiation of active (large aggregates = LA and inactive (small aggregates = SA subtypes. Methods To determine the in vitro effects of meconium and dextran addition on the morphology of a modified porcine natural surfactant (Curosurf, Curosurf samples were either incubated alone or together with meconium or with meconium and dextran, fixed and processed for TEM. Volume fractions of surfactant subtypes [lamellar body-like forms (LBL, multilamellar vesicles (MV, unilamellar vesicles (UV] were determined stereologically. Results All preparations contained LBL and MV (corresponding to LA as well as UV (corresponding to SA. The volume fraction of UV increased with addition of meconium and decreased with further addition of dextran. Correspondingly, the UV/(LBL+MV ratio (resembling the SA/LA ratio increased when meconium was added and decreased when dextran was added to the surfactant-meconium mixture. Conclusion Meconium causes alterations in the ultrastructural composition of Curosurf that can be visualized and analyzed by TEM and stereology. These alterations resemble an increase in the SA/LA ratio and are paralleled by an increase in minimum surface tension. Dextran prevents these effects and may therefore be a useful additive to exogenous surfactant preparations to preserve their structural and functional integrity, thereby improving their resistance to inactivation.

  5. Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper–Lin small composite design

    Directory of Open Access Journals (Sweden)

    El-Say KM

    2016-02-01

    Full Text Available Khalid Mohamed El-Say1,2 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt Abstract: This study was aimed at developing a controlled-release cetirizine hydrochloride (CTZ-loaded polymethacrylate microsphere by optimization technique using software-based response surface methodology. The emulsion solvent evaporation method was utilized in the preparation of microspheres. Four process variables were selected, namely, Eudragit RLPO loading percentage in total polymer, the emulsifier hydrophilic lipophilic balance (HLB, the antitacking percentage, and the dispersed phase volume. The desired responses were particle size, angle of repose, production yield, encapsulation efficiency, loading capacity, initial drug release, and the time for 85% of drug release from the microspheres. Optimization was carried out by fitting the experimental data to the software program (Statgraphics Centurion XV. Moreover, 18 batches were subjected to various characterization tests required for the production of dosage form. The pharmacokinetic parameters were evaluated after the oral administration of 10 mg CTZ in both optimized formulation and commercial product on healthy human volunteers using a double-blind, randomized, cross-over design. The optimized formulation showed satisfactory yield (84.43% and drug encapsulation efficiency (87.1%. Microspheres were of spherical shape, smooth surface, and good flowability with an average size of 142.3 µm. The developed optimized batch of microspheres ensured 28.87% initial release after 2 hours, and the release of CTZ extended for >12 hours. In addition, the relative bioavailability of the optimized formulation was 165.5% with respect to the marketed CTZ tablets indicating a significant enhancement of CTZ bioavailability. Thus

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

    Energy Technology Data Exchange (ETDEWEB)

    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.

  7. Synthesis and Characterization of Graft Copolymer of Dextran and 2-Acrylamido-2-methylpropane Sulphonic Acid

    Directory of Open Access Journals (Sweden)

    Venkanna Azmeera

    2012-01-01

    Full Text Available A novel biodegradable graft copolymer of dextran (Dx and 2-acrylamido-2-methyl-1-propane sulphonic acid (AMPS was synthesized by grafting poly-AMPS chains onto dextran backbone by free radical polymerization using ceric ammonium nitrate (CAN as an initiator. Different amounts of AMPS were used to synthesize four different grades of graft copolymers with different side chain lengths. These grafted polymers were characterized by elemental analysis, FTIR, 1HNMR, rheological technique, scanning electron microscopy (SEM, thermogravimetric analysis (TGA, and X-ray diffractometry (XRD. They exhibited efficient flocculation performance in kaolin suspension.

  8. Camomile autofermentation in polyethylene glycol/dextran two-phase system

    Directory of Open Access Journals (Sweden)

    Đaković Sanja D.

    2008-01-01

    Full Text Available The objective of this study was the investigation of the extractive bioconversion of apigenin-7-O-β-glucoside in camomile ligulate flowers into apigenin by autofermentation in polyethylene glycol 6000/dextran 200000 two-phase system. In 22.5% polyethylene glycol/14% dextran aqueous two-phase system the obtained yield of apigenin in the top phase was 96.5%. In the presence of plant material that partiotioned to the interphase, the yield of apigenin in the top phase was 3.5 times higher in comparison to the model system.

  9. Rye bran as fermentation matrix boosts in situ dextran production by Weissella confusa compared to wheat bran.

    Science.gov (United States)

    Kajala, Ilkka; Mäkelä, Jari; Coda, Rossana; Shukla, Shraddha; Shi, Qiao; Maina, Ndegwa Henry; Juvonen, Riikka; Ekholm, Päivi; Goyal, Arun; Tenkanen, Maija; Katina, Kati

    2016-04-01

    The consumption of fiber-rich foods such as cereal bran is highly recommended due to its beneficial health effects. Pre-fermentation of bran with lactic acid bacteria can be used to improve the otherwise impaired flavor and textural qualities of bran-rich products. These positive effects are attributed to enzymatic modification of bran components and the production of functional metabolites like organic acids and exopolysaccharides such as dextrans. The aim of this study was to investigate dextran production in wheat and rye bran by fermentation with two Weissella confusa strains. Bran raw materials were analyzed for their chemical compositions and mineral content. Microbial growth and acidification kinetics were determined from the fermentations. Both strains produced more dextran in rye bran in which the fermentation-induced acidification was slower and the acidification lag phase longer than in wheat bran. Higher dextran production in rye bran is expected to be due to the longer period of optimal pH for dextran synthesis during fermentation. The starch content of wheat bran was higher, which may promote isomaltooligosaccharide formation at the expense of dextran production. W. confusa Cab3 produced slightly higher amounts of dextran than W. confusa VTT E-90392 in all raw materials. Fermentation with W. confusa Cab3 also resulted in lower residual fructose content which has technological relevance. The results indicate that wheat and particularly rye bran are promising matrices for producing technologically significant amounts of dextran, which facilitates the use of nutritionally valuable raw bran in food applications.

  10. Activation of Human Complement System by Dextran-Coated Iron Oxide Nanoparticles Is Not Affected by Dextran/Fe Ratio, Hydroxyl Modifications, and Crosslinking

    DEFF Research Database (Denmark)

    Wang, Guankui; Chen, Fangfang; Banda, Nirmal K

    2016-01-01

    While having tremendous potential as therapeutic and imaging tools, the clinical use of engineered nanoparticles has been associated with serious safety concerns. Activation of the complement cascade and the release of proinflammatory factors C3a and C5a may contribute to infusion-related reactions......, whereas opsonization with C3 fragments promotes rapid recognition and clearance of nanomaterials by mononuclear phagocytes. We used dextran-coated superparamagnetic iron oxide nanoparticles (SPIO), which are potent activators of the complement system, to study the role of nanoparticle surface chemistry...... in inciting complement in human serum. Using complement inhibitors and measuring levels of fluid phase markers (sC5b-9, C5a, and Bb), we found that the majority of human complement activation by SPIO is through the alternative pathways (AP). SPIO prepared with high dextran/iron ratio showed some complement...

  11. Glucose-sensitive gel rheology of dextran-concanavalin A mixtures suitable for self-regulating insulin delivery.

    Science.gov (United States)

    Taylor, M Joan; Tanna, Sangeeta; Sahota, Tarsem S

    2010-01-01

    Aqueous concentrated plain mixtures of dextran and concanavalin A (con A) were examined for their rheological response to glucose for comparison with previously studied partially photopolymerized acrylic derivatives. Non-destructive oscillatory tests were undertaken within the linear viscoelastic range to examine the relationship between the rheometry and the stoichiometry of the interactive materials and to examine rheological parameters as affected by molecular weight, component ratio, temperature and glucose concentrations between 0 and 1% w/w. These simple formulations were studied at 1 and 10 Hz at 0.5% strain at both 20 and 37 degrees C. A second simplified rheological test was undertaken to demonstrate gel-sol reversibility and to produce a measure of equilibria created between these gels and glucose solutions with which they are in contact. This mimics the conditions in which the gel acts as a responsive gateway in the insulin delivery device. It proved that the gels equilibrate with glucose solutions, rather than indiscriminately removing glucose. This is important in terms of producing a delivery device that can respond in a reversible, glucose concentration-dependent manner. The method used for this is capable of relative values only but provides information not obtainable from conventional rheometry.

  12. Biodegradable poly(lactic-co-glycolic acid) microspheres loaded with S-nitroso-N-acetyl-D-penicillamine for controlled nitric oxide delivery.

    Science.gov (United States)

    Lautner, Gergely; Meyerhoff, Mark E; Schwendeman, Steven P

    2016-03-10

    Nitric oxide (NO) is a fascinating and important endogenous free-radical gas with potent antimicrobial, vasodilating, smooth muscle relaxant, and growth factor stimulating effects. However, its wider biomedical applicability is hindered by its cumbersome administration, since NO is unstable especially in biological environments. In this work, to ultimately develop site-specific controlled release vehicles for NO, the NO donor S-nitroso-N-acetyl-D-penicillamine (SNAP) was encapsulated within poly(lactic-co-glycolic acid) 50:50 (PLGA) microspheres by using a solid-in-oil-in-water emulsion solvent evaporation method. The highest payload was 0.56(±0.01) μmol SNAP/mg microspheres. The in vitro release kinetics of the donor were controlled by the bioerosion of the PLGA microspheres. By using an uncapped PLGA (Mw=24,000-38,000) SNAP was slowly released for over 10days, whereas by using the ester capped PLGA (Mw=38,000-54,000) the release lasted for over 4weeks. The presence of copper ions and/or ascorbate in solution was necessary to efficiently decompose the released NO donor and obtain sustained NO release. It was also demonstrated that light can be used to induce rapid NO release from the microspheres over several hours. SNAP exhibited excellent storage stability when encapsulated in the PLGA microspheres. These new microsphere formulations may be useful for site-specific administration and treatment of pathologies associated with dysfunction in endogenous NO production, e.g. treatment of diabetic wounds, or in diseases involving other biological functions of NO including vasodilation, antimicrobial, anticancer, and neurotransmission. Copyright © 2016 Elsevier B.V. All rights reserved.

  13. Novel magnetic nanoparticles coated by benzene- and β-cyclodextrin-bearing dextran, and the sorption of polycyclic aromatic hydrocarbon.

    Science.gov (United States)

    Cho, Eunae; Tahir, Muhammad Nazir; Choi, Jae Min; Kim, Hwanhee; Yu, Jae-Hyuk; Jung, Seunho

    2015-11-20

    We present the synthesis of novel magnetic nanoparticles functionalized by benzene- and β-cyclodextrin-derivatized dextran. The grafting strategy was based on the [alkynyl-iron] cluster in the modified dextrans, which were prepared by click reaction from alkyne-modified dextran and benzyl azide or mono-6-O-deoxy-monoazido β-cyclodextrin. Characterization was then carried out by thermogravimetric analysis, Fourier transform infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, and vibrating sample magnetometry. Using the developed magnetic nanoparticles, the potential for removing polycyclic aromatic hydrocarbons such as phenanthrene and pyrene by sorption onto the nanomaterials was assessed. In the sorption, pi-stacking interactions of the benzene-derivatized dextran and host-guest chemistry of the β-cyclodextrin-derivatized dextran were considered to be significant. Furthermore, the polysaccharide derivative-coated magnetic adsorbents could be recovered by an external magnet for reuse. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Effects of Liposomal Compositions with Oxidized Dextrans on Functional Activity of U937 Macrophage-Like Cells In Vitro.

    Science.gov (United States)

    Kozhin, P M; Chechushkov, A V; Zaitseva, N S; Lemza, A E; Men'shchikova, E B; Troitskii, A V; Shkurupy, V A

    2015-11-01

    We studied the effects of liposomal pharmaceutical compositions with oxidized dextrans on functional activity of U937 monocyte/macrophage-like cells. Liposomes in the emulsion contained oxidized dextran with a molecular weights of 40 kDa or 70 kDa or isonicotinic acid hydrazide (INAH) conjugated with oxidized dextran (40 kDa). Cell viability was evaluated by MTT test; mitochondrial transmembrane potential and production of superoxide anion and H2O2 were studied by fluorescent methods. The studied compositions exhibited no cytotoxic effect and even improved cell viability and mitochondrial respiration. Liposomes with oxidized 40 kDa dextran, including those with INAH-conjugated dextran, inhibited production of superoxide anion, but increased H2O2 generation.

  15. PREPARATION AND CHARACTERIZATION OF TRAMADOL HYDROCHLORIDE MICROSPHERES

    Directory of Open Access Journals (Sweden)

    Patel Keyur

    2015-10-01

    Full Text Available Tramadol HCl was microencapsulated with Ethylcellulose using multiple emulsion solvent evaporation method. A 32 factorial design employed to study the effect of drug: polymer ratio and volume of External phase (1% PVA on % yield, % encapsulation efficiency, particle size, % drug release rate. The drug: polymer ratio and volume of continuous phase were significant effect on % yield, % entrapment efficiency, particle size, % drug release rate. % drug release was Biphasic system first initially bursting effect and finally sustained. Higher Percentage yield (77.4% and Higher Percentage Encapsulation Efficiency(31.1% were observed in Batch EC3. All the microspheres were spherical in nature its surface was smooth observed in SEM report.

  16. Formulation and drug-content assay of microencapsulated antisense oligonucleotide to NF-κB using ATR-FTIR

    Science.gov (United States)

    Siwale, Rodney; Meadows, Fred; Mody, Vicky V.; Shah, Samit

    2013-09-01

    Antisense oligonucleotide to NF-κB sequence: 5‧-GGA AAC ACA TCC TCC ATG-3‧, was microencapsulated in an albumin matrix by the method of spray dryingTM. Spectral analysis was performed on varying drug loading formulations of both drugs by mid-IR attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR). An out of plane O-H bending vibration at 948 cm-1, unique to both the native and microencapsulated drugs was identified. The calculated peak areas corresponded to the drug loadings in the microsphere formulations. A standard curve could then be used to determine the drug content of an unknown microsphere formulation. Accuracy and precision were determined to be comparable to other analytical techniques such as HPLC.

  17. Measurements of extrinsic fluorescence in Intralipid and polystyrene microspheres

    Science.gov (United States)

    Du Le, Vinh Nguyen; Nie, Zhaojun; Hayward, Joseph E.; Farrell, Thomas J.; Fang, Qiyin

    2014-01-01

    The fluorescence of Intralipid and polystyrene microspheres with sphere diameter of 1 µm at a representative lipid and microsphere concentration for simulation of mucosal tissue scattering has not been a subject of extensive experimental study. In order to elucidate the quantitative relationship between lipid and microsphere concentration and the respective fluorescent intensity, the extrinsic fluorescence spectra between 360 nm and 650 nm (step size of 5 nm) were measured at different lipid concentrations (from 0.25% to 5%) and different microsphere concentrations (0.00364, 0.0073, 0.0131 spheres per cubic micrometer) using laser excitation at 355 nm with pulse energy of 2.8 µJ. Current findings indicated that Intralipid has a broadband emission between 360 and 650 nm with a primary peak at 500 nm and a secondary peak at 450 nm while polystyrene microspheres have a single peak at 500 nm. In addition, for similar scattering properties the fluorescence of Intralipid solutions is approximately three-fold stronger than that of the microsphere solutions. Furthermore, Intralipid phantoms with lipid concentrations ~2% (simulating the bottom layer of mucosa) produce up to seven times stronger fluorescent emission than phantoms with lipid concentration ~0.25% (simulating the top layer of mucosa). The fluoresence decays of Intralipid and microsphere solutions were also recorded for estimation of fluorescence lifetime. PMID:25136497

  18. 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.

