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Sample records for albendazole-encapsulated nanosize liposomes

  1. Targeted Therapy for Acute Autoimmune Myocarditis with Nano-Sized Liposomal FK506 in Rats

    Science.gov (United States)

    Matsuzaki, Takashi; Araki, Ryo; Tsuchida, Shota; Thanikachalam, Punniyakoti V.; Fukuta, Tatsuya; Asai, Tomohiro; Yamato, Masaki; Sanada, Shoji; Asanuma, Hiroshi; Asano, Yoshihiro; Asakura, Masanori; Hanawa, Haruo; Hao, Hiroyuki; Oku, Naoto; Takashima, Seiji; Kitakaze, Masafumi; Sakata, Yasushi; Minamino, Tetsuo

    2016-01-01

    Immunosuppressive agents are used for the treatment of immune-mediated myocarditis; however, the need to develop a more effective therapeutic approach remains. Nano-sized liposomes may accumulate in and selectively deliver drugs to an inflammatory lesion with enhanced vascular permeability. The aims of this study were to investigate the distribution of liposomal FK506, an immunosuppressive drug encapsulated within liposomes, and the drug’s effects on cardiac function in a rat experimental autoimmune myocarditis (EAM) model. We prepared polyethylene glycol-modified liposomal FK506 (mean diameter: 109.5 ± 4.4 nm). We induced EAM by immunization with porcine myosin and assessed the tissue distribution of the nano-sized beads and liposomal FK506 in this model. After liposomal or free FK506 was administered on days 14 and 17 after immunization, the cytokine expression in the rat hearts along with the histological findings and hemodynamic parameters were determined on day 21. Ex vivo fluorescent imaging revealed that intravenously administered fluorescent-labeled nano-sized beads had accumulated in myocarditic but not normal hearts on day 14 after immunization and thereafter. Compared to the administration of free FK506, FK506 levels were increased in both the plasma and hearts of EAM rats when liposomal FK506 was administered. The administration of liposomal FK506 markedly suppressed the expression of cytokines, such as interferon-γ and tumor necrosis factor-α, and reduced inflammation and fibrosis in the myocardium on day 21 compared to free FK506. The administration of liposomal FK506 also markedly ameliorated cardiac dysfunction on day 21 compared to free FK506. Nano-sized liposomes may be a promising drug delivery system for targeting myocarditic hearts with cardioprotective agents. PMID:27501378

  2. Improved skin permeation of methotrexate via nanosized ultradeformable liposomes

    Science.gov (United States)

    Zeb, Alam; Qureshi, Omer Salman; Kim, Hyung-Seo; Cha, Ji-Hye; Kim, Hoo-Seong; Kim, Jin-Ki

    2016-01-01

    The aim of this study is to investigate methotrexate-entrapped ultradeformable liposomes (MTX-UDLs) for potential transdermal application. MTX-UDLs were prepared by extrusion method with phosphatidylcholine as a bilayer matrix and sodium cholate or Tween 80 as an edge activator. The physicochemical properties of MTX-UDLs were determined in terms of particle size, polydispersity index, zeta potential, and entrapment efficiency. The deformability of MTX-UDLs was compared with that of methotrexate-entrapped conventional liposomes (MTX-CLs) using a steel pressure filter device. The skin permeation of MTX-UDLs was investigated using Franz diffusion cell, and the skin penetration depth of rhodamine 6G-entrapped UDLs was determined by confocal laser scanning microscopy. MTX-UDLs showed a narrow size distribution, with the particle size of ~100 nm. The deformability of MTX-UDLs was two to five times greater than that of MTX-CLs. The skin permeation of MTX-UDLs was significantly improved compared with MTX-CLs and free MTX solution. The optimized UDLs (phosphatidylcholine: Tween 80 =7:3, w/w) showed a higher fluorescence intensity than conventional liposomes at every increment of skin depth. Thus, the optimized UDLs could be promising nanocarriers for systemic delivery of MTX across skin. PMID:27540293

  3. Design of liposome-based pH sensitive nanoSPIN probes: nano-sized particles with incorporated nitroxides

    OpenAIRE

    Woldman, Yakov Y.; Semenov, Sergey V.; Bobko, Andrey A.; Kirilyuk, Igor A.; Polienko, Julya F.; Voinov, Maxim A.; Bagryanskaya, Elena G.; Khramtsov, Valery V.

    2009-01-01

    Liposome-based nanoSized Particles with Incorporated Nitroxides, or nanoSPINs, were designed for EPR applications as pH probes in biological systems. Phospholipid membrane of the liposomes with incorporated gramicidin A showed selective permeability to a small analyte, H+, while protecting entrapped sensing nitroxide from biological reductants. An application of the pH-sensitive nanoSPIN in an ischemia model in rat heart homogenate allows for monitoring ischemia-induced acidosis while protect...

  4. Liposomes in biology and medicine

    OpenAIRE

    Schwendener, R.

    2007-01-01

    Drug delivery systems (DDS) have become important tools for the specific delivery of a large number of drug molecules. Since their discovery in the 1960s liposomes were recognized as models to study biological membranes and as versatile DDS of both hydrophilic and lipophilic molecules. Liposomes--nanosized unilamellar phospholipid bilayer vesicles--undoubtedly represent the most extensively studied and advanced drug delivery vehicles. After a long period of research and development efforts, l...

  5. Mild Hyperthermia and Thermosensitive Liposomes for Chemotherapy

    NARCIS (Netherlands)

    L. Li (Li)

    2013-01-01

    textabstractLiposomes are nano-sized drug carriers widely used to deliver chemotherapeutic compounds in cancer treatments. While prolonging drug retention in circulation and preventing certain toxic side-effects, liposomal drugs still need to overcome matters on specific accumulation in the tumor an

  6. LIPOSOMES: AN OVERVIEW

    Directory of Open Access Journals (Sweden)

    Prabhakar Vishvakrama

    2014-06-01

    Full Text Available The discovery of liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon hydration. Liposome drug delivery systems have played a significant role in formulation of potent drug to improve therapeutics. Recently the liposome formulations are targeted to reduce toxicity and increase accumulation at the target site. There are several new methods of liposome preparation based on lipid drug interaction and liposome disposition mechanism including the inhibition of rapid clearance of liposome by controlling particle size, charge and surface hydration. Most clinical applications of liposomal drug delivery are targeting to tissue with or without expression of target recognition molecules on lipid membrane. The liposomes are characterized with respect to physical, chemical and biological parameters. The sizing of liposome is also critical parameter which helps characterize the liposome which is usually performed by sequential extrusion at relatively low pressure through polycarbonate membrane (PCM. This mode of drug delivery lends more safety and efficacy to administration of several classes of drugs like antiviral, antifungal, antimicrobial, vaccines, anti tubercular drugs and gene therapeutics. Present applications of the liposomes are in the immunology, dermatology, vaccine adjuvant, eye disorders, brain targeting, infective disease and in tumour therapy. The new developments in this field are the specific binding properties of a drug-carrying liposome to a target cell such as a tumor cell and specific molecules in the body (antibodies, proteins, peptides etc.; stealth liposomes which are especially being used as carriers for hydrophilic (water soluble anticancer drugs like doxorubicin, mitoxantrone; and bisphosphonate- liposome mediated depletion of macrophages. This review would be a help to the researchers working in the area of liposomal drug delivery.

  7. Synthesis of nanosized sodium titanates

    Science.gov (United States)

    Hobbs, David T.; Taylor-Pashow, Kathryn M. L.; Elvington, Mark C.

    2015-09-29

    Methods directed to the synthesis and peroxide-modification of nanosized monosodium titanate are described. Methods include combination of reactants at a low concentration to a solution including a nonionic surfactant. The nanosized monosodium titanate can exhibit high selectivity for sorbing various metallic ions.

  8. Liposomal formulations for inhalation.

    Science.gov (United States)

    Cipolla, David; Gonda, Igor; Chan, Hak-Kim

    2013-08-01

    No marketed inhaled products currently use sustained release formulations such as liposomes to enhance drug disposition in the lung, but that may soon change. This review focuses on the interaction between liposomal formulations and the inhalation technology used to deliver them as aerosols. There have been a number of dated reviews evaluating nebulization of liposomes. While the information they shared is still accurate, this paper incorporates data from more recent publications to review the factors that affect aerosol performance. Recent reviews have comprehensively covered the development of dry powder liposomes for aerosolization and only the key aspects of those technologies will be summarized. There are now at least two inhaled liposomal products in late-stage clinical development: ARIKACE(®) (Insmed, NJ, USA), a liposomal amikacin, and Pulmaquin™ (Aradigm Corp., CA, USA), a liposomal ciprofloxacin, both of which treat a variety of patient populations with lung infections. This review also highlights the safety of inhaled liposomes and summarizes the clinical experience with liposomal formulations for pulmonary application. PMID:23919478

  9. Multi-liposomal containers.

    Science.gov (United States)

    Yaroslavov, A A; Sybachin, A V; Zaborova, O V; Zezin, A B; Talmon, Y; Ballauff, M; Menger, F M

    2015-12-01

    Small unilamellar liposomes, 40-60 nm in diameter, composed of anionic diphosphatidylglycerol (cardiolipin, CL(2-)) or phosphatidylcerine (PS(1-)) and zwitter-ionic egg yolk lecithin (EL) or dipalmitoylphosphatidylcholine (DPPC), electrostatically complex with polystyrene microspheres, ca. 100 nm in diameter, grafted by polycationic chains ("spherical polycationic brushes", SPBs). Polymer/liposome binding studies were carried out using electrophoretic mobility (EPM), dynamic light scattering (DLS), fluorescence, conductometry, differential scanning calorimetry (DSC), and cryogenic transmission electron microscopy (cryo-TEM) as the main analytical tools. By these means a remarkably detailed picture emerges of molecular events inside a membrane. The following are among the most important conclusions that arose from the experiments: (a) binding of liposomes to SPBs is accompanied by flip-flop of anionic lipids from the inner to the outer leaflet of the liposomal membrane along with lateral lipid segregation into "islands". (b) The SPB-induced structural reorganization of the liposomal membrane, together with the geometry of anionic lipid molecules, determines the maximum molar fraction of anionic lipid (a key parameter designated as ν) that ensures the structural integrity of liposomes upon complexation: ν=0.3 for liposomes with conically-shaped CL(2-) and ν=0.5 for liposomes with anionic cylindrically-shaped PS(1-). (c) The number of intact liposomes per SPB particle varies from 40 for (ν=0.1) to 13 (ν=0.5). (d) By using a mixture of liposomes with variety of encapsulated substances, multi-liposomal complexes can be prepared with a high loading capacity and a controlled ratio of the contents. (e) In order to make the mixed anionic liposomes pH-sensitive, they are additionally modified by 30 mol% of a morpholinocyclohexanol-based lipid that undergoes a conformational flip when changing pH. Being complexed with SPBs, such liposomes rapidly release their contents

  10. Synthesis of nanosized tungsten powder

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Nanosized tungsten powder was synthesized by means of different methods and under different conditions with nanosized WO3 powder. The powder and the intermediate products were characterized using XRD, SEM, TEM, BET (Brunauer Emmett Teller Procedure) and SAXS (X-ray diffracto-spectrometer/Kratky small angle scattering goniometer). The results show that nanosized WO3 can be completely reduced to WO2 at 600℃ after 40 min, and WO2 can be reduced to W at 700℃ after 90 min, moreover, the mean size of W particles is less than 40 nm. Furthermore, the process of WO3→WO2→W excelled that of WO3→W in getting stable nanosized tungsten powder with less grain size.

  11. pH-sensitive liposomes: acid-induced liposome fusion.

    OpenAIRE

    Connor, J.; Yatvin, M B; Huang, L.

    1984-01-01

    Sonicated unilamellar liposomes containing phosphatidylethanolamine and palmitoylhomocysteine fuse rapidly when the medium pH is lowered from 7 to 5. Liposome fusion was demonstrated by (i) mixing of the liposomal lipids as shown by resonance energy transfer, (ii) gel filtration, and (iii) electron microscopy. The pH-sensitive fusion of liposomes was observed only when palmitoylhomocysteine (greater than or equal to 20 mol%) was present in the liposomes. The presence of phosphatidyl-ethanolam...

  12. LIPOSOMES: AN OVERVIEW

    Directory of Open Access Journals (Sweden)

    Sipai Altaf Bhai. M

    2012-02-01

    Full Text Available Drug development technologies constituting innovations at the formulation end in the Pharmaceutical industry has received a lot of attention in past two decades. Drug delivery as an opportunity to extend product life cycles has indeed proved its place in the market with significant advantages of therapeutic gains as well as commercial success. Carrier technology offers an intelligent approach for drug delivery by coupling the drug to a carrier particle such as liposomes, microspheres, nanoparticles, etc. which modulates the release and absorption characteristics of the drug. Liposomes are well known to alter the bio distribution of entrapped substances by protecting the enclosed material. They are widely used as vehicles to target the specific molecule to specific organ. During the last few decades liposomes have attracted great interest as ideal models for biological membranes as well as efficient carriers for drugs, diagnostics, vaccines, nutrients and other bioactive agents. Many techniques and methodologies have involved for the manufacture of liposomes, on small and large scales, since their introduction to the scientific community around 40 years ago. This article intends to provide an overview of the advantages and disadvantages of liposome preparation methods,their stability, bio distribution and their uses as drug delivery systems. The conventional method of preparing liposomes is basically for the multilamellar vesicles (MLVs. However, other methods are used to reduce the size of these MLVs to small unilamellar vesicles (SUVs so as to increase their plasma lifetime and consequently increase the possibility of achieving greater tissue localisation. Some of these methods of size reduction are sonication and high pressure extrusion. Each of these methods has its own advantages and disadvantages. Large unilamellar vesicles (LUVs, on the other hand, are prepared mainly by detergent removal method and reverse phase extrusion technique. There

  13. Polymer Chemistry and Liposome Technology

    OpenAIRE

    Tirrell, David A.

    1988-01-01

    Polymer chemistry has a great deal to offer in the construction of synthetic liposomal membranes for use in biology and medicine. This chapter explores the preparation and properties of polymeric liposomes , with particular emphasis on the use of controlled polyelectrolyte adsorption to manipulate liposomal membrane properties.

  14. Targeting colon cancer cells using PEGylated liposomes modified with a fibronectin-mimetic peptide

    OpenAIRE

    Garg, Ashish; Tisdale, Alison W.; Haidari, Eman; Kokkoli, Efrosini

    2008-01-01

    Integrin α5β1 is expressed on several types of cancer cells, including colon cancer, and plays an important role in tumor growth and metastasis. The ability to target the integrin α5β1 using an appropriate drug delivery nano-vector can significantly help in inhibiting tumor growth, reducing tumor metastasis, and decreasing deleterious side effects associated with different cancer therapies. Liposomes are nano-sized phospholipid bilayer vesicles that have been extensively studied as drug deliv...

  15. Phase Transformation of Nanosized Zirconia

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The nanosized zirconia was synthesized via solid state reaction in the presence of surfactant. The results indicate that crystal phase of zirconia can be controlled by tuning the syn- thesis parameters such as OH-/Zr molar ratio, crystallizing temperature and time. It can be trans- formed among amorphous, tetragonal and monoclinic phases. The transformation is driven by particle size. The research shows the nanocrystalline zirconia possesses the higher thermal stability compared with amorphous framework. The "glow exotherm" can be observed for the amorphous samples. Otherwise, it is in the absence for nanocrystalline samples. Herein, the reason for retention of tetragonal zirconia is demonstrated.

  16. Reduced cytotoxicity and enhanced bioactivity of cationic antimicrobial peptides liposomes in cell cultures and 3D epidermis model against HSV.

    Science.gov (United States)

    Ron-Doitch, Sapir; Sawodny, Beate; Kühbacher, Andreas; David, Mirjam M Nordling; Samanta, Ayan; Phopase, Jaywant; Burger-Kentischer, Anke; Griffith, May; Golomb, Gershon; Rupp, Steffen

    2016-05-10

    Cationic antimicrobial peptides (AMPs) are part of the innate immunity, and act against a wide variety of pathogenic microorganisms by perturbation of the microorganism's plasma membrane. Although attractive for clinical applications, these agents suffer from limited stability and activity in vivo, as well as non-specific interaction with host biological membranes, leading to cytotoxic adverse effects. We hypothesized that encapsulation of AMPs within liposomes could result in reduced cytotoxicity, and with enhanced stability as well as bioactivity against herpes simplex virus 1 (HSV-1). We formulated nano-sized liposomal formulations of LL-37 and indolicidin, and their physicochemical properties, cellular uptake, in vitro cytotoxicity and antiviral efficacy have been determined. Lower cytotoxicity of LL-37 liposomes was found in comparison to indolicidin liposomes attributed to the superior physicochemical properties, and to the different degree of interaction with the liposomal membrane. The disc-like shaped LL-37 liposomes (106.8±10.1nm, shelf-life stability of >1year) were taken up more rapidly and to a significantly higher extent than the free peptide by human keratinocyte cell line (HaCaT), remained intact within the cells, followed by release of the active peptide within the cytoplasm and migration of the vesicles' lipids to the plasma membrane. LL-37 liposomes were found significantly less toxic than both the free agent and liposomal indolicidin. In the new 3D epidermis model (immortalized primary keratinocytes) liposomal LL-37 treatment (>20μM), but not free LL-37, efficiently protected the epidermis, inhibiting HSV-1 infection. This positive antiviral effect was obtained with no cytotoxicity even at very high concentrations (400μM). Thus, the antiviral activity of encapsulated LL-37 was significantly improved, expanding its therapeutic window. Liposomal LL-37 appears to be a promising delivery system for HSV therapy. PMID:27012977

  17. Boronated liposome development and evaluation

    Energy Technology Data Exchange (ETDEWEB)

    Hawthorne, M.F. [Univ. of California, Los Angeles, CA (United States)

    1995-11-01

    The boronated liposome development and evaluation effort consists of two separate tasks. The first is the development of new boron compounds and the synthesis of known boron species with BNCT potential. These compounds are then encapsulated within liposomes for the second task, biodistribution testing in tumor-bearing mice, which examines the potential for the liposomes and their contents to concentrate boron in cancerous tissues.

  18. Temoporfin-loaded liposomes

    DEFF Research Database (Denmark)

    Kuntsche, Judith; Freisleben, Ines; Steiniger, Frank;

    2010-01-01

    Temoporfin (mTHPC) is a potent but highly hydrophobic second-generation photosensitizer and has been approved for the palliative treatment of patients with advanced head and neck cancer by photodynamic therapy. Liposome formulations have been evaluated as carrier system for this drug to overcome ...... investigations indicate the presence of micellar structures in addition to vesicles. Lyophilization and reconstitution led to an alteration in the morphology but had overall no distinct influence on the colloidal stability....

  19. Effects of the protein corona on liposome-liposome and liposome-cell interactions.

    Science.gov (United States)

    Corbo, Claudia; Molinaro, Roberto; Taraballi, Francesca; Toledano Furman, Naama E; Sherman, Michael B; Parodi, Alessandro; Salvatore, Francesco; Tasciotti, Ennio

    2016-01-01

    A thorough understanding of interactions occurring at the interface between nanocarriers and biological systems is crucial to predict and interpret their biodistribution, targeting, and efficacy, and thus design more effective drug delivery systems. Upon intravenous injection, nanoparticles are coated by a protein corona (PC). This confers a new biological identity on the particles that largely determines their biological fate. Liposomes have great pharmaceutical versatility, so, as proof of concept, their PC has recently been implicated in the mechanism and efficiency of their internalization into the cell. In an attempt to better understand the interactions between nanocarriers and biological systems, we analyzed the plasma proteins adsorbed on the surface of multicomponent liposomes. Specifically, we analyzed the physical properties and ultrastructure of liposome/PC complexes and the aggregation process that occurs when liposomes are dispersed in plasma. The results of combined confocal microscopy and flow cytometry experiments demonstrated that the PC favors liposome internalization by both macrophages and tumor cells. This work provides insights into the effects of the PC on liposomes' physical properties and, consequently, liposome-liposome and liposome-cell interactions. PMID:27445473

  20. Tumor targeting and imaging with dual-peptide conjugated multifunctional liposomal nanoparticles

    Directory of Open Access Journals (Sweden)

    Rangger C

    2013-12-01

    Full Text Available Christine Rangger,1 Anna Helbok,1 Jane Sosabowski,2 Christian Kremser,3 Gottfried Koehler,4 Ruth Prassl,5,6 Fritz Andreae,7 Irene J Virgolini,1 Elisabeth von Guggenberg,1 Clemens Decristoforo11Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria; 2Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London, UK; 3Department of Radiology, Innsbruck Medical University, Innsbruck, 4Department of Computational and Structural Biology, Max Perutz Laboratories, University of Vienna, Wien, 5Institute of Biophysics, Medical University of Graz, Graz, 6Ludwig Boltzmann Institute for Lung Vascular Research, 7piCHEM Research and Development, Graz, AustriaBackground: The significant progress in nanotechnology provides a wide spectrum of nanosized material for various applications, including tumor targeting and molecular imaging. The aim of this study was to evaluate multifunctional liposomal nanoparticles for targeting approaches and detection of tumors using different imaging modalities. The concept of dual-targeting was tested in vitro and in vivo using liposomes derivatized with an arginine-glycine-aspartic acid (RGD peptide binding to αvβ3 integrin receptors and a substance P peptide binding to neurokinin-1 receptors.Methods: For liposome preparation, lipids, polyethylene glycol building blocks, DTPA-derivatized lipids for radiolabeling, lipid-based RGD and substance P building blocks and imaging labels were combined in defined molar ratios. Liposomes were characterized by photon correlation spectroscopy and zeta potential measurements, and in vitro binding properties were tested using fluorescence microscopy. Standardized protocols for radiolabeling were developed to perform biodistribution and micro-single photon emission computed tomography/computed tomography (SPECT/CT studies in nude mice bearing glioblastoma and/or melanoma tumor xenografts. Additionally, an initial magnetic resonance

  1. Propulsion of liposomes using bacterial motors

    International Nuclear Information System (INIS)

    Here we describe the utilization of flagellated bacteria as actuators to propel spherical liposomes by attaching bacteria to the liposome surface. Bacteria were stably attached to liposomes using a cross-linking antibody. The effect of the number of attached bacteria on propulsion speed was experimentally determined. The effects of bacterial propulsion on the bacteria–antibody–liposome complex were stochastic. We demonstrated that liposomal mobility increased when bacteria were attached, and the propulsion speed correlated with the number of bacteria. (paper)

  2. Correlation between radioactivity and chemotherapeutics of the 111In-VNB-liposome in pharmacokinetics and biodistribution in rats

    Directory of Open Access Journals (Sweden)

    Tsai TH

    2012-02-01

    Full Text Available Wen-Chuan Lee1,*, Chih-Hsien Chang2,3,*, Chih-Min Huang1, Yu-Tse Wu1, Liang-Cheng Chen2, Chung-Li Ho2, Tsui-Jung Chang2, Te-Wei Lee2, Tung-Hu Tsai1,41Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei, 2Division of Isotope Application, Institute of Nuclear Energy Research, Taoyuan, 3Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, 4Department of Education and Research, Taipei City Hospital, Taipei, Taiwan*These authors contributed equally to this workBackground: The combination of a radioisotope with a chemotherapeutic agent in a liposomal carrier (ie, Indium-111-labeled polyethylene glycol pegylated liposomal vinorelbine, [111In-VNB-liposome] has been reported to show better therapeutic efficiency in tumor growth suppression. Nevertheless, the challenge remains as to whether this therapeutic effect is attributable to the combination of a radioisotope with chemotherapeutics. The goal of this study was to investigate the pharmacokinetics, biodistribution, and correlation of Indium-111 radioactivity and vinorelbine concentration in the 111In-VNB-liposome.Methods: The VNB-liposome and 111In-VNB-liposome were administered to rats. Blood, liver, and spleen tissue were collected to determine the distribution profile of the 111In-VNB-liposome. A liquid chromatography tandem mass spectrometry system and gamma counter were used to analyze the concentration of vinorelbine and radioactivity of Indium-111.Results: High uptake of the 111In-VNB-liposome in the liver and spleen demonstrated the properties of a nanosized drug delivery system. Linear regression showed a good correlation (r = 0.97 between Indium-111 radioactivity and vinorelbine concentration in the plasma of rats administered the 111In-VNB-liposome.Conclusion: A significant positive correlation between the pharmacokinetics and biodistribution of 111Indium radioactivity and vinorelbine in blood, spleen

  3. Liposomal nanocarriers for plasminogen activators.

    Science.gov (United States)

    Koudelka, Stepan; Mikulik, Robert; Mašek, Josef; Raška, Milan; Turánek Knotigová, Pavlína; Miller, Andrew D; Turánek, Jaroslav

    2016-04-10

    Several plasminogen activators (PAs) have been found effective in treating different thromboembolic diseases. However, administration of conventional thrombolytic therapy is limited by a low efficacy of present formulations of PAs. Conventional treatments using these therapeutic proteins are associated with several limitations including rapid inactivation and clearance, short half-life, bleeding complications or non-specific tissue targeting. Liposome-based formulations of PAs such as streptokinase, tissue-plasminogen activator and urokinase have been developed to improve the therapeutic efficacy of these proteins. Resulting liposomal formulations were found to preserve the original activity of PAs, promote their selective delivery and improve thrombus targeting. Therapeutic potential of these liposome-based PAs has been demonstrated successfully in various pre-clinical models in vivo. Reductions in unwanted side effects (e.g., hemorrhage or immunogenicity) as well as enhancements of efficacy and safety were achieved in comparison to currently existing treatment options based on conventional formulations of PAs. This review summarizes present achievements in: (i) preparation of liposome-based formulations of various PAs, (ii) development of PEGylated and targeted liposomal PAs, (iii) physico-chemical characterization of these developed systems, and (iv) testing of their thrombolytic efficacy. We also look to the future and the imminent arrival of theranostic liposomal formulations to move this field forward. PMID:26876783

  4. Innovatives liposomes for overcoming biological barriers

    OpenAIRE

    Chessa, Maura

    2013-01-01

    In this thesis work were prepared and characterized liposomes and liposomes modified with a coating of chitosan called chitosomes. Through these structures were conveyed drugs of natural origin with anti-inflammatory and antioxidant properties: quercetin,phycocyanin and curcumin. The liposomes loading quercetin and phycocyanin are designed for a topical application and were tested on new born pig skin. Liposomes and chitosomes loading curcumin are designed for pulmonary delivery as a cure for...

  5. Liposomal drug delivery in multimodal cancer therapy

    OpenAIRE

    2011-01-01

    Encapsulating cytostatics into lipid vesicles, i.e. liposomes, improves tumour drug accumulation and reduce adverse effects. Liposomal doxorubicin (DXR) has been used in the treatment of a variety of cancers and may also be suitable for combining with other treatment modalities. By modulating liposomal membranes, liposomes can be made ultrasound (US) sensitive releasing encapsulated drug in tumour tissue upon external US stimulation and may thereby improve therapeutic outcome. Moreover, as DX...

  6. Microstructure and application of mesoporous nanosize zirconia

    Institute of Scientific and Technical Information of China (English)

    LIU Xinmei; YAN Zifeng; G.Q.Lu

    2004-01-01

    The mesoporous nanoscale zircoina zeolite was firstly synthesized via solid state -- Structure directing method without addition of any stabilizer. The sample bears lamellar or worm pore structures, relatively high surface area compared with that reported. The mesoporous nanosize structure can also resist higher calcination temperature. The introduction of above zirconia to the catalyst of methanol synthesis dedicates the nanosize particle size to the catalyst, which significantly changes the physical structure and electronic effect of the catalyst. The catalyst shows higher catalytic activity and selectivity to methanol. The active sites for methanol synthesis are demonstrated over various catalysts in this paper.

  7. Filter-extruded liposomes revisited

    DEFF Research Database (Denmark)

    Hinna, Askell; Steiniger, Frank; Hupfeld, Stefan; Stein, Paul C.; Kuntsche, Judith; Brandl, Martin

    (pore-size, number of filter passages, and flow-rate), flow field-flow fractionation in conjunction with multi-angle laser light scattering (AF4-MALLS, Wyatt Technology Corp., Santa Barbara, CA) was employed. Liposome size-distributions determined by AF4-MALLS were compared with those of dynamic light...

  8. Adjuvant effects of liposomes containing lipid A: enhancement of liposomal antigen presentation and recruitment of macrophages.

    OpenAIRE

    Verma, J N; Rao, M.; Amselem, S; Krzych, U; Alving, C R; Green, S J; Wassef, N M

    1992-01-01

    Liposomes containing lipid A induced potent humoral immune responses in mice against an encapsulated malaria antigen (R32NS1) containing NANP epitopes. The immune response was not enhanced by lipid A alone or by empty liposomes containing lipid A. Experiments to investigate the adjuvant mechanisms of liposomes and lipid A revealed that liposome-encapsulated R32NS1 was actively presented by bone marrow-derived macrophages to NANP-specific cloned T cells. The degree of presentation was related ...

  9. Comparison of Conventional Chemotherapy, Stealth Liposomes and Temperature-Sensitive Liposomes in a Mathematical Model

    OpenAIRE

    GASSELHUBER, ASTRID; Dreher, Matthew R.; Rattay, Frank; Bradford J. Wood; Haemmerich, Dieter

    2012-01-01

    Various liposomal drug carriers have been developed to overcome short plasma half-life and toxicity related side effects of chemotherapeutic agents. We developed a mathematical model to compare different liposome formulations of doxorubicin (DOX): conventional chemotherapy (Free-DOX), Stealth liposomes (Stealth-DOX), temperature sensitive liposomes (TSL) with intra-vascular triggered release (TSL-i), and TSL with extra-vascular triggered release (TSL-e). All formulations were administered as ...