  19. Bioavailability enhancement of verapamil HCl via intranasal chitosan microspheres.

    Science.gov (United States)

    Abdel Mouez, Mamdouh; Zaki, Noha M; Mansour, Samar; Geneidi, Ahmed S

    2014-01-23

    Chitosan microspheres are potential drug carriers for maximizing nasal residence time, circumventing rapid mucociliary clearance and enhancing nasal absorption. The aim of the present study was to develop and characterize chitosan mucoadhesive microspheres of verapamil hydrochloride (VRP) for intranasal delivery as an alternative to oral VRP which suffers low bioavailability (20%) due to extensive first pass effect. The microspheres were produced using a spray-drying and precipitation techniques and characterized for morphology (scanning electron microscopy), particle size (laser diffraction method), drug entrapment efficiency, thermal behavior (differential scanning calorimetry) and crystallinity (X-ray diffractometric studies) as well as in vitro drug release. Bioavailability of nasal VRP microspheres was studied in rabbits and the results were compared to those obtained after nasal, oral and intravenous administration of VRP solution. Results demonstrated that the microspheres were spherical with size 21-53 μm suitable for nasal deposition. The spray-drying technique was superior over precipitation technique in providing higher VRP entrapment efficiency and smaller burst release followed by a more sustained one over 6h. The bioavailability study demonstrated that the nasal microspheres exhibited a significantly higher bioavailability (58.6%) than nasal solution of VRP (47.8%) and oral VRP solution (13%). In conclusion, the chitosan-based nasal VRP microspheres are promising for enhancing VRP bioavailability by increasing the nasal residence time and avoiding the first-pass metabolism of the drug substance. Copyright © 2013 Elsevier B.V. All rights reserved.

  20. Development, characterization and solubility enhancement of comparative dissolution study of second generation of solid dispersions and microspheres for poorly water soluble drug

    Directory of Open Access Journals (Sweden)

    Poovi Ganesan

    2015-10-01

    Full Text Available The poor dissolution characteristics of water-insoluble drugs are a major challenge for pharmaceutical scientists. Reduction of the particle size/increase in the surface area of the drug is a widely used and relatively simple method for increasing dissolution rates. The objective of this study was to improve solubility, release and comparability of dissolution of a poorly soluble drug using two different types of formulations (solid dispersions and microspheres. Hydrochlorothiazide was used as a model drug. The solid dispersions and microspheres were prepared by solvent evaporation method using ethyl cellulose, hydroxypropyl methylcellulose in different drug-to-carrier ratios (1:1, 1:2 w:w. The prepared formulations were evaluated for interaction study by Fourier transform infrared spectroscopy, differential scanning calorimetry, percentage of practical yield, drug loading, surface morphology by scanning electron microscopy, optical microscopy and in-vitro release studies. The results showed no interaction between the drug and polymer, amorphous state of solid dispersions and microspheres, percentage yield of 42.53% to 78.10%, drug content of 99.60 % to 99.64%, good spherical appearance in formulation VI and significant increase in the dissolution rate.

  1. O-hexadecyl-dextran entrapped berberine nanoparticles abrogate high glucose stress induced apoptosis in primary rat hepatocytes.

    Directory of Open Access Journals (Sweden)

    Radhika Kapoor

    Full Text Available Nanotized phytochemicals are being explored by researchers for promoting their uptake and effectiveness at lower concentrations. In this study, O-hexadecyl-dextran entrapped berberine chloride nanoparticles (BC-HDD NPs were prepared, and evaluated for their cytoprotective efficacy in high glucose stressed primary hepatocytes and the results obtained compared with bulk berberine chloride (BBR treatment. The nanotized formulation treated primary hepatocytes that were exposed to high glucose (40 mM, showed increased viability compared to the bulk BBR treated cells. BC-HDD NPs reduced the ROS generation by ∼ 3.5 fold during co-treatment, prevented GSH depletion by ∼ 1.6 fold, reduced NO formation by ∼ 5 fold and significantly prevented decline in SOD activity in stressed cells. Lipid peroxidation was also prevented by ∼ 1.9 fold in the presence of these NPs confirming the antioxidant capacity of the formulation. High glucose stress increased Bax/Bcl2 ratio followed by mitochondrial depolarization and activation of caspase-9/-3 confirming involvement of mitochondrial pathway of apoptosis in the exposed cells. Co- and post-treatment of BC-HDD NPs prevented depolarization of mitochondrial membrane, reduced Bax/Bcl2 ratio and prevented externalization of phosphatidyl-serine confirming their anti-apoptotic capacity in those cells. Sub-G1 phase apparent in high glucose stressed cells was not seen in BC-HDD NPs treated cells. The present study reveals that BC-HDD NPs at ∼ 20 fold lower concentration are as effective as BBR in preventing high glucose induced oxidative stress, mitochondrial depolarization and downstream events of apoptotic cell death.

  2. Removal of chloroform from biodegradable therapeutic microspheres by radiolysis.

    Science.gov (United States)

    Zielhuis, S W; Nijsen, J F W; Dorland, L; Krijger, G C; van Het Schip, A D; Hennink, W E

    2006-06-06

    Radioactive holmium-166 loaded poly(l-lactic acid) microspheres are promising systems for the treatment of liver malignancies. These microspheres are loaded with holmium acetylacetonate (HoAcAc) and prepared by a solvent evaporation method using chloroform. After preparation the microspheres (Ho-PLLA-MS) are activated by neutron irradiation in a nuclear reactor. It was observed that relatively large amounts of residual chloroform (1000-6000 ppm) remained in the microspheres before neutron irradiation. Since it is known that chloroform is susceptible for high-energy radiation, we investigated whether neutron and gamma irradiation could result in the removal of residual chloroform in HoAcAc-loaded and placebo PLLA-MS by radiolysis. To investigate this, microspheres with relatively high and low amounts of residual chloroform were subjected to irradiation. The effect of irradiation on the residual chloroform levels as well as other microsphere characteristics (morphology, size, crystallinity, molecular weight of PLLA and degradation products) were evaluated. No chloroform in the microspheres could be detected after neutron irradiation. This was also seen for gamma irradiation at a dose of 200 kGy phosgene, which can be formed as the result of radiolysis of chloroform, was not detected with gas chromatography-mass spectrometry (GC-MS). A precipitation titration showed that radiolysis of chloroform resulted in the formation of chloride. Gel permeation chromatography and differential scanning calorimetry showed a decrease in molecular weight of PLLA and crystallinity, respectively. However, no differences were observed between irradiated microsphere samples with high and low initial amounts of chloroform. In conclusion, this study demonstrates that neutron and gamma irradiation results in the removal of residual chloroform in PLLA-microspheres.

  3. Autonomic shutdown of lithium-ion batteries using thermoresponsive microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Baginska, Marta; White, Scott R. [306 Talbot Laboratory, Department of Aerospace Engineering, University of Illinois Urbana-Champaign, Urbana, IL (United States); Beckman Institute for Advanced Science and Technology, University of Illinois Urbana-Champaign, Urbana, IL (United States); Blaiszik, Benjamin J.; Sottos, Nancy R. [Department of Materials Science and Engineering, Materials Science and Engineering Building, University of Illinois Urbana-Champaign, Urbana, IL (United States); Beckman Institute for Advanced Science and Technology, University of Illinois Urbana-Champaign, Urbana, IL (United States); Merriman, Ryan J. [306 Talbot Laboratory, Department of Aerospace Engineering, University of Illinois Urbana-Champaign, Urbana, IL (United States); Moore, Jeffrey S. [Department of Chemistry, University of Illinois Urbana-Champaign, Urbana, IL (United States); Beckman Institute for Advanced Science and Technology, University of Illinois Urbana-Champaign, Urbana, IL (United States)

    2012-05-15

    Autonomic, thermally-induced shutdown of Lithium-ion (Li-ion) batteries is demonstrated by incorporating thermoresponsive polymer microspheres (ca. 4 {mu}m) onto battery anodes or separators. When the internal battery environment reaches a critical temperature, the microspheres melt and coat the anode/separator with a nonconductive barrier, halting Li-ion transport and shutting down the cell permanently. Three functionalization schemes are shown to perform cell shutdown: 1) poly(ethylene) (PE) microspheres coated on the anode, 2) paraffin wax microspheres coated on the anode, and 3) PE microspheres coated on the separator. Charge and discharge capacity is measured for Li-ion coin cells containing microsphere-coated anodes or separators as a function of capsule coverage. For PE coated on the anode, the initial capacity of the battery is unaffected by the presence of the PE microspheres up to a coverage of 12 mg cm{sup -2} (when cycled at 1C), and full shutdown (>98% loss of initial capacity) is achieved in cells containing greater than 3.5 mg cm{sup -2}. For paraffin microspheres coated on the anode and PE microspheres coated on the separator, shutdown is achieved in cells containing coverages greater than 2.9 and 13.7 mg cm{sup -2}, respectively. Scanning electron microscopy images of electrode surfaces from cells that have undergone autonomic shutdown provides evidence of melting, wetting, and resolidification of PE into the anode and polymer film formation at the anode/separator interface. (Copyright copyright 2012 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  4. Preparation of paclitaxel-loaded microspheres with magnetic nanoparticles

    Institute of Scientific and Technical Information of China (English)

    CUI Sheng; SHEN Xiaodong; SHI Ruihua; LIN Benlan; CHEN Ping

    2007-01-01

    The objective of this paper was to prepare paclitaxel-loaded microspheres,a kind of target-orientation anticancer drug.The paclitaxel-loaded microspheres were prepared with magnetic Fe3O4 nanoparticles and taxo1.The morphology was characterized by scanning electron microscopy(SEM),and the average size and the size distribution were determined by a laser-size distributing instrument.High performance liquid chromatography(HPLC)was used to measure the paclitaxel content.Experimental results indicated that the effective drug loading and the entrapment ratio of paclitaxel-loaded microspheres were 1.83% and 92,62%,respectively.

  5. Locomotion of microspheres for imaging and light focusing applications

    CERN Document Server

    Krivitsky, Leonid A; Wang, Zengbo; Lukiyanchuk, Boris

    2013-01-01

    Super-resolution imaging using sub-diffraction field localization by micron sized transparent beads (microspheres) was recently demonstrated [1]. Practical applications in microscopy require control over the positioning of the microspheres. We present a simple method of positioning and controllable movement of a microsphere by using a glass micropipette. This allows sub-diffraction imaging at arbitrary points in three dimensions, as well as the ability to track moving objects. The results are relevant to a broad scope of applications, including sample inspection, and bio-imaging.

  6. Confocal epifluorescence detection for microspheres delivered on disposable microfluidic chip

    Institute of Scientific and Technical Information of China (English)

    Honghua Hu; Xiyun Hou; Guoguang Yang

    2006-01-01

    @@ The laser induced fluorescence (LIF) detection system for 5-μm microspheres delivered on microfluidic chip is presented employing confocal optical scheme. The parameters of the optical system are specifically optimized for single microsphere detection. With the excitation laser spot size of 4.6 μm and optical sectioning power of 27 μm, the lowest concentration detection limit is 0.45 nmol/L, corresponding to only 122 molecules in probe volume. The microsphere detection is carried on successfully with the maximum signal-to-noise ratio (SNR) of 55.7, which provides good detection sensitivity.

  7. Optical properties of metallo-dielectric microspheres in opal structures

    Energy Technology Data Exchange (ETDEWEB)

    Jiang, Y; Whitehouse, C; Li, Jensen; Tam, Wing Yim; Chan, C T; Sheng Ping [Department of Physics, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong (China)

    2003-09-03

    We report the fabrication of opal structure using metallo-dielectric silica microspheres. Mono-dispersed silica microspheres were coated with silver using an electrode-less wet-plating technique. Thin slabs of opal were obtained by assembling the silver-coated microspheres between two glass plates using a forced-packing method. The optical properties of the resulting opal structure were studied in the infrared range. Good agreement is obtained with the predictions of a multiple scattering approach, provided that the silver layer is modelled as a silver composite.

  8. Packaged chalcogenide microsphere resonator with high Q-factor

    Science.gov (United States)

    Wang, Pengfei; Ding, Ming; Lee, Timothy; Senthil Murugan, Ganapathy; Bo, Lin; Semenova, Yuliya; Wu, Qiang; Hewak, Dan; Brambilla, Gilberto; Farrell, Gerald

    2013-04-01

    The fabrication and characterization of a packaged As2S3 microsphere resonator coupled to a tapered fiber using a low refractive index UV-curable polymer are reported. Embedding provides an efficient means to remove the highest order whispering gallery modes in the microsphere resonator, thus cleaning the resonator spectrum. At wavelengths near 1549.5 nm, high-Q modes up to 1.8 × 105 can be efficiently excited in a 110 μm diameter chalcogenide microsphere via evanescent coupling from a 2 μm diameter tapered silica fiber. The device photosensitivity, useful for tuning, is still present and useable after the packaging process.

  9. Leg amputation following intramuscular injection of iron dextran in a 32 year old woman

    Directory of Open Access Journals (Sweden)

    Gloria Shalviri

    2015-10-01

    Full Text Available To inform healthcare professionals of a rare serious reaction leading to leg amputation following intramuscular injection of iron dextran and report comments for preventing such reactions.A case of leg amputation following intramuscular injection of iron dextran reported to Iranian Pharmacovigilance Center was reviewed. Patient and reaction data was collected by assessing the reported yellow card, patient chart review and interviewing with patient and physicians. World Health Organization definition for serious reactions was used to determine the seriousness of the reaction. Naranjo algorithm was used to determine probability scale. The probability of the reaction was determined based on questionnaire of Schumock et al. The studied case is classified as a rare and serious but preventable reaction induced by intramuscular injection of iron dextran in a 32 year old woman. The probability of the reaction is appeared to be “probable” based on Naranjo algorithm. It seems that Iron dextran could cause serious and life threatening adverse effects. It is necessary for healthcare professionals to be informed of such rare but serious reaction in order to apply preventive actions.

  10. Stability of ketoprofen-dextran ester prodrugs in homogenates of various segments of pig GI tract

    DEFF Research Database (Denmark)

    Larsen, C.; Jensen, Bodil Hamborg; Olesen, H. P.

    1991-01-01

    Initial velocities of ketoprofen formation from ketoprofen-dextran ester prodrugs incubated in homogenates of various segments of the pig GI-tract were determined. Enzyme-mediated drug release was found in caecum and colon homogenates with their contents, whereas release rates in the stomach...

  11. Study on Thermosensitive Micellization of Dextran-g-PNIPAAm in Aqueous Solutions

    Institute of Scientific and Technical Information of China (English)

    Dan ZHAO; Li Qun WANG; Ke Hua TU; Song Wei TAN

    2006-01-01

    The thermosensitive micellization of dextran-g-PNIPAAm in aqueous solutions has been investigated by fluorescence spectroscopy, dynamic light scattering and transmission electron microscope. The formed polymeric micelles showed different diameters of about 20 nm or 100nm, when the solution temperature was below or above the phase transition temperature.