  10. Application of Liposomes in Some Dairy Products.

    Science.gov (United States)

    Khanniri, E; Bagheripoor-Fallah, N; Sohrabvandi, S; Mortazavian, A M; Khosravi-Darani, K; Mohammad, R

    2016-01-01

    The application of liposomes as potential carriers to deliver food components is considerably an innovative technology. While the application of liposome technology has been very limited to date, researches indicating the potential of liposomes for improving the flavor of ripened cheese using accelerated methods, the targeted delivery of functional food ingredients, the synergistic delivery of ascorbic acid and tocopherols for promoting antioxidant activity in foods, and the stabilization of minerals (such as iron) in milk have been performed. In the food industry, liposomes and nanoliposomes have been employed to encapsulate flavoring and nutritive agents, and also, they have been suitable candidates to deliver antimicrobials. In this paper, application of lipase, proteinase, nisin, and flavor-containing liposomes in products during the processing (such as cheese maturity) as well as the application of liposomes-encapsulated micronutrients (such as iron) in milk are reviewed. PMID:25574577

  11. Europium chelate-loaded liposomes: a tool for the study of binding and integrity of liposomes.

    Science.gov (United States)

    Orellana, A; Laukkanen, M L; Keinänen, K

    1996-10-01

    Using the biotin-streptavidin interaction as a model, we investigated the suitability of lanthanide chelates as encapsulated liposomal labels in liposome-based binding assays. Large unilamellar phospholipid:cholesterol liposomes containing europium-DTPA chelate and biotinylated phosphatidylethanolamine were prepared by detergent dialysis. The resulting Eu-liposomes ([symbol: see text] 120 nm) bound specifically to streptavidin in microtiter wells as measured by time-resolved fluorometric assay (TRF). The intensity of fluorescence released from the bound liposomes was dependent on the concentration of biotin in the liposome membrane, the concentration of europium entrapped in the liposomes, the incubation time and the amount of liposomes used in the assay. The sensitivity of the TRF assay allowed the detection of binding of attomole quantities of liposomes. The streptavidin-immobilised liposomes subjected to porcine pancreatic phospholipase A2 (EC 3.1.1.4) and detergents displayed a dose-dependent release of the encapsulated europium. Lanthanide-chelate-liposomes should prove useful for studies addressing binding and stability of liposomes. PMID:8865811

  12. Liposomes - experiment of magnetic resonance imaging application

    International Nuclear Information System (INIS)

    Most pharmaceutical research effort with liposomes has been involved with the investigation of their use as drug carriers to particular target organs. Recently there has been a growing interest in liposomes not only as carrier of drugs but as a tool for the introduction of various substances into the human body. In this study, liposome delivery of nitroxyl radicals as NMR contrast agent for improved tissue imaging is experimented in rats

  13. Liposomes in Double-Emulsion Globules

    OpenAIRE

    Wang, Qing; Tan, Grace; Lawson, Louise B.; John, Vijay T.; Papadopoulos, Kyriakos D.

    2010-01-01

    Tubular liposomes containing a hydrophilic model compound (fluorescein sodium salt, FSS) were entrapped inside the internal aqueous phase (W1) of water-in-oil-in-water (W1/O/W2) double-emulsion globules. Our hypothesis was that the oil membrane of double emulsions can function as a layer of protection to liposomes and their contents and thus better control their release. Liposomes were prepared in bulk, and their release was observed microscopically from individual double-emulsion globules. T...

  14. Liposomal Encapsulated Rhodomyrtone: A Novel Antiacne Drug

    OpenAIRE

    Julalak Chorachoo; Thanaporn Amnuaikit; Voravuthikunchai, Supayang P.

    2013-01-01

    Rhodomyrtone isolated from the leaves of Rhodomyrtus tomentosa possesses antibacterial, anti-inflammatory, and anti-oxidant activities. Since rhodomyrtone is insoluble in water, it is rather difficult to get to the target sites in human body. Liposome exhibited ability to entrap both hydrophilic and hydrophobic compounds and easily penetrate to the target site. The present study aimed to develop a novel liposomal encapsulated rhodomyrtone formulations. In addition, characterization of liposom...

  15. Design of liposomal formulations for cell targeting

    OpenAIRE

    Nogueira, E.; Gomes, Andreia C.; Preto, Ana; Cavaco-Paulo, Artur

    2015-01-01

    Liposomes have gained extensive attention as carriers for a wide range of drugs due to being both nontoxic and biodegradable as they are composed of substances naturally occurring in biological membranes. Active targeting for cells has explored specific modification of the liposome surface by functionalizing it with specific targeting ligands in order to increase accumulation and intracellular uptake into target cells. None of the Food and Drug Administration-licensed liposomes or lipid nanop...

  16. An interaction of helicid with liposome biomembrane

    International Nuclear Information System (INIS)

    An interaction of helicid with phosphatidylcholine liposome biomembrane was studied by transmission electron microscopy, UV-vis, fluorescence, Raman and 31P NMR spectra. The results indicate that most of helicid molecules associate with liposomes at their surface and some of them penetrate the liposomes and locate in the hydrophobic regions of the membrane. The distribution coefficient KD between liposome phases and aqueous phases is 13.5. The liposome becomes more dispersive and stable in the presence of helicid. The microenvironmental micropolarity and the microhydrophobicity of liposome membrane decrease with the increase of helicid concentration. The interaction of helicid molecules with liposome results in a slight decrease of the membrane longitudinal order, and an increase of the membrane lateral order. A model for the interaction of helicid with liposome biomembrane is proposed on the basis of the change of microenvironment parameters of liposome including the micropolarity, microhydrophobicity and membrane order. The change of microenvironment parameters results mainly from hydrogen bonding interaction between the hydroxyl groups of the pyranoside rings of helicid molecules and the polar head groups of phosphatidylcholine.

  17. DNA controlled assembly of liposomes

    DEFF Research Database (Denmark)

    Vogel, Stefan; Jakobsen, Ulla; Simonsen, Adam Cohen

    2009-01-01

    DNA-encoding of solid nanoparticles requires surfacechemistry, which is often tedious and not generally applicable. In the present study non-covalently attached DNA are used to assemble soft nanoparticles (liposomes) in solution. This process displays remarkably sharp thermal transitions from...... assembled to disassembled state for which reason this method allows easy and fast detection of polynucleotides (e.g. DNA or RNA), including single nucleotide polymorphisms as well as insertions and deletions....

  18. GE11-modified liposomes for non-small cell lung cancer targeting: preparation, ex vitro and in vivo evaluation

    Directory of Open Access Journals (Sweden)

    Cheng L

    2014-02-01

    -mediated endocytosis pathway. Importantly, the GE11-modified liposomes showed enhanced accumulation and prolonged retention in tumor tissue, as evidenced by a 2.2-fold stronger mean fluorescence intensity in tumor tissue than the unmodified liposomes at 24 hours. In summary, GE11-modified liposomes may be a promising platform for targeted delivery of chemotherapeutic drugs in NSCLC. Keywords: epidermal growth factor receptor, nanosized carrier, targeted drug delivery, cellular uptake mechanism, in vivo imaging

  19. Nanoparticle Stabilized Liposomes for Acne Therapy

    Science.gov (United States)

    Fu, Victoria

    Acne vulgaris is a common skin disease that affects over 40 million people in the United States alone. The main cause of acne vulgaris is Propionibacterium acnes (P. acnes), resides deep in the pores and follicles of the skin in order to feed on oil produced by the sebaceous glands. The liposome is a lipid based nanoparticle with numerous advantages over free drug molecules as an acne treatment alternative. Bare liposomes loaded with lauric acid (LipoLA) were found to show strong antimicrobial activity against P. acnes while generating minimal toxicity. However, the platform is limited by the spontaneous tendency of liposomes to fuse with each other. Attaching nanoparticles to the surface of liposomes can overcome this challenge by providing steric repulsion and reduce surface tension. Thus, carboxyl-functionalized gold nanoparticles (AuC) were attached to the surface of liposomes (AuC-liposomes) loaded with doxycycline, a general tetracycline antibiotic. These particles were found to have a diameter of 120 nm and a zeta potential of 20.0 mV. Both fluorescent and antimicrobial studies demonstrated that based on electrostatic interaction, negatively charged AuC attached to the liposome's positively charged surface and stabilized liposomes in a neutral pH environment (pH = 7.4). Upon entering the skin's acidic environment (pH = 4), AuC detached from the liposome's surface and liposomes could fuse with P. acnes residing in the pores. Furthermore, toxicity studies showed that AuC-liposomes did not induce any significant toxicity, while two of the leading over-the-counter therapies, benzoyl peroxide and salicylic acid, generated substantial skin irritation.

  20. Biophysical studies on chitosan-coated liposomes.

    Science.gov (United States)

    Mady, Mohsen M; Darwish, Mirhane M; Khalil, Safaa; Khalil, Wafaa M

    2009-10-01

    Liposomes have been used as delivery vehicles for stabilizing drugs, overcoming barriers to cellular and tissue uptake, and for directing their contents toward specific sites in vivo. Chitosan is a biological macromolecule derived from crustacean shells and has several emerging applications in drug development, obesity control, and tissue engineering. In the present work, the interaction between chitosan and dipalmitoyl phosphatidylcholine (DPPC) liposomes was studied by transmission electron microscopy (TEM), zeta potential, solubilization using the nonionic detergent octylglucoside (OG), as well as Fourier transform infrared (FTIR) spectroscopy and viscosity measurements. The coating of DPPC liposomes by a chitosan layer was confirmed by electron microscope images and the zeta potential of liposomes. Coating of liposome by chitosan resulted in an increase in liposomal size by addition of a layer of 92 +/- 27.1 nm. The liposomal zeta potential became increasingly positive as chitosan concentration increased from 0.1 to 0.3% w/v, then it held at a relatively constant value. The amount of detergent needed to completely solubilize the liposomal membrane was increased after coating of liposomes with chitosan, indicating an increased membrane resistance to the detergent and hence a change in the natural membrane permeation properties. In the analysis of FTIR spectra of DPPC, the symmetric and antisymmetric CH(2) (at 2,800-3,000 cm(-1)) bands and the C=O (at 1,740 cm(-1)) stretching band were investigated in the absence and presence of the chitosan. It was concluded that appropriate combining of the liposomal and chitosan characteristics might be utilized for the improvement of the therapeutic efficacy of liposomes as a drug delivery system. PMID:19649627

  1. Development of the Liposomes Entrapped Ultrasound Imaging Gas (``Bubble Liposomes'') as Novel Gene Delivery Carriers

    Science.gov (United States)

    Suzuki, Ryo; Tanaka, Kumiko; Sawamura, Kaori; Takizawa, Tomoko; Utoguchi, Naoki; Negishi, Yoichi; Hagisawa, Kohsuke; Nishioka, Toshihiko; Maruyama, Kazuo

    2006-05-01

    Recently, microbubbles and ultrasound have been investigated with a view to improving the transfection efficiency of nonviral delivery systems for gene by cavitation. However, microbubbles had some problems in terms of stability and targeting ability. To solve these problems, we paid attention to liposomes that had many advantages such as stable and safe in vivo and easy to modify targeting ligand. Previously, we have represented that liposomes are good drug and gene delivery carriers. In addition, we developed that the liposomes ("Bubble liposomes") were entrapped with perfluoropropane known as ultrasound imaging gas. In this study, we assessed about feasibility of "Bubble liposomes" as gene delivery tool utilized cavitation by ultrasound irradiation. "Bubble liposomes" could effectively deliver plasmid DNA to cells by combination of ultrasound irradiation without cyototoxicity. This result suggested that "Bubble liposomes" might be a new class of tool for gene delivery.

  2. Anomalous freezing behavior of nanoscale liposomes

    DEFF Research Database (Denmark)

    Spangler, E. J.; Kumar, P. B. S.; Laradji, M.

    2012-01-01

    The effect of the finite size of one-component liposomes on their phase behavior is investigated via simulations of an implicit-solvent model of self-assembled lipid bilayers. We found that the high curvature of nanoscale liposomes has a significant effect on their freezing behavior. While the lo...

  3. Electrostatically driven complexation of liposomes with a star-shaped polyelectrolyte to low-toxicity multi-liposomal assemblies.

    Science.gov (United States)

    Yaroslavov, Alexander A; Sybachin, Andrey V; Zaborova, Olga V; Pergushov, Dmitry V; Zezin, Alexander B; Melik-Nubarov, Nikolay S; Plamper, Felix A; Müller, Axel H E; Menger, Frederic M

    2014-04-01

    Anionic liposomes are electrostatically complexed to a star-shaped cationic polyelectrolyte. Upon complexation, the liposomes retain their integrity and the resulting liposome-star complexes do not dissociate in a physiological solution with 0.15 M NaCl. This provides a multi-liposomal container for possible use as a high-capacity carrier. PMID:24243764

  4. Quantifying the effects of melittin on liposomes.

    Science.gov (United States)

    Popplewell, J F; Swann, M J; Freeman, N J; McDonnell, C; Ford, R C

    2007-01-01

    Melittin, the soluble peptide of bee venom, has been demonstrated to induce lysis of phospholipid liposomes. We have investigated the dependence of the lytic activity of melittin on lipid composition. The lysis of liposomes, measured by following their mass and dimensions when immobilised on a solid substrate, was close to zero when the negatively charged lipids phosphatidyl glycerol or phosphatidyl serine were used as the phospholipid component of the liposome. Whilst there was significant binding of melittin to the liposomes, there was little net change in their diameter with melittin binding reversed upon salt injection. For the zwitterionic phosphatidyl choline the lytic ability of melittin is dependent on the degree of acyl chain unsaturation, with melittin able to induce lysis of liposomes in the liquid crystalline state, whilst those in the gel state showed strong resistance to lysis. By directly measuring the dimensions and mass changes of liposomes on exposure to melittin using Dual Polarisation Interferometry, rather than following the florescence of entrapped dyes we attained further information about the initial stages of melittin binding to liposomes. PMID:17092481

  5. Topical and mucosal liposomes for vaccine delivery.

    Science.gov (United States)

    Romero, Eder Lilia; Morilla, Maria Jose

    2011-01-01

    Mucosal (and in minor extent transcutanous) stimulation can induce local or distant mucosa secretory IgA. Liposomes and other vesicles as mucosal and transcutaneous adjuvants are attractive alternatives to parenteral vaccination. Liposomes can be massively produced under good manufacturing practices and stored for long periods, at high antigen/vesicle mass ratios. However, their uptake by antigen-presenting cells (APC) at the inductive sites remains as a major challenge. As neurotoxicity is a major concern in intranasal delivery, complexes between archaeosomes and calcium as well as cationic liposomes complexed with plasmids encoding for antigenic proteins could safely elicit secretory and systemic antigen-specific immune responses. Oral bilosomes generate intense immune responses that remain to be tested against challenge, but the admixing with toxins or derivatives is mandatory to reduce the amount of antigen. Most of the current experimental designs, however, underestimate the mucus blanket 100- to 1000-fold thicker than a 100-nm diameter liposome, which has first to be penetrated to access the underlying M cells. Overall, designing mucoadhesive chemoenzymatic resistant liposomes, or selectively targeted to M cells, has produced less relevant results than tailoring the liposomes to make them mucus penetrating. Opposing, the nearly 10 µm thickness stratum corneum interposed between liposomes and underlying APC can be surpassed by ultradeformable liposomes (UDL), with lipid matrices that penetrate up to the limit with the viable epidermis. UDL made of phospholipids and detergents, proved to be better transfection agents than conventional liposomes and niosomes, without the toxicity of ethosomes, in the absence of classical immunomodulators. PMID:21360692

  6. Liposome imaging agents in personalized medicine

    DEFF Research Database (Denmark)

    Petersen, Anncatrine Luisa; Hansen, Anders Elias; Gabizon, Alberto;

    2012-01-01

    that selectively localize in tumor tissue can transport both drugs and imaging agents, which allows for a theranostic approach with great potential in personalized medicine. Radiolabeling of liposomes have for many years been used in preclinical studies for evaluating liposome in vivo performance and...... arena where we start to consider how to use imaging for patient selection and treatment monitoring in connection to nanocarrier based medicines. Nanocarrier imaging agents could furthermore have interesting properties for disease diagnostics and staging. Here, we review the major advances in the...... development of radiolabeled liposomes for imaging as a tool in personalized medicine....

  7. LIPOSOME AS A POTENTIAL DRUG DELIVERY SYSTEM: A REVIEW

    Directory of Open Access Journals (Sweden)

    Dash Tapaswi Rani

    2013-01-01

    Full Text Available Liposomes are microscopic phospholipid vescicles made of lipid bilayer which are the drug carrier for improving the delivery of therapeutic agents. Research on liposome technology has progressed from conventional vesicles (“first-generation liposomes” to “second-generation liposomes”, in which long-circulating liposomes are obtained by modulating the lipid composition, size, and charge of the vesicle. Liposomes with modified surfaces have also been developed using several molecules, such as glycolipids or sialic acid. A significant step in the development of long-circulating liposomes came with inclusion of the synthetic polymer poly-(ethylene glycol (PEG in liposome composition. Due to advancement in liposomal technology a number of liposomal formulations are available in market for clinical use, with gene delivery and cancer therapy and some formulations are under clinical trial. Reformulation of drugs in liposomes has provided an opportunity to enhance the therapeutic indices of various agents mainly through alteration in their biodistribution. This review discusses the basic principles of liposome structures and preparations, evaluation parameters of liposomal formulation, pharmacokinetics of liposomes and liposome-encapsulated drugs, the potential applications of liposomes in drug delivery with examples of formulations approved for clinical use, and the problems associated with further exploitation of this drug delivery system.

  8. Liposomes as delivery systems for antineoplastic drugs

    Science.gov (United States)

    Medina, Luis Alberto

    2014-11-01

    Liposome drug formulations are defined as pharmaceutical products containing active drug substances encapsulated within the lipid bilayer or in the interior aqueous space of the liposomes. The main importance of this drug delivery system is based on its drastic reduction in systemic dose and concomitant systemic toxicity that in comparison with the free drug, results in an improvement of patient compliance and in a more effective treatment. There are several therapeutic drugs that are potential candidates to be encapsulated into liposomes; particular interest has been focused in therapeutic and antineoplastic drugs, which are characterized for its low therapeutic index and high systemic toxicity. The use of liposomes as drug carriers has been extensively justified and the importance of the development of different formulations or techniques to encapsulate therapeutic drugs has an enormous value in benefit of patients affected by neoplastic diseases.

  9. Liposomal Simvastatin Attenuates Neointimal Hyperplasia in Rats

    OpenAIRE

    Afergan, Eyal; Ben David, Meital; Epstein, Hila; Koroukhov, Nickolay; Gilhar, Dalia; Rohekar, Keren; Danenberg, Haim D.; Golomb, Gershon

    2010-01-01

    Monocytes, macrophages, and inflammation play a key role in the process of neointimal proliferation and restenosis. The present study evaluated whether systemic and transient depletion of monocytes could be obtained by a single intravenous (IV) injection of simvastatin liposomes, for the inhibition of neointima formation. Balloon-injured carotid artery rats (n = 30) were randomly assigned to treatment groups of free simvastatin, simvastatin in liposomes (3 mg/kg), and saline (control). Stenos...

  10. PREPARATION OF LIPOSOMES CONTAINING WHEY PROTEINS

    Directory of Open Access Journals (Sweden)

    A. Suha Yalçın

    2010-01-01

    Full Text Available Aim: In recent years, it has been shown that whey and its components have a number of health-promoting effects. We aimed to isolate fractions containing whey proteins using chromatography and then to prepare antioxidant liposomes in order to obtain a gel suitable for cosmetic preparations.Methods: Fractionation of whey proteins was achieved by extraction, filtration and centrifugation followed by liquid chromatography. The antioxidant activities of the fractions was determined by their copper ion reducing capacity. Gel electrophoresis was used to analyze the proteins. Liposomes were made by the thin film hydration method.Results and Conclusion: Using Sephadex G-50 chromatography, two fractions were obtained. The first fraction contained major whey proteins, while the second fraction had small peptides. We have then determined the antioxidant activities of these fractions. The first fraction had the highest antioxidant activity. We prepared liposomes containing whey protein fractions and analyzed their sizes. Then, we investigated the liposome structures under a light microscope, electron microscope and atomic force microscope. Finally, we prepared a cosmetic formula from liposomes containing the whey fractions. We believe that preparing antioxidant liposomes containing whey proteins will be an important contribution to the cosmetic formulas for dermal applications.

  11. Plasmon resonant liposomes for controlled drug delivery

    Science.gov (United States)

    Knights-Mitchell, Shellie S.; Romanowski, Marek

    2015-03-01

    Nanotechnology use in drug delivery promotes a reduction in systemic toxicity, improved pharmacokinetics, and better drug bioavailability. Liposomes continue to be extensively researched as drug delivery systems (DDS) with formulations such as Doxil® and Ambisome® approved by FDA and successfully marketed in the United States. However, the limited ability to precisely control release of active ingredients from these vesicles continues to challenge the broad implementation of this technology. Moreover, the full potential of the carrier to sequester drugs until it can reach its intended target has yet to be realized. Here, we describe a liposomal DDS that releases therapeutic doses of an anticancer drug in response to external stimulus. Earlier, we introduced degradable plasmon resonant liposomes. These constructs, obtained by reducing gold on the liposome surface, facilitate spatial and temporal release of drugs upon laser light illumination that ultimately induces an increase in temperature. In this work, plasmon resonant liposomes have been developed to stably encapsulate and retain doxorubicin at physiological conditions represented by isotonic saline at 37o C and pH 7.4. Subsequently, they are stimulated to release contents either by a 5o C increase in temperature or by laser illumination (760 nm and 88 mW/cm2 power density). Successful development of degradable plasmon resonant liposomes responsive to near-infrared light or moderate hyperthermia can provide a new delivery method for multiple lipophilic and hydrophilic drugs with pharmacokinetic profiles that limit clinical utility.

  12. Octanol-assisted liposome assembly on chip

    Science.gov (United States)

    Deshpande, Siddharth; Caspi, Yaron; Meijering, Anna E. C.; Dekker, Cees

    2016-01-01

    Liposomes are versatile supramolecular assemblies widely used in basic and applied sciences. Here we present a novel microfluidics-based method, octanol-assisted liposome assembly (OLA), to form monodisperse, cell-sized (5-20 μm), unilamellar liposomes with excellent encapsulation efficiency. Akin to bubble blowing, an inner aqueous phase and a surrounding lipid-carrying 1-octanol phase is pinched off by outer fluid streams. Such hydrodynamic flow focusing results in double-emulsion droplets that spontaneously develop a side-connected 1-octanol pocket. Owing to interfacial energy minimization, the pocket splits off to yield fully assembled solvent-free liposomes within minutes. This solves the long-standing fundamental problem of prolonged presence of residual oil in the liposome bilayer. We demonstrate the unilamellarity of liposomes with functional α-haemolysin protein pores in the membrane and validate the biocompatibility by inner leaflet localization of bacterial divisome proteins (FtsZ and ZipA). OLA offers a versatile platform for future analytical tools, delivery systems, nanoreactors and synthetic cells.

  13. Mannosylated liposomes for targeted gene delivery

    Directory of Open Access Journals (Sweden)

    Kong F

    2012-02-01

    Full Text Available Fansheng Kong1, Fang Zhou1, Linfu Ge1, Ximin Liu1, Yong Wang21Department of Hematology, 2Department of Rehabilitation and Physiotherapy, General Hospital of Ji'nan Command, PLA, Ji'nan, People's Republic of ChinaBackground: Liposomes can be modified with different ligands to control their biological properties, such as longevity, targeting ability, and intracellular penetration, in a desired fashion. The aim of this study was to modify liposomes with a novel mannosylated polyethylene glycol-phosphatidylethanolamine (M-PEG-PE ligand to achieve active targeted gene delivery.Methods: Rat Kupffer cells were isolated and used as model cells for in vitro evaluation of cytotoxicity and transfection efficiency. The modified liposomes were intravenously injected into the rats, and Kupffer cells were isolated and analyzed by flow cytometry for in vivo gene delivery and expression.Results: The M-PEG-PE-modified liposome-enhanced green fluorescence protein plasmid (M-PEG-PE-Lipo-pEGFP complexes had a particle size of 237 nm and a loading efficiency of 90%. The M-PEG-PE-Lipo-pEGFP complexes displayed remarkably higher transfection efficiency than unmodified Lipo-pEGFP, both in vitro (51%–30% and in vivo (43%–27%.Conclusion: M-PEG-PE could function as an excellent active targeting ligand, and M-PEG-PE-modified liposomes could be promising active targeted drug delivery vectors.Keywords: gene delivery, active targeting, mannosylated, polyethylene glycol, phosphatidylethanolamine, liposomes

  14. Pulsed ultrasound enhances the delivery of nitric oxide from bubble liposomes to ex vivo porcine carotid tissue

    Directory of Open Access Journals (Sweden)

    Sutton JT

    2014-10-01

    Full Text Available JT Sutton,1 JL Raymond,1 MC Verleye,2 GJ Pyne-Geithman,3 CK Holland4 1University of Cincinnati, Biomedical Engineering Program, Cincinnati, OH, 2University of Notre Dame Department of Chemical Engineering, Notre Dame, IN, 3University of Cincinnati, College of Medicine, Department of Neurosurgery and the University of Cincinnati Neuroscience Institute, and Mayfield Clinic, Cincinnati, OH, 4University of Cincinnati, College of Medicine, Internal Medicine, Division of Cardiovascular Diseases, Cincinnati, OH, USA Abstract: Ultrasound-mediated drug delivery is a novel technique for enhancing the penetration of drugs into diseased tissue beds noninvasively. By encapsulating drugs into microsized and nanosized liposomes, the therapeutic can be shielded from degradation within the vasculature until delivery to a target site by ultrasound exposure. Traditional in vitro or ex vivo techniques to quantify this delivery profile include optical approaches, cell culture, and electrophysiology. Here, we demonstrate an approach to characterize the degree of nitric oxide (NO delivery to porcine carotid tissue by direct measurement of ex vivo vascular tone. An ex vivo perfusion model was adapted to assess ultrasound-mediated delivery of NO. This potent vasodilator was coencapsulated with inert octafluoropropane gas to produce acoustically active bubble liposomes. Porcine carotid arteries were excised post mortem and mounted in a physiologic buffer solution. Vascular tone was assessed in real time by coupling the artery to an isometric force transducer. NO-loaded bubble liposomes were infused into the lumen of the artery, which was exposed to 1 MHz pulsed ultrasound at a peak-to-peak acoustic pressure amplitude of 0.34 MPa. Acoustic cavitation emissions were monitored passively. Changes in vascular tone were measured and compared with control and sham NO bubble liposome exposures. Our results demonstrate that ultrasound-triggered NO release from bubble liposomes

  15. Nanomedicine for glaucoma: liposomes provide sustained release of latanoprost in the eye

    Directory of Open Access Journals (Sweden)

    Natarajan JV

    2012-01-01

    Full Text Available Jayaganesh V Natarajan1*, Marcus Ang2*, Anastasia Darwitan1, Sujay Chattopadhyay3, Tina T Wong2, Subbu S Venkatraman1 1Materials Science and Engineering, Nanyang Technological University, Singapore; 2Singapore Eye Research Institute, Singapore; 3Polymer Division, Indian Institute of Technology Roorkee, India*These authors contributed equally to this workPurpose: To report the development and therapeutic evaluation of a liposomal nanocarrier for sustained release of latanoprost, in the rabbit eye.Methods: We fabricated latanoprost-loaded egg-phosphatidylcholine (EggPC liposomes using the film hydration technique. The delivery vehicles were nano-sized (Z avg = 109 ± 18 nm, had a narrow poly dispersity index (PDI = 0.19 ± 0.04, and a very high loading efficiency (94% ± 5%. Based on in vitro data, we evaluated this formulation for lowering intraocular pressure (IOP in rabbit eyes. Following a single subconjunctival injection of the latanoprost loaded formulation, the eyes were clinically monitored and the IOP recorded.Results: Latanoprost-loaded EggPC liposomes demonstrated a high drug/lipid mole ratio of 0.181, remained stable for at least 6 months on storage (4°C, and at least 1 month at 25°C. A slow and sustained release of 60% of latanoprost was achieved by 14 days in the in vitro release study. The same formulation demonstrated a greater sustained IOP lowering effect compared with daily administration of topical latanoprost beyond 90 days (4.8 ± 1.5 vs 2.5 ± 0.9 mmHg; P < 0.001. No signs of inflammation were evident in the eyes from slit-lamp examination analysis.Conclusion: The loading required for a long-term sustained delivery of latanoprost for up to 90 days in the rabbit eyes was achieved with EggPC liposomes. A single injection of latanoprost-loaded EggPC liposomes can lower the IOP for up to 90 days, with a greater IOP lowering effect than daily topical administration of latanoprost.Keywords: nanomedicine, nanoliposomes, Egg

  16. Preparation of nanosized ZnO using α brass

    International Nuclear Information System (INIS)

    Nanosized ZnOs were synthesized on the surface of α brass coated a film of nickel catalyst at 500-700 deg. C under atmosphere of O2 and CH4 gases. The nanosized ZnOs have shapes including pillar, leaf, sheet and rod, which were determined by the synthesis temperature and the flow rates of O2 and CH4 gases. The nanosized ZnOs were characterized by electron microscopy including transmission electron microscope for crystal structure, morphology and high resolution images, both field emission scanning electron microscope and scanning electron microscope for morphology, and energy dispersive X-ray spectroscope equipped in electron microscope for chemical composition. A mechanism was proposed for the growth of nanosized ZnO obtained in this work

  17. Synthesis of beta carbon nitride nanosized crystal through mechanochemical reaction

    CERN Document Server

    Yin Long Wei; Liu Yu Xian; Sui Jin Ling; Wang Jing Min

    2003-01-01

    Nanosized beta carbon nitride (beta-C sub 3 N sub 4), of grain size several tens of nanometres, has been synthesized by mechanochemical reaction processing. The low-cost synthetic method developed facilitates the novel and effective synthesis of nanosized crystalline beta-C sub 3 N sub 4 (a = 6.36 A, c = 4.648 A) powders. The graphite powders were first milled to a nanoscale state, then the nanosized graphite powders were milled in an atmosphere of NH sub 3 gas. It was found that nanosized beta-C sub 3 N sub 4 was formed after high-energy ball milling under an NH sub 3 atmosphere. After thermal annealing, the shape of the beta-C sub 3 N sub 4 changes from flake-like to sphere-like. The nanosized beta-C sub 3 N sub 4 formed was characterized by x-ray diffraction, Fourier transformation infrared spectroscopy, and transmission electron microscopy. A solid-gas reaction mechanism was proposed for the formation of nanosized beta-C sub 3 N sub 4 at room temperature induced by mechanochemical activation.

  18. Toxicology of nanosized titanium dioxide: an update.

    Science.gov (United States)

    Zhang, Xiaochen; Li, Wen; Yang, Zhuo

    2015-12-01

    Nanosized titanium dioxide (nano-TiO2) has tremendous potential for a host of applications, and TiO2 nanoparticles (NP) possess different physicochemical properties compared to their fine particle analogs, which might alter their bioactivity. Their adverse effects on living cells have raised serious concerns recently for their use in health care and consumer sectors such as sunscreens, cosmetics, pharmaceutical additives and implanted biomaterials. Many researches have demonstrated that the physicochemical properties including shape, size, surface characteristics and inner structure of nano-TiO2 particles have different degrees of toxicity to different organism groups under different conditions. Some former reports have demonstrated that nano-TiO2 materials could enter into human body through different routes such as inhalation, dermal penetration and ingestion. After being taken by human body, NP might induce oxidative stress, cytotoxicity, genotoxicity, inflammation and cell apoptosis ultimately in mammal organs and systems. Here, we summarized the update about toxicity of nano-TiO2 and aimed to supply a safety usage guideline of this nanomaterial. PMID:26391178

  19. Urinary microalbumin measurement using a homogeneous liposomal immunoassay.

    Science.gov (United States)

    Frost, S J; Chakraborty, J; Firth, G B

    1996-08-14

    A homogeneous colorimetric immunoassay which has been developed for urinary microalbumin utilizes complement-mediated immunolysis of liposomes containing the dye, sulphorhodamine B. Unlike a previously described model complement-mediated liposomal assay for serum albumin (Frost et al., 1994) which was competitive, this assay uses a sandwich-type format and Fab' (antialbumin)-coated liposomes to increase the assay sensitivity. The liposomal assay, performed using a Cobas Bio analyser (Roche, Welwyn Garden City, UK), gave an acceptable correlation with a radioimmunoassay (NETRIA, London, UK): r = 0.94; y (liposomal assay) = 1.09 x (radioimmunoassay) - 1.54 mg/1. The imprecisions of the assays were similar and matrix effects due to the use of urine samples were determined to be acceptably small. The assay demonstrates the advantage of using Fab'-coated liposomes in sandwich-type liposomal immunoassays over liposomes coated with intact antibody, which failed to elicit complement-mediated immunolysis. PMID:8765163

  20. A Review on Composite Liposomal Technologies for Specialized Drug Delivery

    Directory of Open Access Journals (Sweden)

    Maluta S. Mufamadi

    2011-01-01

    Full Text Available The combination of liposomes with polymeric scaffolds could revolutionize the current state of drug delivery technology. Although liposomes have been extensively studied as a promising drug delivery model for bioactive compounds, there still remain major drawbacks for widespread pharmaceutical application. Two approaches for overcoming the factors related to the suboptimal efficacy of liposomes in drug delivery have been suggested. The first entails modifying the liposome surface with functional moieties, while the second involves integration of pre-encapsulated drug-loaded liposomes within depot polymeric scaffolds. This attempts to provide ingenious solutions to the limitations of conventional liposomes such as short plasma half-lives, toxicity, stability, and poor control of drug release over prolonged periods. This review delineates the key advances in composite technologies that merge the concepts of depot polymeric scaffolds with liposome technology to overcome the limitations of conventional liposomes for pharmaceutical applications.

  1. Effect of diglucosamine on the entrapment of protein into liposomes.

    Science.gov (United States)

    Murakami, S; Ono, T; Sakai, S; Ijima, H; Kawakami, K

    2006-01-01

    Liposomes, which had entrapped bovine serum albumin (BSA), were modified with diglucosamine by two methods. The liposome was prepared by a freeze-thawing method in the presence of the disaccharide, or the disaccharide was added to the liposome prepared in advance without it. To examine the effects of diglucosamine, the morphology, mean particle size, and zeta potential of both liposomes were compared with those of BSA-entrapping liposome prepared without the disaccharide. Diglucosamine caused no remarkable change in shape and no aggregation of the liposome. The presence of the disaccharide was confirmed on the surfaces of modified liposomes, and the entrapment of BSA into the liposomes was increased by the disaccharide. The entrapment behavior was affected by the way the disaccharide was added, and the difference in the way the BSA was entrapped was also indicated. PMID:16753965

  2. Anaphylaxis to Pegylated Liposomal Doxorubicin: A Case Report

    Science.gov (United States)

    Sharma, LR; Subedi, A; Shah, BK

    2014-01-01

    Liposomal doxorubicin is used for the treatment of various cancers like epithelial ovarian cancers, multiple myeloma and sarcomas. We report the first case of anaphylaxis to pegylated liposomal doxorubicin. PMID:25429486

  3. Anaphylaxis to Pegylated Liposomal Doxorubicin: A Case Report

    OpenAIRE

    Sharma, LR; A. Subedi; Shah, BK

    2014-01-01

    Liposomal doxorubicin is used for the treatment of various cancers like epithelial ovarian cancers, multiple myeloma and sarcomas. We report the first case of anaphylaxis to pegylated liposomal doxorubicin.

  4. Liposomal dry powders as aerosols for pulmonary delivery of proteins

    OpenAIRE

    Lu, Dongmei; Hickey, Anthony J.

    2005-01-01

    The purpose of this research was to develop liposomal dry powder aerosols for protein delivery. The delivery of stable protein formulations is essential for protein subunit vaccine delivery, which requires local delivery to macrophages in the lungs. β-Glucuronidase (GUS) was used as a model protein to evaluate dry powder liposomes as inhaled delivery vehicles. Dimyristoyl phosphatylcholine:cholesterol (7∶3) was selected as the liposome composition. The lyophilization of liposomes, micronizati...

  5. MRI shows clodronate-liposomes attenuating liverinjuryinratswithsevereacutepancreatitis

    Institute of Scientific and Technical Information of China (English)

    Jian-Xin Zhang; Sheng-Chun Dang; Yong Zhang; Xin Sha; Li-Rong Zhang; Chuan-She Wei; Min Chen; De-Li Jiang

    2010-01-01

    BACKGROUND: Studies have revealed that macrophages play an important role in the development of severe acute pancreatitis (SAP). Activated macrophages can lead to a systemic inlfammatory response, induce lipid peroxidation, impair membrane structure, result in injury to the liver and the other extrahepatic organs, and eventually result in multiple organ dysfunction syndrome by promoting excessive secretion of cytokines. Liver injury can further aggravate the systemic inlfammatory response and increase mortality by affecting the metabolism of toxins and the release of excessive inlfammatory mediators. Clodronate is a synthetic bisphosphonate, which is often used for treating bone changes caused by osteoporosis and other factors. In the current study, we created liposomes containing superparamagnetic iron oxide particles (SPIOs) for macrophage labeling and magnetic resonance imaging, using a novel method that can bind the clodronate to induce apoptosis and deplete macrophages. METHODS: Superparamagnetic Fe3O4 nanoparticles were prepared by chemical coprecipitation. SPIO-containing liposomes and SPIO-clodronate-containing liposomes were prepared by the thin iflm method. SAP models were prepared by injection of sodium taurocholate (2 ml/kg body weight) into the subcapsular space of the pancreas. Sprague-Dawley rats were randomly divided into a control group, a SAP plus SPIO-liposome group, and a SAP plus SPIO-clodronate-containing group. Two and six hours after SAP models were available, T2-weighted MRI scans (in the same plane) of the livers of rats in each group were performed. At the end of the scans, 2 ml of blood was taken from the superior mesenteric vein to measure the levels of serum amylase, ALT, AST, TNF-α, and IL-6. Pathological changes in the liver and pancreas were assessed. RESULTS: Transmission electron microscopy showed that the liposomes had a uniform size. No pathological changes in the pancreata of rats in the control group were noted. The

  6. Physico-chemical characterization of liposomes and drug substance-liposome interactions in pharmaceutics using capillary electrophoresis and electrokinetic chromatography

    DEFF Research Database (Denmark)

    Franzen, Ulrik; Østergaard, Jesper

    2012-01-01

    electrophoresis and liposome electrokinetic chromatography for the characterization of liposomes in a pharmaceutical context. Capillary electrophoretic techniques have been used for the measurement of electrophoretic mobility, which provides information on liposome surface charge, size and membrane permeability...... of liposomes. The use of liposome electrokinetic chromatography and capillary electrophoresis for determination of liposome/water partitioning and characterization of drug-liposome interactions is reviewed. A number of studies indicate that capillary electrophoresis may have a role in the...... characterization of liposome drug delivery systems, e.g., for the investigation of encapsulation efficiency and drug leakage. The well-known characteristics of capillary electrophoresis, i.e., low sample volume requirement, high separation efficiency in aqueous media without a stationary phase, minimal sample...

  7. Liposomes for scintigraphic imaging: optimization of in vivo behavior

    Energy Technology Data Exchange (ETDEWEB)

    Boerman, O.C.; Oyen, W.J.G.; Corstens, F.H.M. [Univ. Hospital Nijmegen (Netherlands). Dept. of Nuclear Medicine; Storm, G. [Utrecht Univ. (Netherlands). Utrecht Inst. for Pharmaceutics

    1998-12-01

    Liposomes, microscopic lipid vesicles consisting of concentric phospholipid bilayers enclosing discrete aqueous spaces, have been investigated extensively as carriers for drugs in attempts to achieve selective deposition and/or reduced toxicity. Liposomes radiolabeled with gamma emitters ({sup 67}Ga, {sup 111}In and {sup 99m}Tc) have been used for imaging purposes. Liposomes as formulated in the past, are rapidly taken up by cells of the mononuclear phagocyte system, primarily those located in liver and spleen. However, it has been shown during the last two decades that in vivo behavior of liposomes can be modulated by modifying their formulation. The size and the lipid composition have a major influence on the blood clearance rate, hepatic uptake and splenic uptake of liposomes. The development of long circulating liposomes, in particular coating of the bilayer with polyethyleneglycol (PEG) resulted in liposomes that oppose recognition by the MPS, thus displaying even longer circulatory half-lives. By carefully adjusting the liposomal formulation, the in vivo characteristics of liposomes can be tailored such that they become suitable vehicles for imaging various pathological processes in vivo. Liposomes have been proposed for tumor imaging, for infection imaging and as blood pool markers. Here, the factors that determine the in vivo behavior of liposomes and the current status of liposome-based radiopharmaceuticals are reviewed.

  8. Liposomes for scintigraphic imaging: optimization of in vivo behavior.

    Science.gov (United States)

    Boerman, O C; Oyen, W J; Corstens, F H; Storm, G

    1998-12-01

    Liposomes, microscopic lipid vesicles consisting of concentric phospholipid bilayers enclosing discrete aqueous spaces, have been investigated extensively as carries for drugs in attempts to achieve selective deposition and/or reduced toxicity. Liposomes radiolabeled with gamma emitters (67Ga, 111In and 99mTc) have been used for imaging purposes. Liposomes as formulated in the past, are rapidly taken up by cells of the mononuclear phagocyte system, primarily those located in liver and spleen. However, it has been shown during the last two decades that the in vivo behavior of liposomes can be modulated by modifying their formulation. The size and the lipid composition have a major influence on the blood clearance rate, hepatic uptake and splenic uptake of liposomes. The development of long circulating liposomes, in particular coating of the bilayer with polyethyleneglycol (PEG) resulted in liposomes that oppose recognition by the MPS, thus displaying even longer circulatory half-lives. By carefully adjusting the liposomal formulation, the in vivo characteristics of liposomes can be tailored such that they become suitable vehicles for imaging various pathological processes in vivo. Liposomes have been proposed for tumor imaging, for infection imaging and as blood pool markers. Here, the factors that determine the in vivo behavior of liposomes and the current status of liposome-based radiopharmaceuticals are reviewed. PMID:9973842

  9. Tumor targeting using liposomal antineoplastic drugs

    Directory of Open Access Journals (Sweden)

    Jörg Huwyler

    2008-03-01

    Full Text Available Jörg Huwyler1, Jürgen Drewe2, Stephan Krähenbühl21University of Applied Sciences Northwestern Switzerland, Institute of Pharma Technology, Muttenz, Switzerland; 2Department of Research and Division of Clinical Pharmacology, University Hospital Basel, Basel, SwitzerlandAbstract: During the last years, liposomes (microparticulate phospholipid vesicles have beenused with growing success as pharmaceutical carriers for antineoplastic drugs. Fields of application include lipid-based formulations to enhance the solubility of poorly soluble antitumordrugs, the use of pegylated liposomes for passive targeting of solid tumors as well as vector-conjugated liposomal carriers for active targeting of tumor tissue. Such formulation and drug targeting strategies enhance the effectiveness of anticancer chemotherapy and reduce at the same time the risk of toxic side-effects. The present article reviews the principles of different liposomal technologies and discusses current trends in this field of research.Keywords: tumor targeting, antineoplastic drugs, liposomes, pegylation, steric stabilization, immunoliposomes

  10. Miniaturized bioanalytical systems: enhanced performance through liposomes.

    Science.gov (United States)

    Edwards, Katie A; Bolduc, Olivier R; Baeumner, Antje J

    2012-08-01

    Biorecognition-element labeled liposomes are simple and versatile tools used to amplify signals for the detection of analytes of environmental, clinical, food safety, and national security interest. Relying on measurement of encapsulated species via electrochemical or spectroscopic techniques, or properties inherent to liposomes themselves (such as mass, refractive index, or charge), many advances have been made in both bench-scale and microfluidic applications. Some of these measurement techniques are inherently sensitivity limited, but through the inclusion of liposomes, reduced limits of detection potentially broaden the utility towards otherwise challenging levels of analytes. Other advances took advantage of the hydrophobic environment required by many biorecognition elements to expand the target selectivity range or utilized the amphipathic nature of the lipid bilayer to provide enhanced separation capabilities. Novel handling approaches included wavelength-specific release of contents encapsulated within thermosensitive liposomes or application of electric fields to move, concentrate, and strategically lyse liposomes. These and other topics are discussed in terms of either present incorporation or adaptation to microfluidic devices. PMID:22673065

  11. Liposome-Loaded Cell Backpacks.

    Science.gov (United States)

    Polak, Roberta; Lim, Rosanna M; Beppu, Marisa M; Pitombo, Ronaldo N M; Cohen, Robert E; Rubner, Michael F

    2015-12-30

    Cell backpacks, or micron-scale patches of a few hundred nanometers in thickness fabricated by layer-by-layer (LbL) assembly, are potentially useful vehicles for targeted drug delivery on the cellular level. In this work, echogenic liposomes (ELIPs) containing the anticancer drug doxorubicin (DOX) are embedded into backpacks through electrostatic interactions and LbL assembly. Poly(allylamine hydrochloride)/poly(acrylic acid) (PAH/PAA)n , and poly(diallyldimethylammonium chloride)/poly(styrene sulfonate) (PDAC/SPS)n film systems show the greatest ELIP incorporation of the films studied while maintaining the structural integrity of the vesicles. The use of ELIPs for drug encapsulation into backpacks facilitates up to three times greater DOX loading compared to backpacks without ELIPs. Cytotoxicity studies reveal that monocyte backpack conjugates remain viable even after 72 h, demonstrating promise as drug delivery vehicles. Because artificial vesicles can load many different types of drugs, ELIP containing backpacks offer a unique versatility for broadening the range of possible applications for cell backpacks. PMID:26616471

  12. Preferential spin canting in nanosize zinc ferrite

    Energy Technology Data Exchange (ETDEWEB)

    Pandey, Brajesh, E-mail: bpandey@gmail.com [Department of Applied Science, Symbiosis Institute of Technology, SIU, Lavale, Pune 411112 (India); Centro Brasileiro de Pesquisas Físicas, Rua Dr. Xavier Sigaud 150, 22290-180 Rio de Janeiro (Brazil); Litterst, F.J. [Centro Brasileiro de Pesquisas Físicas, Rua Dr. Xavier Sigaud 150, 22290-180 Rio de Janeiro (Brazil); Institut für Physik der Kondensierten Materie,Technische Universität Braunschweig, Mendelssohnstr. 3, 38106 Braunschweig (Germany); Baggio-Saitovitch, E.M. [Centro Brasileiro de Pesquisas Físicas, Rua Dr. Xavier Sigaud 150, 22290-180 Rio de Janeiro (Brazil)

    2015-07-01

    Zinc ferrite nanoparticles powder with average size of 10.0±0.5 nm was synthesized by the citrate precursor route. We studied the structural and magnetic properties using X-ray diffraction, vibrating sample magnetometry and Mössbauer spectroscopy. X-ray diffraction patterns show that the synthesized zinc ferrite possesses good spinel structure. Both Mössbauer and magnetization data indicate superparamagnetic ferrimagnetic particles at room temperature. The magnetic behavior is determined by a considerable degree of cation inversion with Fe{sup III} in tetrahedral A-sites. Mössbauer spectroscopy at low temperature and in high applied magnetic field reveals that A-site spins are aligned antiparallel to the applied field with some possible angular scatter whereas practically all octahedral B-site spins are canted contrasting some earlier reported partial B-site spin canting in nanosize zinc ferrite. Deviations from the antiferromagnetic arrangement of B-site spins are supposed to be caused by magnetic frustration effects. - Highlights: • Spinel structure ZnFe{sub 2}O{sub 4} nanoparticles in the uniform size range of 10.0±0.5 nm have been synthesized using the citrate precursor route. • Canting of the spins of A- and B-sublattice sites has been studied by low temperature and high magnetic field Mössbauer spectroscopy. • A-site spins are aligned antiparallel to the applied field with only small angular scatter. • B-site spins are strongly canted in contrast to earlier quoted only partial canting. • B site spin structure deviates significantly from a collinear antiferromagnetic arrangement.

  13. Liposomal cancer therapy: exploiting tumor characteristics

    DEFF Research Database (Denmark)

    Kaasgaard, Thomas; Andresen, Thomas Lars

    2010-01-01

    Importance of the field: More than 10 million people worldwide are diagnosed with cancer each year, and the development of effective cancer treatments is consequently of great significance. Cancer therapy is unfortunately hampered by severe dose-limiting side effects that reduce the efficacy of...... cancer treatments. In the search for more effective cancer treatments, nanoparticle- based drug delivery systems, such as liposomes, that are capable of delivering their drug payload selectively to cancer cells are among the most promising approaches. Areas covered in this review: This review provides an...... overview of current strategies for improving the different stages of liposomal cancer therapy, which involve transporting drug-loaded liposomes through the bloodstream, increasing tumor accumulation, and improving drug release and cancer cell uptake after accumulation at the tumor target site. What the...

  14. Dehydration resistance of liposomes containing trehalose glycolipids

    Science.gov (United States)

    Nyberg, Kendra; Goulding, Morgan; Parthasarathy, Raghuveer

    2010-03-01

    The pathogen, Mycobacterium tuberculosis, has an unusual outer membrane containing trehalose glycolipids that may contribute to its ability to survive freezing and dehydration. Based on our recent discovery that trehalose glycolipids confer dehydration resistance to supported lipid monolayers (Biophys. J. 94: 4718-4724 (2008); Langmuir 25: 5193-5198, (2009)), we hypothesized that liposomes containing synthetic trehalose glycolipids may be dehydration-resistant as well. To test this, we measured the leakage of encapsulated fluorophores and larger macromolecular cargo from such liposomes subject to freeze drying. Both leakage assays and size measurements show that the liposomes are dehydration-resistant. In addition to demonstrating a possibly technologically useful encapsulation platform, our results corroborate the view that encapsulation in a trehalose-glycolipid-rich membrane is a biophysically viable route to protection of mycobacteria from environmental stresses.

  15. Microfluidic-enabled liposomes elucidate size-dependent transdermal transport.

    Directory of Open Access Journals (Sweden)

    Renee R Hood

    Full Text Available Microfluidic synthesis of small and nearly-monodisperse liposomes is used to investigate the size-dependent passive transdermal transport of nanoscale lipid vesicles. While large liposomes with diameters above 105 nm are found to be excluded from deeper skin layers past the stratum corneum, the primary barrier to nanoparticle transport, liposomes with mean diameters between 31-41 nm exhibit significantly enhanced penetration. Furthermore, multicolor fluorescence imaging reveals that the smaller liposomes pass rapidly through the stratum corneum without vesicle rupture. These findings reveal that nanoscale liposomes with well-controlled size and minimal size variance are excellent vehicles for transdermal delivery of functional nanoparticle drugs.

  16. Recent Trends of Polymer Mediated Liposomal Gene Delivery System

    Directory of Open Access Journals (Sweden)

    Shyamal Kumar Kundu

    2014-01-01

    Full Text Available Advancement in the gene delivery system have resulted in clinical successes in gene therapy for patients with several genetic diseases, such as immunodeficiency diseases, X-linked adrenoleukodystrophy (X-ALD blindness, thalassemia, and many more. Among various delivery systems, liposomal mediated gene delivery route is offering great promises for gene therapy. This review is an attempt to depict a portrait about the polymer based liposomal gene delivery systems and their future applications. Herein, we have discussed in detail the characteristics of liposome, importance of polymer for liposome formulation, gene delivery, and future direction of liposome based gene delivery as a whole.

  17. Liposomes as a gene delivery system

    Directory of Open Access Journals (Sweden)

    C. Ropert

    1999-02-01

    Full Text Available Gene therapy is an active field that has progressed rapidly into clinical trials in a relatively short time. The key to success for any gene therapy strategy is to design a vector able to serve as a safe and efficient gene delivery vehicle. This has encouraged the development of nonviral DNA-mediated gene transfer techniques such as liposomes. Many liposome-based DNA delivery systems have been described, including molecular components for targeting given cell surface receptors or for escaping from the lysosomal compartment. Another recent technology using cationic lipids has been evaluated and has generated substantial interest in this approach to gene transfer.

  18. Metalloporphyrin intercalation in liposome membranes: ESR study

    OpenAIRE

    Man, Dariusz; Słota, Rudolf; Małgorzata A. Broda; Mele, Giuseppe; Li, Jun

    2010-01-01

    Liposomes characterized by membranes featuring diverse fluidity (liquid-crystalline and/or gel phase), prepared from egg yolk lecithin (EYL) and dipalmitoylphosphatidylcholine (DPPC), were doped with selected metalloporphyrins and the time-related structural and dynamic changes within the lipid double layer were investigated. Porphyrin complexes of Mg(II), Mn(III), Fe(III), Co(II), Ni(II), Cu(II), Zn(II), and the metal-free base were embedded into the particular liposome systems and tested fo...

  19. Application of Liposomes for Construction of Vaccines

    Czech Academy of Sciences Publication Activity Database

    Turánek, J.; Mašek, J.; Raška, M.; Ledvina, Miroslav

    Rijeka: InTech, 2012 - (Ghista, D.), s. 653-678 ISBN 978-953-307-471-9 R&D Projects: GA ČR(CZ) GAP304/10/1951; GA AV ČR(CZ) KAN200520703; GA AV ČR KAN200100801 Institutional research plan: CEZ:AV0Z40550506 Keywords : liposomes * metallochelation * recombinant vaccines * adjuvants Subject RIV: CC - Organic Chemistry http://www.intechopen.com/books/biomedical-science-engineering-and-technology/application-of-liposomes-for-construction-of-vaccines

  20. Overcoming cellular and tissue barriers to improve liposomal drug delivery

    Science.gov (United States)

    Kohli, Aditya G.

    Forty years of liposome research have demonstrated that the anti-tumor efficacy of liposomal therapies is, in part, driven by three parameters: 1) liposome formulation and lipid biophysics, 2) accumulation and distribution in the tumor, and 3) release of the payload at the site of interest. This thesis outlines three studies that improve on each of these delivery steps. In the first study, we engineer a novel class of zwitterlipids with an inverted headgroup architecture that have remarkable biophysical properties and may be useful for drug delivery applications. After intravenous administration, liposomes accumulate in the tumor by the enhanced permeability and retention effect. However, the tumor stroma often limits liposome efficacy by preventing distribution into the tumor. In the second study, we demonstrate that depletion of hyaluronan in the tumor stroma improves the distribution and efficacy of DoxilRTM in murine 4T1 tumors. Once a liposome has distributed to the therapeutic site, it must release its payload over the correct timescale. Few facile methods exist to quantify the release of liposome therapeutics in vivo. In the third study, we outline and validate a simple, robust, and quantitative method for tracking the rate and extent of release of liposome contents in vivo. This tool should facilitate a better understanding of the pharmacodynamics of liposome-encapsulated drugs in animals. This work highlights aspects of liposome behavior that have prevented successful clinical translation and proposes alternative approaches to improve liposome drug delivery.

  1. Liposome size and charge optimization for intraarterial delivery to gliomas.

    Science.gov (United States)

    Joshi, Shailendra; Cooke, Johann R N; Chan, Darren K W; Ellis, Jason A; Hossain, Shaolie S; Singh-Moon, Rajinder P; Wang, Mei; Bigio, Irving J; Bruce, Jeffrey N; Straubinger, Robert M

    2016-06-01

    Nanoparticles such as liposomes may be used as drug delivery vehicles for brain tumor therapy. Particle geometry and electrostatic properties have been hypothesized to be important determinants of effective tumor targeting after intraarterial injection. In this study, we investigate the combined roles of liposome size and surface charge on the effectiveness of delivery to gliomas after intraarterial injection. Intracarotid injection of liposomes was performed in separate cohorts of both healthy and C6 glioma-bearing Sprague Dawley rats after induction of transient cerebral hypoperfusion. Large (200 nm) and small (60-80 nm) fluorescent dye-loaded liposomes that were either cationic or neutral in surface charge were utilized. Delivery effectiveness was quantitatively measured both with real-time, in vivo and postmortem diffuse reflectance spectroscopy. Semi-quantitative multispectral fluorescence imaging was also utilized to assess the pattern and extent of liposome targeting within tumors. Large cationic liposomes demonstrated the most effective hemispheric and glioma targeting of all the liposomes tested. Selective large cationic liposome retention at the site of glioma growth was observed. The liposome deposition pattern within tumors after intraarterial injection was variable with both core penetration and peripheral deposition observed in specific tumors. This study provides evidence that liposome size and charge are important determinants of effective brain and glioma targeting after intraarterial injection. Our results support the future development of 200-nm cationic liposomal formulations of candidate intraarterial anti-glioma agents for further pre-clinical testing. PMID:27091339

  2. CLINICAL PHARMACOKINETIC ASPECTS OF STEALTH LIPOSOMES: A REVIEW

    Directory of Open Access Journals (Sweden)

    Drabu Sushma, Khanna Surabhi

    2010-12-01

    Full Text Available Stealth liposomes are long-circulating liposomes with inclusion of the synthetic polymer poly-(ethylene glycol (PEG in liposome composition. The presence of PEG on the surface of the liposomal carrier has been shown to extend bloodcirculation time while reducing mononuclear phagocyte system uptake. Further these liposomes exhibit increasing drug stability and solubility, lowering toxicity, increasing half-life, decreasing clearance and immunogenicity. Sterically stabilized vesicles can act either as long circulating micro reservoirs or tumour (or site of inflammation and infection targeting vehicles. The former applications require larger liposomes (0.2µm while the latter one is due to the ability of small vesicles to leave the blood circulation. The altered biodistribution of stealth liposomes, in addition to the accumulation at the sites characterised with porous blood capillaries, such as in tumors, inflammations, and infections. A pharmacogenomic approach for delivery of siRNA to cells is the use of liposomes as targeted delivery vehicles. Stealth technology summarizes pre-clinical and clinical data relating to the principal liposome formulations, encapsulating active molecules, with high target efficiency and activity. Further these liposomes offer improvements in bioreclamation and various monitoring and analytical-diagnostic applications. The paper reviews the clinical aspects of these liposomes with longer therapeutic half lives in diseases like Reconstitution of membrane proteins into artificial membranes, model biological membranes, cell function, fusion, recognition , pharmaceutics studies of drug action , medicine drug-delivery and medical diagnostics, gene therapy and there extensive use in the pharmaceutical industry.

  3. Liposomes of terbutaline sulphate: in vitro and in vivo studies.

    Science.gov (United States)

    Joshi, M R; Misra, A N

    1999-09-01

    In vitro studies were conducted to understand the comparative drug diffusion pattern, across artificial membrane, of the drug and of the prepared liposomes of different liposomal membrane composition. In vivo studies were carried out to determine the extent and time-course of pulmonary tissue uptake of administered liposomes containing terbutaline sulphate(TER) on rat lungs. In vitro studies revealed that the drug released from the prepared liposomes obeys Higuchi's diffusion controlled model. Different loading doses and release patterns of drug from the liposomes can be obtained by altering the PC:CHOL ratio and incorporation of cholesterol was found to reduce permeability of the membrane. Similarly drug absorption in vivo in rat's lung following intratracheal instillation, prolonged over 12 hr by liposomal entrapment of TER. The findings of present investigation indicated that liposomally encapsulated TER can be used for pulmonary delivery for maximizing the therapeutic efficacy and reducing undesirable side effects. PMID:10687283

  4. Preparation of nanosized non-oxide powders using diatomaceous earth

    Directory of Open Access Journals (Sweden)

    Šaponjić A.