  12. Phase separation of aqueous mixtures of poly(ethylene oxide) and dextran

    NARCIS (Netherlands)

    Edelman, M.W.; Linden, van der E.; Tromp, R.H.

    2003-01-01

    Abstract: The phase behavior of aqueous mixtures of poly(ethylene oxide) (PEO) and dextran is studied as a function of the polymer concentration, the PEO molar mass, and temperature. The molar mass distributions of the two polymers in the coexisting phases are measured. From the temperature dependen

  13. Chitosan-dextran sulfate hydrogels as a potential carrier for probiotics

    DEFF Research Database (Denmark)

    Yucel Falco, Cigdem; Falkman, Peter; Risbo, Jens

    2017-01-01

    Physical and chemical (crosslinked with genipin) hydrogels based on chitosan and dextran sulfate were developed and characterized as novel bio-materials suitable for probiotic encapsulation. The swelling of the hydrogels was dependent on the composition and weakly influenced by the pH of the media...

  14. Synthesis and characterization of Schiff base contained dextran microgels in water-in-oil inverse microemulsion.

    Science.gov (United States)

    Su, Hongying; Jia, Qingming; Shan, Shaoyun

    2016-11-05

    Polysaccharide-based microgels with high water content, excellent biocompatibility and controllable particle size have been widely studied as ideal candidates for drug release and delivery. In this study, microgels based on dextran were developed via the Schiff base formation between aldehyded dextran and ethylenediamine in a water-in-oil (W/O) microemulsion. Particle size of the resulted microgel was controllable between 800 and 1100nm by modulating the amount of the employed co-surfactants (Span 80/Tween 80). Furthermore, fluoresceins (e.g., aminofluorescein) and drugs (e.g., doxorubicin) with free amino groups can be conjugated onto the network of the dextran-based microgel via Schiff base linkages. Since the Schiff base linkages are degradable via hydrolysis and their stability decreases with the environmental pH decreases, the resulted Schiff bases contained microgel showed a pH dependent degradation profile. These results indicated that the pH-sensitive microgel based on dextran could be used as promising drug delivery systems for biomedical applications.

  15. 77 FR 50121 - Hospira, Inc.; Withdrawal of Approval of a New Drug Application for DEXTRAN 70

    Science.gov (United States)

    2012-08-20

    ... From the Federal Register Online via the Government Publishing Office DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration Hospira, Inc.; Withdrawal of Approval of a New Drug... Drug Administration (FDA) is withdrawing approval of a new drug application (NDA) for DEXTRAN 70...

  16. Formulation of a charcoal suspension for intratumoral injection. Study of galenical excipients.

    Science.gov (United States)

    Bonhomme-Faivre, L; Mathieu, M C; Depraetere, P; Grossiord, J L; Orbach-Arbouys, S; Puisieux, F; Seiller, M

    1999-02-01

    To tattoo human breast cancer prior to chemotherapy, radiotherapy, or surgery, thus allowing a better localization of the remaining tumor by the surgeon, we developed a formulation containing 10% charcoal suspended in water for parenteral preparations. The present study concerns a new step in the development of the charcoal suspension. We sought to determine whether the addition of various excipients could improve the formulation properties and affect the labeling of tumor by the suspension. We have tested surfactants (egg lecithin, polysorbate 80, Cremophor EL, and Pluronic F68), isotonisants (sugars such as glucose and mannitol), polysaccharides (dextrans 20 and 40), and Cabosil, a pyrogenated silica. Except for glucose and mannitol, which were added at a 5% concentration, the other excipients were added at a 0.1% concentration, they were dissolved in water for parenteral injection and sterilized at 120 degrees C for 20 min. We then measured diffusion in vivo in mammary tumor. In vivo, when injected intratumorally in mice, a greater diffusion of charcoal particles was noted within the tumor (in the case of egg lecithin, polysorbate 80, dextran 20 and 40, and glucose) and sometimes in some organs (e.g., Cremophor EL and mannitol). Pluronic F68 slightly improved the stability of the suspension and did not lead to marked diffusion at the injection site, but it showed slight toxicity and cannot be used in the formulation. We concluded that the best formulation was an aqueous 10% micronized peat charcoal suspension.

  17. Explosive Formulation Pilot Plant

    Data.gov (United States)

    Federal Laboratory Consortium — The Pilot Plant for Explosive Formulation supports the development of new explosives that are comprised of several components. This system is particularly beneficial...

  18. A biodegradable polymeric system for peptide–protein delivery assembled with porous microspheres and nanoparticles, using an adsorption/infiltration process

    Directory of Open Access Journals (Sweden)

    Alcalá-Alcalá S

    2013-06-01

    Full Text Available Sergio Alcalá-Alcalá, Zaida Urbán-Morlán, Irene Aguilar-Rosas, David Quintanar-Guerrero Laboratorio de Investigación y Posgrado en Tecnología Farmacéutica, Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, Estado de México, México Abstract: A biodegradable polymeric system is proposed for formulating peptides and proteins. The systems were assembled through the adsorption of biodegradable polymeric nanoparticles onto porous, biodegradable microspheres by an adsorption/infiltration process with the use of an immersion method. The peptide drug is not involved in the manufacturing of the nanoparticles or in obtaining the microspheres; thus, contact with the organic solvent, interfaces, and shear forces required for the process are prevented during drug loading. Leuprolide acetate was used as the model peptide, and poly(D,L-lactide-co-glycolide (PLGA was used as the biodegradable polymer. Leuprolide was adsorbed onto different amounts of PLGA nanoparticles (25 mg/mL, 50 mg/mL, 75 mg/mL, and 100 mg/mL in a first stage; then, these were infiltrated into porous PLGA microspheres (100 mg by dipping the structures into a microsphere suspension. In this way, the leuprolide was adsorbed onto both surfaces (ie, nanoparticles and microspheres. Scanning electron microscopy studies revealed the formation of a nanoparticle film on the porous microsphere surface that becomes more continuous as the amount of infiltrated nanoparticles increases. The adsorption efficiency and release rate are dependent on the amount of adsorbed nanoparticles. As expected, a greater adsorption efficiency (~95% and a slower release rate were seen (~20% of released leuprolide in 12 hours when a larger amount of nanoparticles was adsorbed (100 mg/mL of nanoparticles. Leuprolide acetate begins to be released immediately when there are no infiltrated nanoparticles, and 90% of the peptide is released in the first 12 hours

  19. Hydroxyethyl starch as a substitute for dextran 40 for thawing peripheral blood progenitor cell products.

    Science.gov (United States)

    Zhu, Fenlu; Heditke, Sarah; Kurtzberg, Joanne; Waters-Pick, Barbara; Hari, Parameswaran; Margolis, David A; Keever-Taylor, Carolyn A

    2015-12-01

    Removing DMSO post-thaw results in: reduced infusion reactions, improved recovery and stability of viable CD34+ cells. Validated methods use 5%-8.3% Dextran 40 with 2.5%-4.2% HSA for this purpose. Recent shortages of clinical grade Dextran require identification of suitable alternatives. PBPC were used to compare a standard 2X wash medium of 5 parts 10% Dextran 40 in saline (DEX) with 1 part 25% HSA (8.3% DEX/ 4.2% HSA) with Hydroxyethyl Starch (HES)-based solutions. Cells in replicate bags were diluted with an equal volume of wash solution, equilibrated 5 minutes, the bag filled with wash medium, pelleted and the supernatant expressed. Bags were restored to the frozen volume in wash medium and tested by single platform flow cytometry and CFU. Total viability, viable TNC, MNC, and CD34+ cell recovery, and CD34+ cell viability were compared immediately post-thaw and after 90 minutes. 5.2% HES/4.2% HSA did not differ from our standard in CD34 recovery or viability. Due to concerns that high concentrations of HES could affect renal function we tested 0.6% HES/2.5% HSA resulting in significantly poorer CD34 recovery and viability. Results improved using 2.4% HES/4.2% HSA and when 0.6% HES/4.2%HSA was used no significant differences were seen. CFU assays confirmed no differences between the standard dextran arm and HES at 2.4% or 0.6% so long as HSA was at 4.2%. We conclude that HES from 0.6% to 5.2% with 4.2% HSA is a suitable substitute for Dextran 40 as a reconstitution/washing medium for PBPC products. Copyright © 2015 International Society for Cellular Therapy. Published by Elsevier Inc. All rights reserved.

  20. Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties

    Directory of Open Access Journals (Sweden)

    Xiaohong Chen

    2014-04-01

    Full Text Available Emodin (1,3,8-trihydroxy-6-methylanthraquinone has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres (ED-PLA-MS were prepared and their characteristics were studied. ED-PLA-MS were prepared by the organic phase dispersion-solvent diffusion method. By applying an orthogonal design, our results indicated that the optimal formulation was 12 mg/mL PLA, 0.5% gelatin, and an organic phase:glycerol ratio of 1:20. Using the optimal experimental conditions, the drug loading and encapsulation efficiencies were (19.0 ± 1.8% and (62.2 ± 2.6%, respectively. The average particle size was 9.7 ± 0.7 μm. In vitro studies indicated that the ED-PLA-MS demonstrated a well-sustained release efficacy. The microspheres delivered emodin, primarily to the lungs of mice, upon intravenous injection. It was also detected by microscopy that partial lung inflammation was observed in lung tissues and no pathological changes were found in other tissues of the ED-PLA-MS-treated animals. These results suggested that ED-PLA-MS are of potential value in treating lung diseases in animals.

  1. Effect of Glycerol, as Cryoprotectant in the Encapsulation and Freeze Drying of Microspheres Containing Probiotic Cells

    Directory of Open Access Journals (Sweden)

    Oana Lelia Pop

    2015-05-01

    Full Text Available It is reported that probiotics provide several health benefits as they help in maintaining a good balance and composition of intestinal flora, and increase the resistance against invasion of pathogens. Ensuring adequate dosages of probiotics at the time of consumption is a challenge, because several factors during processing and storage affect the viability of probiotic organisms. Major emphasis has been given to protect the microorganisms with the help of encapsulation technique, by addition of different protectants. In this study, probiotic cells (Bifidobacterium lactis 300B were entrapped in alginate/pullulan microspheres. In the encapsulation formula glycerol was used as cryoprotectant in the freeze drying process for long time storage. It was observed that the survival of Bifidobacterium lactis 300B when encapsulated without cryoprotectant was higher than the formula with glycerol in the fresh obtained microspheres. The addition of glycerol was in order to reduce the deep freezing and freeze drying damages. In the chosen formulations, glycerol did not proved protection for the entrapped probiotic cells in the freeze drying process, for which the use of glycerol as cryoprotectant for alginate/pullulan Bifidobacterium lactis 300B entrapment is not recommended.

  2. Controlled Release Inhalable Polymeric Microspheres for Treatment of Pulmonary Arterial Hypertension.

    Science.gov (United States)

    Saigal, Aparna; Ng, Wai Kiong; Tan, Reginald B H; Chan, Sui Yung

    2015-01-01

    Pulmonary arterial hypertension (PAH) is a chronic ailment of the lungs, exhibiting elevated arterial pressure and vascular resistance; with a mean arterial pressure above 25 mmHg at rest and above 30 mmHg during exercise. It is associated with poor prognosis, and its prevalence is estimated to be 15 cases per one million. The current treatment options for PAH are discussed with the prostanoid class of drugs being the most effective. The latter drugs act by dilating systemic and pulmonary arterial vascular beds and, with sustained long-term usage, altering pulmonary remodelling. They are administered as IV infusions or inhalation solutions. Despite their clinical effectiveness, prostanoids have short half-lives requiring frequent administration of 6-9 times daily and thus suffer from poor compliance. Controlled release inhalation delivery systems for treatment of PAH, ranging from liposomes, biodegradable nano- and microparticles, formation of co-precipitates and complexation with cyclodextrins, are explored. Arising from these formulation strategies, we developed novel polymeric microspheres for inhalation to reduce dosing frequency and improve medication compliance. These microspheres are designed with release modifiers, to reside in the lung which is the site of drug action for a longer duration so as to release the drug slowly and consistently over a prolonged period. This could lead to the development of the first commercially available controlled release inhalation product.

  3. High impact of in situ dextran coating on biocompatibility, stability and magnetic properties of iron oxide nanoparticles.

    Science.gov (United States)

    Shaterabadi, Zhila; Nabiyouni, Gholamreza; Soleymani, Meysam

    2017-06-01

    Biocompatible ferrofluids based on dextran coated iron oxide nanoparticles were fabricated by conventional co-precipitation method. The experimental results show that the presence of dextran in reaction medium not only causes to the appearance of superparamagnetic behavior but also results in significant suppression in saturation magnetization of dextran coated samples. These results can be attributed to size reduction originated from the role of dextran as a surfactant. Moreover, weight ratio of dextran to magnetic nanoparticles has a remarkable influence on size and magnetic properties of nanoparticles, so that the sample prepared with a higher weight ratio of dextran to nanoparticles has the smaller size and saturation magnetization compare with the other samples. In addition, the ferrofluids containing such nanoparticles have an excellent stability at physiological pH for several months. Furthermore, the biocompatibility studies reveal that surface modification of nanoparticles by dextran dramatically decreases the cytotoxicity of bare nanoparticles and consequently improves their potential application for diagnostic and therapeutic purposes. Copyright © 2017 Elsevier B.V. All rights reserved.

  4. Derivatization of Dextran for Multiply Charged Ion Formation and Electrospray Ionization Time-of-Flight Mass Spectrometric Analysis

    Science.gov (United States)

    Tapia, Jesus B.; Hibbard, Hailey A. J.; Reynolds, Melissa M.

    2017-10-01

    We present the use of a simple, one-pot derivatization to allow the polysaccharide dextran to carry multiple positive charges, shifting its molecular weight distribution to a lower m/ z range. We performed this derivatization because molecular weight measurements of polysaccharides by mass spectrometry are challenging because of their lack of readily ionizable groups. The absence of ionizable groups limits proton abstraction and suppresses proton adduction during the ionization process, producing mass spectra with predominantly singly charged metal adduct ions, thereby limiting the detection of large polysaccharides. To address this challenge, we derivatized dextran T1 (approximately 1 kDa) by attaching ethylenediamine, giving dextran readily ionizable, terminal amine functional groups. The attached ethylenediamine groups facilitated proton adduction during the ionization process in positive ion mode. Using the low molecular weight dextran T1, we tracked the number of ethylenediamine attachments by measuring the mass shift from underivatized to derivatized dextran T1. Using electrospray ionization time-of-flight mass spectrometry, we observed derivatized dextran chains ranging from two to nine glucose residues with between one and four attachments/charges. Our success in shifting derivatized dextran T1 toward the low m/ z range suggests potential for this derivatization as a viable route for analysis of high molecular weight polysaccharides using electrospray ionization time-of-flight mass spectrometry. [Figure not available: see fulltext.

  5. Spray dried microspheres based on chitosan: A promising new carrier for intranasal administration of polymeric antigen BLSOmp31 for prevention of ovine brucellosis.

    Science.gov (United States)

    Díaz, Alejandra Graciela; Quinteros, Daniela Alejandra; Llabot, Juan Manuel; Palma, Santiago Daniel; Allemandi, Daniel Alberto; Ghersi, Giselle; Zylberman, Vanesa; Goldbaum, Fernando Alberto; Estein, Silvia Marcela

    2016-05-01

    Previous studies have demonstrated that parenteral immunization with polymeric antigen BLSOmp31 induced a strong immune response and conferred protection against Brucella ovis in rams. This work describes the development of a novel formulation strategy for the delivery of BLSOmp31 in the nasal mucosa. Chitosan microparticles were prepared by spray-drying technology processes and recombinant chimera BLSOmp31 was loaded by passive adsorption onto chitosan microspheres, which were characterized by means of the evaluation of size, zeta potential, morphology, and loading and release rate of BLSOmp31. The mucoadhesive properties of microspheres were evaluated by studying the interaction between microparticles and mucin. The antigen BLSOmp31 integrity was investigated by SDS-PAGE. The yield of production of spray-drying process was 68.95%. Microspheres had a good sphericity, 1-10 μm of particle size and had a positive charge. The loading capacity was found to be 45.19%. The initial fast release of BLSOmp31 from chitosan microparticles was 60%. The BLSOmp31 integrity was not affected by passive adsorption (ionic interaction). The amount of mucin adsorbed on the surface of CMs-BLSOmp31 was lower than on the surface of blank CMs at neutral pH. In vivo studies were carried out in rams. Intranasal immunization induced systemic and local antibodies. In conclusion, the use of BLSOmp31-loaded chitosan spray-drying microspheres offers a promising way for nasal mucosal vaccination in sheep against brucellosis.

  6. Preparation and in vitro release performance of sustained-release captopril/Chitosan-gelatin net-polymer microspheres

    Science.gov (United States)

    Zhou, Li; Xu, Junming; Song, Yimin; Gao, Yuanyuan; Chen, Xiguang

    2007-07-01

    The captopril/Chitosan-gelatin net-polymer microspheres (CTP/CGNPMs) were prepared using Chitosan (CTS) and gelatin (GT) by the methods of emulsification, cross-linked reagent alone or in combination and microcrystalline cellulose (MCC) added in the process of preparation of microspheres, which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (CTP). The results indicated that CTP/CGNPMs had a spherical shape, smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio (EMR) and composition of cross linking reagents. Among these factors, the EMR (1/4), CLR (FA+SPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER, DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%, 9.95±0.77% and 261±42%, respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.

  7. Preparation and in vitro Release Performance of Sustained-release Captopril/Chitosan-gelatin Net-polymer Microspheres

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    The captopril/Chitosan-gelatin net-polymer microspheres (CTP/CGNPMs) were prepared using Chitosan (CTS) and gelatin (GT) by the methods of emulsification, cross-linked reagent alone or in combination and microcrystalline cellulose (MCC) added in the process of preparation of microspheres, which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (CTP). The results indicated that CTP/CGNPMs had a spherical shape, smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio (EMR) and composition of cross linking reagents. Among these factors, the EMR (1/4), CLR (FA+SPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER, DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%, 9.95±0.77% and 261±42%, respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.

  8. Preparation of Hollow Silica Microspheres via Poly(N-isopropylacrylamide)

    Institute of Scientific and Technical Information of China (English)

    Mo-zhen Wang; Yu-chen Chen; Xue-ping Ge; Xue-wu Ge

    2012-01-01

    Core-shell structured SiO2/poly(N-isopropylacrylamide) (SiO2/PNIPAM) microspheres were successfully fabricated through hydrolysis and condensation reaction of tertraethyl orthosilicate (TEOS) on the surface of PNIPAM template at 50 ℃.The PNIPAM template can be easily removed by water at room temperature so that SiO2 hollow microspheres were finally obtained.The transmission electron microscope and scanning electron microscope observations indicated that SiO2 hollow microspheres with an average diameter of 150 nm can be formed only if there are enough concentration of PNIPAM and TEOS,and the hydrolysis time of TEOS.FTIR analysis showed that part of PNIPAM remained on the wall of SiO2 because of the strong interaction between PNIPAM and silica.This work provides a clean and efficient way to prepare hollow microspheres.

  9. MULTI-SCALE STRUCTURES IN EMULSION AND MICROSPHERE COMPLEX SYSTEMS

    Institute of Scientific and Technical Information of China (English)

    Guanghui Ma; Fangling Gong; Guohua Hu; Dongxia Hao; Rong Liu; Renwei Wang

    2005-01-01

    Multi-scale structures involved in emulsion and microsphere complex systems are presented and discussed. The stability and spatio-temporal structures of emulsions, as well as nano-structures formed on the surface of microspheres after polymerization, are affected by the molecular emulsifier/stabilizer structures and the adsorbed emulsifier/stabilizer nano-structures on the oil/water interface. The broad size distribution and variation of surface features of droplets are responsible for variations of the adsorbed emulsifier/stabilizer structures and the stability of the emulsions.On the other hand, preparation of a uniformly sized emulsion and employment of a combined emulsifier/stabilizer system can preserve the stability of the emulsions and microspheres. The above phenomena should be modeled by a multiscale method, in order to maintain the stability of individual emulsion systems and realize the desired nano-structures of microspheres by choosing adequate emulsifier/stabilizer and experimental parameters.

  10. Super-Resolution Real Imaging in Microsphere-Assisted Microscopy

    Science.gov (United States)

    Wang, Feifei; Li, Yi; Jia, Boliang; Liu, Lianqing; Li, Wen Jung

    2016-01-01

    Microsphere-assisted microscopy has received a lot of attention recently due to its simplicity and its capability to surpass the diffraction limit. However, to date, sub-diffraction-limit features have only been observed in virtual images formed through the microspheres. We show that it is possible to form real, super-resolution images using high-refractive index microspheres. Also, we report on how changes to a microsphere’s refractive index and size affect image formation and planes. The relationship between the focus position and the additional magnification factor is also investigated using experimental and theoretical methods. We demonstrate that such a real imaging mode, combined with the use of larger microspheres, can enlarge sub-diffraction-limit features up to 10 times that of wide-field microscopy’s magnification with a field-of-view diameter of up to 9 μm. PMID:27768774

  11. 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.

  12. 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.

  13. Amorphous and nanostructured silica and aluminosilicate spray-dried microspheres

    Science.gov (United States)

    Todea, M.; Turcu, R. V. F.; Frentiu, B.; Tamasan, M.; Mocuta, H.; Ponta, O.; Simon, S.

    2011-08-01

    Amorphous silica and aluminosilicate microspheres with diameters in the 0.1-20 μm range were produced by spray drying method. SEM, TEM and AFM images showed the spherical shape of the obtained particles. Based on thermal analysis data, several heat treatments have been applied on the as-prepared samples in order to check the amorphous state stability of the microspheres and to develop nanosized crystalline phases. As-prepared microspheres remain amorphous up to 1400 °C. By calcination at 1400 °C, cristobalite type nanocrystals are developed on silica sample, while in aluminosilicate sample first are developed mullite type nanocrystals and only after prolonged treatment are developed also cristobalite type nanocrystals. 29Si and 27Al MAS NMR results show that the local order around aluminum and silicon atoms strongly depend on the thermal history of the microspheres.

  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. Development and characterization of ethylcellulose based microsphere for sustained release of nifedipine$

    Institute of Scientific and Technical Information of China (English)

    Patitapabana Parida; Subash Chandra Mishra; Subhashree Sahoo; Ajit Behera; Bibhukalyan Prasad Nayak

    2016-01-01

    This article introduced the work of ethylcellulose based polymeric microsphere loaded with nifedipine for reduction in frequency of administration with low solubility in aqueous medium and high rate of absorption in the stomach. The non-aqueous polymeric suspension was put dropwise into an aqueous medium containing polyvinyl alcohol as a surfactant for the synthesis of microsphere by solvent eva-poration. The microspheres were characterized by different techniques, namely, XRD, SEM, and NMR. The formation of microspheres was confirmed by SEM. XRD analysis revealed the semi-crystallinity nature of microspheres. The NMR study indicated the presence of hetero-aromatic nucleus in the microsphere.

  16. Pharmacokinetics and distributions of bevacizumab by intravitreal injection of bevacizumab-PLGA microspheres in rabbits

    Directory of Open Access Journals (Sweden)

    Zhuo Ye

    2015-08-01

    Full Text Available AIM:To investigate the pharmacokinetics and distributions of bevacizumab by intravitreal injection of prepared bevacizumab-poly (L-lactic-co-glycolic acid (PLGA microspheres in rabbits, to provide evidence for clinical application of this kind of bevacizumab sustained release dosage form.METHODS:Bevacizumab was encapsulated into PLGA microsphere via the solid-in-oil-in-hydrophilic oil (S/O/hO method. Fifteen healthy New Zealand albino-rabbits were used in experiments. The eyes of each rabbit received an intravitreal injection. The left eyes were injected with prepared bevacizumab-PLGA microspheres and the right eyes were injected with bevacizumab solution. After intravitreal injection, rabbits were randomly selected at days 3, 7, 14, 28 and 42 respectively, three animals each day. Then we used immunofluorescence staining to observe the distribution and duration of bevacizumab in rabbit eye tissues, and used the sandwich ELISA to quantify the concentration of free bevacizumab from the rabbit aqueous humor and vitreous after intravitreal injection.RESULTS:The results show that the concentration of bevacizumab in vitreous and aqueous humor after administration of PLGA formulation was higher than that of bevacizumab solution. The T1/2 of intravitreal injection of bevacizumab-PLGA microspheres is 9.6d in vitreous and 10.2d in aqueous humor, and the T1/2 of intravitreal injection of soluble bevacizumab is 3.91d in vitreous and 4.1d in aqueous humor. There were statistical significant difference for comparison the results of the bevacizumab in vitreous and aqueous humor between the left and right eyes (P<0.05. The AUC0-t of the sustained release dosage form was 1-fold higher than that of the soluble form. The relative bioavailability was raised significantly. The immunofluorescence staining of PLGA-encapsulated bevacizumab (b-PLGA in rabbit eye tissues was still observed up to 42d. It was longer than that of the soluble form.CONCLUSION: The result of

  17. Pharmacokinetics and distributions of bevacizumab by intravitreal injection of bevacizumab-PLGA microspheres in rabbits

    Institute of Scientific and Technical Information of China (English)

    Zhuo; Ye; Yan-Li; Ji; Xiang; Ma; Jian-Guo; Wen; Wei; Wei; Shu-Man; Huang

    2015-01-01

    · AIM: To investigate the pharmacokinetics and distributions of bevacizumab by intravitreal injection of prepared bevacizumab-poly(L-lactic-co-glycolic acid)(PLGA) microspheres in rabbits, to provide evidence for clinical application of this kind of bevacizumab sustained release dosage form.·METHODS: Bevacizumab was encapsulated into PLGA microsphere via the solid- in- oil- in- hydrophilic oil(S/O/h O) method. Fifteen healthy New Zealand albino-rabbits were used in experiments. The eyes of each rabbit received an intravitreal injection. The left eyes were injected with prepared bevacizumab-PLGA microspheres and the right eyes were injected with bevacizumab solution. After intravitreal injection, rabbits were randomly selected at day 3, 7, 14, 28 and 42 respectively, three animals each day. Then we used immunofluorescence staining to observe the distribution and duration of bevacizumab in rabbit eye tissues, and used the sandwich ELISA to quantify the concentration of free bevacizumab from the rabbit aqueous humor and vitreous after intravitreal injection.·RESULTS: The results show that the concentration of bevacizumab in vitreous and aqueous humor after administration of PLGA formulation was higher than thatof bevacizumab solution. The T1/2of intravitreal injection of bevacizumab-PLGA microspheres is 9.6d in vitreous and 10.2d in aqueous humor, and the T1/2of intravitreal injection of soluble bevacizumab is 3.91 d in vitreous and4.1d in aqueous humor. There were statistical significant difference for comparison the results of the bevacizumab in vitreous and aqueous humor between the left and right eyes(P <0.05). The AUC0-tof the sustained release dosage form was 1-fold higher than that of the soluble form. The relative bioavailability was raised significantly.The immunofluorescence staining of PLGA-encapsulated bevacizumab(b-PLGA) in rabbit eye tissues was still observed up to 42 d. It was longer than that of the soluble form.· CONCLUSION: The result of this

  18. Quality by design approach for developing chitosan-Ca-alginate microspheres for colon delivery of celecoxib-hydroxypropyl-β-cyclodextrin-PVP complex.

    Science.gov (United States)

    Mennini, N; Furlanetto, S; Cirri, M; Mura, P

    2012-01-01

    The aim of the present work was to develop a new multiparticulate system, designed for colon-specific delivery of celecoxib for both systemic (in chronotherapic treatment of arthritis) and local (in prophylaxis of colon carcinogenesis) therapy. The system simultaneously benefits from ternary complexation with hydroxypropyl-β-cyclodextrin and PVP (polyvinylpyrrolidone), to increase drug solubility, and vectorization in chitosan-Ca-alginate microspheres, to exploit the colon-specific carrier properties of these polymers. Statistical experimental design was employed to investigate the combined effect of four formulation variables, i.e., % of alginate, CaCl₂, and chitosan and time of cross-linking on microsphere entrapment efficiency (EE%) and drug amount released after 4h in colonic medium, considered as the responses to be optimized. Design of experiment was used in the context of Quality by Design, which requires a multivariate approach for understanding the multifactorial relationships among formulation parameters. Doehlert design allowed for defining a design space, which revealed that variations of the considered factors had in most cases an opposite influence on the responses. Desirability function was used to attain simultaneous optimization of both responses. The desired goals were achieved for both systemic and local use of celecoxib. Experimental values obtained from the optimized formulations were in both cases very close to the predicted values, thus confirming the validity of the generated mathematical model. These results demonstrated the effectiveness of the proposed jointed use of drug cyclodextrin complexation and chitosan-Ca-alginate microsphere vectorization, as well as the usefulness of the multivariate approach for the preparation of colon-targeted celecoxib microspheres with optimized properties.

  19. Formulations in first encounters

    NARCIS (Netherlands)

    A. Hak (Tony); F. de Boer (Fijgje)

    1994-01-01

    markdownabstractThe paper describes and compares the use and function of the formulation--decision pair in three types of diagnostic interviewing. The investigatory type of interviewing, which typically occurs in the medical interview, is characterized by the absence of formulations. In the explora

  20. Preparation of biodegradable microspheres and matrix devices containing naltrexone

    OpenAIRE

    DINARVAND, RASSOUL; Moghadam, Shadi H.; Mohammadyari-Fard, Leyla; Atyabi, Fatemeh

    2003-01-01

    In this study, the use of biodegradable polymers for microencapsulation of naltrexone using solvent evaporation technique is investigated. The use of naltrexone microspheres for the preparation of matrix devices is also studied. For this purpose, poly(L-lactide) (PLA) microspheres containing naltrexone prepared by solvent evaporation technique were compressed at temperatures above the Tg of the polymer. The effect of different process parameters, such as drug/polymer ratio and stirring rate d...

  1. In vitro and in vivo toxicity of magnetic microspheres

    Science.gov (United States)

    Häfeli, Urs O.; Pauer, Gayle J.