    2009-01-01

    Full Text Available In this paper the nanosized non-oxide powders were prepared by carbothermal reduction and subsequent nitridation of diatomaceous earth which is a waste product from coal exploitation. Our scope was to investigate the potential use of diatomaceous earth as a main precursor for low-cost nanosized non-oxide powder preparation as well as to solve an environmental problem. The influence of carbon materials (carbonized sucrose, carbon cryogel and carbon black as a reducing agent on synthesis and properties of low-cost nanosized nonoxide powders was also studied. The powders were characterized by specific surface area, X-ray and SEM investigations. It was found that by using diatomaceous earth it is was possible to produce either a mixture of non-oxide powders (Si3N4/SiC or pure SiC powders depending on temperature.

  5. Synthesis of nanosize MnO2 and its performence

    Institute of Scientific and Technical Information of China (English)

    顾大明; 魏杰

    2003-01-01

    Sol sol-gel method and solid phase redox reaction were respectively applied in preparation of Nanos-ize MnO2 powders. The experiments showed that only Mn2O3 could be obtained from ignition of Mn( Ⅱ ) in themuffle furnace in air, and Mn2O3 had to be disproportionated in acids to gain MnO2. The analysis of XRD andTEM technique revealed that the diameters of nanosize MnO2 obtained by sol-gel method was 35 ~45 nm andthe x in MnOx was 1.9; the particle size of MnO2 produced from solid phase redox reaction was 10 ~ 20 nm andthe x in MnOx equaled 1.94. The test results have proved that the discharge property of alkaline-manganese bat-tery could be improved by nanosize MnO2.

  6. Template-free nanosized faujasite-type zeolites

    Science.gov (United States)

    Awala, Hussein; Gilson, Jean-Pierre; Retoux, Richard; Boullay, Philippe; Goupil, Jean-Michel; Valtchev, Valentin; Mintova, Svetlana

    2015-04-01

    Nanosized faujasite (FAU) crystals have great potential as catalysts or adsorbents to more efficiently process present and forthcoming synthetic and renewable feedstocks in oil refining, petrochemistry and fine chemistry. Here, we report the rational design of template-free nanosized FAU zeolites with exceptional properties, including extremely small crystallites (10-15 nm) with a narrow particle size distribution, high crystalline yields (above 80%), micropore volumes (0.30 cm3 g-1) comparable to their conventional counterparts (micrometre-sized crystals), Si/Al ratios adjustable between 1.1 and 2.1 (zeolites X or Y) and excellent thermal stability leading to superior catalytic performance in the dealkylation of a bulky molecule, 1,3,5-triisopropylbenzene, probing sites mostly located on the external surface of the nanosized crystals. Another important feature is their excellent colloidal stability, which facilitates a uniform dispersion on supports for applications in catalysis, sorption and thin-to-thick coatings.

  7. Synthesis and characterization of nanosized lead oxide

    Science.gov (United States)

    Laak, Sheau Tyan

    Nanosized lead oxide as well as copper-doped lead oxide are prepared using two different synthetic techniques; hydrothermal and precipitation. The precipitation method involves simply reacting lead (IV) acetate with distilled water. On the other hand, the hydrothermal process used an autoclave with the presence of Polyvinyl Pyrrolidone (PVP) to prepare lead oxide (PbO 2) hollow spheres, and lead oxide (Pb3O4) microtubes at reaction temperatures of 90°C and 180°C, respectively. Characterization of the synthesized material was carried out using X-Ray Diffraction (XRD), Thermal Gravimetric Analysis (TGA), Differential Thermal Analysis (DTA), and Scanning Electron Microscopy (SEM). X-Ray Diffraction shows that the prepared lead oxides using the hydrothermal process with a reaction a temperature of 90°C is crystalline α PbO 2. SEM shows that the prepared particles are hollow spheres. It also shows uniformity in shape and size. In contrast, X-Ray Diffraction and SEM show that the prepared lead oxide using the hydrothermal process with a reaction temperature of 180°C is nanofiber crystalline α PbO2. It also shows uniformity in shape and size. As to the precipitation method, X-Ray Diffraction shows that the sample is crystalline β PbO2. X-Ray Diffraction revealed that these lead oxides show two different transitions, from β PbO2 to Pb3O4, and Pb3O4 to PbO. These observations were supported by TGA and DTA at 400°C and 700°C, respectively. SEM analysis shows that the prepared β PbO2 sample does not show uniformity, neither in size nor in shape. Indeed, particles appear to congregate and form much larger particles. The results from our study suggest that simple precipitation can lead to the product of PbO2, it however cannot guarantee uniformity. The use of an autoclave in the presence of a polymer such as PVP allowed the precipitation of uniform nano PbO2. In addition, the temperature appeared to affect the morphology of the final product. When low temperature is

  8. Study on Leakage of Sesame (Sesamum indicum L. and Coconut (Cocos nucifera L. Liposomes

    Directory of Open Access Journals (Sweden)

    Dwi Hudiyanti

    2015-03-01

    Full Text Available Leakage phenomena on sesame (Sesamum indicum L. and coconut (Cocos nucifera L. liposomes has been studied to evaluate their ability as drug delivery materials. Permeation of carboxyfluorescein through the liposomes with and without added cholesterol was examined. Sesame liposomes release carboxyfluorescein less than coconut liposomes in all circumstances. Sesame liposomes save about 50% of payload after 17 hours of storage while coconut liposomes only 10%. Addition of cholesterol has increase storage capability of all liposomes. The sesame-cholesterol and coconut-cholesterol liposomes save greater amount of payload compare to the original. Sesame liposomes have better potency as drug delivery systems.

  9. Root uptake and phytotoxicity of nanosized molybdenum octahedral clusters

    International Nuclear Information System (INIS)

    Highlights: ► We investigated the effect of nanosized Mo6 clusters on the growth of rapeseed plants. ► The aggregation state of the clusters depends on the dispersion medium. ► The concentration-dependant toxicity of the clusters depends on aggregation state. ► We took into account the possible contribution to toxicity of dissolved ionic species. ► The root uptake of the clusters was followed by NanoSIMS. - Abstract: Here are examined the root uptake and phytotoxicity of octahedral hexamolybdenum clusters on rapeseed plants using the solid state compound Cs2Mo6Br14 as cluster precursor. [Mo6Br14]2− cluster units are nanosized entities offering a strong and stable emission in the near-infrared region with numerous applications in biotechnology. To investigate cluster toxicity on rapeseed plants, two different culture systems have been set up, using either a water-sorbing suspension of cluster aggregates or an ethanol-sorbing solution of dispersed nanosized clusters. Size, shape, surface area and state of clusters in both medium were analyzed by FE-SEM, BET and XPS. The potential contribution of cluster dissolution to phytotoxicity was evaluated by ICP-OES and toxicity analysis of Mo, Br and Cs. We showed that the clusters did not affect seed germination but greatly inhibited plant growth. This inhibition was much more important when plants were treated with nanosized entities than with microsized cluster aggregates. In addition, nanosized clusters affected the root morphology in a different manner than microsized cluster aggregates, as shown by FE-SEM observations. The root penetration of the clusters was followed by secondary ion mass spectroscopy with high spatial resolution (NanoSIMS) and was also found to be much more important for treatments with nanosized clusters.

  10. Processing of silicon nitride and alumina nanosize powders

    Energy Technology Data Exchange (ETDEWEB)

    Gonzalez, E.J.; Piermarini, G.; Hockey, B.; Malghan, S.G. [National Inst. of Standard and Technology, Gaithersburg, MD (United States)

    1995-08-01

    The effects of pressure on the compaction and subsequent processing of nanosize {gamma} alumina powders were studied. A 3 mm diameter piston/cylinder die was used to compact the nanosize powders to pressures of 1 and 2.5 GPa. The green bodies were sintered at temperatures up to 1600{degrees}C. Results show that green body density can be increased by higher compaction pressures. It appears that as a result of the {gamma}-to-{alpha} transformation in alumina, higher green density does not necessarily produce a higher density sintered alumina body. The microstructures of the sintered bodies are described in terms of porosity and phase content.

  11. Wear Behavior of Austempered Ductile Iron with Nanosized Additives

    OpenAIRE

    J. Kaleicheva

    2014-01-01

    The microstructure and properties of austempered ductile iron (ADI) strengthened with nanosized addtives of titanium nitride + titanium carbonitride (TiN + TiCN), titanium nitride TiN and cubic boron nitride cBN are investigated. The TiN, TiCN and cBN, nanosized particles are coated by electroless nickel coating EFTTOM-NICKEL prior to the edition to the melt. The spheroidal graphite iron samples are undergoing an austempering, including heating at 900 оС for an hour, after that isotherma...

  12. Properties of liposomal membranes containing lysolecithin.

    Science.gov (United States)

    Kitagawa, T; Inoue, K; Nojima, S

    1976-06-01

    Liposomes have been prepared with lysolecithin (1-acyl-sn-3-glycerylphosphorylcholine), egg lecithin (3-sn-phosphatidylcholine), dicetyl phosphate, and cholesterol. The ability to function as a barrier to the diffusion of glucose marker and the sensitivities of the liposomes to hypotonic treatment and other reagents which modified the permeability were examined. Generally, lysolecithin incorporation decreased the effectiveness of the membranes as a barrier to glucose and made the membranes more "osmotically fragile." Cholesterol incorporation counteracted the effect of incorporated lysolecithin. The more cholesterol incorporated into liposomes, the more lysolecthin could be incorporated into the membrane without loss of function as a barrier. With more than 50 mole% of colesterol, lysolecithin alone could form membranes which were practically impermeable to glucose. The hemolytic activity of lysolecithin was affected by mixing with various lecithins or cholesterol. Liposomes containing lysolecithin, which have the ability to trap glucose marker, showed poor hemolytic activity, while lipid micelles with lysolecithin (which could trap little glucose) showed almost the same hemolytic activity as lysolecithin itself. There seems to be a close correlation between hemolytic activity and barrier function of lipid micelles. PMID:986392

  13. Liposomal encapsulated rhodomyrtone: a novel antiacne drug.

    Science.gov (United States)

    Chorachoo, Julalak; Amnuaikit, Thanaporn; Voravuthikunchai, Supayang P

    2013-01-01

    Rhodomyrtone isolated from the leaves of Rhodomyrtus tomentosa possesses antibacterial, anti-inflammatory, and anti-oxidant activities. Since rhodomyrtone is insoluble in water, it is rather difficult to get to the target sites in human body. Liposome exhibited ability to entrap both hydrophilic and hydrophobic compounds and easily penetrate to the target site. The present study aimed to develop a novel liposomal encapsulated rhodomyrtone formulations. In addition, characterization of liposome, stability profiles, and their antiacne activity were performed. Three different formulations of total lipid concentrations 60, 80, and 100  μ mol/mL were used. Formulation with 60  μ mol/mL total lipid (phosphatidylcholine from soybean and cholesterol from lanolin in 4 : 1, w/w) exhibited the highest rhodomyrtone encapsulation efficacy (65.47 ± 1.7%), average particle size (209.56 ± 4.8 nm), and ζ -potential (-41.19 ± 1.3 mV). All formulations demonstrated good stability when stored for 2 months in dark at 4°C as well as room temperature. Minimal inhibitory concentration and minimal bactericidal concentration values of liposomal formulation against 11 clinical bacterial isolates and reference strains ranged from 1 to 4 and from 4 to 64  μ g/mL, respectively, while those of rhodomyrtone were 0.25-1 and 0.5-2  μ g/mL, respectively. The MIC and MBC values of liposome formulation were more effective than topical drugs against Staphylococcus aureus and Staphylococcus epidermidis. PMID:23762104

  14. Liposomal Encapsulated Rhodomyrtone: A Novel Antiacne Drug

    Directory of Open Access Journals (Sweden)

    Julalak Chorachoo

    2013-01-01

    Full Text Available Rhodomyrtone isolated from the leaves of Rhodomyrtus tomentosa possesses antibacterial, anti-inflammatory, and anti-oxidant activities. Since rhodomyrtone is insoluble in water, it is rather difficult to get to the target sites in human body. Liposome exhibited ability to entrap both hydrophilic and hydrophobic compounds and easily penetrate to the target site. The present study aimed to develop a novel liposomal encapsulated rhodomyrtone formulations. In addition, characterization of liposome, stability profiles, and their antiacne activity were performed. Three different formulations of total lipid concentrations 60, 80, and 100 μmol/mL were used. Formulation with 60 μmol/mL total lipid (phosphatidylcholine from soybean and cholesterol from lanolin in 4 : 1, w/w exhibited the highest rhodomyrtone encapsulation efficacy (65.47 ± 1.7%, average particle size (209.56 ± 4.8 nm, and ζ-potential (–41.19 ± 1.3 mV. All formulations demonstrated good stability when stored for 2 months in dark at 4°C as well as room temperature. Minimal inhibitory concentration and minimal bactericidal concentration values of liposomal formulation against 11 clinical bacterial isolates and reference strains ranged from 1 to 4 and from 4 to 64 μg/mL, respectively, while those of rhodomyrtone were 0.25–1 and 0.5–2 μg/mL, respectively. The MIC and MBC values of liposome formulation were more effective than topical drugs against Staphylococcus aureus and Staphylococcus epidermidis.

  15. Internalization of paramagnetic phosphatidylserine-containing liposomes by macrophages

    Directory of Open Access Journals (Sweden)

    Geelen Tessa

    2012-08-01

    Full Text Available Abstract Background Inflammation plays an important role in many pathologies, including cardiovascular diseases, neurological conditions and oncology, and is considered an important predictor for disease progression and outcome. In vivo imaging of inflammatory cells will improve diagnosis and provide a read-out for therapy efficacy. Paramagnetic phosphatidylserine (PS-containing liposomes were developed for magnetic resonance imaging (MRI and confocal microscopy imaging of macrophages. These nanoparticles also provide a platform to combine imaging with targeted drug delivery. Results Incorporation of PS into liposomes did not affect liposomal size and morphology up to 12 mol% of PS. Liposomes containing 6 mol% of PS showed the highest uptake by murine macrophages, while only minor uptake was observed in endothelial cells. Uptake of liposomes containing 6 mol% of PS was dependent on the presence of Ca2+ and Mg2+. Furthermore, these 6 mol% PS-containing liposomes were mainly internalized into macrophages, whereas liposomes without PS only bound to the macrophage cell membrane. Conclusions Paramagnetic liposomes containing 6 mol% of PS for MR imaging of macrophages have been developed. In vitro these liposomes showed specific internalization by macrophages. Therefore, these liposomes might be suitable for in vivo visualization of macrophage content and for (visualization of targeted drug delivery to inflammatory cells.

  16. Stimuli-Responsive Liposomes for Controlled Drug Delivery

    KAUST Repository

    Li, Wengang

    2014-09-01

    Liposomes are promising drug delivery vesicles due to their biodegradibility, large volume and biocompatibility towards both hydrophilic and hydrophobic drugs. They suffer, however, from poor stability which limits their use in controlled delivery applications. Herein, a novel method was devised for modification of liposomes with small molecules, polymers or nanoparticles to afford stimuli responsive systems that release on demand and stay relatively stable in the absence of the trigger.. This dissertation discusses thermosensitive, pH sensitive, light sensitive and magnetically triggered liposomes that have been prepared for controlled drug delivery application. RAFT polymerization was utilized for the preparation of thermosensitive liposomes (Cholesterol-PNIPAm) and acid-labile liposomes (DOPE-PAA). With low Mw Cholesterol-PNIPAm, the thermosensitive liposomes proved to be effective for controlled release and decreased the cytotoxicity of PNIPAm by eliciting the polymer doses. By crosslinking the DOPE-PAA on liposome surface with acid-labile diamine linkers, DOPE-PAA liposomes were verified to be sensitive at low pH. The effects of polymer structures (linear or hyperbranched) have also been studied for the stability and release properties of liposomes. Finally, a dual-responsive Au@SPIO embedded liposome hybrid (ALHs) was prepared with light-induced “on-and-off” function by photo-thermal process (visible light) and instant release properties triggered by alternating magnetic field, respectively. The ALH system would be further applied into the cellular imaging field as MRI contrast agent.

  17. Covalent immobilization of liposomes on plasma functionalized metallic surfaces.

    Science.gov (United States)

    Mourtas, S; Kastellorizios, M; Klepetsanis, P; Farsari, E; Amanatides, E; Mataras, D; Pistillo, B R; Favia, P; Sardella, E; d'Agostino, R; Antimisiaris, S G

    2011-05-01

    A method was developed to functionalize biomedical metals with liposomes. The novelty of the method includes the plasma-functionalization of the metal surface with proper chemical groups to be used as anchor sites for the covalent immobilization of the liposomes. Stainless steel (SS-316) disks were processed in radiofrequency glow discharges fed with vapors of acrylic acid to coat them with thin adherent films characterized by surface carboxylic groups, where liposomes were covalently bound through the formation of amide bonds. For this, liposomes decorated with polyethylene glycol molecules bearing terminal amine-groups were prepared. After ensuring that the liposomes remain intact, under the conditions applying for immobilization; different attachment conditions were evaluated (incubation time, concentration of liposome dispersion) for optimization of the technique. Immobilization of calcein-entrapping liposomes was evaluated by monitoring the percent of calcein attached on the surfaces. Best results were obtained when liposome dispersions with 5mg/ml (liposomal lipid) concentration were incubated on each disk for 24h at 37°C. The method is proposed for developing drug-eluting biomedical materials or devices by using liposomes that have appropriate membrane compositions and are loaded with drugs or other bioactive agents. PMID:21273051

  18. Bladder uptake of liposomes after intravesical administration occurs by endocytosis.

    Directory of Open Access Journals (Sweden)

    Bharathi Raja Rajaganapathy

    Full Text Available Liposomes have been used therapeutically and as a local drug delivery system in the bladder. However, the exact mechanism for the uptake of liposomes by bladder cells is unclear. In the present study, we investigated the role of endocytosis in the uptake of liposomes by cultured human UROtsa cells of urothelium and rat bladder. UROtsa cells were incubated in serum-free media with liposomes containing colloidal gold particles for 2 h either at 37°C or at 4°C. Transmission Electron Microscopy (TEM images of cells incubated at 37°C found endocytic vesicles containing gold inside the cells. In contrast, only extracellular binding was noticed in cells incubated with liposomes at 4°C. Absence of liposome internalization at 4°C indicates the need of energy dependent endocytosis as the primary mechanism of entry of liposomes into the urothelium. Flow cytometry analysis revealed that the uptake of liposomes at 37°C occurs via clathrin mediated endocytosis. Based on these observations, we propose that clathrin mediated endocytosis is the main route of entry for liposomes into the urothelial layer of the bladder and the findings here support the usefulness of liposomes in intravesical drug delivery.

  19. Liposome disposition in vivo. VI: Delivery to the lung

    International Nuclear Information System (INIS)

    The effect of negatively charged liposome components and vesicle size on the time course and dose dependency of liposome disposition in mice was studied with a view to optimizing liposome delivery to the lung. The disposition of large multilamellar liposomes was followed using 125I-labeled p-hydroxybenzamidine phosphatidyl ethanolamine. Of the three negatively charged liposome compositions studied (phosphatidyl choline-X-cholesterol-alpha-tocopherol, molar ratio: 4:1:5:0.1; X . phosphatidyl serine, dipalmitoyl phosphatidic acid, or phosphatidyl glycerol), phosphatidyl serine liposomes resulted in the greatest accumulation in lungs. Lung levels decreased up to 95 h postdose, at which time 6% of the liposome dose present at 2 h still remained. The disposition of phosphatidyl serine-containing liposomes was independent of dose for the range 0.04-21 mumol/animal. When liposomes containing phosphatidyl choline were prepared using a variety of extrusion and dialysis conditions, a strong link between liposome size and lung accumulation was revealed. A maximum lung accumulation of 30.9% of the administered dose was achieved with no detectable gross pathological lung lesions up to 24 h postdose

  20. Effect of chitosan coating on the characteristics of DPPC liposomes

    Directory of Open Access Journals (Sweden)

    Mohsen M. Mady

    2010-07-01

    Full Text Available Because it is both biocompatible and biodegradable, chitosan has been used to provide a protective capsule in new drug formulations. The present work reports on investigations into some of the physicochemical properties of chitosan-coated liposomes, including drug release rate, transmission electron microscopy (TEM, zeta potential and turbidity measurement. It was found that chitosan increases liposome stability during drug release. The coating of DPPC liposomes with a chitosan layer was confirmed by electron microscopy and the zeta potential of liposomes. The coating of liposomes by chitosan resulted in a marginal increase in the size of the liposomes, adding a layer of (92 ± 27.1 nm. The liposomal zeta potential was found to be increasingly positive as chitosan concentration increased from 0.1% to 0.3% (w/v, before stabilising at a relatively constant value. Turbidity studies revealed that the coating of DPPC liposomes with chitosan did not significantly modify the main phase transition temperature of DPPC at examined chitosan concentrations. The appropriate combination of liposomal and chitosan characteristics may produce liposomes with specific, prolonged and controlled release.

  1. Membrane with Stable Nanosized Microstructure and Method for Producing same

    DEFF Research Database (Denmark)

    2010-01-01

    The present invention provides a membrane, comprising in this order a first catalyst layer, an electronically and ionically conducting layer having a nanosized microstructure, and a second catalyst layer, characterized in that the electronically and ionically conducting layer is formed from an...... electrolyte material, a grain growth inhibitor and/or grain boundary modifier, and a method for producing same....

  2. Synthesis of Nano-sized Boehmites for Optimum Phosphate Sorption

    DEFF Research Database (Denmark)

    Watanabe, Yujiro; Kasama, Takeshi; Fukushi, Keisuke;

    2011-01-01

    Nano-sized boehmites with different crystallinity were synthesized at the temperature range of 25 to 200°C in order to produce phosphate absorbents with high capacity. The physicochemical property of boehmites was depended on the synthesis temperature: the particle size was increased and the...

  3. Biomolecular coronas provide the biological identity of nanosized materials

    NARCIS (Netherlands)

    Monopoli, Marco P; Åberg, Christoffer; Salvati, Anna; Dawson, Kenneth A

    2012-01-01

    The search for understanding the interactions of nanosized materials with living organisms is leading to the rapid development of key applications, including improved drug delivery by targeting nanoparticles, and resolution of the potential threat of nanotechnological devices to organisms and the en

  4. AHE measurements of very thin films and nanosized dots

    NARCIS (Netherlands)

    Kikuchi, N.; Murillo, R.; Lodder, J.C.

    2005-01-01

    In this paper we present anomalous Hall effect analysis from very thin Co (0.5 nm) film, Co/Pt multilayers and large areas of nanosized dots as well as from a few magnetic dots having a diameter of 120 nm. The dot arrayis prepared from Co/Pt multilayer by using laser interference lithography (LIL) w

  5. Synthesis of nanosized metal particles from an aerosol

    Directory of Open Access Journals (Sweden)

    Srećko R. Stopić

    2013-10-01

    Full Text Available The synthesis of metallic nanoparticles from the precursor solution of salts using the ultrasonic spray pyrolysis method was considered in this work. During the control of process parameters (surface tension and density, the concentration of solution, residence time of aerosol in the reactor, presence of additives, gas flow rate, decomposition temperature of aerosol, type of precursor and working atmosphere it is possible to guide the process in order to obtain powders with such a morphology which satisfies more complex requirements for the desired properties of advanced engineering materials.  Significant advance in the improvement of powder characteristics (lower particles sizes, better spheroidity, higher surface area was obtained by the application of the ultrasonic generator for the preparation of aerosols. Ultrasonic spray pyrolysis is performed by the action of a powerful source of ultrasound on the corresponding precursor solution forming the aerosol with a constant droplet size, which depends on the characteristics of liquid and the frequency of ultrasound. The produced aerosols were transported into the hot reactor, which enables the reaction to occur in a very small volume of a particle and formation of  nanosized powder. Spherical, nanosized particles of metals (Cu, Ag, Au, Co were produced with new and improved physical and chemical characteristics at the IME, RWTH Aachen University. The high costs associated with small quantities of produced nanosized particles represent a limitation of the USP-method. Therefore, scale up of the ultrasonic spray pyrolysis was performed as a final target in the synthesis of nanosized powder.

  6. Albumin coated liposomes: a novel platform for macrophage specific drug delivery

    OpenAIRE

    Clément Vuarchey; Sushil Kumar; Reto Schwendener

    2011-01-01

    Here we report a new and efficient approach of macrophage specific drug delivery by coating liposomes with albumin. Activated albumin was reacted with liposomes containing polyethylene glycol (PEG) as hydrophilic spacers to create a flexible layer of covalently bound albumin molecules on the liposome surface. Albumin coated liposomes were taken up faster and more efficiently than uncoated liposomes by murine macrophages. Liposome uptake was significantly higher in macropha - ges as compared t...

  7. Study on Leakage of Sesame (Sesamum indicum L.) and Coconut (Cocos nucifera L.) Liposomes

    OpenAIRE

    Dwi Hudiyanti; Tri Joko Raharjo; Narsito Narsito; Sri Noegrohati

    2015-01-01

    Leakage phenomena on sesame (Sesamum indicum L.) and coconut (Cocos nucifera L.) liposomes has been studied to evaluate their ability as drug delivery materials. Permeation of carboxyfluorescein through the liposomes with and without added cholesterol was examined. Sesame liposomes release carboxyfluorescein less than coconut liposomes in all circumstances. Sesame liposomes save about 50% of payload after 17 hours of storage while coconut liposomes only 10%. Addition of cholesterol has increa...

  8. A hypersensitive reaction in potato tuber tissue treated with nanosized metal particles and conducting polymer

    International Nuclear Information System (INIS)

    Nanosized metal particles and aniline are well known as materials used in a biosensor. However, it has not been reported how these materials affect the environment like a soil, plant and water system. This study showed that nanosized silver particles induced a hypersensitive reaction (HR) and aniline induced a toxic necrosis in potato tuber tissue. But a nanosized gold particle did not induce toxic phenomenon and GR. The nanosized metal particles were prepared by irradiating a solution comprising of a silver salt or a gold salt with radiation. Our results suggest that nanosized gold particles can be recommended as an environmental-friendly material to produce a biosensor

  9. A hypersensitive reaction in potato tuber tissue treated with nanosized metal particles and conducting polymer

    Energy Technology Data Exchange (ETDEWEB)

    Park, He Jun; Kim, Hwa Jung; Park, Sang Hyun [Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of)

    2009-12-15

    Nanosized metal particles and aniline are well known as materials used in a biosensor. However, it has not been reported how these materials affect the environment like a soil, plant and water system. This study showed that nanosized silver particles induced a hypersensitive reaction (HR) and aniline induced a toxic necrosis in potato tuber tissue. But a nanosized gold particle did not induce toxic phenomenon and GR. The nanosized metal particles were prepared by irradiating a solution comprising of a silver salt or a gold salt with radiation. Our results suggest that nanosized gold particles can be recommended as an environmental-friendly material to produce a biosensor.

  10. Liposome-based drug delivery in breast cancer treatment

    International Nuclear Information System (INIS)

    Drug delivery systems can in principle provide enhanced efficacy and/or reduced toxicity for anticancer agents. Long circulating macromolecular carriers such as liposomes can exploit the 'enhanced permeability and retention' effect for preferential extravasation from tumor vessels. Liposomal anthracyclines have achieved highly efficient drug encapsulation, resulting in significant anticancer activity with reduced cardiotoxicity, and include versions with greatly prolonged circulation such as liposomal daunorubicin and pegylated liposomal doxorubicin. Pegylated liposomal doxorubucin has shown substantial efficacy in breast cancer treatment both as monotherapy and in combination with other chemotherapeutics. Additional liposome constructs are being developed for the delivery of other drugs. The next generation of delivery systems will include true molecular targeting; immunoliposomes and other ligand-directed constructs represent an integration of biological components capable of tumor recognition with delivery technologies

  11. Development of monodispersed and functional magnetic polymeric liposomes via simple liposome method

    International Nuclear Information System (INIS)

    We are reporting a simple and rapid method to prepare superparamagnetic, controlled size, and monodispersed magnetic cationic polymeric liposomes (MCPL) by octadecyl quaternized carboxymethyl chitosan (OQCMC) and cholesterol. The whole process is only about 25 min with simple thin-film dispersion and solvent evaporation method. Hydrophilic magnetic nanoparticles (LM) and hydrophobic magnetic nanoparticles (BM) can be encapsulated into these cationic polymeric liposomes, simultaneously or respectively. A model hydrophobic drug indomethacin can be successfully filled in MCPL with high drug loading capacity 22%. MCPL encapsulating BM also showed strong DNA (pEGFP) binding ability. Drug-loaded MCPL have a long and controlled sustained release profile by changing the number of polymeric lipid layer. These functional MCPL nanospheres can be allowed to serve as ideal candidates for many biomedical applications.Graphical AbstractA simple and rapid liposome method was reported to prepare superparamagnetic, controlled size, and monodispersed magnetic cationic polymeric liposomes (MCPL) by polymeric surfactant, octadecyl quaternized carboxymethyl chitosan (OQCMC), and cholesterol. Hydrophilic Fe3O4 ferrofluid and hydrophobic magnetic nanoparticles can be encapsulated into these cationic polymeric liposomes, simultaneously or respectively. Hydrophobic drug indomethacin can be encapsulated into this MCPL with high encapsulating efficiency and with controlled release profile by changing the number of polymeric lipid layer.