    1999-04-01

    The interaction of magnetic microspheres with cells was studied using an in vitro 3-[4,5-dimethylthiazol-2yl]-2,5-diphenyltetrazolium bromide (=MTT) assay. Viability and metabolic activity were reduced in all examples. The MTT assay is not recommended for this application due to high variability and non-specificity. Poly(lactic acid) microspheres were further tested in vivo. Intrathecal injection in rats produced no obvious side effects over 12 months.

  2. Multiplexed magnetic microsphere immunoassays for detection of pathogens in foods

    OpenAIRE

    Kim, Jason S.; Chris R Taitt; Ligler, Frances S.; Anderson, George P.

    2010-01-01

    Foodstuffs have traditionally been challenging matrices for conducting immunoassays. Proteins, carbohydrates, and other macromolecules present in food matrices may interfere with both immunoassays and PCR-based tests, and removal of particulate matter may also prove challenging prior to analyses. This has been found true when testing for bacterial contamination of foods using the standard polystyrene microspheres utilized with Luminex flow cytometers. Luminex MagPlex microspheres are encoded ...

  3. CHARACTERIZATION OF CAPTOPRIL-ETHYL CELLULOSE MICROSPHERES BY THERMAL ANALYSIS

    Directory of Open Access Journals (Sweden)

    RakeshGupta

    2010-06-01

    Full Text Available The objective of the present study was to study the physical characterization of Captopril-ethyl cellulose microspheres by thermal analysis such as Differential Scanning Calorimetry (DSC, Differential thermal analysis (DTA and Thermo gravimetry (TG. Drug polymer interaction can directly affect the dosage form stability, drug encapsulation into polymers and dissolution patterns. In this study thermal analysis has been carried out for the physical mixtures and microspheres of captopril and ethyl cellulose prepared by solvent evaporation method.

  4. Novel magnetic nanoparticles coated by benzene- and β-cyclodextrin-bearing dextran, and the sorption of polycyclic aromatic hydrocarbon

    DEFF Research Database (Denmark)

    Cho, Eunae; Tahir, Muhammad Nazir; Min Choi, Jae

    2015-01-01

    We present the synthesis of novel magnetic nanoparticles functionalized by benzene- and β-cyclodextrin-derivatized dextran. The grafting strategy was based on the [alkynyl-iron] cluster in the modified dextrans, which were prepared by click reaction from alkyne-modified dextran and benzyl azide...... or mono-6-O-deoxy-monoazido β-cyclodextrin. Characterization was then carried out by thermogravimetric analysis, Fourier transform infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, and vibrating sample magnetometry. Using the developed magnetic nanoparticles...... to be significant. Furthermore, the polysaccharide derivative-coated magnetic adsorbents could be recovered by an external magnet for reuse....

  5. Inherently fluorescent polystyrene microspheres for coating, sensing and cellular imaging.

    Science.gov (United States)

    Qu, Jian-Bo; Xu, Yu-Liang; Liu, Yu; Wang, Yanan; Sui, Yuanhong; Liu, Jian-Guo; Wang, Xiaojuan

    2017-04-01

    Commercially available polystyrene (PS) fluorescent microspheres are widely used in biological field for tracing, in vivo imaging and calibration of flow cytometry, among other applications. However, these particles do suffer from some drawbacks such as the leakage and photobleaching of organic dyes within them. In the present study, inherently fluorescent properties of PS based microspheres have been explored for the first time. Here we find that a simple chloromethylation reaction endows the polystyrene particles with inherent fluorescence without any subsequent conjugation of an external fluorophore. A possible mechanism for fluorescence is elucidated by synthesizing and investigating p-ethylbenzyl chloride, a compound with similar structure. Significantly, no photobleaching or leaking issues were observed owing to the stable structure of the microspheres. Chloromethylated PS (CMPS) microspheres can keep their perpetual blue fluorescence even in dry powder state making them attractive as a potential coating material. Furthermore, the chloromethyl groups on CMPS microspheres make them very convenient for further functionalization. Poly(ethylene glycol) (PEG) grafted microspheres showed good biocompatibility and negligible cytotoxicity, and could be used to image intracellular Fe(3+) due to the selective fluorescence quenching effect of aqueous Fe(3+) in cytoplasm.

  6. Mucoadhesive microspheres prepared by interpolymer complexation and solvent diffusion method.

    Science.gov (United States)

    Chun, Myung-Kwan; Cho, Chong-Su; Choi, Hoo-Kyun

    2005-01-20

    Mucoadhesive microspheres were prepared to increase gastric residence time using an interpolymer complexation of poly(acrylic acid) (PAA) with poly(vinyl pyrrolidone) (PVP) and a solvent diffusion method. The complexation between poly(acrylic acid) and poly(vinyl pyrrolidone) as a result of hydrogen bonding was confirmed by the shift in the carbonyl absorption bands of poly(acrylic acid) using FT-IR. A mixture of ethanol/water was used as the internal phase, corn oil was used as the external phase of emulsion, and span 80 was used as the surfactant. Spherical microspheres were prepared and the inside of the microspheres was completely filled. The optimum solvent ratio of the internal phase (ethanol/water) was 8/2 and 7/3, and the particle size increased as the content of water was increased. The mean particle size increased with the increase in polymer concentration. The adhesive force of microspheres was equivalent to that of Carbopol. The release rate of acetaminophen from the complex microspheres was slower than the PVP microspheres at pH 2.0 and 6.8.

  7. Validity of microsphere depositions for regional myocardial flows

    Energy Technology Data Exchange (ETDEWEB)

    Bassingthwaighte, J.B.; Malone, M.A.; Moffett, T.C.; King, R.B.; Little, S.E.; Link, J.M.; Krohn, K.A.

    1987-07-01

    Due to the particulate nature of microspheres, their deposition in small-tissue regions may not be strictly flow dependent. To evaluate the importance of rheological and geometric factors and random error, their deposition densities in small regions of rabbit hearts were examined in comparison with those of a new molecular microsphere, 2-iododesmethylimipramine (IDMI), whose high lipid solubility allows it to be delivered into tissue in proportion to flow, and whose binding in tissue prevents rapid washout. /sup 141/Ce- and /sup 103/Ru-labeled 16.5-..mu..m spheres in one syringe and (/sup 125/I)- and (/sup 131/I)DMI in another syringe were injected simultaneously into the left atrium of open-chest rabbits, while obtaining reference blood samples from the femoral artery. Hearts were removed 1 min after injection, cut into /approximately/ 100 pieces averaging 54 mg, and the regional deposition densities calculated for each tracer from the isotopic counts. Scatter plots of sphere densities vs. IDMI densities showed that differences between microspheres and IDMI had substantial scatter and were not random. Microsphere depositions tended to be lower that IDMI deposition at low flows and higher at high flows. The authors conclude that microspheres are generally adequate for estimating regional flows but suffer systematic error when the regions of interest are supplied via arteries of diameters only a few times those of microspheres.

  8. Microspheres and Nanotechnology for Drug Delivery.

    Science.gov (United States)

    Jóhannesson, Gauti; Stefánsson, Einar; Loftsson, Thorsteinn

    2016-01-01

    Ocular drug delivery to the posterior segment of the eye can be accomplished by invasive drug injections into different tissues of the eye and noninvasive topical treatment. Invasive treatment involves the risks of surgical trauma and infection, and conventional topical treatments are ineffective in delivering drugs to the posterior segment of the eye. In recent years, nanotechnology has become an ever-increasing part of ocular drug delivery. In the following, we briefly review microspheres and nanotechnology for drug delivery to the eye, including different forms of nanotechnology such as nanoparticles, microparticles, liposomes, microemulsions and micromachines. The permeation barriers and anatomical considerations linked to ocular drug delivery are discussed and a theoretical overview on drug delivery through biological membranes is given. Finally, in vitro, in vivo and human studies of x03B3;-cyclodextrin nanoparticle eyedrop suspensions are discussed as an example of nanotechnology used for drug delivery to the eye.

  9. Nonstationary photonic jet from dielectric microsphere

    CERN Document Server

    Geints, Yu; Zemlyanov, A

    2014-01-01

    A photonic jet commonly denotes the specific spatially localized region in the near-field forward scattering of a light wave at a dielectric micron-sized particle. We present the detailed calculations of the transient response of an airborne silica microsphere illuminated by a femtosecond laser pulse. The spatial area constituting the photonic jet is theoretically investigated and the temporal dynamics of jet dimensions as well as of jet peak intensity is analyzed. The role of morphology-dependent resonances in jet formation is highlighted. The evolution scenario of a nonstationary photonic jet generally consists of the non-resonant and resonant temporal phases. In every phase, the photonic jet can change its spatial form and intensity.

  10. Thermal analysis of SYNROC gel microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Knipschild, K.E.; Lee, D.A.

    1981-11-01

    Thermoanalytical methods were used to characterize SYNROC microspheres at three stages of the internal gelation process: unwashed spheres, washed spheres, and washed-and-dried spheres. Linear-programmed heating experiments were performed using thermogravimetric analysis, differential scanning calorimetry, differential thermal analysis, and mass spectrometry for producing the thermograms. The data were used to elucidate thermal reactions occurring between ambient and 800/sup 0/C. The principal reactions were the release of waters from various sources, the decomposition and combustion of gelation additives (hexamethylenetetramine and urea), and the decomposition of carbonates. Data also demonstrated the efficiency of the washing process. Kinetic studies were carried out by differential scanning calorimetry and differential thermal analysis to determine activation energies for certain pyrolysis reactions. 8 figures.

  11. Permeability of Hollow Microspherical Membranes to Helium

    Science.gov (United States)

    Zinoviev, V. N.; Kazanin, I. V.; Pak, A. Yu.; Vereshchagin, A. S.; Lebiga, V. A.; Fomin, V. M.

    2016-01-01

    This work is devoted to the study of the sorption characteristics of various hollow microspherical membranes to reveal particles most suitable for application in the membrane-sorption technologies of helium extraction from a natural gas. The permeability of the investigated sorbents to helium and their impermeability to air and methane are shown experimentally. The sorption-desorption dependences of the studied sorbents have been obtained, from which the parameters of their specific permeability to helium are calculated. It has been established that the physicochemical modification of the original particles exerts a great influence on the coefficient of the permeability of a sorbent to helium. Specially treated cenospheres have displayed high efficiency as membranes for selective extraction of helium.

  12. Preparation and evaluation of Levosalbutamol sulphate chitosan microsphere for the treatment of asthma

    Directory of Open Access Journals (Sweden)

    D Dinal Patel

    2012-01-01

    Full Text Available Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In present work, mucoadhesive chitosan microspheres of Levosalbutamol sulphate were prepared by Spray drying method. Formulations were characterized for various physicochemical attributes size, encapsulation efficiency, swelling ability, in vitro release study and mucoadhesion study by rat ileum. Through these parameters we conclude that the batch B 2 was found to be best mainly by mucoadhesion study and in vitro drug release. Mucoadhesion was found to be increased with incresed concentration of polymer and visa versa in case of drug release. Batch B 3 had also similar results with that of Batch B 2 . That′s why here Batch B 2 was said to be the best batch with less polymeric content as compare to Batch B 3 .

  13. Formulation of microspheres containing Crataegus monogyna Jacq. extract with free radical scavenging activity.

    Science.gov (United States)

    Lucconi, Giulia; Chlapanidas, Theodora; Martino, Emanuela; Gaggeri, Raffaella; Perteghella, Sara; Rossi, Daniela; Faragò, Silvio; Vigo, Daniele; Faustini, Massimo; Collina, Simona; Torre, Maria Luisa

    2014-02-01

    Extracts of Crataegus monogyna Jacq. (hawthorn) show an interesting free radical scavenging (FRS) effect, related to their flavonoids content. Unfortunately, their oral administration is affected by their low bioavailability. The aim of this work is to obtain a multiparticulate drug delivery system for hawthorn extracts for oral administration. The extracts from flowering tops (FL) or fruits (FR) of hawthorn were obtained with maceration, using ethanol as an extraction solvent, and their antioxidant activity was evaluated. FL extract showed the highest FRS activity (EC50 3.72 ± 1.21 µg/ml), so it was selected to prepare microparticulate systems by a spray-drying technique, which were characterized by granulometric analysis, scanning electron microscopy-energy dispersive X-ray spectroscopy, confocal fluorescence microscopy and hyperoside content. Antioxidant activity was evaluated before and after gastrointestinal transit in vitro simulation. Results indicate that the microparticulate systems maintained the antioxidant activity of hawthorn also after gastrointestinal transit in vitro simulation, exhibiting properties suitable for oral administration.

  14. Formulation And Performance Evaluation Of Betahistine Dihydrochloride Microspheres As Sustained Release Systems

    Directory of Open Access Journals (Sweden)

    Pilicheva Bissera A.

    2014-09-01

    Full Text Available Бетагистин дигидрохлорид представляет собой гистаминовый аналог, широко применяемый для облегчения симптомов, сопутствующих синдром Мениера. По данным фармакокинетических исследований бетагистамин имеет краткую плазменную полужизнь - 3.4 ч. В таких случаях, чтобы поддерживать концентрацию плазмы во время терапевтического „окна”, приходится вводить лекарственное вещество часто, через небольшие интервалы. Это может привести к отсутствию содействия при проведении лечения со стороны пациента, как и к ухудшению его комфорта. Современный подход достижения удлиненного освобождения лекарства заключается в его включении в частицы-носители. ЦЕЛЬ: Разработать лекарство-доставляющую систему с удлиненным освобождением бетагистина, что способствовало бы уменьшению частоты приема и снижению риска появления нежелательных лекарственных реакций. МАТЕРИАЛЫ И МЕТОДЫ: Микросферы получены через W/О эмульсионную технику с испарением растворителя и охарактеризованы по отношению к их размеру, оличественному содержанию бетагистина и эффективности нагрузки. Освобождение с бетагистином, приготовленные через эмульсионную технику с испарением растворителя, показывают склонность к удлиненному освобождению и имеют потенциал лекарствено-освобождающих систем при лечении синдрома Мениера

  15. Formulation techniques for nanofluids.

    Science.gov (United States)

    Rivera-Solorio, Carlos I; Payán-Rodríguez, Luis A; García-Cuéllar, Alejandro J; Ramón-Raygoza, E D; L Cadena-de-la-Peña, Natalia; Medina-Carreón, David

    2013-11-01

    Fluids with suspended nanoparticles, commonly known as nanofluids, may be formulated to improve the thermal performance of industrial heat transfer systems and applications. Nanofluids may show enhanced thermal and electrical properties such as thermal conductivity, viscosity, heat transfer coefficient, dielectric strength, etc. However, stability problems may arise as nanoparticles usually have the tendency to agglomerate and sediment producing deterioration in the increment of these properties. In this review, we discuss patents that report advances in the formulation of nanofluids including: production methods, selection of components (nanoparticles, base fluid and surfactants), their chemical compositions and morphologies, and characterization techniques. Finally, current and future directions in the development of nanofluid formulation are discussed.

  16. Formation of nanoparticles by cooperative inclusion between (S-camptothecin-modified dextrans and β-cyclodextrin polymers

    Directory of Open Access Journals (Sweden)

    Thorbjørn Terndrup Nielsen

    2015-01-01

    Full Text Available Novel (S-camptothecin–dextran polymers were obtained by “click” grafting of azide-modified (S-camptothecin and alkyne-modified dextrans. Two series based on 10 kDa and 70 kDa dextrans were prepared with a degree of substitution of (S-camptothecin between 3.1 and 10.2%. The binding properties with β-cyclodextrin and β-cyclodextrin polymers were measured by isothermal titration calorimetry and fluorescence spectroscopy, showing no binding with β-cyclodextrin but high binding with β-cyclodextrin polymers. In aqueous solution nanoparticles were formed from association between the (S-camptothecin–dextran polymers and the β-cyclodextrin polymers.

  17. Demagnetization treatment of remanent composite microspheres studied by alternating current susceptibility measurements

    NARCIS (Netherlands)

    van Berkum, S.; Erné, B.H.

    2013-01-01

    The magnetic remanence of silica microspheres with a low concentration of embedded cobalt ferrite nanoparticles is studied after demagnetization and remagnetization treatments. When the microspheres are dispersed in a liquid, alternating current (AC) magnetic susceptibility spectra reveal a constant

  18. In Vitro Cytotoxicity and Protein Drug Release Properties of Chitosan/Heparin Microspheres

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Chitosan/heparin microspheres were prepared using the water-in-oil emulsification solvent evaporation technique. The microsphere diameters were controlled by selecting the fabrication process parameters. Scanning electron micrographs showed that the chitosan/heparin microspheres were regular and the surface morphology was smooth. Fourier transform infrared showed that the chitosan amino groups reacted with heparin carboxylic groups to form acylamides in the microspheres. Analysis of the microsphere cytotoxicity showed that they had no cytotoxic effect and behaved very similar to the negative control (polystyrene).To analyze the protein drug release profiles of the microspheres, bovine serum albumin was loaded as a model drug into the microspheres and released in vitro. Marked retardation was observed in the BSA release profiles. The results show that chitosan/heparin microspheres may provide a useful controlled release protein drug system for used in pharmaceutics.

  19. Preparation of polysulfone hollow microspheres encapsulating DNA and their functional utilization.

    Science.gov (United States)

    Zhao, C; Liu, X D; Nomizu, M; Nishi, N

    2004-05-01

    Polysulfone hollow microspheres encapsulating DNA were prepared using a liquid-liquid phase separation technique. The microspheres were then used to absorb a DNA-binding intercalating material--ethidium bromide. The amount of DNA encapsulated in the microspheres depended on the concentration of the DNA solution used to prepare the microspheres, and the microsphere morphology depended on both the polymer concentration and the preparation conditions. The amount of ethidium bromide in the microspheres depended mainly on the amount of encapsulated DNA, and the microsphere morphology also affected the removal of the ethidium bromide. The new method of DNA encapsulation is proposed, and the microspheres encapsulating the DNA have the potential to be used in environmental applications.

  20. The effects of synthesis method on the physical and chemical properties of dextran coated iron oxide nanoparticles.

    Science.gov (United States)

    Hauser, Anastasia K; Mathias, Ronita; Anderson, Kimberly W; Hilt, J Zach

    2015-06-15

    Iron oxide nanoparticles coated with dextran were synthesized via four variations on the co-precipitation method. The methods ranged from in situ formation of the nanoparticles within the dextran solution to the adsorption of dextran to the nanoparticle surface following nucleation and extensive washing. The timing of the addition of dextran into the reaction mixture was found to greatly influence the physical and chemical properties of the magnetic nanoparticles. Batches of dextran coated iron oxide nanoparticles were synthesized by each method in triplicate, and the nanoparticles were further crosslinked with epichlorohydrin. The properties of the nanoparticles such as size, percentage of dextran coating, stability in solution, crystallinity, and magnetic properties were evaluated. The simultaneous semi-two-step method injected the reducing agent and the dextran solution into the reaction vessel at the same time. This method resulted in the greatest batch-to-batch reproducibility of nanoparticle properties and the least variation in nanoparticles synthesized in the same batch. The two-step method resulted in the greatest variation of the characteristics examined between batches. The one-step method was synthesized with both five grams and one gram of dextran to investigate the effects of solution viscosity on the resulting nanoparticle characteristics. The one-step method with five grams of dextran resulted in nanoparticles with significantly smaller crystal sizes (5.4 ± 1.9 nm) and lower specific adsorption rate (SAR) values (138.4 ± 13.6 W/g) in an alternating magnetic field (58 kA/m, 292 kHz). However, this method resulted in nanoparticles that were very stable in PBS over 12 hours, which is most likely due to the greater dextran coating (60.0 ± 2.7 weight percent). For comparison, the simultaneous semi-two-step method generated nanoparticles 179.2 ± 18.3 nm in diameter (crystal size 12.1 ± 0.2 nm) containing 18.3 ± 1.2 weight percent dextran with a SAR

  1. Stability and in vitro DNA packaging of bacteriophages: effects of dextrans, sugars, and polyols

    Energy Technology Data Exchange (ETDEWEB)

    Serwer, P. (The Univ. of Texas Health Science Center, San Antonio); Masker, W.E.; Allen, J.L.

    1983-02-01

    Attempts were made to increase the efficiency of infectious particle formation during the in vitro assembly of bacteriophage T7 from procapsids and DNA. It was found that dextrans and some smaller, related compounds (sucrose and sorbitol) increase this efficiency by a factor of 8 to 50. Dextrans also inhibited elevated temperature-induced emptying of DNA from bacteriophages T7, P22, and T4, suggesting that the stimulation of assembly is caused, at least in part, by the stabilization of packaged DNA in capsids. The data indicated that the sugars and polyols can slow DNA emptying from bacteriophages at elevated temperature whether they permeate the bacteriophage capsid or not. In contrast, the data suggested that permeation of some particle, probably a capsid, results in inhibition of in vitro T7 assembly.

  2. Hemodynamic and regional blood flow distribution responses to dextran, hydralazine, isoproterenol and amrinone during experimental cardiac tamponade

    Energy Technology Data Exchange (ETDEWEB)

    Millard, R.W.; Fowler, N.O.; Gabel, M.

    1983-06-01

    Four different interventions were examined in dogs with cardiac tamponade. Infusion of 216 to 288 ml saline solution into the pericardium reduced cardiac output from 3.5 +/- 0.3 to 1.7 +/- 0.2 liters/min as systemic vascular resistance increased from 4,110 +/- 281 to 6,370 +/- 424 dynes . s . cm-5. Left ventricular epicardial and endocardial blood flows were 178 +/- 13 and 220 +/- 12 ml/min per 100 g, respectively, and decreased to 72 +/- 14 and 78 +/- 11 ml/min per 100 g with tamponade. Reductions of 25 to 65% occurred in visceral and brain blood flows and in a composite brain sample. Cardiac output during tamponade was significantly increased by isoproterenol, 0.5 microgram/kg per min intravenously; hydralazine, 40 mg intravenously; dextran infusion or combined hydralazine and dextran, but not by amrinone. Total systemic vascular resistance was reduced by all interventions. Left ventricular epicardial flow was increased by isoproterenol, hydralazine and the hydralazine-dextran combination. Endocardial flow was increased by amrinone and the combination of hydralazine and dextran. Right ventricular myocardial blood flow increased with all interventions except dextran. Kidney cortical and composite brain blood flows were increased by both dextran alone and by the hydralazine-dextran combinations. Blood flow to small intestine was increased by all interventions as was that to large intestine by all except amrinone and hydralazine. Liver blood flow response was variable. The most pronounced hemodynamic and tissue perfusion improvements during cardiac tamponade were effected by combined vasodilation-blood volume expansion with a hydralazine-dextran combination. Isoproterenol had as dramatic an effect but it was short-lived. Amrinone was the least effective intervention.

  3. Capillary Zone Electrophoresis Investigation of Interactions between Granulocyte-colony Stimulating Factor and Dextran Sulfate / Carrageenan Oligosaccharide

    Institute of Scientific and Technical Information of China (English)

    Ai Ye LIANG; Yu Guang DU; Ke Yi WANG; Bing Cheng LIN

    2005-01-01

    The interactions between granulocyte-colony stimulating factor (G-CSF) and dextran sulfate / κ-carrageenan oligosa1ccharide were studied by capillary zone electrophoresis. Dextran sulfate could strongly interact with G-CSF and the complex was detected. The binding constant and stoichiometry were determined to be 1.2x106 (mol/L)-1 and 3:1, respectively. However, the interaction between κ-carrageenan oligosaccharide and G-CSF was not found.

  4. Assessment of strategy formulation

    DEFF Research Database (Denmark)

    Acur, Nuran; Englyst, Linda

    2006-01-01

    . Practical implications – The integration of three different strategy assessment approaches has been made to obtain a holistic, multi-perspective reflection on strategy formulation. Such reflection is assumed to enable managers to proactively evaluate the potential outcome and performance of their chosen......Purpose – Today, industrial firms need to cope with competitive challenges related to innovation, dynamic responses, knowledge sharing, etc. by means of effective and dynamic strategy formulation. In light of these challenges, the purpose of the paper is to present and evaluate an assessment tool...... for strategy formulation processes that ensures high quality in process and outcome. Design/methodology/approach – A literature review was conducted to identify success criteria for strategy formulation processes. Then, a simple questionnaire and assessment tool was developed and used to test the validity...

  5. Magnetic investigation of zero-field-cooled dextran-coated magnetite-based magnetic fluid

    Energy Technology Data Exchange (ETDEWEB)

    Morais, P.C. [Universidade de Brasilia, Instituto de Fisica, Fisica Aplicada, C.P. 004455, Campus Universitario, Brasilia-DF 70919 970 (Brazil)]. E-mail: pcmor@unb.br; Santos, J.G. [Universidade de Brasilia, Instituto de Fisica, Fisica Aplicada, C.P. 004455, Campus Universitario, Brasilia-DF 70919 970 (Brazil); Silveira, L.B. [Universidade de Brasilia, Instituto de Fisica, Fisica Aplicada, C.P. 004455, Campus Universitario, Brasilia-DF 70919 970 (Brazil); Nunes, W.C. [Universidade Federal doRio de Janeiro, Instituto de Fisica, 21945-970, Rio de Janeiro-RJ (Brazil); Sinnecker, J.P. [Universidade Federal doRio de Janeiro, Instituto de Fisica, 21945-970, Rio de Janeiro-RJ (Brazil); Novak, M.A. [Universidade Federal doRio de Janeiro, Instituto de Fisica, 21945-970, Rio de Janeiro-RJ (Brazil)

    2005-03-15

    In this study, we investigate the temperature dependence of the zero-field-cooled magnetization of a quasi-monodisperse dextran-coated magnetite-based magnetic fluid. The well-defined maximum in the magnetization versus temperature curve and its downshift with the applied external field is explained by a simple model considering thermally activated dynamics of the nanoparticles magnetic moment and the temperature dependence of the saturation magnetization.

  6. Dextran X 500. sup(99m)Tc in abdominal lymphoscintillation

    Energy Technology Data Exchange (ETDEWEB)

    Ceriani, J.; Caneda, G.; Rozados, I. (Hospital Ramos Mejia, Buenos Aires (Argentina). Div. Medicina Nuclear); Arguelles, M.G.; Canellas, C.O.; Mitta, A.E.A. (Comision Nacional de Energia Atomica, Buenos Aires (Argentina))

    1984-01-01

    The preparation of Dextran X 500 sup(99m)Tc, its control and biological behaviour in animals are described. Its use in the study of lymphatic system in human beings is also indicated. This method is of easy preparation and of great stability, both in vitro and in vivo, and besides it can be used in lymphoscintillation as well as for the study of blood pool.

  7. Fabrication and characterization of ultrathin dextran layers: Time dependent nanostructure in aqueous environments revealed by OWLS.

    Science.gov (United States)

    Saftics, Andras; Kurunczi, Sándor; Szekrényes, Zsolt; Kamarás, Katalin; Khánh, Nguyen Quoc; Sulyok, Attila; Bősze, Szilvia; Horvath, Robert

    2016-10-01

    Surface coatings of the polysaccharide dextran and its derivatives are key ingredients especially in label-free biosensors for the suppression of non-specific binding and for receptor immobilization. Nevertheless, the nanostructure of these ultrathin coatings and its tailoring by the variation of the preparation conditions have not been profoundly characterized and understood. In this work carboxymethylated dextran (CMD) was prepared and used for fabricating ultrathin surface coatings. A grafting method based on covalent coupling to aminosilane- and epoxysilane-functionalized surfaces was applied to obtain thin CMD layers. The carboxyl moiety of the CMD was coupled to the aminated surface by EDC-NHS reagents, while CMD coupling through epoxysilane molecules was performed without any additional reagents. The surface analysis following the grafting procedures consisted of X-ray photoelectron spectroscopy (XPS), attenuated total reflection infrared spectroscopy (ATR-IR), spectroscopic ellipsometry, atomic force microscopy (AFM) and optical waveguide lightmode spectroscopy (OWLS). The XPS and AFM measurements showed that the grafting resulted in a very thin dextran layer of a few nanometers. The OWLS method allowed devising the structure of the interfacial dextran layers by the evaluation of the optogeometrical parameters. The alteration in the nanostructure of the CMD layer with the chemical composition of the silane coverage and the pH of the grafting solution was revealed by in situ OWLS, specifically, lain down chains were found to be prevalent on the surface under neutral and basic conditions on epoxysilylated surfaces. The developed methodologies allowed to design and fabricate nanometer scale CMD layers with well-controlled surface structure, which are very difficult to characterize in aqueous environments using present instrumentations and highly hydrated surface layers.

  8. Safety and efficacy of iron sucrose in patients sensitive to iron dextran: North American clinical trial.

    Science.gov (United States)

    Van Wyck, D B; Cavallo, G; Spinowitz, B S; Adhikarla, R; Gagnon, S; Charytan, C; Levin, N

    2000-07-01

    Sensitivity to iron dextran is a potent obstacle to maintaining optimum iron status in patients with dialysis-associated anemia. As part of the North American clinical trials for iron sucrose injection, we examined the effect of intravenous (IV) iron sucrose in 23 hemodialysis patients with documented sensitivity to iron dextran, ongoing epoetin alfa therapy, and below-target-range hemoglobin (Hgb) levels (iron dextran were judged to be mild (n = 16; group A) or severe (n = 7; group B). We prospectively examined adverse events and vital signs after administering 100 mg of IV iron sucrose in each of 10 consecutive dialysis treatment sessions and compared results with those recorded in each of three consecutive dialysis sessions without iron treatment. We administered iron sucrose by IV push over 5 minutes to group A patients and by IV push over 5 minutes or IV infusion over 15 to 30 minutes to group B patients. We did not administer a test dose. Results showed no serious adverse drug reactions after a total of 223 doses of iron sucrose (184 doses by IV push, 39 doses by IV infusion). Intradialytic blood pressure changes after IV iron sucrose injection did not differ from those recorded during dialysis sessions without treatment. An increase in values for Hgb, hematocrit, transferrin saturation, and ferritin, coupled with no significant change in epoetin dose and a decrease in total iron-binding capacity, confirmed the efficacy of iron sucrose injection in managing anemia. We conclude that iron sucrose injection is safe and effective in the management of anemia in patients sensitive to iron dextran and can be administered without a test dose by IV push or infusion.