  12. Development of monodispersed and functional magnetic polymeric liposomes via simple liposome method

    Energy Technology Data Exchange (ETDEWEB)

    Liang Xiaofei; Wang Hanjie [Tianjin University and Tianjin Key Laboratory of Composites and Functional Materials, Institute of Nanobiotechnology, School of Materials Science and Engineering (China); Jiang Xinguo [Fudan University, School of Pharmacy (China); Chang Jin, E-mail: jinchang@tju.edu.c [Tianjin University and Tianjin Key Laboratory of Composites and Functional Materials, Institute of Nanobiotechnology, School of Materials Science and Engineering (China)

    2010-06-15

    We are reporting a simple and rapid method to prepare superparamagnetic, controlled size, and monodispersed magnetic cationic polymeric liposomes (MCPL) by octadecyl quaternized carboxymethyl chitosan (OQCMC) and cholesterol. The whole process is only about 25 min with simple thin-film dispersion and solvent evaporation method. Hydrophilic magnetic nanoparticles (LM) and hydrophobic magnetic nanoparticles (BM) can be encapsulated into these cationic polymeric liposomes, simultaneously or respectively. A model hydrophobic drug indomethacin can be successfully filled in MCPL with high drug loading capacity 22%. MCPL encapsulating BM also showed strong DNA (pEGFP) binding ability. Drug-loaded MCPL have a long and controlled sustained release profile by changing the number of polymeric lipid layer. These functional MCPL nanospheres can be allowed to serve as ideal candidates for many biomedical applications.Graphical AbstractA simple and rapid liposome method was reported to prepare superparamagnetic, controlled size, and monodispersed magnetic cationic polymeric liposomes (MCPL) by polymeric surfactant, octadecyl quaternized carboxymethyl chitosan (OQCMC), and cholesterol. Hydrophilic Fe{sub 3}O{sub 4} ferrofluid and hydrophobic magnetic nanoparticles can be encapsulated into these cationic polymeric liposomes, simultaneously or respectively. Hydrophobic drug indomethacin can be encapsulated into this MCPL with high encapsulating efficiency and with controlled release profile by changing the number of polymeric lipid layer.

  13. Microfluidic-Enabled Liposomes Elucidate Size-Dependent Transdermal Transport

    OpenAIRE

    Renee R Hood; Kendall, Eric L.; Junqueira, Mariana; Vreeland, Wyatt N.; Quezado, Zenaide; Julia C Finkel; DeVoe, Don L.

    2014-01-01

    Microfluidic synthesis of small and nearly-monodisperse liposomes is used to investigate the size-dependent passive transdermal transport of nanoscale lipid vesicles. While large liposomes with diameters above 105 nm are found to be excluded from deeper skin layers past the stratum corneum, the primary barrier to nanoparticle transport, liposomes with mean diameters between 31–41 nm exhibit significantly enhanced penetration. Furthermore, multicolor fluorescence imaging reveals that the small...

  14. [Novel possibilities of development and therapeutical application of liposomes].

    Science.gov (United States)

    Bozó, Tamás; Pál, Szilárd; Dévay, Attila

    2008-01-01

    Properties and possibilities of application of liposomal drug delivery systems are summarized in this review. Technological and biopharmeceutical criteria that have to be taken into consideration in the course of development of biocompatible liposomes are discussed. The manner and possibilities of active and passive targeting are shown according to the literary data and special liposome-based drug delivery systems responsible for pathologic or arteficial stimuli are introduced. PMID:18986087

  15. Effect of chitosan coating on the characteristics of DPPC liposomes

    OpenAIRE

    Mady, Mohsen M; Mirhane M. Darwish

    2010-01-01

    Because it is both biocompatible and biodegradable, chitosan has been used to provide a protective capsule in new drug formulations. The present work reports on investigations into some of the physicochemical properties of chitosan-coated liposomes, including drug release rate, transmission electron microscopy (TEM), zeta potential and turbidity measurement. It was found that chitosan increases liposome stability during drug release. The coating of DPPC liposomes with a chitosan layer was con...

  16. Increased Liposome Extravasation in Selected Tissues: Effect of Substance P

    Science.gov (United States)

    Rosenecker, Joseph; Zhang, Weiming; Hong, Keelung; Lausier, James; Geppetti, Pierangelo; Yoshihara, Shigemi; Papahadjopoulos, Demetrios; Nadel, Jay A.

    1996-07-01

    We have used a pharmacologic mediator to open intercellular connections in selected vessels to allow liposomes to escape from the blood stream and to extravasate into tissues that have appropriate receptors. We have examined the effects of substance P (SP), a peptide known to increase vascular permeability in selected tissues, such as trachea, esophagus, and urinary bladder in rats. We used quantitative fluorescence analysis of tissues to measure two fluorescent markers, one attached to the lipid (rhodamine-phosphatidylethanolamine) and another, doxorubicin (an antitumor drug), encapsulated within the aqueous interior. We have also examined the deposition of liposomes microscopically by the use of encapsulated colloidal gold and silver enhancement. Analysis of the biochemical and morphological observations indicate the following: (i) Injection of SP produces a striking increase in both liposome labels, but only in tissues that possess receptors for SP in postcapillary venules; (ii) liposome material in these tissues has extravasated and is found extracellularly near a variety of cells beyond the endothelial layer over the first few hours; (iii) 24 h following injection of liposomes and SP, liposome material is found in these tissues, localized intracellularly in both endothelial cells and macrophages. We propose that appropriate application of tissue-specific mediators can result in liposome extravasation deep within tissues that normally do not take up significant amounts of liposomes from the blood. Such liposomes are able to carry a variety of pharmacological agents that can be released locally within selected target tissues for therapeutic purposes.

  17. Analyzing Protein-Phosphoinositide Interactions with Liposome Flotation Assays.

    Science.gov (United States)

    Busse, Ricarda A; Scacioc, Andreea; Schalk, Amanda M; Krick, Roswitha; Thumm, Michael; Kühnel, Karin

    2016-01-01

    Liposome flotation assays are a convenient tool to study protein-phosphoinositide interactions. Working with liposomes resembles physiological conditions more than protein-lipid overlay assays, which makes this method less prone to detect false positive interactions. However, liposome lipid composition must be well-considered in order to prevent nonspecific binding of the protein through electrostatic interactions with negatively charged lipids like phosphatidylserine. In this protocol we use the PROPPIN Hsv2 (homologous with swollen vacuole phenotype 2) as an example to demonstrate the influence of liposome lipid composition on binding and show how phosphoinositide binding specificities of a protein can be characterized with this method. PMID:26552682

  18. Application of long-circulating liposomes to cancer photodynamic therapy.

    Science.gov (United States)

    Oku, N; Saito, N; Namba, Y; Tsukada, H; Dolphin, D; Okada, S

    1997-06-01

    Photodynamic therapy (PDT) as a cancer treatment is notable for its quite low side effects in comparison with those of chemotherapy and radiotherapy. However, the accumulation of porphyrin derivatives used in PDT into tumor tissues is rather low. Since long-circulating liposomes are known to accumulate passively into tumor tissues, we liposomalized a porphyrin derivative, benzoporphyrin derivative monoacid ring A (BPD-MA), and used these liposomes to investigate the usefulness of PDT for tumor-bearing mice. BPD-MA was liposomalized into glucuronate-modified liposomes, which are known to be long-circulating. These liposomes were injected i.v. into Balb/c mice bearing Meth A sarcoma, and tumor regression and survival time were monitored after irradiation with laser light. Tumor regression and complete curing of tumor (80% cure rate by the treatment with 6 mg/kg BPD-MA) were observed when long circulating liposomalized BPD-MA was injected and laser-irradiated. In contrast, only a 20% cure rate was obtained when the animals were treated with BPD-MA solution or BPD-MA entrapped in conventional liposomes. These results suggest that a long-circulating liposomal formulation of photo-sensitive agents is useful for PDT. PMID:9212988

  19. Ultrasound effects on brain-targeting mannosylated liposomes: in vitro and blood–brain barrier transport investigations

    Directory of Open Access Journals (Sweden)

    Zidan AS

    2015-07-01

    Full Text Available Ahmed S Zidan,1,2 Hibah Aldawsari1 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, Zagazig University, Zagazig, Egypt Abstract: Delivering drugs to intracerebral regions can be accomplished by improving the capacity of transport through blood–brain barrier. Using sertraline as model drug for brain targeting, the current study aimed at modifying its liposomal vesicles with mannopyranoside. Box-Behnken design was employed to statistically optimize the ultrasound parameters, namely ultrasound amplitude, time, and temperature, for maximum mannosylation capacity, sertraline entrapment, and surface charge while minimizing vesicular size. Moreover, in vitro blood–brain barrier transport model was established to assess the transendothelial capacity of the optimized mannosylated vesicles. Results showed a dependence of vesicular size, mannosylation capacity, and sertraline entrapment on cavitation and bubble implosion events that were related to ultrasound power amplitude, temperature. However, short ultrasound duration was required to achieve >90% mannosylation with nanosized vesicles (<200 nm of narrow size distribution. Optimized ultrasound parameters of 65°C, 27%, and 59 seconds for ultrasound temperature, amplitude, and time were elucidated to produce 81.1%, 46.6 nm, and 77.6% sertraline entrapment, vesicular size, and mannosylation capacity, respectively. Moreover, the transendothelial ability was significantly increased by 2.5-fold by mannosylation through binding with glucose transporters. Hence, mannosylated liposomes processed by ultrasound could be a promising approach for manufacturing and scale-up of brain-targeting liposomes. Keywords: CNS delivery, sizing, lipid based formulations, quality by design, sertraline hydrochloride

  20. Tumor targeting using liposomal antineoplastic drugs

    OpenAIRE

    Jörg Huwyler; Jürgen Drewe; Stephan Krähenbühl

    2008-01-01

    Jörg Huwyler1, Jürgen Drewe2, Stephan Krähenbühl21University of Applied Sciences Northwestern Switzerland, Institute of Pharma Technology, Muttenz, Switzerland; 2Department of Research and Division of Clinical Pharmacology, University Hospital Basel, Basel, SwitzerlandAbstract: During the last years, liposomes (microparticulate phospholipid vesicles) have beenused with growing success as pharmaceutical carriers for antineoplastic drugs. Fields of applicatio...

  1. PREPARATION OF LIPOSOMES CONTAINING WHEY PROTEINS

    OpenAIRE

    A. Suha Yalçın; Murat Türkoğlu

    2010-01-01

    Aim: In recent years, it has been shown that whey and its components have a number of health-promoting effects. We aimed to isolate fractions containing whey proteins using chromatography and then to prepare antioxidant liposomes in order to obtain a gel suitable for cosmetic preparations.Methods: Fractionation of whey proteins was achieved by extraction, filtration and centrifugation followed by liquid chromatography. The antioxidant activities of the fractions was determined by their copper...

  2. Phototriggerable Liposomes: Current Research and Future Perspectives

    Directory of Open Access Journals (Sweden)

    Anu Puri

    2013-12-01

    Full Text Available The field of cancer nanomedicine is considered a promising area for improved delivery of bioactive molecules including drugs, pharmaceutical agents and nucleic acids. Among these, drug delivery technology has made discernible progress in recent years and the areas that warrant further focus and consideration towards technological developments have also been recognized. Development of viable methods for on-demand spatial and temporal release of entrapped drugs from the nanocarriers is an arena that is likely to enhance the clinical suitability of drug-loaded nanocarriers. One such approach, which utilizes light as the external stimulus to disrupt and/or destabilize drug-loaded nanoparticles, will be the discussion platform of this article. Although several phototriggerable nanocarriers are currently under development, I will limit this review to the phototriggerable liposomes that have demonstrated promise in the cell culture systems at least (but not the last. The topics covered in this review include (i a brief summary of various phototriggerable nanocarriers; (ii an overview of the application of liposomes to deliver payload of photosensitizers and associated technologies; (iii the design considerations of photoactivable lipid molecules and the chemical considerations and mechanisms of phototriggering of liposomal lipids; (iv limitations and future directions for in vivo, clinically viable triggered drug delivery approaches and potential novel photoactivation strategies will be discussed.

  3. A Combination of Targeted Sunitinib Liposomes and Targeted Vinorelbine Liposomes for Treating Invasive Breast Cancer.

    Science.gov (United States)

    Shi, Ji-Feng; Sun, Meng-Ge; Li, Xiu-Ying; Zhao, Yao; Ju, Rui-Jun; Mu, Li-Min; Yan, Yan; Li, Xue-Tao; Zeng, Fan; Lu, Wan-Liang

    2015-09-01

    Regular chemotherapy cannot eradicate invasive breast cancer cells and the residual cancer cells will form vasculogenic mimicry (VM) channels under hypoxic conditions to provide nutrients for cancer masses prior to angiogenesis. This phenomenon is a major reason for the recurrence of invasive breast cancer after treatment. In this study, a novel type of targeted liposomes was developed by modifying a mitochondria-tropic material, D-a-tocopheryl polyethylene glycol 1000 succinate- triphenylphosphine conjugate (TPGS1000-TPP), to encapsulate sunitinib and vinorelbine separately and a combination of the two targeted drug liposomes was used to treat invasive breast cancer as well as VM channels. Evaluations were performed in breast cancer MCF-7 cells and highly invasive breast cancer MDA-MB-435S cells in vitro and in mice. The results determined that the functional material (TPGS1000-TPP) and suitable size of the liposomes (90-100 nm) resulted in prolonged blood circulation, an enhanced permeability retention (EPR) effect in cancer tissue, and a mitochondrial targeting effect. Targeted drug liposomes were internalized via cellular uptake and accumulated in the mitochondria of invasive breast cancer cells or VM channel-forming cancer cells to induce acute cytotoxic injury and apoptosis. Activated apoptotic enzymes caspase 9 and caspase 3 as well as down-regulated VM channel-forming indicators (MMP-9, EphA2, VE-Cadherin, FAK and HIF-1α) contributed to significantly enhanced efficacy. Therefore, a combination of targeted sunitinib liposomes and targeted vinorelbine liposomes may provide an effective strategy for treating invasive breast cancer and prevent relapse arising from VM channels. PMID:26485927

  4. Liposomal nanoparticles as a drug delivery vehicle against osteosarcoma

    Science.gov (United States)

    Dhule, Santosh Subhashrao

    The delivery of curcumin, a broad-spectrum anticancer drug, has been explored in the form of liposomal nanoparticles to treat osteosarcoma (OS). Curcumin is water insoluble and an effective delivery route is through encapsulation in cyclodextrins followed by a second encapsulation in liposomes. Liposomal curcumin's potential was evaluated against cancer models of mesenchymal (OS) and epithelial origin (breast cancer). The resulting 2-Hydroxypropyl-gamma-cyclodextrin/curcumin - liposome complex shows promising anticancer potential both in vitro and in vivo against KHOS OS cell line and MCF-7 breast cancer cell line. An interesting aspect is that liposomal curcumin initiates the caspase cascade that leads to apoptotic cell death in vitro in comparison with DMSO-curcumin induced autophagic cell death. In addition, the efficiency of the liposomal curcumin formulation was confirmed in vivo using a xenograft OS model. Curcumin-loaded gamma-cyclodextrin liposomes indicate significant potential as delivery vehicles for the treatment of cancers of different tissue origin. The second part of this study examines the anti-tumor potential of curcumin and C6 ceramide (C6) against osteosarcoma cell lines when both are encapsulated in the bilayer of liposomal nanoparticles. Curcumin in combination with C6 showed 1.5 times enhanced cytotoxic effect in the case of MG-63 and KHOS OS cell lines, in comparison with systems with curcumin alone. Interestingly, C6-curcumin liposomes were found to be less toxic on untransformed human cells in comparison to OS cell lines. In addition, cell cycle assays on a KHOS cell line after treatment revealed that curcumin only liposomes induced G 2/M arrest by upregulation of cyclin B1, while C6 only liposomes induced G1 arrest by downregulation of cyclin D1. C6-curcumin liposomes induced G2/M arrest and showed a combined effect in the expression levels of cyclin D1 and cyclin B1. Using pegylated liposomes to increase the plasma half-life and tagging

  5. Binding of Diphtheria Toxin to Phospholipids in Liposomes

    Science.gov (United States)

    Alving, Carl R.; Iglewski, Barbara H.; Urban, Katharine A.; Moss, Joel; Richards, Roberta L.; Sadoff, Jerald C.

    1980-04-01

    Diphtheria toxin bound to the phosphate portion of some, but not all, phospholipids in liposomes. Liposomes consisting of dimyristoyl phosphatidylcholine and cholesterol did not bind toxin. Addition of 20 mol% (compared to dimyristoyl phosphatidylcholine) of dipalmitoyl phosphatidic acid, dicetyl phosphate, phosphatidylinositol phosphate, cardiolipin, or phosphatidylserine in the liposomes resulted in substantial binding of toxin. Inclusion of phosphatidylinositol in dimyristol phosphatidylcholine / cholesterol liposomes did not result in toxin binding. The calcium salt of dipalmitoyl phosphatidic acid was more effective than the sodium salt, and the highest level of binding occurred with liposomes consisting only of dipalmitoyl phosphatidic acid (calcium salt) and cholesterol. Binding of toxin to liposomes was dependent on pH, and the pattern of pH dependence varied with liposomes having different compositions. Incubation of diphtheria toxin with liposomes containing dicetyl phosphate resulted in maximal binding at pH 3.6, whereas binding to liposomes containing phosphatidylinositol phosphate was maximal above pH 7. Toxin did not bind to liposomes containing 20 mol% of a free fatty acid (palmitic acid) or a sulfated lipid (3-sulfogalactosylceramide). Toxin binding to dicetyl phosphate or phosphatidylinositol phosphate was inhibited by UTP, ATP, phosphocholine, or p-nitrophenyl phosphate, but not by uracil. We conclude that (a) diphtheria toxin binds specifically to the phosphate portion of certain phospholipids, (b) binding to phospholipids in liposomes is dependent on pH, but is not due only to electrostatic interaction, and (c) binding may be strongly influenced by the composition of adjacent phospholipids that do not bind toxin. We propose that a minor membrane phospholipid (such as phosphatidylinositol phosphate or phosphatidic acid), or that some other phosphorylated membrane molecule (such as a phosphoprotein) may be important in the initial binding of

  6. Preliminary Studies on X-Ray-sensitive Liposome

    Institute of Scientific and Technical Information of China (English)

    MENG Fan-xu; XU Hua-ping; QI Yan-fei; XU Kun; SONG Xiu-ling; NIU Shu; LI Juan

    2012-01-01

    The synthesis of a new type of X-ray-sensitive compound “di-(1-hydroxylundecyl)diselenide” and its application in the preparation of a new type of liposome with X-ray sensitivity was reported.This new liposome was synthesized to encapsulate doxorubicin hydrochloride(Dox),with its physical and chemical properties,stability,and radiation sensitivity determined.Based on the pH-gradient method,liposomal Dox was prepared via ultrasonic emulsification and then purified on a Sephadex G50 mini-column.UV spectrophotometry and liquid chromatography were used to detect the encapsulation efficiency and radiation sensitivity of the Dox-loaded liposome.The results show that through changes in release rate,this liposome shows a relative radiosensitivity.In terms of radiation sensitivity,the drug leak rate of the X-ray-sensitive Dox-loaded liposome increased gradually and peaked at 65.4% under the X-ray radiation of a dose of 10 Gy or more than 10 Gy,which is significantly different from that of ordinary liposomes.Meanwhile,X-ray-sensitive Dox-loaded liposome has a good dispersion stability,with an average particle size of approximate 120 nm.The efficiency of this liposome encapsulating Dox was 75.84%,slightly lower than that of ordinary liposomes.The X-ray-sensitive Dox-loaded liposome exhibited suspension stability within 30 d of storage at 4 ℃,without visible precipitation.Di-(1-hydroxylundecyl)diselenide is safe and noncytotoxic and compared with those of synthetic phospholipids its synthesis is low cost and does not require complex conditions.

  7. Nanosized strontium aluminate phosphors prepared via a reverse microemulsion route

    International Nuclear Information System (INIS)

    Nanosized strontium aluminate phosphors co-activated by Eu2+ and Dy3+ were prepared via a novel reverse microemulsion process. This new synthesis technique lowered the synthesis temperature of SrAl2O4: Eu2+, Dy3+ phosphors to as low as 900 deg. C, and also reduced the particle size to the nanometer scale (around 40 nm). In the microemulsion process, the constituent cations were trapped by numerous nano-scaled micelles, leading to a shortening of the inter-diffusion length and enhancement of the precursor reactivity. The excitation intensity and emission peaks of nanosized SrAl2O4: Eu2+, Dy3+ phosphors significantly increased with increasing heating temperatures

  8. Superconducting film magnetic flux transformer with micro- and nanosized branches

    Directory of Open Access Journals (Sweden)

    Levan Ichkitidze

    2013-06-01

    Full Text Available The object of the study is a superconducting film magnetic flux transformer comprising two square shaped loops with the tapering active strips and a magnetosensitive film element between them. It is shown that splitting of the active strips into parallel micro- and nanosized superconducting branches and slits increases the gain factor of the transformer, i. e., the concentration of an external magnetic field on the magnetosensitive element, by a factor of more than four.

  9. Fluorescent labels based on nanosized silicon and diamonds

    Czech Academy of Sciences Publication Activity Database

    Fučíková, A.; Valenta, Jan; Pelant, Ivan; Březina, V.

    Roma : ENEA, 2010. S1-4. ISBN 978-88-8286-218-3. [Breakthroughs in Nanoparticles for Bio-imaging. BONSAI project symposium. 08.04.2010-09.04.2010, Frascati] R&D Projects: GA AV ČR KAN400100701; GA MŠk LC510 Institutional research plan: CEZ:AV0Z10100521 Keywords : nanosized silicon * nanodiamonds * nanolabeling * biocompatibility of nanopaticles Subject RIV: BM - Solid Matter Physics ; Magnetism

  10. Screen printed nanosized ZnO thick film

    Indian Academy of Sciences (India)

    Bindu Krishnan; V P N Nampoori

    2005-06-01

    Nanosized ZnO was prepared by polyol synthesis. Fluorescence spectrum of the ZnO colloid at varying pump intensities was studied. The powder was extracted and characterized by XRD and BET. The extracted powder was screen printed on glass substrates using ethyl cellulose as binder and turpinol as solvent. Coherent back scattering studies were performed on the screen printed sample which showed evidence of weak localization. The screen printed pattern showed strong UV emission.

  11. Synthesis of nanosized powders for preparing ceramic membranes

    International Nuclear Information System (INIS)

    Magnesium-stabilized zirconia have been synthesized by a chemical route. The aim of this work is to obtain powders with suitable chemical and physical properties to be used as ceramic membranes for nanofiltration. The coprecipitation technique with an azeotropic distillation step has been employed for this purpose. Several powder characterization techniques have been utilized. The main results show that nanosized powders with high a degree of purity, high chemical homogeneity and elevated reactivity have been obtained. (orig.)

  12. Electrospun nanosized cellulose fibers using ionic liquids at room temperature

    OpenAIRE

    Freire, Mara G.; Teles, Ana Rita R.; Ferreira, Rute A. S.; Carlos, Luís D.; José A. Lopes-da-Silva; Coutinho, João A. P.

    2011-01-01

    Aiming at replacing the noxious solvents commonly employed, ionic-liquid-based solvents have been recently explored as novel non-volatile and non-flammable media for the electrospinning of polymers. In this work, nanosized and biodegradable cellulose fibers were obtained by electrospinning at room temperature using a pure ionic liquid or a binary mixture of two selected ionic liquids. The electrospinning of 8 wt% cellulose in 1-ethyl-3-methylimidazolium acetate medium (a low viscosity and roo...

  13. Quantum transport in the cylindrical nanosize silicon-based MOSFET

    OpenAIRE

    Balaban, S. N.; Pokatilov, E. P.; Fomin, V. M.; Gladilin, V. N.; Devreese, J. T.; Magnus, W.; W. Schoenmaker; Van Rossum, M.; Soree, B.

    2000-01-01

    A model is developed for a detailed investigation of the current flowing through a cylindrical nanosize MOSFET with a close gate electrode. The quantum mechanical features of the lateral charge transport are described by Wigner distribution function which is explicitly dealing with electron scattering due to acoustic phonons and acceptor impurities. A numerical simulation is carried out to obtain a set of I-V characteristics for various channel lengths. It is demonstrated that inclusion of th...

  14. Wear Behavior of Austempered Ductile Iron with Nanosized Additives

    Directory of Open Access Journals (Sweden)

    J. Kaleicheva

    2014-03-01

    Full Text Available The microstructure and properties of austempered ductile iron (ADI strengthened with nanosized addtives of titanium nitride + titanium carbonitride (TiN + TiCN, titanium nitride TiN and cubic boron nitride cBN are investigated. The TiN, TiCN and cBN, nanosized particles are coated by electroless nickel coating EFTTOM-NICKEL prior to the edition to the melt. The spheroidal graphite iron samples are undergoing an austempering, including heating at 900 оС for an hour, after that isothermal retention at 280 оС, 2 h and 380 оС, 2h. The metallographic analysis by optical metallographic microscope GX41 OLIMPUS and hardness measurements by Vickers Method are performed. The structure of the austempered ductile iron consists of lower bainite and upper bainite.Experimental investigation of the wear by fixed abrasive are also carried out. The influence of the nanosized additives on the microstructure, mechanical and tribological properties of the austempered ductile irons (ADI is studied.

  15. The clearance of liposomes administered by the intramuscular route

    International Nuclear Information System (INIS)

    Iodine 131-labelled lecithin was used to label liposomes entrapping cortisone-21-palmitate. The lecithin was injected into the fascia latae muscles of rabbits and the percentage of the initial dose remaining at certain time intervals was calculated from gamma camera image data. Release from the intramuscular site occurs by diffusion from intact liposomes. (U.K.)

  16. 64Cu loaded liposomes as positron emission tomography imaging agents

    DEFF Research Database (Denmark)

    Petersen, Anncatrine Luisa; Binderup, Tina; Rasmussen, Palle;

    2011-01-01

    -radionuclide (64Cu) using a new ionophore, 2-hydroxyquinoline, to carry 64Cu(II) across the membrane of preformed liposomes and deliver it to an encapsulated copper-chelator. Using this ionophore we achieved very efficient loading (95.5 ± 1.6%) and retention stability (>99%), which makes the 64Cu-liposomes highly...

  17. Liposomal budesonide for dry powder inhaler: Preparation and stabilization

    OpenAIRE

    Joshi, Mayank R.; Misra, Ambikanandhan

    2001-01-01

    The purpose of the study was to prepare stable liposomally entrapped budesonide (BUD) for a dry powder inhaler (DPI) formulation. BUD liposomes composed of egg phosphatidyl choline and cholesterol were prepared by lipid film hydration technique and sonicated to have the desired size (

  18. Immunological Effect of Subunit Influenza Vaccine Entrapped by Liposomes

    Institute of Scientific and Technical Information of China (English)

    SHUI-HUA ZHANG; JIA-XU LIANG; SHU-YAN DAI; XIAO-LIN QIU; YAN-RONG YI; YUN PAN

    2009-01-01

    Objective To elevate the immunological effect of subunit influenza vaccine in infants and aged people (over 60) using liposomal adjuvant in the context of its relatively low immunity and to investigate the relation between vaccine antigens and liposomal characteristics. Methods Several formulations of liposomal subunit influenza vaccine were prepared. Their relevant characteristics were investigated to optimize the preparation method. Antisera obtained from immunizinged mice were used to evaluate the antibody titers of various samples by HI and ELISA. Results Liposomal trivalent influenza vaccine prepared by film evaporation in combinedation with freeze-drying significantly increased its immunological effect in SPF Balb/c mice. Liposomal vaccine stimulated the antibody titer of H3N2, H1N1, and B much stronger than conventional influenza vaccine. As a result, liposomal vaccine (mean size: 4.5-5.5 μm, entrapment efficiency: 30%-40%) significantly increased the immunological effect of subunit influenza vaccine. Conclusion The immune effect of liposomal vaccine depends on different antigens, and enhanced immunity is not positively correlated with the mean size of liposome or its entrapped efficiency.

  19. Current Trends in Development of Liposomes for Targeting Bacterial Biofilms

    OpenAIRE

    Zora Rukavina; Željka Vanić

    2016-01-01

    Biofilm targeting represents a great challenge for effective antimicrobial therapy. Increased biofilm resistance, even with the elevated concentrations of very potent antimicrobial agents, often leads to failed therapeutic outcome. Application of biocompatible nanomicrobials, particularly liposomally-associated nanomicrobials, presents a promising approach for improved drug delivery to bacterial cells and biofilms. Versatile manipulations of liposomal physicochemical properties, such as the b...

  20. Biophysical characterization of gold nanoparticles-loaded liposomes.

    Science.gov (United States)

    Mady, Mohsen Mahmoud; Fathy, Mohamed Mahmoud; Youssef, Tareq; Khalil, Wafaa Mohamed

    2012-10-01

    Gold nanoparticles were prepared and loaded into the bilayer of dipalmitoylphosphatidylcholine (DPPC) liposomes, named as gold-loaded liposomes. Biophysical characterization of gold-loaded liposomes was studied by transmission electron microscopy (TEM) and Fourier transform infrared (FTIR) spectroscopy as well as turbidity and rheological measurements. FTIR measurements showed that gold nanoparticles made significant changes in the frequency of the CH(2) stretching bands, revealing that gold nanoparticles increased the number of gauche conformers and create a conformational change within the acyl chains of phospholipids. The transmission electron micrographs (TEM) revealed that gold nanoparticles were loaded in the liposomal bilayer. The zeta potential of DPPC liposomes had a more negative value after incorporating of Au NPs into liposomal membranes. Turbidity studies revealed that the loading of gold nanoparticles into DPPC liposomes results in shifting the temperature of the main phase transition to a lower value. The membrane fluidity of DPPC bilayer was increased by loading the gold nanoparticles as shown from rheological measurements. Knowledge gained in this study may open the door to pursuing liposomes as a viable strategy for Au NPs delivery in many diagnostic and therapeutic applications. PMID:22027546

  1. Encapsulation of antitumor drug methotrexate in liposome vesicles

    International Nuclear Information System (INIS)

    Liposome vesicles containing antitumor drug methotrexate (MTX) were prepared. MTX was labelled by the tritium ion beam method. After purification by TLC, the specific radioactivity of 3H-MTX was 1.19 GBq/mmol with radiochemical purity orver 95%. Under various forming conditions of liposome vesicles, the efficiency of encapsulation was 21-53%

  2. Characteristics of photosensitization of Pheophorbide a in liposomal media

    Institute of Scientific and Technical Information of China (English)

    杨红英; 李美芬; 张文庚; 赵红霞; 张志义

    1999-01-01

    Pheophorbide a (PPa), a decomposition product of chlorophyll a, is a photosensitizer. The photosensitization mechanisms (Type Ⅰ and Type Ⅱ) of PPa in simple buffer solutions and in buffer solutions containing double-layered DPPC liposomes have been studied using techniques of ESR, spin-trapping, spin-counteraction and laser flash photolysis. The results showed that adding DPPC liposomes to the buffer solution caused an increase of efficiency of generating 1O2 and PPa- by photoactivating PPa. The increase could be ascribed to the disaggregation of hydrophobic PPa caused by the addition of liposomes and the protective effect of liposomal media on the triplet state of PPa. It is concluded that the photosensitization of PPa in liposomal systems is different from that in simple aqueous solutions, and shows higher efficacy. The results will be useful to elucidating the mechanisms of photodynamic therapy of cancer.

  3. Preparation and characterization of clove essential oil-loaded liposomes.

    Science.gov (United States)

    Sebaaly, Carine; Jraij, Alia; Fessi, Hatem; Charcosset, Catherine; Greige-Gerges, Hélène

    2015-07-01

    In this study, suitable formulations of natural soybean phospholipid vesicles were developed to improve the stability of clove essential oil and its main component, eugenol. Using an ethanol injection method, saturated (Phospholipon 80H, Phospholipon 90H) and unsaturated soybean (Lipoid S100) phospholipids, in combination with cholesterol, were used to prepare liposomes at various eugenol and clove essential oil concentrations. Liposomal batches were characterized and compared for their size, polydispersity index, Zeta potential, loading rate, encapsulation efficiency and morphology. The liposomes were tested for their stability after storing them for 2 months at 4°C by monitoring changes in their mean size, polydispersity index and encapsulation efficiency (EE) values. It was found that liposomes exhibited nanometric oligolamellar and spherical shaped vesicles and protected eugenol from degradation induced by UV exposure; they also maintained the DPPH-scavenging activity of free eugenol. Liposomes constitute a suitable system for encapsulation of volatile unstable essential oil constituents. PMID:25704683

  4. Multimodal targeted high relaxivity thermosensitive liposome for in vivo imaging

    Science.gov (United States)

    Kuijten, Maayke M. P.; Hannah Degeling, M.; Chen, John W.; Wojtkiewicz, Gregory; Waterman, Peter; Weissleder, Ralph; Azzi, Jamil; Nicolay, Klaas; Tannous, Bakhos A.

    2015-11-01

    Liposomes are spherical, self-closed structures formed by lipid bilayers that can encapsulate drugs and/or imaging agents in their hydrophilic core or within their membrane moiety, making them suitable delivery vehicles. We have synthesized a new liposome containing gadolinium-DOTA lipid bilayer, as a targeting multimodal molecular imaging agent for magnetic resonance and optical imaging. We showed that this liposome has a much higher molar relaxivities r1 and r2 compared to a more conventional liposome containing gadolinium-DTPA-BSA lipid. By incorporating both gadolinium and rhodamine in the lipid bilayer as well as biotin on its surface, we used this agent for multimodal imaging and targeting of tumors through the strong biotin-streptavidin interaction. Since this new liposome is thermosensitive, it can be used for ultrasound-mediated drug delivery at specific sites, such as tumors, and can be guided by magnetic resonance imaging.

  5. Surface Modification of Liposomal Vaccines by Peptide Conjugation

    Directory of Open Access Journals (Sweden)

    Hazra M2

    2011-01-01

    Full Text Available The aim of the present work was to prepare liposomal vaccine formulation by incorporating naked plasmid DNA that can trigger humoral and cell mediated protective immunity against infection. For these cationic lipids like dimyristoyl phosphatidylcholine (DMPC, dioleyl phosphatidyl ethanolamine (DOPE, [1, 2 – dioleyloxy -3-(trimethyl ammonium propane] (DOTAP, were taken in the ratio of 4:2:1 respectively. The liposomal formulations thus prepared were surface modified by peptide conjugation with the help of EDC and NHS. Physical characterization of liposomal formulationswas done by estimating the average size distribution, which gives an average liposomal size of 53.0nm. Concentration of peptide bound liposomes wasestimated by Lowry method which entails that bound protein concentration was 30.5 µg/ml.

  6. Current Trends in Development of Liposomes for Targeting Bacterial Biofilms.

    Science.gov (United States)

    Rukavina, Zora; Vanić, Željka

    2016-01-01

    Biofilm targeting represents a great challenge for effective antimicrobial therapy. Increased biofilm resistance, even with the elevated concentrations of very potent antimicrobial agents, often leads to failed therapeutic outcome. Application of biocompatible nanomicrobials, particularly liposomally-associated nanomicrobials, presents a promising approach for improved drug delivery to bacterial cells and biofilms. Versatile manipulations of liposomal physicochemical properties, such as the bilayer composition, membrane fluidity, size, surface charge and coating, enable development of liposomes with desired pharmacokinetic and pharmacodynamic profiles. This review attempts to provide an unbiased overview of investigations of liposomes destined to treat bacterial biofilms. Different strategies including the recent advancements in liposomal design aiming at eradication of existing biofilms and prevention of biofilm formation, as well as respective limitations, are discussed in more details. PMID:27231933

  7. Shrinkage of pegylated and non-pegylated liposomes in serum.

    Science.gov (United States)

    Wolfram, Joy; Suri, Krishna; Yang, Yong; Shen, Jianliang; Celia, Christian; Fresta, Massimo; Zhao, Yuliang; Shen, Haifa; Ferrari, Mauro

    2014-02-01

    An essential requisite for the design of nanodelivery systems is the ability to characterize the size, homogeneity and zeta potential of nanoparticles. Such properties can be tailored in order to create the most efficient drug delivery platforms. An important question is whether these characteristics change upon systemic injection. Here, we have studied the behavior of phosphatidylcholine/cholesterol liposomes exposed to serum proteins. The results reveal a serum-induced reduction in the size and homogeneity of both pegylated and non-pegylated liposomes, implicating the possible role of osmotic forces. In addition, changes to zeta-potential were observed upon exposing liposomes to serum. The liposomes with polyethylene glycol expressed different characteristics than their non-polymeric counterparts, suggesting the potential formation of a denser protein corona around the non-pegylated liposomes. PMID:24216620

  8. Interactions of a Photochromic Spiropyran with Liposome Model Membranes

    KAUST Repository

    Jonsson, Fabian

    2013-02-19

    The interactions between anionic or zwitterionic liposomes and a water-soluble, DNA-binding photochromic spiropyran are studied using UV/vis absorption and linear dichroism (LD) spectroscopy. The spectral characteristics as well as the kinetics of the thermal isomerization process in the absence and presence of the two different liposome types provide information about the environment and whether or not the spiropyran resides in the liposome membrane. By measuring LD on liposomes deformed and aligned by shear flow, further insight is obtained about interaction and binding geometry of the spiropyran at the lipid membranes. We show that the membrane interactions differ between the two types of liposomes used as well as the isomeric forms of the spiropyran photoswitch. © 2013 American Chemical Society.

  9. The Treatment of Breast Cancer Using Liposome Technology

    Directory of Open Access Journals (Sweden)

    Sarah Brown

    2012-01-01

    Full Text Available Liposome-based chemotherapeutics used in the treatment of breast cancer can in principle enhance the therapeutic index of otherwise unencapsulated anticancer drugs. This is partially attributed to the fact that encapsulation of cytotoxic agents within liposomes allows for increased concentrations of the drug to be delivered to the tumor site. In addition, the presence of the phospholipid bilayer prevents the encapsulated active form of the drug from being broken down in the body prior to reaching tumor tissue and also serves to minimize exposure of the drug to healthy sensitive tissue. While clinically approved liposome-based chemotherapeutics such as Doxil have proven to be quite effective in the treatment of breast cancer, significant challenges remain involving poor drug transfer between the liposome and cancerous cells. In this review, we discuss the recent advancements made in the development of liposome-based chemotherapeutics with respect to improved drug transfer for use in breast cancer therapy.

  10. Nanosized Selenium: A Novel Platform Technology to Prevent Bacterial Infections

    Science.gov (United States)

    Wang, Qi

    As an important category of bacterial infections, healthcare-associated infections (HAIs) are considered an increasing threat to the safety and health of patients worldwide. HAIs lead to extended hospital stays, contribute to increased medical costs, and are a significant cause of morbidity and mortality. In the United States, infections encountered in the hospital or a health care facility affect more than 1.7 million patients, cost 35.7 billion to 45 billion, and contribute to 88,000 deaths in hospitals annually. The most conventional and widely accepted method to fight against bacterial infections is using antibiotics. However, because of the widespread and sometimes inappropriate use of antibiotics, many strains of bacteria have rapidly developed antibiotic resistance. Those new, stronger bacteria pose serious, worldwide threats to public health and welfare. In 2014, the World Health Organization (WHO) reported antibiotic resistance as a global serious threat that is no longer a prediction for the future but is now reality. It has the potential to affect anyone, of any age, in any country. The most effective strategy to prevent antibiotic resistance is minimizing the use of antibiotics. In recent years, nanomaterials have been investigated as one of the potential substitutes of antibiotics. As a result of their vastly increased ratio of surface area to volume, nanomaterials will likely exert a stronger interaction with bacteria which may affect bacterial growth and propagation. A major concern of most existing antibacterial nanomaterials, like silver nanoparticles, is their potential toxicity. But selenium is a non-metallic material and a required nutrition for the human body, which is recommended by the FDA at a 53 to 60 μg daily intake. Nanosized selenium is considered to be healthier and less toxic compared with many metal-based nanomaterials due to the generation of reactive oxygen species from metals, especially heavy metals. Therefore, the objectives of

  11. A Liposomal Formulation Able to Incorporate a High Content of Paclitaxel and Exert Promising Anticancer Effect

    OpenAIRE

    Pei Kan; Chih-Wan Tsao; Ae-June Wang; Wu-Chou Su; Hsiang-Fa Liang

    2011-01-01

    A liposome formulation for paclitaxel was developed in this study. The liposomes, composed of naturally unsaturated and hydrogenated phosphatidylcholines, with significant phase transition temperature difference, were prepared and characterized. The liposomes exhibited a high content of paclitaxel, which was incorporated within the segregated microdomains coexisting on phospholipid bilayer of liposomes. As much as 15% paclitaxel to phospholipid molar ratio were attained without precipitates o...

  12. Image-Guided Predictions of Liposome Transport in Solid Tumours

    Science.gov (United States)

    Stapleton, Shawn

    Due to the ability to preferentially accumulate and deliver drug payloads to solid tumours, liposomes have emerged as an exciting therapeutic strategy for cancer therapy. Unfortunately, the initial excitement was dampened by limited clinical results, where only negligible increases in patient survival following liposome therapy have been observed. What are the reasons for the limited clinical efficacy? Is the nanoparticle formulation optimal? Is the enhanced permeability and retention effect overstated? What are the barriers limiting the delivery of drugs to cancer cells? What is the optimal dosing and treatment schedule? Addressing these questions requires developing quantitative tools to understand the behaviour of liposomes in vivo, such as pharmacokinetics, biodistribution, intra-tumoural accumulation, and drug release. Central to each of these questions is the concept of transport - the collection of biophysical processes responsible for the delivery of molecules to tissues. Understanding transport means understanding the crucial links between the spatio-temporal accumulation of liposomes, the physicochemical properties of liposomes, and properties of the tumour microenvironment. In this thesis, a biophysical mathematical transport model is developed that when used in combination with non-invasive imaging methods can predict liposome transport in solid tumours. The mathematical transport framework is validated in its ability to predict the bulk and intra-tumoural accumulation of liposomes based on biophysical transport properties of solid tumours. Furthermore, novel imaging methods are developed and used to elucidate the crucial links between transport barriers and spatial heterogeneity in liposome accumulation. Finally, methods are presented to integrate quantitative imaging and mathematical modelling such that an accurate prediction of liposome transport in solid tumours is possible. In summary, this thesis presents and validates an image-guided mathematical

  13. Liposomal nanoparticles encapsulating iloprost exhibit enhanced vasodilation in pulmonary arteries

    Directory of Open Access Journals (Sweden)

    Jain PP

    2014-07-01

    Full Text Available Pritesh P Jain,1 Regina Leber,1,2 Chandran Nagaraj,1 Gerd Leitinger,3 Bernhard Lehofer,4 Horst Olschewski,1,5 Andrea Olschewski,1,6 Ruth Prassl,1,4 Leigh M Marsh11Ludwig Boltzmann Institute for Lung Vascular Research, 2Biophysics Division, Institute of Molecular Biosciences, University of Graz, 3Research Unit Electron Microscopic Techniques, Institute of Cell Biology, Histology, and Embryology, 4Institute of Biophysics, 5Division of Pulmonology, Department of Internal Medicine, 6Department of Anesthesiology and Intensive Care Medicine, Medical University of Graz, Graz, AustriaAbstract: Prostacyclin analogues are standard therapeutic options for vasoconstrictive diseases, including pulmonary hypertension and Raynaud’s phenomenon. Although effective, these treatment strategies are expensive and have several side effects. To improve drug efficiency, we tested liposomal nanoparticles as carrier systems. In this study, we synthesized liposomal nanoparticles tailored for the prostacyclin analogue iloprost and evaluated their pharmacologic efficacy on mouse intrapulmonary arteries, using a wire myograph. The use of cationic lipids, stearylamine, or 1,2-di-(9Z-octadecenoyl-3-trimethylammonium-propane (DOTAP in liposomes promoted iloprost encapsulation to at least 50%. The addition of cholesterol modestly reduced iloprost encapsulation. The liposomal nanoparticle formulations were tested for toxicity and pharmacologic efficacy in vivo and ex vivo, respectively. The liposomes did not affect the viability of human pulmonary artery smooth muscle cells. Compared with an equivalent concentration of free iloprost, four out of the six polymer-coated liposomal formulations exhibited significantly enhanced vasodilation of mouse pulmonary arteries. Iloprost that was encapsulated in liposomes containing the polymer polyethylene glycol exhibited concentration-dependent relaxation of arteries. Strikingly, half the concentration of iloprost in liposomes elicited

  14. Silica-Coated Liposomes for Insulin Delivery

    Directory of Open Access Journals (Sweden)

    Neelam Dwivedi

    2010-01-01

    Full Text Available Liposomes coated with silica were explored as protein delivery vehicles for their enhanced stability and improved encapsulation efficiency. Insulin was encapsulated within the fluidic phosphatidylcholine lipid vesicles by thin film hydration at pH 2.5, and layer of silica was formed above lipid bilayer by acid catalysis. The presence of silica coating and encapsulated insulin was identified using confocal and electron microscopy. The native state of insulin present in the formulation was evident from Confocal Micro-Raman spectroscopy. Silica coat enhances the stability of insulin-loaded delivery vehicles. In vivo study shows that these silica coated formulations were biologically active in reducing glucose levels.

  15. Delivery of aerosolized drugs encapsulated in liposomes

    Energy Technology Data Exchange (ETDEWEB)

    Cheng, Yung-Sung; Lyons, C.R. [Univ. of New Mexico, Albuquerque, NM (United States); Schmid, M.H.

    1995-12-01

    Mycobacterium tuberculosis (Mtb) is an infectious disease that resides in the human lung. Due to the difficulty in completely killing off the disease in infected individuals, Mtb has developed drug-resistant forms and is on the rise in the human population. Therefore, ITRI and the University of New Mexico are collaborating to explore the treatment of Mtb by an aerosolized drug delivered directly to the lungs. In conclusion, it is feasible to obtain an appropriate size and concentration of the liposomes before and after aerosolization.

  16. The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes

    OpenAIRE

    Parvin Zakeri-Milani; Hadi Valizadeh; Saeed Ghanbarzadeh

    2013-01-01

    Purpose: The major limitation in the widespread use of liposome drug delivery system is its instability. Lyophilization is a promising approach to ensure the long-term stability of liposomes. The aim of this study was to prepare sirolimus-loaded liposomes, study their stability and investigate the effect of lyophilization either in the presence or in the absence of lyoprotectant on liposome properties. Methods: Two types of multi-lamellar liposomes, conventional and fusogenic, containing siro...

  17. Effect of Lipid Composition on In Vitro Release and Skin Deposition of Curcumin Encapsulated Liposomes

    Directory of Open Access Journals (Sweden)

    Geethi Pamunuwa

    2016-01-01

    Full Text Available Liposomal encapsulation improves numerous physiochemical and biological properties of curcumin. The aim of this work was to impart slow release and skin delivery of curcumin via liposomal encapsulation. Liposomes were made using egg yolk phosphatidylcholine as the staple lipid while incorporating polysorbate 80 and stearylamine to prepare hybrid liposomes and positively charged liposomes, respectively. Negatively charged liposomes exhibited the highest encapsulation efficiencies (87.8±4.3% and loading capacities (3.4±0.2%. The sizes of all formulations were about 250 nm, while stearylamine increased the polydispersity index. Positively charged liposomes showed lower degradation temperatures than negatively charged liposomes by 10–15°C, attributable to the presence of stearylamine. The melting temperatures of positively charged liposomes (40–50°C were much higher than those of negatively charged liposomes (14-15°C, which may have affected release and skin deposition behavior of liposomes. The positively charged liposomes exhibited the slowest release of curcumin in phosphate buffered saline (pH 6.8 and the release profiles of all liposomal formulations conformed to the Gompertz model. The negatively charged liposomes facilitated the highest skin deposition of curcumin as revealed by studies conducted using excised pig ear skin. Concisely, positively and negatively charged liposomes were optimal for slow release and skin deposition of curcumin, respectively.

  18. Spectroscopic studies of alpha tocopherol interaction with a model liposome and its influence on oxidation dynamics

    Science.gov (United States)

    Krilov, Dubravka; Kosović, Marin; Serec, Kristina

    2014-08-01

    The influence of α-tocopherol on the surface conformation of liposome, as a model component of lipoproteins, and its role in oxidation process were studied. FT-IR spectra from suspensions of neat liposome, mixtures of liposome and α-tocopherol and liposome with incorporated α-tocopherol were analyzed. When α-tocopherol was incorporated into liposome, intensities of some bands were decreased or increased in comparison with the spectra of liposome and α-tocopherol mixture. These changes reflect the different localization of α-tocopherol in two types of liposome suspensions. The oxidation of liposome suspensions was initiated by addition of cupric ions. After prolonged oxidation, the differences in FT-IR spectra of oxidized samples were recorded. Differences were observed in comparison with spectra of native and oxidized liposomes were analyzed. The rate of oxidation was measured by EPR oximetry. Oxidation was generally very slow, but faster in liposome without α-tocopherol, indicating the protective role of α-tocopherol against liposome oxidation. On the other hand, liposome suspensions with EDTA in the buffer were not oxidized at all, while those with α-tocopherol and liposome mixture were only slightly oxidized. In this case the consumption of oxygen was the result of liposome oxidation supported by α-tocopherol. These results reflect the ambivalent role of α-tocopherol in liposome oxidation, similarly to findings in studies of lipoprotein oxidation.

  19. Liposomal cytarabine for leukemic and lymphomatous meningitis: recent developments.

    Science.gov (United States)

    Benesch, Martin; Urban, Christian

    2008-02-01

    Liposomal cytarabine (Depocyte) is a sustained-release formulation of cytarabine developed for intrathecal administration, ensuring prolonged cytotoxic drug concentrations of cytarabine in cerebrospinal fluid. Although liposomal cytarabine is increasingly used for the treatment (and prophylaxis) of CNS involvement in patients with leukemia/lymphoma, many of the recently presented clinical trials on liposomal cytarabine were retrospective in nature or used this drug on a compassionate basis. So far, one randomized Phase III study has shown significantly better response rates in patients with lymphomatous meningitis who received liposomal cytarabine compared with free cytarabine. Considerable concerns about the safety of this drug arose from recent observations that liposomal cytarabine might contribute to neurologic side effects when given too closely to high-dose systemic chemotherapy known to penetrate the brain-blood barrier. Superior efficacy of liposomal cytarabine compared with standard intrathecal therapy should be confirmed in prospective clinical trials. Careful adherence with preventive measures might help physicians to minimize side effects possibly related to the administration of liposomal cytarabine. PMID:18201152

  20. ELASTIC LIPOSOME: DRUG DELIVERY ACROSS HUMAN SKIN

    Directory of Open Access Journals (Sweden)

    Vardhan Harsh

    2012-04-01

    Full Text Available Transdermal drug delivery is hardly an old technology, since 1800’s and the technology is no longer just adhesive patches. Due to recent advances in technology and the ability to apply the drug to the site of action without rupturing the skin membrane, transdermal route is becoming a widely accepted route of drug administration. Recently, various strategies have been used to augment the transdermal delivery of bioactives. Mainly, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, micro needles, and vesicular system. Among these strategies elastic liposomes appear promising. Elastic liposomes possess an infrastructure consisting of hydrophobic and hydrophilic moieties together and as a result can accommodate drug molecules with wide range of solubility. It is an ultra deformable vesicle, elastic in nature which can squeeze itself through a pore which is many times smaller than its size owing to its elasticity. They can deform and pass through narrow constriction (from 5 to 10 times less than their own diameter without measurable loss. This high deformability gives better penetration of intact vesicles. This system is much more efficient at delivering a low and high molecular weight drug to the skin in terms of quantity and depth. The article speaks specifically on various phenomenon associated with the properties of these vesicles and their transport mechanisms. It also throws light on the effectiveness of conventional and deformable vesicles as drug delivery systems as well as their possible mode of action as transdermal drug carriers.

  1. Preparation and Characterization of Danofloxacin Mmesylate Liposomes

    Institute of Scientific and Technical Information of China (English)

    ZHANG Dexian; LI Jichang

    2011-01-01

    Five different methods were tested and compared to prepare danofloxacin mesylate liposomes, the ammonium sulfate gradient method with freeze-thawing steps was validated as the best one; the optimal preparation condition confirmed by orthogonal experiment was as follows: EPC-CH ratio was 3 : 2 and 2.6% SA was added to gain the positive electricity; drug-lipoid was 2 : 5, the concentration of ammonium sulfate was 250 mmol·L-1, water-oil ratio was 1:5, and they were incubated at 35℃ for 15 min. The prepared liposome products were ivory white semitransparent suspension, the electron microscope appearance was intact and globular or globular-like vesicles with uniformed distribution; the particle size was centralized from 3 to 7 gm, zeta-electric potential valued+ (15.92+1.49) mV, pH valued 6.02~0.09; HPLC method was established in quantitative analyses of danofloxacin and reverse dialysis with RP-HPLC method was validated for determination of entrapment efficiency. The entrapment efficiency results were all above 90%. They were stored at 4℃ with satisfied stability. Six months later, the appearance, characters and entrapment efficiency were almost with no change

  2. Crystallization of Organic Semiconductor Molecules in Nanosized Cavities

    DEFF Research Database (Denmark)

    Milita, Silvia; Dionigi, Chiara; Borgatti, Francesco;

    2008-01-01

    The crystallization of an organic semiconductor, viz., tetrahexil-sexithiophene (H4T6) molecules, confined into nanosized cavities of a self-organized polystyrene beads template, has been investigated by means of in situ grazing incidence X-ray diffraction measurements, during the solvent evapora...... system and the enhanced transistor performance has been established. These results, which can be extended to a wide range of organic materials, are useful for developing an attractive sustainable process for fabrication of organic devices with enhanced performance....

  3. Electrical and magnetic properties of nano-sized magnesium ferrite

    Science.gov (United States)

    T, Smitha; X, Sheena; J, Binu P.; Mohammed, E. M.

    2015-02-01

    Nano-sized magnesium ferrite was synthesized using sol-gel techniques. Structural characterization was done using X-ray diffractometer and Fourier Transform Infrared Spectrometer. Vibration Sample Magnetometer was used to record the magnetic measurements. XRD analysis reveals the prepared sample is single phasic without any impurity. Particle size calculation shows the average crystallite size of the sample is 19nm. FTIR analysis confirmed spinel structure of the prepared samples. Magnetic measurement study shows that the sample is ferromagnetic with high degree of isotropy. Hysterisis loop was traced at temperatures 100K and 300K. DC electrical resistivity measurements show semiconducting nature of the sample.

  4. Waste utilization for the controlled synthesis of nanosized hydroxyapatite

    Energy Technology Data Exchange (ETDEWEB)

    Nayar, Suprabha, E-mail: Suprabha.nayar@gmail.com [National Metallurgical Laboratory, Jamshedpur (India); Guha, Avijit [National Metallurgical Laboratory, Jamshedpur (India)

    2009-05-05

    This work uses biomolecules in waste and medicinally important materials for the synthesis of hydroxyapatite nanoparticles. Orange and potato peel, eggshell, papaya leaf and calendula flower extracts have varied biomolecules, which exert a significant, control on the in situ synthesis of nanosized hydroxyapatite particles. The biomimetic synthesis of inorganic particles using known matrices is already well established, however, there are only a few reports using compound extracts. The synthesized nanocomposite has been characterized using X-ray diffraction, Fourier transform infrared spectroscopy and scanning electron microscopy studies. Role of varied biomolecules in controlled inorganic synthesis may have tremendous technological impact.

  5. Synthesis of nanosized silver colloids by microwave dielectric heating

    Indian Academy of Sciences (India)

    Kirti Patel; Sudhir Kapoor; D P Dave; Tulsi Mukherjee

    2005-01-01

    Silver nanosized crystallites have been synthesized in aqueous and polyols viz., ethylene glycol and glycerol, using a microwave technique. Dispersions of colloidal silver have been prepared by the reduction of silver nitrate both in the presence and absence of stabilizer poly(vinylpyrolidone) (PVP). It was observed that PVP is capable of complexing and stabilizing Ag nanoparticles formed through the reduction of Ag+ ions in water and ethylene glycol. In the case of ethylene glycol, it has been shown that the use of PVP leads to particles with a high degree of stability. The colloids are stable in glycerol for months even in the absence of stabilizer.

  6. Waste utilization for the controlled synthesis of nanosized hydroxyapatite

    International Nuclear Information System (INIS)

    This work uses biomolecules in waste and medicinally important materials for the synthesis of hydroxyapatite nanoparticles. Orange and potato peel, eggshell, papaya leaf and calendula flower extracts have varied biomolecules, which exert a significant, control on the in situ synthesis of nanosized hydroxyapatite particles. The biomimetic synthesis of inorganic particles using known matrices is already well established, however, there are only a few reports using compound extracts. The synthesized nanocomposite has been characterized using X-ray diffraction, Fourier transform infrared spectroscopy and scanning electron microscopy studies. Role of varied biomolecules in controlled inorganic synthesis may have tremendous technological impact.

  7. Ductility and work hardening in nano-sized metallic glasses

    International Nuclear Information System (INIS)

    In-situ nano-tensile experiments on 70 nm-diameter free-standing electroplated NiP metallic glass nanostructures reveal tensile true strains of ∼18%, an amount comparable to compositionally identical 100 nm-diameter focused ion beam samples and ∼3 times greater than 100 nm-diameter electroplated samples. Simultaneous in-situ observations and stress-strain data during post-elastic deformation reveal necking and work hardening, features uncharacteristic for metallic glasses. The evolution of free volume within molecular dynamics-simulated samples suggests a free surface-mediated relaxation mechanism in nano-sized metallic glasses

  8. Application of liposomes in medicine and drug delivery.

    Science.gov (United States)

    Daraee, Hadis; Etemadi, Ali; Kouhi, Mohammad; Alimirzalu, Samira; Akbarzadeh, Abolfazl

    2016-01-01

    Liposomes provide an established basis for the sustainable development of different commercial products for treatment of medical diseases by the smart delivery of drugs. The industrial applications include the use of liposomes as drug delivery vehicles in medicine, adjuvants in vaccination, signal enhancers/carriers in medical diagnostics and analytical biochemistry, solubilizers for various ingredients as well as support matrices for various ingredients and penetration enhancers in cosmetics. In this review, we summarize the main applications and liposome-based commercial products that are currently used in the medical field. PMID:25222036

  9. Studies on precellular evolution - The encapsulation of polyribonucleotides by liposomes

    Science.gov (United States)

    Baeza, I.; Ibanez, M.; Santiago, J. C.; Wong, C.; Lazcano, A.

    1986-01-01

    Liposomes have been suggested as possible models of precellular systems formed in the early Archean earth from lipids of nonenzymatic origin. Since it is generally accepted that RNA molecules preceded double-stranded DNA molecules as genetic material, the encapsulation of polyribonucleotides within liposomes (made from dipalmitoyl phosphatidylcholine and from egg yolk phosphatidylcholine) was studied. Quantitative determinations show that approximately 50 percent of the available lipids form liposomes, and that up to 5 percent of the polyribonucleotides can be entrapped by them. Also studied was the encapsulation of polyribonucleotides in the presence of urea and cyanamide and of Zn(2+) and Pb(2+).

  10. Calcipotriol delivery into the skin with PEGylated liposomes

    DEFF Research Database (Denmark)

    Knudsen, Nina Østergaard; Rønholt, Stine; Salte, Ragnhild Djønne;

    2012-01-01

    The d-vitamin analogue calcipotriol is commonly used for topical treatment of psoriasis, but skin penetration is required for calcipotriol to reach its pharmacological target: the keratinocytes in the lower epidermis. Liposomes can enhance the delivery of drugs into the skin, but a major challenge...... of the liposomes and the ability to deliver membrane-intercalated calcipotriol into the skin. Inclusion of 0.5, l and 5mol% PEG-DSPE in the membrane enhanced the colloidal stability of the liposomes without compromising the delivery of calcipotriol from the vehicle into excised pig skin. Calcipotriol...