  9. Effects of orally administered bovine lactoperoxidase on dextran sulfate sodium-induced colitis in mice.

    Science.gov (United States)

    Shin, Kouichirou; Horigome, Ayako; Yamauchi, Koji; Takase, Mitsunori; Yaeshima, Tomoko; Iwatsuki, Keiji

    2008-07-01

    The effect of lactoperoxidase (LPO) on dextran sulfate sodium-induced colitis was examined in mice. After 9 d of colitis induction, weight loss, colon shortening, and the histological score were significantly suppressed in mice orally administered LPO (62.5 mg/body/d) as compared to a group administered bovine serum albumin. These results suggest that LPO exhibits anti-inflammatory effects in the gastrointestinal tract.

  10. Fabrication and characterization of porous hydroxyapatite microspheres by spray-drying method

    Institute of Scientific and Technical Information of China (English)

    Rui-xue SUN; Yu-peng LU

    2008-01-01

    In the present paper, porous hydroxyapatite (HA) microspheres were fabricated using gelatin as a pore-forming agent by spray-drying method. The mean particle size of the microspheres is about 7 μm and the surface area is about 53.4 m2/g. The experimental results showed that the porosity of the prepared microspheres is higher and the pores are more interconnected compared with the microspheres obtained without any additives.

  11. Silica Microspheres Are Superior to Polystyrene for Microvesicle Analysis by Flow Cytometry

    Science.gov (United States)

    2015-02-16

    Regular Article Silica microspheres are superior to polystyrene for microvesicle analysis by flow cytometry☆ Bijaya Kumar Parida ⁎, Hiram Garrastazu...February 2015 Available online 16 February 2015 Keywords: Microvesicles Cell-derived microparticles Silica microspheres Polystyrene microspheres ...is used to characterize MVs. Polystyrene microspheres are often used in flow cytometry to distinguish MV from cells by setting a 1-μm MV gate in a

  12. Preparation of Dysprosium Ferrite/Polyacrylamide Magnetic Composite Microsphere and Its Characterization

    Institute of Scientific and Technical Information of China (English)

    Hidehiro Kumazawa; Wang Zhifeng; Zhou Lanxiang; Zhang Hong; Li Yourong; Zhang Ming

    2005-01-01

    Using the technique of microemulsion polymerization with nano-reactor, dysprosium ferrite/polyacrylamide magnetic composite microsphere was prepared by one-step method in a single inverse microemulsion. The structure, average particle size, morphology of composite microsphere were characterized by FTIR, XRD, TEM and TGA. The magnetic responsibility of composite microsphere was also investigated. The results indicate that the magnetic composite microsphere possess high magnetic responsibility and suspension stability.

  13. The synthesis and photocatalytic activity of ZnSe microspheres.

    Science.gov (United States)

    Cao, Huaqiang; Xiao, Yujiang; Zhang, Sichun

    2011-01-07

    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.

  14. The synthesis and photocatalytic activity of ZnSe microspheres

    Science.gov (United States)

    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 (C4H4 Se) and ZnCl2 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.

  15. A quality by design (QbD) study on enoxaparin sodium loaded polymeric microspheres for colon-specific delivery.

    Science.gov (United States)

    Hales, Dana; Vlase, Laurian; Porav, Sebastian Alin; Bodoki, Andreea; Barbu-Tudoran, Lucian; Achim, Marcela; Tomuță, Ioan

    2017-03-30

    The aim of this study was to apply quality by design (QbD) for pharmaceutical development of enoxaparin sodium microspheres for colon-specific delivery. The Process Parameters (CPPs) and Critical Quality Attributes (CQAs) were identified. A central composite experimental design was used in order to develop the design space of microspheres for colon-specific delivery that have the desired Quality Target Product Profile (QTPP). The CPPs studied were Eudragit® FS-30D/Eudragit® RS-PO ratio, poly(vinyl alcohol) (PVA) concentration and sodium chloride (NaCl) concentration. The encapsulation efficiency increased with NaCl concentration increase, the percentages of enoxaparin sodium reaching 94% for some formulations. Increasing the ratio Eudragit® FS-30D/Eudragit® RS-PO ensured a relatively complete release of enoxaparin sodium in the environment simulating the colonic pH. Based on these results, the optimum conditions were decided and the optimum formulation was prepared. The results obtained for the latter in terms of in vitro enoxaparin sodium release were good, the microparticles releasing only 9.42% enoxaparin sodium in acidic environment and 15.16% in the medium which simulated duodenal pH, but allowing the release of up to 89.24% in the medium which simulated colonic pH. The in vitro release profile of enoxaparin sodium was close to the ideal one, therefore the system was successfully designed using QbD approach.

  16. Correlation between UV-VIS spectra and the structure of Cu(II complexes with hydrogenated dextran in alkaline solutions

    Directory of Open Access Journals (Sweden)

    Nikolić Goran S.

    2005-01-01

    Full Text Available UV-VIS spectrophotometric investigations of Cu(II complexes with hydroge-nated dextran showed that the complexation of Cu(II-ions began at pH > 7. The formation of Cu(II complexes with dextran monomer units was observed at pH 7-12. With further increase in solution pH > 12, the Cu(II-dextran complex decomposed to Cu(OH42~-ions and dextran. With increasing solution pH the absorption maximum of complex solutions increased and shifted to shorter wavelength (hypsochromic shift compared with uncomplexed Cu(II. The UV spectra displayed bathochromic shifts. The changes of UV-VIS spectra with increasing in solution pH confirmed the formation of different kinds of complex species. The correlation between the results of UV-VIS spectrophotometry and the central metal ionligand coordination predicted that the copper binding within the complex depended on the pH and participation H2O molecules. Dextran complexes with Cu(II were formed by the displacement of water molecules from the coordination sphere of copper by OH groups. The analysis indicated that the Cu(II center was coordinated to two glucopyranose units of dextran. The spectrophotometric parameters of the investigated complexes were characteristic of a Cu(II-ion in a square-planar or tetragon ally distorted octahedral coordination.

  17. Differential inhibition of polymorphonuclear leukocyte recruitment in vivo by dextran sulphate and fucoidan

    Directory of Open Access Journals (Sweden)

    N. Van Osselaer

    1996-01-01

    Full Text Available The selectin-mediated rolling of leukocytes along the endothelial cells is a prerequisite step followed by firm adhesion and extravasation into the inflamed tissue. This initial contact can be suppressed by sulphated polysaccharides. We have studied the effect of sulphated polysaccharides on the ultimate polymorphonuclear leukocyte (PMN recruitment and plasma leakage in rabbit skin in response to intradermal injection of various inflammatory mediators. PMN infiltration evoked by various PMN chemoattractants (FMLP, C5a desArg, LTB4 and IL-8 was significantly inhibited after intravenous injection of dextran sulphate (25 mg/kg, heparin (2 × 90 mg/kg or fucoidan (1 mg/kg. PMN-dependent plasma leakage was equally well reduced by the different sulphated polymers. Vascular permeability induced by histamine or thrombin acting via a PMN-independent mechanism was not reduced. Fucoidan was the only polysaccharide able to suppress IL-1-induced PMN infiltration for 60–70%. Local administration of dextran sulphate had no effect on PMN-dependent plasma leakage. Differential inhibition of PMN recruitment was determined after injection of dextran sulphate or fucoidan depending on the type of insult. Therefore, these results suggest that different adhesion pathways are utilized during PMN recruitment in vivo in response to chemoattractants and IL-1.

  18. Magnetic retardance and magnetic heating in dextran-citrate coated ferrofluids

    Directory of Open Access Journals (Sweden)

    Jing-Fung Lin

    2017-02-01

    Full Text Available The Fe3O4 magnetic nanoparticles (MNPs coated by citrate and dextran prepared by the co-precipitation method was described. Influence induced by the mass variation of coating dextran was investigated. Magneto-optical birefringence of biocompatible dextran-citrate (DC coated ferrofluids (FFs was obtained by the Stokes polarimeter. Next, uniform design method was used to find the DC coated FF with high retardance and low dichroism. Retardance of the optimized A9 sample with 1 g/ml was measured as 56.7898° (dichroism was 0.3716 under 64.5 mT. Further, magnetic heating effect in alternating magnetic field was investigated. When the concentrations of A9 were of 2 mg/ml and 50 mg/ml, under the external alternating magnetic field with applied apparent current of 210 A, after heating 5 s the temperature of the DC coated FFs was greater than 47 °C, respectively, reached the requirements for the magnetic inductive heating treatment of cancer tumor. The potential of DC coated FFs in hyperthermia was highly evaluated.

  19. Hybridization chain reaction amplification for highly sensitive fluorescence detection of DNA with dextran coated microarrays.

    Science.gov (United States)

    Chao, Jie; Li, Zhenhua; Li, Jing; Peng, Hongzhen; Su, Shao; Li, Qian; Zhu, Changfeng; Zuo, Xiaolei; Song, Shiping; Wang, Lianhui; Wang, Lihua

    2016-07-15

    Microarrays of biomolecules hold great promise in the fields of genomics, proteomics, and clinical assays on account of their remarkably parallel and high-throughput assay capability. However, the fluorescence detection used in most conventional DNA microarrays is still limited by sensitivity. In this study, we have demonstrated a novel universal and highly sensitive platform for fluorescent detection of sequence specific DNA at the femtomolar level by combining dextran-coated microarrays with hybridization chain reaction (HCR) signal amplification. Three-dimensional dextran matrix was covalently coated on glass surface as the scaffold to immobilize DNA recognition probes to increase the surface binding capacity and accessibility. DNA nanowire tentacles were formed on the matrix surface for efficient signal amplification by capturing multiple fluorescent molecules in a highly ordered way. By quantifying microscopic fluorescent signals, the synergetic effects of dextran and HCR greatly improved sensitivity of DNA microarrays, with a detection limit of 10fM (1×10(5) molecules). This detection assay could recognize one-base mismatch with fluorescence signals dropped down to ~20%. This cost-effective microarray platform also worked well with samples in serum and thus shows great potential for clinical diagnosis.

  20. DNA replication by a possible continuous--discontinuous mechanism in homogenates of Physarum polycephalum containing dextran

    Energy Technology Data Exchange (ETDEWEB)

    Brewer, E.N.

    1975-01-01

    Nuclear DNA synthesis in homogenates of Physarum is greatly stimulated by the presence of dextran in the homogenizing medium. In this cell-free system, the DNA precursor is incorporated approximately equally into two classes of DNA intermediates. One of these is similar in size to that observed previously in the intact organism, i.e., its sedimentation rate in alkaline sucrose density gradients increases, presumably by chain elongation, as the organism progresses through the S phase. The other class (approx. 10S) is similar to ''Okazaki'' fragments. Thus, nuclear DNA synthesis in homogenates of Physarum may occur by a continuous-discontinuous mechanism. Substantial DNA-synthetic activity is obtained by the addition of dextran to dextran-free homogenates. Maximal activity in this system requires the presence of both the nuclear and post-nuclear supernatant fractions. It is possible that a partial separation and recombination of a DNA polymerase and the endogenous template is effected by this procedure. (auth)

  1. Prevent Effects of Lactobacillus Fermentum HY01 on Dextran Sulfate Sodium-Induced Colitis in Mice

    Science.gov (United States)

    Chen, Xiaoyong; Zhao, Xin; Wang, Hongwei; Yang, Zelin; Li, Jian; Suo, Huayi

    2017-01-01

    The aim of this study is to assess the preventive effects of Lactobacillus fermentum HY01 (LF-HY01) to dextran sulfate sodium induced-colitis. We observed the ratio of colon weight to its length, colon pathological changes, and the concentrations of pro-inflammatory factors (IFN-γ, IL-12, TNFα, and IL-6) in serum. We also took account of the protein levels of IκBα, NF-κB p65, iNOS, and COX-2, and we measured the best effects of different doses of Lactobacillus fermentum HY01 (low dose group was 109 CFU/kg·bw, high dose group was 1010 CFU/kg·bw) on dextran sulfate sodium-induced colitis mice. The results were remarkable, suggesting that Lactobacillus fermentum HY01 had significant preventive effects in dextran sulfate sodium induced-colitis; simultaneously, the high dose group showed the best results among other groups. It can effectively alleviate the shortened colon length, reduce the ratio of colon weight to its length, reduce edema, inflammatory cells infiltration, and colon mucosa injury, and play an important role in the down-regulation of concentrations of pro-inflammatory factors (IFN-γ, IL-12, TNFα, and IL-6). Above all, Lactobacillus fermentum HY01 shows promising prevention for IκBα degradation, inhibition of NF-κB p65 phosphorylation cascades, and decreases the protein levels of iNOS and COX-2 as well. PMID:28587089

  2. Dextran-coated superparamagnetic amorphous Fe–Co nanoalloy for magnetic resonance imaging applications

    Energy Technology Data Exchange (ETDEWEB)

    An, Lu; Yu, Yanrong; Li, Xuejian; Liu, Wei [The Key Laboratory of Resource Chemistry of Ministry of Education and Shanghai Key Laboratory of Rare Earth Functional Materials, Department of Chemistry, Shanghai Normal University, Shanghai 200234 (China); Yang, Hong, E-mail: yanghong@shnu.edu.cn [The Key Laboratory of Resource Chemistry of Ministry of Education and Shanghai Key Laboratory of Rare Earth Functional Materials, Department of Chemistry, Shanghai Normal University, Shanghai 200234 (China); Wu, Dongmei [Shanghai Key Laboratory of Magnetic Resonance, Department of Physics, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062 (China); Yang, Shiping, E-mail: shipingy@shnu.edu.cn [The Key Laboratory of Resource Chemistry of Ministry of Education and Shanghai Key Laboratory of Rare Earth Functional Materials, Department of Chemistry, Shanghai Normal University, Shanghai 200234 (China)

    2014-01-01

    Graphical abstract: A dextran-coated Fe–Co nanoalloy was developed serving as a sensitive contrast agent for magnetic resonance imaging applications. - Highlights: • Amorphous Fe–Co nanoalloy was prepared via wet chemical reduction approach. • The Fe–Co nanoalloy is water-soluble, stable, and biocompatible. • The Fe–Co nanoalloy is superparamagnetic. • The Fe–Co nanoalloy exhibits T{sub 2}-weighted MR enhancement both in vitro and in vivo. - Abstract: For magnetic resonance imaging applications, a facile approach for water-soluble dextran coated amorphous Fe–Co nanoalloy was developed. The as-synthesized nanoalloy had a diameter of 9 nm with a narrow size distribution and showed superparamagnetic property with a saturated magnetization (Ms) of 25 emu/g. In vitro cytotoxicity test revealed that it was biocompatible at a concentration below 120 μg/mL. It can be uptaken by HeLa cells effectively and resulted in the obvious T{sub 2} effect after internalization. Biodistribution studies in conjunction with inductively coupled plasma-atomic emission spectroscopy (ICP-AES) confirmed that Fe–Co nanoalloy was preferentially accumulated in lung and spleen after intravenous injection for 4 h. In vivo MRI, dextran-coated Fe–Co nanoalloy can serve as a sensitive contrast agent for MR imaging, especially in the spleen, so we believe that it maybe hold great promise for diagnosis of splenic disease by appropriately functionalizing their surface.