  11. Liposomal Drug Products: A Quality by Design Approach

    Science.gov (United States)

    Xu, Xiaoming

    Quality by Design (QbD) principles has been applied to the development of two liposomal formulations, containing a hydrophilic small molecule therapeutic (Tenofovir) and a protein therapeutic (superoxide dismutase). The goal of the research is to provide critical information on 1) how to reduce the preparation variability in liposome formulations, and 2) how to increase drug encapsulation inside liposomes to reduce manufacturing cost. Most notably, an improved liposome preparation method was developed which increased the encapsulation efficiency of hydrophilic molecules. In particular, this method allows for very high encapsulation efficiency. For example, encapsulation efficiencies of up to 50% have been achieved, whereas previously only 20% or less have been reported. Another significant outcome from this research is a first principle mathematical model to predict the encapsulation efficiency of hydrophilic drugs in unilamellar liposomes. This mathematical model will be useful in: formulation development to rapidly achieve optimized formulations; comparison of drug encapsulation efficiencies of liposomes prepared using different methods; and assisting in the development of suitable process analytical technologies to achieve real-time monitoring and control of drug encapsulation during manufacturing. A novel two-stage reverse dialysis in vitro release testing method has also been developed for passively targeted liposomes, which uses the first stage to mimic the circulation of liposomes in the body and the second stage to imitate the drug release process at the target. The developed in vitro release testing method can be used to distinguish formulations with varied compositions for quality control testing purposes. This developed method may pave the way to the development of more biorelevant quality control testing methods for liposomal drug products in the future. The QbD case studies performed in this research are examples of how this approach can be used to

  12. Effect of liposomal fluidity on skin permeation of sodium fluorescein entrapped in liposomes

    OpenAIRE

    Subongkot T; Ngawhirunpat T

    2015-01-01

    Thirapit Subongkot,1 Tanasait Ngawhirunpat21Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, Thailand; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, ThailandAbstract: The purpose of this study was to investigate the effect of ultradeformable liposome components, Tween 20 and terpenes, on vesicle fluidity. The fluidity was evaluated by electron spin resonance spectroscopy using 5-dox...

  13. In Vitro Evaluation of the Efficacy of Liposomal and Pegylated Liposomal Hydroxyurea

    OpenAIRE

    Alavi, Seyed Ebrahim; Esfahani, Maedeh Koohi Moftakhari; Ghassemi, Soheil; Akbarzadeh, Azim; Hassanshahi, Gholamhossein

    2013-01-01

    Breast cancer is one of the most frequent cancer types within women population. Hydroxyurea (HU) is a chemotherapy compound for treatment of patients with cancer diagnosis, including breast cancer associated with several adverse effects. In this study, we applied nanotechnology to decreased drug side effects along with improvement of therapeutic index. Liposomation is widely used in modern pharmacological developments in order to enhance the effects of the drugs. To achieve this, in this stud...

  14. Superresolution and Fluorescence Dynamics Evidence Reveal That Intact Liposomes Do Not Cross the Human Skin Barrier

    DEFF Research Database (Denmark)

    Dreier, Jes; Sørensen, Jens A; Brewer, Jonathan R

    2016-01-01

    skin, a POPC liposome and a more flexible liposome containing the surfactant sodium cholate. Stimulated emission depletion microscopy (STED) images of intact skin and cryo-sections of skin treated with labeled liposomes were recorded displaying an optical resolution low enough to resolve the 100 nm......In this study we use the combination of super resolution optical microscopy and raster image correlation spectroscopy (RICS) to study the mechanism of action of liposomes as transdermal drug delivery systems in human skin. Two different compositions of liposomes were applied to newly excised human...... liposomes in the skin. The images revealed that virtually none of the liposomes remained intact beneath the skin surface. RICS two color cross correlation diffusion measurements of double labeled liposomes confirmed these observations. Our results suggest that the liposomes do not act as carriers that...

  15. Chemoselective Oxidation of Bio-Glycerol with Nano-Sized Metal Catalysts

    DEFF Research Database (Denmark)

    Li, Hu; Kotni, Ramakrishna; Zhang, Qiuyun;

    2015-01-01

    selectively oxidize glycerol and yield products with good selectivity is the use of nano-sized metal particles as heterogeneous catalysts. In this short review, recent developments in chemoselective oxidation of glycerol to specific products over nano-sized metal catalysts are described. Attention is drawn to...

  16. Plasma-Chemical Synthesis of Nanosized Powders-Nitrides, Carbides, Oxides, Carbon Nanotubes and Fullerenes

    International Nuclear Information System (INIS)

    In this article the plasma-chemical synthesis of nanosized powders (nitrides, carbides, oxides, carbon nanotubes and fullerenes) is reviewed. Nanosized powders - nitrides, carbides, oxides, carbon nanotubes and fullerenes have been successfully produced using different techniques, technological apparatuses and conditions for their plasma-chemical synthesis. (plasma technology)

  17. Nanosizing and nanoconfinement: new strategies towards meeting hydrogen storage goals.

    Science.gov (United States)

    de Jongh, Petra E; Adelhelm, Philipp

    2010-12-17

    Hydrogen is expected to play an important role as an energy carrier in a future, more sustainable society. However, its compact, efficient, and safe storage is an unresolved issue. One of the main options is solid-state storage in hydrides. Unfortunately, no binary metal hydride satisfies all requirements regarding storage density and hydrogen release and uptake. Increasingly complex hydride systems are investigated, but high thermodynamic stabilities as well as slow kinetics and poor reversibility are important barriers for practical application. Nanostructuring by ball-milling is an established method to reduce crystallite sizes and increase reaction rates. Since five years attention has also turned to alternative preparation techniques that enable particle sizes below 10 nanometers and are often used in conjunction with porous supports or scaffolds. In this Review we discuss the large impact of nanosizing and -confinement on the hydrogen sorption properties of metal hydrides. We illustrate possible preparation strategies, provide insight into the reasons for changes in kinetics, reversibility and thermodynamics, and highlight important progress in this field. All in all we provide the reader with a clear view of how nanosizing and -confinement can beneficially affect the hydrogen sorption properties of the most prominent materials that are currently considered for solid-state hydrogen storage. PMID:21080405

  18. Annealing simulations of nano-sized amorphous structures in Sic

    International Nuclear Information System (INIS)

    A two-dimensional model of a nano-sized amorphous layer embedded in a perfect crystal has been developed, and the amorphous-to-crystalline (a-c) transition in 3C-Sic at 2000 K has been studied using molecular dynamics methods, with simulation times of up to 88 ns. Analysis of the a-c interfaces reveals that the recovery of the bond defects existing at the a-c interfaces plays an important role in recrystallization. During the recrystallization process, a second ordered phase, crystalline 2H-SiC, nucleates and grows, and this phase is stable for long simulation times. The crystallization mechanism is a two-step process that is separated by a longer period of second-phase stability. The kink sites formed at the interfaces between 2H- and 3C-SiC provide a low energy path for 2H-SiC atoms to transfer to 3C-SiC atoms, a process which can be defined as a solid-phase epitaxial transformation (SPET). It is observed that the nano-sized amorphous structure can be fully recrystallized at 2000 K in SiC, which is in agreement with experimental observations

  19. Antigenic composition of single nano-sized extracellular blood vesicles.

    Science.gov (United States)

    Arakelyan, Anush; Ivanova, Oxana; Vasilieva, Elena; Grivel, Jean-Charles; Margolis, Leonid

    2015-04-01

    Extracellular vesicles (EVs) are important in normal physiology and are altered in various pathologies. EVs produced by different cells are antigenically different. Since the majority of EVs are too small for routine flow cytometry, EV composition is studied predominantly in bulk, thus not addressing their antigenic heterogeneity. Here, we describe a nanoparticle-based technique for analyzing antigens on single nano-sized EVs. The technique consists of immuno-capturing of EVs with 15-nm magnetic nanoparticles, staining captured EVs with antibodies against their antigens, and separating them from unbound EVs and free antibodies in a magnetic field, followed by flow analysis. This technique allows us to characterize EVs populations according to their antigenic distribution, including minor EV fractions. We demonstrated that the individual blood EVs carry different sets of antigens, none being ubiquitous, and quantified their distribution. The physiological significance of antigenically different EVs and their correlation with different pathologies can now be directly addressed. From the clinical editor: This study reports a nanoparticle-based technique for analyzing antigens on single nano-sized extracellular vehicles (EV). The technique consists of immuno-capturing of EVs with 15-nm magnetic nanoparticles, followed by staining the captured EVs with antibodies and separating them via a magnetic field, followed by flow analysis. This technique enables studies of antigenic properties of individual EVs that conventionally can only be studied in bulk. PMID:25481806

  20. Temperature-controlled interaction of thermosensitive polymer-modified cationic liposomes with negatively charged phospholipid membranes.

    Science.gov (United States)

    Kono, K; Henmi, A; Takagishi, T

    1999-09-21

    To obtain cationic liposomes of which affinity to negatively charged membranes can be controlled by temperature, cationic liposomes consisting of 3beta-[N-(N', N'-dimethylaminoethane)carbamoyl]cholesterol and dioleoylphosphatidylethanolamine were modified with poly(N-acryloylpyrrolidine), which is a thermosensitive polymer exhibiting a lower critical solution temperature (LCST) at ca. 52 degrees C. The unmodified cationic liposomes did not change its zeta potential between 20-60 degrees C. The polymer-modified cationic liposomes revealed much lower zeta potential values below the LCST of the polymer than the unmodified cationic liposomes. However, their zeta potential increased significantly above this temperature. The unmodified cationic liposomes formed aggregates and fused intensively with anionic liposomes consisting of egg yolk phosphatidylcholine and phosphatidic acid in the region of 20-60 degrees C, due to the electrostatic interaction. In contrast, aggregation and fusion of the polymer-modified cationic liposomes with the anionic liposomes were strongly suppressed below the LCST. However, these interactions were enhanced remarkably above the LCST. In addition, the polymer-modified cationic liposomes did not cause leakage of calcein from the anionic liposomes below the LCST, but promoted the leakage above this temperature as the unmodified cationic liposomes did. Temperature-induced conformational change of the polymer chains from a hydrated coil to a dehydrated globule might affect the affinity of the polymer-modified cationic liposomes to the anionic liposomes. PMID:10561483

  1. Cholesterol Derivatives Based Charged Liposomes for Doxorubicin Delivery: Preparation, In Vitro and In Vivo Characterization

    Directory of Open Access Journals (Sweden)

    Yu Nie, Li Ji, Hong Ding, Li Xie, Li Li, Bin He, Yao Wu, Zhongwei Gu

    2012-01-01

    Full Text Available Cholesterol plays a critical role in liposome composition. It has great impact on the behavior of liposome in vitro and in vivo. In order to verify the possible effects from cholesterol charge, surface shielding and chemical nature, two catalogs of liposomes with charged and PEGylated cholesterols were synthesized. Anionic liposomes (AL and cationic liposomes (CL were prepared, with charges from hemisuccinate and lysine in cholesterol derivatives, respectively. Characteristics of different formulated liposomes were investigated after doxorubicin encapsulation, using neutral liposomes (NL as control. Results showed that after PEGylation, AL and CL liposomes displayed prolonged retention release profile, while kept similar size distribution, encapsulation efficiency, low cytotoxicity and hemolysis comparing with NL. Confocal laser scanning microscopy and flow cytometry experiments confirmed the significantly higher cell uptake from AL and CL vesicles than the NL in mouse breast carcinoma and melanoma cells, human epithelial carcinoma and hepatoma cells. It was in accordance with our corresponding cellular mortality studies of DOX-loaded liposomes. The in vivo anti-tumor effect experiments from charged liposomes also presented much higher tumor inhibition effect (70% vs 45%, p < 0.05 than NL liposomes. This is the first time reporting anti-cancer effect from charged cholesterol liposome with/without PEGylation. It may give deeper understanding on the liposome formulation which is critical for liposome associated drug research and development.

  2. Sustained distribution of aerosolized PEGylated liposomes in epithelial lining fluids on alveolar surfaces.

    Science.gov (United States)

    Kaneko, Keita; Togami, Kohei; Yamamoto, Eri; Wang, Shujun; Morimoto, Kazuhiro; Itagaki, Shirou; Chono, Sumio

    2016-10-01

    The distribution characteristics of aerosolized PEGylated liposomes in alveolar epithelial lining fluid (ELF) were examined in rats, and the ensuing mechanisms were investigated in the in vitro uptake and protein adsorption experiments. Nonmodified or PEGylated liposomes (particle size 100 nm) were aerosolized into rat lungs. PEGylated liposomes were distributed more sustainably in ELFs than nonmodified liposomes. Furthermore, the uptake of PEGylated liposomes by alveolar macrophages (AMs) was less than that of nonmodified liposomes. In further in vitro uptake experiments, nonmodified and PEGylated liposomes were opsonized with rat ELF components and then added to NR8383 cells as cultured rat AMs. The uptake of opsonized PEGylated liposomes by NR8383 cells was lower than that of opsonized nonmodified liposomes. Moreover, the protein absorption levels in opsonized PEGylated liposomes were lower than those in opsonized nonmodified liposomes. These findings suggest that sustained distributions of aerosolized PEGylated liposomes in ELFs reflect evasion of liposomal opsonization with surfactant proteins and consequent reductions in uptake by AMs. These data indicate the potential of PEGylated liposomes as aerosol-based drug delivery system that target ELF for the treatment of respiratory diseases. PMID:27334278

  3. Atmospheric-pressure guided streamers for liposomal membrane disruption

    Science.gov (United States)

    Svarnas, P.; Matrali, S. H.; Gazeli, K.; Aleiferis, Sp.; Clément, F.; Antimisiaris, S. G.

    2012-12-01

    The potential to use liposomes (LIPs) as a cellular model in order to study interactions of cold atmospheric-pressure plasma with cells is herein investigated. Cold atmospheric-pressure plasma is formed by a dielectric-barrier discharge reactor. Large multilamellar vesicle liposomes, consisted of phosphatidylcholine and cholesterol, are prepared by the thin film hydration technique, to encapsulate a small hydrophilic dye, i.e., calcein. The plasma-induced release of calcein from liposomes is then used as a measure of liposome membrane integrity and, consequently, interaction between the cold atmospheric plasma and lipid bilayers. Physical mechanisms leading to membrane disruption are suggested, based on the plasma characterization including gas temperature calculation.

  4. Atmospheric-pressure guided streamers for liposomal membrane disruption

    International Nuclear Information System (INIS)

    The potential to use liposomes (LIPs) as a cellular model in order to study interactions of cold atmospheric-pressure plasma with cells is herein investigated. Cold atmospheric-pressure plasma is formed by a dielectric-barrier discharge reactor. Large multilamellar vesicle liposomes, consisted of phosphatidylcholine and cholesterol, are prepared by the thin film hydration technique, to encapsulate a small hydrophilic dye, i.e., calcein. The plasma-induced release of calcein from liposomes is then used as a measure of liposome membrane integrity and, consequently, interaction between the cold atmospheric plasma and lipid bilayers. Physical mechanisms leading to membrane disruption are suggested, based on the plasma characterization including gas temperature calculation.

  5. Avoiding failed reconstitution of ultradeformable liposomes upon dehydration.

    Science.gov (United States)

    Montanari, J; Roncaglia, D I; Lado, L A; Morilla, M J; Romero, E L

    2009-05-01

    Although freeze-drying is an ordinarily used technique to dehydrate conventional liposomes, we have found that ultradeformable liposomes (UDLs) suffered irreversible aggregation when rehydrated upon freeze-drying (99.4% water elimination), even in high sugar content (4/1 sucrose/lipid mass ratio). When dehydrated by speed vac and vacuum drying, two alternative techniques that rendered less pronounced dehydration (94.27 and 96.2% water elimination, respectively) and avoid ice formation, however, UDL could only be successfully rehydrated when vacuum dried in 4/1 sucrose/lipid mass ratios. Conventional liposomes, on the other hand, were successfully reconstituted upon dehydrated by the three methods in lower sugar content (2/1 sucrose/lipid mass ratio). These results indicated that the 27% mole sodium cholate within the UDL lipid matrix was responsible for a greater and differential mechanical sensitivity of the bilayers to the different dehydration stress, as compared to conventional liposomes. PMID:19429279

  6. Atmospheric-pressure guided streamers for liposomal membrane disruption

    Energy Technology Data Exchange (ETDEWEB)

    Svarnas, P.; Aleiferis, Sp. [High Voltage Laboratory, Department of Electrical and Computer Engineering, University of Patras, Rion 26504 (Greece); Matrali, S. H. [Pharmaceutical Technology Laboratory, Department of Pharmacy, University of Patras, Rion 26504 (Greece); Gazeli, K. [High Voltage Laboratory, Department of Electrical and Computer Engineering, University of Patras, Rion 26504 (Greece); IPREM-LCABIE, Plasmas et Applications, UPPA, 64000 Pau (France); Clement, F. [IPREM-LCABIE, Plasmas et Applications, UPPA, 64000 Pau (France); Antimisiaris, S. G. [Pharmaceutical Technology Laboratory, Department of Pharmacy, University of Patras, Rion 26504 (Greece); Institute of Chemical Engineering Sciences (ICES)-FORTH, Rion 26504 (Greece)

    2012-12-24

    The potential to use liposomes (LIPs) as a cellular model in order to study interactions of cold atmospheric-pressure plasma with cells is herein investigated. Cold atmospheric-pressure plasma is formed by a dielectric-barrier discharge reactor. Large multilamellar vesicle liposomes, consisted of phosphatidylcholine and cholesterol, are prepared by the thin film hydration technique, to encapsulate a small hydrophilic dye, i.e., calcein. The plasma-induced release of calcein from liposomes is then used as a measure of liposome membrane integrity and, consequently, interaction between the cold atmospheric plasma and lipid bilayers. Physical mechanisms leading to membrane disruption are suggested, based on the plasma characterization including gas temperature calculation.

  7. Antigen-specific suppression of inflammatory arthritis using liposomes.

    Science.gov (United States)

    Capini, Christelle; Jaturanpinyo, Montree; Chang, Hsin-I; Mutalik, Srinivas; McNally, Alice; Street, Shayna; Steptoe, Raymond; O'Sullivan, Brendan; Davies, Nigel; Thomas, Ranjeny

    2009-03-15

    Existing therapies for rheumatoid arthritis and other autoimmune diseases are not Ag specific, which increases the likelihood of systemic toxicity. We show that egg phosphatidylcholine liposomes loaded with Ag (OVA or methylated BSA) and a lipophilic NF-kappaB inhibitor (curcumin, quercetin, or Bay11-7082) suppress preexisting immune responses in an Ag-specific manner. We injected loaded liposomes into mice primed with Ag or into mice suffering from Ag-induced inflammatory arthritis. The liposomes targeted APCs in situ, suppressing the cells' responsiveness to NF-kappaB and inducing Ag-specific FoxP3(+) regulatory T cells. This regulatory mechanism suppressed effector T cell responses and the clinical signs of full-blown Ag-induced arthritis. Thus, liposomes encapsulate Ags and NF-kappaB inhibitors stably and efficiently and could be readily adapted to deliver Ags and inhibitors for Ag-specific suppression of other autoimmune and allergic diseases. PMID:19265134

  8. Bioreactor droplets from liposome-stabilized all-aqueous emulsions

    Science.gov (United States)

    Dewey, Daniel C.; Strulson, Christopher A.; Cacace, David N.; Bevilacqua, Philip C.; Keating, Christine D.

    2014-08-01

    Artificial bioreactors are desirable for in vitro biochemical studies and as protocells. A key challenge is maintaining a favourable internal environment while allowing substrate entry and product departure. We show that semipermeable, size-controlled bioreactors with aqueous, macromolecularly crowded interiors can be assembled by liposome stabilization of an all-aqueous emulsion. Dextran-rich aqueous droplets are dispersed in a continuous polyethylene glycol (PEG)-rich aqueous phase, with coalescence inhibited by adsorbed ~130-nm diameter liposomes. Fluorescence recovery after photobleaching and dynamic light scattering data indicate that the liposomes, which are PEGylated and negatively charged, remain intact at the interface for extended time. Inter-droplet repulsion provides electrostatic stabilization of the emulsion, with droplet coalescence prevented even for submonolayer interfacial coatings. RNA and DNA can enter and exit aqueous droplets by diffusion, with final concentrations dictated by partitioning. The capacity to serve as microscale bioreactors is established by demonstrating a ribozyme cleavage reaction within the liposome-coated droplets.

  9. Analysis of liposomes using asymmetrical flow field-flow fractionation

    DEFF Research Database (Denmark)

    Kuntsche, Judith; Decker, Christiane; Fahr, Alfred

    2012-01-01

    Liposomes composed of dipalmitoylphosphatidylcholine and dipalmitoylphosphatidylglycerol were analyzed by asymmetrical flow field-flow fractionation coupled with multi-angle laser light scattering. In addition to evaluation of fractionation conditions (flow conditions, sample mass, carrier liquid...

  10. Mn3O4 nano-sized crystals: Rapid synthesis and extension to preparation of nanosized LiMn2O4 materials

    Indian Academy of Sciences (India)

    Xiao-Ling Cui; Yong-Li Li; Shi-You Li; Guo-Cun Sun; Jin-Xia Ma; Lu Zhang; Tian-Ming Li; Rong-Bo Ma

    2014-05-01

    With a novel gas-liquid reaction, a facile and rapid method has been successfully developed for the synthesis of nano-sized Mn3O4 crystals. Coupled with complementary experiments, preparation mechanisms of Mn(II) and Mn(III)Mn(III)Mn(II) coordination complexes as well as nano-sized Mn3O4 crystals are studied. Besides, as the extension of synthesis of nano-sized Mn3O4 crystals, the intermediate ammonia alkaline solution containing Mn(III)Mn(III)Mn(II) coordination complexes, which tend to decompose into nano-sized Mn3O4 crystals spontaneously, are used to prepare nanosized LiMn2O4 materials. Although any physical treatment has been done to disperse powders, the as-synthesized LiMn2O4 nanoparticles are still existence with homogeneous size distribution (about 24.2 nm) without any obvious agglomeration. That is to say, the novel method is constructive not only to accelerate reaction rates for the elevated oxidation state of manganese ions, but also to prepare dispersed nanosized LiMn2O4 materials with good electrochemical properties.

  11. Effect of liposomal amphotericin B on murine macrophages and lymphocytes.

    OpenAIRE

    Mehta, R T; Mehta, K; Lopez-Berestein, G; Juliano, R. L.

    1985-01-01

    The effect of liposome-encapsulated amphotericin B on mouse macrophages and on T- and B-lymphocyte functions in vitro was compared with that of free amphotericin B. Liposomal amphotericin B was generally less toxic than the free form of the drug. Low concentrations of free amphotericin B completely inhibited the serum-dependent induction of transglutaminase, a marker for macrophage differentiation, and production of superoxide anion by macrophages, whereas encapsulation of the drug within lip...

  12. Targeted liposomal drug delivery to monocytes and macrophages.

    OpenAIRE

    Ciara Kelly; Caroline Jefferies; Sally-Ann Cryan

    2011-01-01

    As the role of monocytes and macrophages in a range of diseases is better understood, strategies to target these cell types are of growing importance both scientifically and therapeutically. As particulate carriers, liposomes naturally target cells of the mononuclear phagocytic system (MPS), particularly macrophages. Loading drugs into liposomes can therefore offer an efficient means of drug targeting to MPS cells. Physicochemical properties including size, charge and lipid composition can ha...

  13. Gadolinium-containing phosphatidylserine liposomes for molecular imaging of atherosclerosis

    OpenAIRE

    Maiseyeu, Andrei; Mihai, Georgeta; Kampfrath, Thomas; Simonetti, Orlando P.; Sen, Chandan K.; Roy, Sashwati; Rajagopalan, Sanjay; Parthasarathy, Sampath

    2009-01-01

    Exteriorized phosphatidylserine (PS) residues in apoptotic cells trigger rapid phagocytosis by macrophage scavenger receptor pathways. Mimicking apoptosis with liposomes containing PS may represent an attractive approach for molecular imaging of atherosclerosis. We investigated the utility of paramagnetic gadolinium liposomes enriched with PS (Gd-PS) in imaging atherosclerotic plaque. Gd-PS-containing Gd-conjugated lipids, fluorescent rhodamine, and PS were prepared and characterized. Cellula...

  14. Engineering hybrid exosomes by membrane fusion with liposomes

    OpenAIRE

    Sato, Yuko T.; Kaori Umezaki; Shinichi Sawada; Sada-atsu Mukai; Yoshihiro Sasaki; Naozumi Harada; Hiroshi Shiku; Kazunari Akiyoshi

    2016-01-01

    Exosomes are a valuable biomaterial for the development of novel nanocarriers as functionally advanced drug delivery systems. To control and modify the performance of exosomal nanocarriers, we developed hybrid exosomes by fusing their membranes with liposomes using the freeze–thaw method. Exosomes embedded with a specific membrane protein isolated from genetically modified cells were fused with various liposomes, confirming that membrane engineering methods can be combined with genetic modifi...

  15. Labelling of liposomes with intercalating perylene fluorescent dyes

    OpenAIRE

    Schott, H; Cunow, D. von; Langhals, Heinz

    1992-01-01

    The high fluorescent potential and the exceptional photostability of lipophilic derivatives of perylene-3,4:9,10-bis(dicarboximides) are utilized for the fluorescence-labelling of liposomes. The preparation of the liposomes is affected by supersonic starting from a lipid mixture consisting of the matrix lipids soy lecithin, cholesterol, -tocopherol and the perylene dyes. From a multitude of perylene derivatives investigated only those are optimally incorporated inot the bilayer membrane of un...

  16. Influence of osmotic stress on liposome size and morphology

    OpenAIRE

    Moen, Helene

    2008-01-01

    Liposomes are currently being investigated as potential parenterally used drug carriers. The main factor that influences the in vivo behavior of such liposomes is their vesicle size. A detailed and reliable knowledge of vesicle size is therefore necessary in order to interpret results of physical and biological investigations in a correct manner. It has earlier been discovered that it is feasible to determine the size distribution of vesicle dispersions in a reliable manner and it appears...

  17. Liposome-coated quantum dots targeting the sentinel lymph node

    Energy Technology Data Exchange (ETDEWEB)

    Chu Maoquan, E-mail: mqchu98@tongji.edu.cn; Zhuo Shu; Xu Jiang; Sheng Qiunan; Hou Shengke; Wang Ruifei [Tongji University, School of Life Science and Technology (China)

    2010-01-15

    Sentinel lymph node (SLN) mapping with near-infrared (NIR) quantum dot (QDs) have many advantages over traditional methods. However, as an inorganic nanomaterial, QDs have low biocompatibility and low affinity to the lymphatic system. Here, we encapsulated QDs into nanoscale liposomes and then used these liposome-coated QDs for SLN mapping. The results showed that the liposome-coated QDs exhibited core-shell characterization, and their fluorescence emission did not decrease but slightly increased after being continuously excited by a xenon lamp source (150 W) at 488 nm at 37 {sup o}C for 1 h. After storing at 4 {sup o}C for more than one and half years, the liposome-coated QDs were found to have retained their spherical structure containing a large amount of QDs. When liposome-coated QDs with average size of 55.43 nm were injected intradermally into the paw of a mouse, the SLN was strongly fluorescent within only a few seconds and visualized easily in real time. Moreover, the fluorescence of the QDs trapped in the SLN could be observed for at least 24 h. Compared with the SLN mapping of QDs absent of liposomes and liposome-coated QDs with a larger average size (100.3 and 153.6 nm), more QDs migrated into the SLN when the liposome-coated QDs with smaller average size (55.43 nm) were injected. This technique may make a great contribution to the improvement of the biocompatibility of QDs and the targeting delivery capacity of QDs into the SLN.

  18. Technology of Liposomal Tiosens, Cifelin and Lysomustin for Industrial Purposes

    Science.gov (United States)

    Sanarova, E. V.; Kotova, E. A.; Lantsova, A. V.

    2012-02-01

    This work is devoted to the development of national antineoplastic drug (Tiosens, Cifelin, Lysomustin) liposomal dosage form (LDF) circuit technology and their manufacturing technology. In modern oncology liposomes, which are hollow phospholipid vesicles, are used as delivery systems protected drugs from biodegradation, and healthy cells from the toxic effect of chemotherapeutic agents. The technology of their production is stretching and multistage. It is also necessary to give consideration a lot of factors that influence on the finished product quality.

  19. Liposome-coated quantum dots targeting the sentinel lymph node

    International Nuclear Information System (INIS)

    Sentinel lymph node (SLN) mapping with near-infrared (NIR) quantum dot (QDs) have many advantages over traditional methods. However, as an inorganic nanomaterial, QDs have low biocompatibility and low affinity to the lymphatic system. Here, we encapsulated QDs into nanoscale liposomes and then used these liposome-coated QDs for SLN mapping. The results showed that the liposome-coated QDs exhibited core-shell characterization, and their fluorescence emission did not decrease but slightly increased after being continuously excited by a xenon lamp source (150 W) at 488 nm at 37 oC for 1 h. After storing at 4 oC for more than one and half years, the liposome-coated QDs were found to have retained their spherical structure containing a large amount of QDs. When liposome-coated QDs with average size of 55.43 nm were injected intradermally into the paw of a mouse, the SLN was strongly fluorescent within only a few seconds and visualized easily in real time. Moreover, the fluorescence of the QDs trapped in the SLN could be observed for at least 24 h. Compared with the SLN mapping of QDs absent of liposomes and liposome-coated QDs with a larger average size (100.3 and 153.6 nm), more QDs migrated into the SLN when the liposome-coated QDs with smaller average size (55.43 nm) were injected. This technique may make a great contribution to the improvement of the biocompatibility of QDs and the targeting delivery capacity of QDs into the SLN.