  3. Highly Selective Photothermal Therapy by a Phenoxylated-Dextran-Functionalized Smart Carbon Nanotube Platform.

    Science.gov (United States)

    Han, Seungmin; Kwon, Taeyun; Um, Jo-Eun; Haam, Seungjoo; Kim, Woo-Jae

    2016-05-01

    Near-infrared (NIR) photothermal therapy using biocompatible single-walled carbon nanotubes (SWNTs) is advantageous because as-produced SWNTs, without additional size control, both efficiently absorb NIR light and demonstrate high photothermal conversion efficiency. In addition, covalent attachment of receptor molecules to SWNTs can be used to specifically target infected cells. However, this technique interrupts SWNT optical properties and inevitably lowers photothermal conversion efficiency and thus remains major hurdle for SWNT applications. This paper presents a smart-targeting photothermal therapy platform for inflammatory disease using newly developed phenoxylated-dextran-functionalized SWNTs. Phenoxylated dextran is biocompatible and efficiently suspends SWNTs by noncovalent π-π stacking, thereby minimizing SWNT bundle formations and maintaining original SWNT optical properties. Furthermore, it selectively targets inflammatory macrophages by scavenger-receptor binding without any additional receptor molecules; therefore, its preparation is a simple one-step process. Herein, it is experimentally demonstrated that phenoxylated dextran-SWNTs (pD-SWNTs) are also biocompatible, selectively penetrate inflammatory macrophages over normal cells, and exhibit high photothermal conversion efficiency. Consequently, NIR laser-triggered macrophage treatment can be achieved with high accuracy by pD-SWNT without damaging receptor-free cells. These smart targeting materials can be a novel photothermal agent candidate for inflammatory disease.

  4. Magnetic field dependence of the diffusion of single dextran molecules within a hydrogel containing magnetite nanoparticles.

    Science.gov (United States)

    Al-Baradi, Ateyyah M; Mykhaylyk, Oleksandr O; Blythe, Harry J; Geoghegan, Mark

    2011-03-07

    We consider the effect of applied magnetic fields on the diffusion of single dextran molecules labeled with fluorescein isothiocyanate within a ferrogel [a composite of magnetite nanoparticles in a poly(methacrylic acid) hydrogel] using fluorescence correlation spectroscopy. We show that the mesh size of the ferrogel is controlled by the applied magnetic field, B, and scales as exp(-(4)√ξ(3)B(2)/2μ(0)k(B)T), where ξ is a correlation length, μ(0) the magnetic constant, k(B) the Boltzmann constant, and T is the absolute temperature. The diffusion coefficient of the dextran can be modeled with a simple Stokes-Einstein law, containing the same scaling behavior with magnetic field as the swelling of the hydrogel. Furthermore, the magnetic field-dependent release of dextran from the hydrogel is also controlled by the same relationship. The samples were characterized by small angle x-ray scattering (SAXS) and magnetometry experiments. Magnetic hysteresis loops from these ferrogels and zero field cooled∕field cooled measurements reveal single domain ferromagnetic behavior at room temperature with a similar coercivity for both as-prepared and fully swollen ferrogels, and for increasing magnetic nanoparticle concentration. SAXS experiments, such as the hysteresis loops, show that magnetite does not aggregate in these gels.

  5. New shell crosslinked micelles from dextran with hydrophobic end groups and their interaction with bioactive molecules.

    Science.gov (United States)

    Mocanu, Georgeta; Nichifor, Marieta; Stanciu, Magdalena C

    2015-03-30

    Micelles formed in aqueous solution by dextran with hydrophobic (alkyl) end-groups were stabilized through divinyl sulfone crosslinking of the dextran shell. The efficacy of the crosslinking reaction was influenced by the divinyl sulfone amount, the pH and micelle concentration. Crosslinked micelles with a moderate crosslinking degree were further functionalized by attachment of 10 and 17 moles% N-(2-hydroxypropyl)-N,N-dimethyl-N-benzylammonium chloride groups along the dextran chain. The size and shape of both crosslinked micelles and their cationic derivatives were analyzed by DLS and TEM. The prepared micelles were able to bind anionic diclofenac (60-370 mg/g), hydrophobic anionic indometacin (70-120 mg/g), and hydrophobic alpha-tocopherol (170-220 mg/g) or ergocalciferol (90-110 mg/g) by hydrophobic or/and electrostatic forces. The release experiments and the antioxidant activity of bound alpha-tocopherol highlighted the potential of the new nano-sized micelles mainly as carriers for prolonged and controlled delivery of hydrophobic drugs.

  6. [Indirect articular lymphography using Tc 99m-labeled Dextran in animals].

    Science.gov (United States)

    Albuquerque, M; Pedroso de Lima, J; Cardoso, A; Mendes, F; Pires, J; Canha, N; Branco, R

    1990-01-01

    Looking for a standardization of the articular lymphoscintigraphy, an experimental research was conducted on 14 dogs injected in the ankle, with 2.5 mCi of 99m Tc-labeled dextran (P.M. = 70,000). Good scintigraphic images of the lymphatic system have been obtained. After having collected blood samples during the experimentation as well as aliquots of organs and of tissues, after the necropsy of the animal, it was verified that the 99m Tc-labeled dextran was useful for quantitative studies of the articular lymphatic drainage. The activities attained, in the drainage lymph nodes of injected articulation, are 152 times superior to those obtained in the kidney and one gramma of popliteal ganglion was 8929 times more active than one gramma of blood. The dextran 70,000, widely used in our clinical routine, can be injected to the human being, without any risk, and it may be the tracer which permits studies of the articular lymphatic drainage and the usage of the lymphoscintigraphy, already in expansion in many other Medicine branches, in the articular studies, nowadays.

  7. A novel strategy for the preparation of porous microspheres and its application in peptide drug loading.

    Science.gov (United States)

    Wei, Yi; Wang, Yuxia; Zhang, Huixia; Zhou, Weiqing; Ma, Guanghui

    2016-09-15

    A new strategy is developed to prepare porous microspheres with narrow size distribution for peptides controlled release, involving a fabrication of porous microspheres without any porogens followed by a pore closing process. Amphiphilic polymers with different hydrophobic segments (poly(monomethoxypolyethylene glycol-co-d,l-lactide) (mPEG-PLA), poly(monomethoxypolyethylene glycol-co-d,l-lactic-co-glycolic acid) (mPEG-PLGA)) are employed as microspheres matrix to prepare porous microspheres based on a double emulsion-premix membrane emulsification technique combined with a solvent evaporation method. Both microspheres possess narrow size distribution and porous surface, which are mainly caused by (a) hydrophilic polyethylene glycol (PEG) segments absorbing water molecules followed by a water evaporation process and (b) local explosion of microspheres due to fast evaporation of dichloromethane (MC). Importantly, mPEG-PLGA microspheres have a honeycomb like structure while mPEG-PLA microspheres have a solid structure internally, illustrating that the different hydrophobic segments could modulate the affinity between solvent and matrix polymer and influence the phase separation rate of microspheres matrix. Long term release patterns are demonstrated with pore-closed microspheres, which are prepared from mPEG-PLGA microspheres loading salmon calcitonin (SCT). These results suggest that it is potential to construct porous microspheres for drug sustained release using permanent geometric templates as new porogens.

  8. Real time monitoring of coating status for microsphere target with digital image difference method

    Institute of Scientific and Technical Information of China (English)

    Baixuan Shi(施柏煊); Xiao Huang(黄晓); Caifeng Li(李彩凤)

    2003-01-01

    Digital image difference method monitorring coating status of microsphere targets automatically is sug-gested. A CCD micro-imaging system is developed for monitoring the status of bouncing and adherencebetween microspheres and the bouncing pan. A new bouncing pan with multiple holes is adopted formicrosphere coating to enhance the microsphere coating efficiency.

  9. PLGA microsphere/calcium phosphate cement composites for tissue engineering: in vitro release and degradation characteristics.

    NARCIS (Netherlands)

    Habraken, W.J.E.M.; Wolke, J.G.C.; Mikos, A.G.; Jansen, J.A.

    2008-01-01

    Bone cements with biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres have already been proven to provide a macroporous calcium phosphate cement (CPC) during in situ microsphere degradation. Furthermore, in vitro/in vivo release studies with these PLGA microsphere/CPC composites (PLGA/CP

  10. Preparation of etoposide Polylactic Acid Microspheres%依托泊苷聚乳酸微球的制备

    Institute of Scientific and Technical Information of China (English)

    姜素芳; 张云坤; 周学军

    2011-01-01

    目的::用生物可降解材料聚乳酸制备依托泊苷微球,并对其体外释药特性进行研究.方法:采用乳化-溶剂扩散法制备依托泊苷聚乳酸微球,通过正交试验确定最佳处方工艺;采用紫外分光光度法测定微球载药量、包封率和体外药物释放,利用光学显微镜观察微球形态和粒径分布.结果:所得微球外观圆整,平均粒径为12.87 μm,载药量为14.79%,药物包封率为61.09%,体外释药符合Higuchi方程.结论:依托泊苷聚乳酸微球制备工艺稳定,体外释药符合长效制剂特征.%Objective To prepare etoposide microspheres using thg biodegradable meterials-polylactic acid and to study its release characteristics in vitro. Methods The polylactic acid microspheres were prepared by emulsion-solvent diffusion method and the orthogonal test design was used to optimize the formulation and technology .The drug-loading,emcapsulation and release in vitro were determined by ultraviolet spectrophotometry and the appearance and particle size of microspheres was observed by light microscope. Results The shape of etoposide microspheres was spherical with mean particle size of 12.87 ujn.The drug loading and encapsulation efficiency were 14.79% and 61.09%, respectively. The in vitro release characteristics of microspheres was found to agree with Higuchi equation. Conclusion The technology of preparation was successful and etoposide polylactic acid micropheres showed significant sustained release.

  11. Thermal expansion of an epoxy-glass microsphere composite

    Science.gov (United States)

    Price, H. L.; Burks, H. D.

    1977-01-01

    The thermal expansion of a composite of epoxy (diglycidyl ether of bisphenol A) and solid glass microspheres was investigated. The microspheres had surfaces which were either untreated or treated with a silicone release agent, an epoxy coupling agent, or a general purpose silane coupling agent. Both room temperature (about 300 K) and elevated temperature (about 475 K) cures were used for the epoxy. Two microsphere size ranges were used, about 50 microns, which is applicable in filled moldings, and about 125 microns, which is applicable as bond line spacers. The thermal expansion of the composites was measured from 300 to 350 K or from 300 to 500 K, depending on the epoxy cure temperature. Measurements were made on composites containing up to .6 volume fraction microspheres. Two predictive models, which required only the values of thermal expansion of the polymer and glass and their specific gravities, were tested against the experimental data. A finite element analysis was made of the thermal strain of a composite cell containing a single microsphere surrounded by a finite-thickness interface.

  12. Study of electrodepositing Au on hollow polystyrene microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Jin Rong [Research Center of Laser Fusion, China Academy of Engineering Physics, P.O. Box 919-987, Mianyang 621900 (China); School of Material Science and Engineering, Xihua University, Chengdu 610039 (China); Zhang Yunwang [Research Center of Laser Fusion, China Academy of Engineering Physics, P.O. Box 919-987, Mianyang 621900 (China); Zhang Lin, E-mail: zhlmy@sina.com [Research Center of Laser Fusion, China Academy of Engineering Physics, P.O. Box 919-987, Mianyang 621900 (China); Wei Chengfu, E-mail: wcf@mail.xhu.edu.cn [School of Material Science and Engineering, Xihua University, Chengdu 610039 (China); Guo Jianjun [School of Material Science and Engineering, Xihua University, Chengdu 610039 (China)

    2013-01-15

    Highlights: Black-Right-Pointing-Pointer The gold is electrodeposited on hollow polystyrene microspheres by self-designed setup in this paper. Black-Right-Pointing-Pointer The Au electrodeposit is finer and more uniform on account of the microspheres freely move on the cathode. Black-Right-Pointing-Pointer The morphology, thickness and roughness of Au electrodeposits were analyzed using Scanning Electron Microscopy, X-ray diffraction and Atomic Force Microscope, respectively. - Abstract: The electrodeposited Au film on hollow polystyrene microspheres is successfully prepared by a set of self-designed device. The film is more compact and uniform on account of the microspheres freely moving on the cathode. These experiments mainly focus on the analysis of spherical symmetry, thickness and roughness of electrodeposited Au film. Under conditions of current density 1.5-3 mA cm{sup -2}, the temperature 25 Degree-Sign C, and the stirring rate 150 rpm, the electrodeposited microsphere is coated with a considerably orbicular film. The morphology, thickness and roughness of Au electrodeposits are studied by Scanning Electron Microscopy (SEM), X-ray diffraction (XRD) and Atomic Force Microscope (AFM), respectively.

  13. 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.

  14. Quantitating error in blood flow measurements with radioactive microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Austin, R.E. Jr.; Hauck, W.W.; Aldea, G.S.; Flynn, A.E.; Coggins, D.L.; Hoffman, J.I.

    1989-07-01

    Accurate determination of the reproducibility of measurements using the microsphere technique is important in assessing differences in blood flow to different organs or regions within organs, as well as changes in perfusion under various experimental conditions. The sources of error of the technique are briefly reviewed. In addition, we derived a method for combining quantifiable sources of error into a single estimate that was evaluated experimentally by simultaneously injecting eight or nine sets of microspheres (each with a different radionuclide label) into four anesthetized dogs. Each nuclide was used to calculate blood flow in 145-190 myocardial regions. We compared each flow determination (using a single nuclide label) with a weighted mean for the piece (based on the remaining nuclides). The difference was defined as ''measured'' error. In all, there were a total of 5,975 flow observations. We compared measured error with theoretical estimates based on the Poisson error of radioactive disintegration and microsphere entrapment, nuclide separation error, and reference flow error. We found that combined estimates based on these sources completely accounted for measured error in the relative distribution of microspheres. In addition, our estimates of the error in measuring absolute flows (which were established using microsphere reference samples) slightly, but significantly, underestimated measured error in absolute flow.

  15. Local blood flow measured by fluorescence excitation of nonradioactive microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Morita, Y.; Payne, B.D.; Aldea, G.S.; McWatters, C.; Husseini, W.; Mori, H.; Hoffman, J.I.; Kaufman, L. (Univ. of California, San Francisco (USA))

    1990-05-01

    An X-ray fluorescence system with low Compton background and high counting efficiency was developed to measure regional blood flow with nonradioactive microspheres. The performance of the system was tested in vitro by counting mixed aqueous solutions of either Mo, Ag, and I; Nb, Ag, and Ba; or Zr, Mo, Rh, Ag, Sn, I, and Ba, as well as a mixture of Ag and Ba nonradioactive microspheres. Mixtures containing 2-20 ppm of each element were counted for 10 min by the fluorescence system, and the individual elements in mixtures of three to seven nonradioactive elements were measured with high accuracy. The best counting statistics were obtained for Ag. For 10-min counts, the system measures as few as 120 Ag microspheres with 30% standard deviation but measures 800 Ag microspheres per sample with 3.6% standard deviation. We compared regional myocardial blood flows determined simultaneously by fluorescence and radioactive microsphere methods; the latter samples were counted by a 3-in. NaI (Tl) well detector and pulse-height analyzer. The radioactive and nonradioactive measurements showed good correlat