  20. Development of a liposomal nanodelivery system for nevirapine

    Directory of Open Access Journals (Sweden)

    Krishnan Uma M

    2010-07-01

    Full Text Available Abstract Background The treatment of AIDS remains a serious challenge owing to high genetic variation of Human Immunodeficiency Virus type 1 (HIV-1. The use of different antiretroviral drugs (ARV is significantly limited by severe side-effects that further compromise the quality of life of the AIDS patient. In the present study, we have evaluated a liposome system for the delivery of nevirapine, a hydrophobic non-nucleoside reverse transcriptase inhibitor. Liposomes were prepared from egg phospholipids using thin film hydration. The parameters of the process were optimized to obtain spherical liposomes below 200 nm with a narrow polydispersity. The encapsulation efficiency of the liposomes was optimized at different ratios of egg phospholipid to cholesterol as well as drug to total lipid. The data demonstrate that encapsulation efficiency of 78.14% and 76.25% were obtained at egg phospholipid to cholesterol ratio of 9:1 and drug to lipid ratio of 1:5, respectively. We further observed that the size of the liposomes and the encapsulation efficiency of the drug increased concomitantly with the increasing ratio of drug and lipid and that maximum stability was observed at the physiological pH. Thermal analysis of the drug encapsulated liposomes indicated the formation of a homogenous drug-lipid system. The magnitude of drug release from the liposomes was examined under different experimental conditions including in phosphate buffered saline (PBS, Dulbecco's Modified Eagle's Medium (DMEM supplemented with 10% fetal bovine serum or in the presence of an external stimulus such as low frequency ultrasound. Within the first 20 minutes 40, 60 and 100% of the drug was released when placed in PBS, DMEM or when ultrasound was applied, respectively. We propose that nevirapine-loaded liposomal formulations reported here could improve targeted delivery of the anti-retroviral drugs to select compartments and cells and alleviate systemic toxic side effects as a

  1. Improved Delivery of Caffeic Acid through Liposomal Encapsulation

    OpenAIRE

    Katuwavila, Nuwanthi P.; A. D. L. Chandani Perera; V. Karunaratne; Gehan A. J. Amaratunga; D. Nedra Karunaratne

    2016-01-01

    Photoageing resulting from long term exposure of the skin to UV light can be minimized by scavenging the reactive photochemical intermediates with antioxidants. For effective photoprotection, the antioxidant must overcome the barrier properties of the skin and reach the target site in significant amounts. The present study aims to improve the skin penetration of caffeic acid, a very effective free radical scavenger, by encapsulating in liposomes. Caffeic acid loaded liposomes prepared using t...

  2. DESIGN, DEVELOPMENT AND CHARACTERIZATION OF LIPOSOMAL NEEM GEL

    Directory of Open Access Journals (Sweden)

    ASMITA SINGH

    2014-04-01

    Full Text Available Purpose: Liposomal formulations have been successfully used in the treatment of a number of dermatological diseases. Various synthetic as well as herbal drugs are incorporated into liposome to improve its efficacy. Incorporation of herbal extract into liposome reduces side effects which are associated with the synthetic ones. Azadirachta indica leaves possesse good anti bacterial activity, confirming the great potential of bioactive compounds of neem. Among aqueous extract and alcoholic extract, alcoholic leaf extracts of A. indica were found to be more active towards the bacterial species. Hence, this extract was incorporated into liposomes to enhance its activity in skin delivery. The objective of the present research work is to convert this age old miraculous herb into nanotechnology based formulations i.e. liposomes. An attempt has been made to prepare liposomal Neem gel for topical use for anti-microbial activity. Methods: Methanolic Neem Extract (MeNE was incorporated into liposomes by thin film hydration method. The batch having lipid ratio i.e. Soya lecithin: Cholesterol (4:1; MeNE concentration 80 mg with entrapment efficiency 69.52 ±1.9% was finalized. Results and Conclusions: The vesicle size was found to be 3.2μm ± 0.67. In vitro drug diffusion and skin retention from liposomal gel was found to be 62.178% ± 0.91 and 20.03% ± 0.63 respectively. Stability studies indicated that formulation was stable over a period of 3 months when stored at 2-8°C.

  3. Engineering of an Inhalable DDA/TDB Liposomal Adjuvant

    DEFF Research Database (Denmark)

    Ingvarsson, Pall Thor; Yang, Mingshi; Mulvad, Helle;

    2013-01-01

    The purpose of this study was to identify and optimize spray drying parameters of importance for the design of an inhalable powder formulation of a cationic liposomal adjuvant composed of dimethyldioctadecylammonium (DDA) bromide and trehalose-6,6'-dibehenate (TDB).......The purpose of this study was to identify and optimize spray drying parameters of importance for the design of an inhalable powder formulation of a cationic liposomal adjuvant composed of dimethyldioctadecylammonium (DDA) bromide and trehalose-6,6'-dibehenate (TDB)....

  4. Liposome production by microfluidics: potential and limiting factors

    OpenAIRE

    Dario Carugo; Elisabetta Bottaro; Joshua Owen; Eleanor Stride; Claudio Nastruzzi

    2016-01-01

    This paper provides an analysis of microfluidic techniques for the production of nanoscale lipid-based vesicular systems. In particular we focus on the key issues associated with the microfluidic production of liposomes. These include, but are not limited to, the role of lipid formulation, lipid concentration, residual amount of solvent, production method (including microchannel architecture), and drug loading in determining liposome characteristics. Furthermore, we propose microfluidic archi...

  5. Advanced strategies in liposomal cancer therapy

    DEFF Research Database (Denmark)

    Andresen, Thomas Lars; Jensen, Simon Skøde; Jørgensen, Kent

    2005-01-01

    Tumor specific drug delivery has become increasingly interesting in cancer therapy, as the use of chemotherapeutics is often limited due to severe side effects. Conventional drug delivery systems have shown low efficiency and a continuous search for more advanced drug delivery principles is...... therefore of great importance. In the first part of this review, we present current strategies in the drug delivery field, focusing on site-specific triggered drug release from liposomes in cancerous tissue. Currently marketed drug delivery systems lack the ability to actively release the carried drug and......, none of them have yet led to marketed drugs and are still far from achieving this goal. The most advanced and prospective technologies are probably the prodrug strategies where nontoxic drugs are carried and activated specifically in the malignant tissue by overexpressed enzymes. In the second part of...

  6. Size of thermosensitive liposomes influences content release.

    Science.gov (United States)

    Hossann, Martin; Wang, Tungte; Wiggenhorn, Michael; Schmidt, Rebecca; Zengerle, Anja; Winter, Gerhard; Eibl, Hansjörg; Peller, Michael; Reiser, Maximilian; Issels, Rolf D; Lindner, Lars H

    2010-11-01

    Thermosensitive liposomes (TSL) in combination with regional hyperthermia represent a powerful tool for tumor specific drug delivery. The objective of this study was to investigate the influence of vesicle size on the biophysical properties of TSL. TSL were composed of DPPC/DSPC/1,2-dipalmitoyl-sn-glycero-3-phosphoglyceroglycerol (DPPG(2)) 50:20:30 (mol/mol) (DPPG(2)-TSL) and DPPC/P-Lyso-PC/DSPE-PEG2000 90:10:4 (mol/mol) (PEG/Lyso-TSL) with encapsulated fluorescent dye carboxyfluorescein, anticancer drug doxorubicin or magnetic resonance contrast agent gadodiamide. Extrusion was performed with polycarbonate filters of distinct pore size to obtain TSL with different diameters (50 to 200nm). Phase transition temperature (T(m)) of the bilayer forming phospholipids was not influenced by vesicle size in the tested range. However, vesicle size had a major impact on in vitro content release properties of TSL in the investigated temperature range between 30 and 45°C. Generally, vesicle size was inversely related to content release properties with increased content release rates for decreased vesicle sizes. Size dependency of content release properties varied between all tested formulations and DPPG(2)-TSL were generally less affected by size changes in the range of 100 to 150nm as compared to PEG/Lyso-TSL. Independent from gadodiamide release, vesicle size influenced the signal intensity of DPPG(2)-TSL also at temperatures below T(m) due to improved water exchange for smaller vesicles. Liposomes around 100nm in size are routinely used in vivo, hence a quality control for TSL preparations is required prior to use. Even small changes in size or a wider size distribution might affect stability and release properties and thus yield in decreased efficacy or unwanted side effects of drug loaded TSL during in vivo applications. PMID:20727921

  7. Ultrasonic Activation of Thermally Sensitive Liposomes

    Science.gov (United States)

    Mylonopouloua, Eleonora; Arvanitisa, Costas D.; Bazan-Peregrinoa, Miriam; Arora, Manish; Coussios, Constantin C.

    2010-03-01

    Cancerous cells are known to be more vulnerable to mild hyperthermia than healthy cells, which can survive temperatures above 43° C for brief periods of time. Currently in phase III clinical trials for liver cancer, ThermoDox® (Celsion Corporation) is a drug delivery system containing doxorubicin, a common anti-cancer agent, encapsulated within a thermally sensitive liposome designed to release its contents above 39.5° C. Activation of such an agent with the use of HIFU, which can generate localized heating non-invasively, would combine the benefits of targeted chemotherapy and hyperthermia while minimizing undesirable systemic side-effects. To that end, the resolution and reliability with which HIFU-induced hyperthermia can achieve Thermodox® release was investigated using a novel agar-based gel embedding liposomes at clinically relevant concentrations (0.02 mg/ml). The gel was exposed to 1.15 MHz HIFU (Sonic Concepts H102) using a range of clinically relevant pressure amplitudes (0-6 MPa peak rarefactional), duty cycles (10-100%) and exposure durations to identify optimal insonation conditions for complete doxorubicin release. The corresponding temperature profiles were mapped with 0.5 mm spatial resolution using an embedded needle thermocouple; drug release was quantified using fluorimetry. Complete release over the HIFU focal area was obtained for 6-s continuous wave exposure at 5.2 MPa peak rarefactional pressure, i.e. under exposure conditions for which the temperature exceeded 43° C throughout the focal volume. For a given HIFU energy input, both the final temperature reached and the rate of heating were found to affect release significantly. However, ThermoDox® release was achieved only due to thermal effects of HIFU, and not by other ultrasound effects, such as cavitation without heating, showing robustness of HIFU-induced hyperthermia as a release mechanism.

  8. Photodynamic ultradeformable liposomes: Design and characterization.

    Science.gov (United States)

    Montanari, J; Perez, A P; Di Salvo, F; Diz, V; Barnadas, R; Dicelio, L; Doctorovich, F; Morilla, M J; Romero, E L

    2007-02-01

    Hydrophobic ([tetrakis(2,4-dimetil-3-pentyloxi)-phthalocyaninate]zinc(II)) (ZnPc) and hydrophilic ([tetrakis(N,N,N-trimethylammoniumetoxi)-phthalocyaninate]zinc(II) tetraiodide) (ZnPcMet) phthalocyanines were synthesized and loaded in ultradeformable liposomes (UDL) of soybean phosphatidylcholine and sodium cholate (6:1, w/w, ratio), resulting 100 nm mean size vesicles of negative Zeta potential, with encapsulation efficiencies of 85 and 53%, enthalpy of phase transition of 5.33 and 158 J/mmol for ZnPc and ZnPcMet, respectively, indicating their deep and moderate partition into UD matrices. Matrix elasticity of UDL-phthalocyanines resulted 28-fold greater than that of non-UDL, leaking only 25% of its inner aqueous content after passage through a nanoporous barrier versus 100% leakage for non-UDL. UDL-ZnPc made ZnPc soluble in aqueous buffer while kept the monomeric state, rendering singlet oxygen quantum yield (Phi(Delta)) similar to that obtained in ethanol (0.61), whereas UDL-ZnPcMet had a four-fold higher Phi(Delta) than that of free ZnPcMet (0.21). Free phthalocyanines were non-toxic at 1 and 10 microM, both in dark or upon irradiation at 15 J/cm2 on Vero and J-774 cells (MTT assay). Only liposomal ZnPc at 10 microM was toxic for J-774 cells under both conditions. Additionally, endo-lysosomal confinement of the HPTS dye was kept after irradiation at 15 J/cm2 in the presence of UDL-phtalocyanines. This could lead to improve effects of singlet oxygen against intra-vesicular pathogen targets inside the endo-lysosomal system. PMID:17157460

  9. Peptide Anchor for Folate-Targeted Liposomal Delivery.

    Science.gov (United States)

    Nogueira, Eugénia; Mangialavori, Irene C; Loureiro, Ana; Azoia, Nuno G; Sárria, Marisa P; Nogueira, Patrícia; Freitas, Jaime; Härmark, Johan; Shimanovich, Ulyana; Rollett, Alexandra; Lacroix, Ghislaine; Bernardes, Gonçalo J L; Guebitz, Georg; Hebert, Hans; Moreira, Alexandra; Carmo, Alexandre M; Rossi, Juan Pablo F C; Gomes, Andreia C; Preto, Ana; Cavaco-Paulo, Artur

    2015-09-14

    Specific folate receptors are abundantly overexpressed in chronically activated macrophages and in most cancer cells. Directed folate receptor targeting using liposomes is usually achieved using folate linked to a phospholipid or cholesterol anchor. This link is formed using a large spacer like polyethylene glycol. Here, we report an innovative strategy for targeted liposome delivery that uses a hydrophobic fragment of surfactant protein D linked to folate. Our proposed spacer is a small 4 amino acid residue linker. The peptide conjugate inserts deeply into the lipid bilayer without affecting liposomal integrity, with high stability and specificity. To compare the drug delivery potential of both liposomal targeting systems, we encapsulated the nuclear dye Hoechst 34580. The eventual increase in blue fluorescence would only be detectable upon liposome disruption, leading to specific binding of this dye to DNA. Our delivery system was proven to be more efficient (2-fold) in Caco-2 cells than classic systems where the folate moiety is linked to liposomes by polyethylene glycol. PMID:26241560

  10. Modification of wool surface by liposomes for dyeing with weld.

    Science.gov (United States)

    Montazer, Majid; Zolfaghari, Alireza; Toliat, Taibeh; Moghadam, Mohammad Bameni

    2009-01-01

    In this research work, wool surface has been modified by liposome to investigate its effects on dyeing with weld, a yellow natural dye. To do this, samples were first treated with aluminium sulphate and afterward with different concentrations of liposomes at various temperatures for 30 minutes and, finally, dyed with weld at 75, 85, and 95 degrees C for 30, 45, and 60 minutes. K/S values of fabric samples were calculated and washing, light and rub fastness properties of the samples were indicated. The results proposed that the sample treated with 1% liposomes and dyed at 75 degrees C for 60 min has the highest K/S value. The central composite design (CCD) used for the experimental plan with three variables on the results of color strength and statistical analysis confirms the optimum conditions obtained by the experimental results. It was also found that washing, light, wet, and dry rub fastness properties of samples dyed with weld, including liposomes, have not significantly changed. The results of water drop absorption indicated that the hydrophobicity is higher for the samples pretreated with liposomes. The SEM picture of wool sample treated with mordant and liposomes and finally dyed with weld shows a coated layer on the fiber surface. PMID:19552578

  11. Effectiveness of liposomal paclitaxel against MCF-7 breast cancer cells.

    Science.gov (United States)

    Heney, Melanie; Alipour, Misagh; Vergidis, Dimitrios; Omri, Abdelwahab; Mugabe, Clement; Th'ng, John; Suntres, Zacharias

    2010-12-01

    Paclitaxel is an effective chemotherapeutic agent that is widely used for the treatment of several cancers, including breast, ovarian, and non-small-cell lung cancer. Due to its high lipophilicity, paclitaxel is difficult to administer and requires solubilization with Cremophor EL (polyethoxylated castor oil) and ethanol, which often lead to adverse side effects, including life-threatening anaphylaxis. Incorporation of paclitaxel in dimyristoylphosphatidylcholine:dimyristoylphosphatidylglycerol (DPPC:DMPG) liposomes can facilitate its delivery to cancer cells and eliminate the adverse reactions associated with the Cremophor EL vehicle. Accordingly, the effectiveness of liposomal paclitaxel on MCF-7 breast cancer cells was examined. The results from this study showed that (i) the lipid components of the liposomal formulation were nontoxic, (ii) the cytotoxic effects of liposomal paclitaxel were improved when compared with those seen with conventional paclitaxel, and (iii) the intracellular paclitaxel levels were higher in MCF-7 cells treated with the liposomal paclitaxel formulation. The results of these studies showed that delivery of paclitaxel as a liposomal formulation could be a promising strategy for enhancing its chemotherapeutic effects. PMID:21164564

  12. Interaction of dipalmitoyl phosphatidylcholine (DPPC) liposomes and insulin

    Science.gov (United States)

    Mady, Mohsen M.; Elshemey, Wael M.

    2011-06-01

    Insulin, a peptide that has been used for decades in the treatment of diabetes, has well-defined properties and delivery requirements. Liposomes, which are lipid bilayer vesicles, have gained increasing attention as drug carriers which reduce the toxicity and increase the pharmacological activity of various drugs. The molecular interaction between (uncharged lipid) dipalmitoyl phosphatidylcholine (DPPC) liposomes and insulin has been characterized by using Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction. The characteristic protein absorption band peaks, Amide I (at about 1660 cm-1) and Amide II band (at about 1546 cm-1) are potentially reduced in the liposome insulin complex. Wide-angle x-ray scattering measurements showed that the association of insulin with DPPC lipid of liposomes still maintains the characteristic DPPC diffraction peaks with almost no change in relative intensities or change in peak positions. The absence of any shift in protein peak positions after insulin being associated with DPPC liposomes indicates that insulin is successfully forming complex with DPPC liposomes with possibly no pronounced alterations in the structure of insulin molecule.

  13. Topical delivery of DNA oligonucleotide to induce p53 generation in the skin via thymidine dinucleotide (pTT-encapsulated liposomal carrier

    Directory of Open Access Journals (Sweden)

    Fang YP

    2011-12-01

    Full Text Available Yi-Ping FangDepartment of Biotechnology, Yuanpei University, Hsinchu, TaiwanIntroduction: Transcription factor p53 has a powerful tumor suppressing function that is associated with many cancers. Since the molecular weight of p53 is 53 kDa, it is difficult to transport across cell membranes. Thymidine dinucleotide (pTT is an oligonucleotide that can activate the p53 transcription factor and trigger the signal transduction cascade. However, the negative charge and high water solubility of pTT limit its transport through cellular membranes, thereby preventing it from reaching its target in the nucleus. A suitable delivery carrier for pTT is currently not available.Objective: The purpose of this study was to employ a nanoscale liposomal carrier to resolve the delivery problem, and increase the bioavailability and efficiency of pTT.Methodology: The approach was to employ liposomes to deliver pTT and then evaluate the particle size and zeta potential by laser light scattering (LLS, and permeation properties of pTT in vitro in a Franz diffusion assembly, and in vivo in a murine model using confocal laser scanning microscopy (CLSM.Results: We found that dioleoylphosphatidylethanolamine (DOPE combined with cholesterol 3 sulfate (C3S were the best ingredients to achieve an average desired vehicle size of 133.6 ± 2.8 nm, a polydispersity index (PDI, representing the distribution of particle sizes of 0.437, and a zeta potential of −93.3 ± 1.88. An in vitro penetration study showed that the liposomal carrier was superior to the free form of pTT at 2–24 hours. CLSM study observed that the penetration depth of pTT reached the upper epidermis and potential of penetration maintained up to 24 hours.Conclusion: These preliminary data demonstrate that nanosized DOPE/C3S liposomes can be exploited as a potential carrier of drugs for topical use in treating skin diseases.Keywords: thymidine dinucleotide, p53, liposome, permeation ability, confocal laser

  14. Luminescent liposome labeling technology with PKH-26 solution and absorption and distribution assessment of lipid multilammelar vesicles and small liposomes in liver following intravenous administration

    International Nuclear Information System (INIS)

    This study examined the possibility to form liposomal compositions containing PKH-26 fluorescent dye and to use those compositions in order to assess absorption and tissue distribution of the liposomes in rat liver. Liposomal compositions consisted of egg lecithin and cholesterol (Sigma) in a 7:5 ratio, respectively. The dye was incorporated into the lipid layer while preparing multilammelar vesicles with the extruder. The obtained labeled liposomal compositions allowed to quantitatively assess how the vesicles are absorbed by the liver and visualize the dye distribution in different liver cells. The study presents the data on the absorption and distribution of the dye in the liver, according to the size of the lipid vesicles, 1, 2 and 24 hours after the intravenous administration. Key words : luminescent labeling, absorption of the liposomes, visualization of the liposomes, liposomal distribution in the cells, PKH -26, liver

  15. Intrinsic and extrinsic luminescence of nanosize transition alumina powders

    International Nuclear Information System (INIS)

    Luminescence spectroscopy in the VUV-visible range under electron-beam excitation and synchrotron radiation was applied to investigate electronic properties of alumina nanopowders, which were prepared using the combustion synthesis method. By varying reaction and post treatment conditions we were able to prepare phase pure samples and powders with mixtures of α- and γ-phases mainly. In addition to the well-known 7.6 eV luminescence of STE of α-alumina, all samples possessed complex emission bands in UV range (3–5 eV) which originate from intrinsic excitonic emissions and extrinsic electronic excitations. -- Highlights: ► Luminescent spectroscopy of nanosized alumina powders was studied at 8 K. ► The crystalline structure of samples was analysed. ► Luminescent spectra, lifetimes and absorption onsets were discussed

  16. Continuous wave approach for simulating Ferromagnetic Resonance in nanosized elements

    CERN Document Server

    Wagner, K; Farle, M

    2015-01-01

    We present a numerical approach to simulate the Ferromagnetic Resonance (FMR) of micron and nanosized magnetic elements by a micromagnetic finite di?erence method. In addition to a static magnetic field a linearly polarized oscillating magnetic field is utilized to excite and analyze the spin wave excitations observed by Ferromagnetic Resonance in the space- and time-domain. Our continuous wave approach (CW) provides an alternative to the common simulation method, which uses a pulsed excitation of the magnetic system. It directly models conventional FMR-experiments and permits the determination of the real and imaginary part of the complex dynamic susceptibility without the need of post-processing. Furthermore not only the resonance fields, but also linewidths, ellipticity, phase relations and relative intensities of the excited spin wave modes in a spectrum can be determined and compared to experimental data. The magnetic responses can be plotted as a function of spatial dimensions yielding a detailed visual...

  17. Metastable nanosized aluminum powder as a reactant in energetic formulations

    Energy Technology Data Exchange (ETDEWEB)

    Katz, J. [Los Alamos National Lab., NM (United States); Tepper, F. [Argonide Corp., Sanford, FL (United States); Ivanov, G.V. [Inst. of Petroleum Chemistry, Tomsk (Russian Federation); Lerner, M.I.; Davidovich, V. [Republic Engineering Center, Tomsk (Russian Federation)

    1998-12-01

    Aluminum powder is an important ingredient in many propellant, explosives and pyrotechnic applications. The production of nanosized aluminum powder by the electroexplosion of metal wire has been practices in the former USSR since the mid 1970`s. Differential scanning calorimetry, differential thermal analysis and x-ray phase analysis was performed on aluminum powder both before and after air passivation, as well as aluminum that was protected under kerosene, pentane, toluene and hexane. Earlier Soviet reports of unexplained thermal releases and metastable behavior have been investigated. Anomalous behavior previously reported included phase transformations at temperatures far below melting with the release of heat and chemoluminescence and self sintering of particles with a heat release large enough to melt the powders.

  18. Hot isostatic pressing of nanosized WC-Co hardmetals

    International Nuclear Information System (INIS)

    A new technique based on hot isostatic pressing (HIP) has been developed to produce dense nanosized WC-Co hardmetals without the addition of grain growth inhibitors. The glass encapsulation process is the key for the effective application of isostatic pressure at temperatures well below those usually required for reaching the closed porosity state in the WC-Co system. Fully dense WC-Co samples with cobalt contents ranging from 10 to 12 wt. % have been obtained by this technique at temperatures between 1000 oC and 1200 oC with 150 MPa of applied isostatic pressure for 30 minutes. The role of isostatic pressure on the activation of densification mechanisms is discussed. (author)

  19. MONODISPERSED AND NANOSIZED DENDRIMER/POLYSTYRENE LATEX PARTICLES

    Institute of Scientific and Technical Information of China (English)

    Changfeng Yi; Zushun Xu; Warren T. Ford

    2004-01-01

    Emulsion polymerization of styrene was carried out using dendrimer DAB-dendr-(NH2)64 as seed. The size and size distribution of the emulsion particles were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS), and the effects of emulsion polymerization conditions on the preparation of emulsion particle were investigated. It has been found that the nanosized dendrimer/polystyrene polymer emulsion particles obtained were in the range of 26~64 nm in diameter, and were monodisperse; the size and size distribution of emulsion particles were influenced by the contents of dendrimer DAB-dendr-(NH2)64, emulsifier and initiator, as well as the pH value.

  20. Tissue distribution of radiolabeled phosphatidylserine-containing liposome in mice

    International Nuclear Information System (INIS)

    Liposomes are used as drug delivery systems to modify pharmacokinetic of drugs and also to improve their action in target cells. Liposomes containing phosphatidylserine are efficiently eliminated from the blood by cells of the mononuclear phagocytic system (MPS), predominantly Kupffer cells in the liver. In this way, this is a valuable approach to treat infectious diseases involving MPS, especially leishmaniasis. Leishmaniasis is a severe parasitic disease, caused by intramacrophage protozoa Leishmania sp., and is fatal if left untreated. Leishmania resides mainly in the liver and the spleen. Antileishmanial agents containing-liposomes showed more effective therapies with reduction of toxicity and adverse side effects. The purpose of this study was to investigate the tissue distribution of radioactive meglumine antimoniate encapsulated in phosphatidylserine-containing liposome. Meglumine antimoniate was neutron irradiated inside the IEA-R1 nuclear reactor to produce antimony radiotracers, 122Sb and 124Sb, and encapsulated in liposome. Healthy mice received a single intraperitoneal dose of the radiolabeled drug. Analysis of the mean radioactive tissue concentration-time data curves showed that liver and spleen had the highest levels of radioactivity. In addition these levels of drug remained for more than 48 hours. The dominant route of elimination was via biliary excretion with slow rate. Small fraction of the drug was found in the kidneys with very fast elimination. In conclusion, the phosphatidylserine-containing liposome showed to be a very useful tool to target antileishmanial agents to MPS and to sustain the drug levels for longer times. Besides, radiolabeled liposome is the easiest approach to perform biodistribution evaluation. (author)

  1. Molecular targeting of liposomal nanoparticles to tumor microenvironment

    Directory of Open Access Journals (Sweden)

    Zhao G

    2012-12-01

    Full Text Available Gang Zhao,1,2 B Leticia Rodriguez21Institute of Materia Medica, Shandong Academy of Medical Science, Shandong, China; 2Pharmaceutics Division, College of Pharmacy, The University of Texas at Austin, Austin, TX, USAAbstract: Liposomes are biodegradable and can be used to deliver drugs at a much higher concentration in tumor tissues than in normal tissues. Both passive and active drug delivery by liposomal nanoparticles can significantly reduce the toxic side effects of anticancer drugs and enhance the therapeutic efficacy of the drugs delivered. Active liposomal targeting to tumors is achieved by recognizing specific tumor receptors through tumor-specific ligands or antibodies coupled onto the surface of the liposomes, or by stimulus-sensitive drug carriers such as acid-triggered release or enzyme-triggered drug release. Tumors are often composed of tumor cells and nontumor cells, which include endothelial cells, pericytes, fibroblasts, stromal, mesenchymal cells, innate, and adaptive immune cells. These nontumor cells thus form the tumor microenvironment, which could be targeted and modified so that it is unfavorable for tumor cells to grow. In this review, we briefly summarized articles that had taken advantage of liposomal nanoparticles as a carrier to deliver anticancer drugs to the tumor microenvironment, and how they overcame obstacles such as nonspecific uptake, interaction with components in blood, and toxicity. Special attention is devoted to the liposomal targeting of anticancer drugs to the endothelium of tumor neovasculature, tumor associated macrophages, fibroblasts, and pericytes within the tumor microenvironment.Keywords: tumor microenvironment, endothelium, neovasculature, tumor-associated macrophages, cationic liposomes, ligand- or antibody-mediated targeting

  2. Tissue distribution of radiolabeled phosphatidylserine-containing liposome in mice

    Energy Technology Data Exchange (ETDEWEB)

    Borborema, Samanta E.T.; Nascimento, Nanci do [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Biotecnologia], e-mail: samanta@usp.br, e-mail: nnascime@ipen.br; Andrade Junior, Heitor F. de [Instituto de Medicina Tropical de Sao Paulo (IMTSP), Sao Paulo, SP (Brazil)], e-mail: hfandrad@usp.br; Osso Junior, Joao A. [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Radiofarmacia], e-mail: jaosso@ipen.br

    2009-07-01

    Liposomes are used as drug delivery systems to modify pharmacokinetic of drugs and also to improve their action in target cells. Liposomes containing phosphatidylserine are efficiently eliminated from the blood by cells of the mononuclear phagocytic system (MPS), predominantly Kupffer cells in the liver. In this way, this is a valuable approach to treat infectious diseases involving MPS, especially leishmaniasis. Leishmaniasis is a severe parasitic disease, caused by intramacrophage protozoa Leishmania sp., and is fatal if left untreated. Leishmania resides mainly in the liver and the spleen. Antileishmanial agents containing-liposomes showed more effective therapies with reduction of toxicity and adverse side effects. The purpose of this study was to investigate the tissue distribution of radioactive meglumine antimoniate encapsulated in phosphatidylserine-containing liposome. Meglumine antimoniate was neutron irradiated inside the IEA-R1 nuclear reactor to produce antimony radiotracers, {sup 122}Sb and {sup 124}Sb, and encapsulated in liposome. Healthy mice received a single intraperitoneal dose of the radiolabeled drug. Analysis of the mean radioactive tissue concentration-time data curves showed that liver and spleen had the highest levels of radioactivity. In addition these levels of drug remained for more than 48 hours. The dominant route of elimination was via biliary excretion with slow rate. Small fraction of the drug was found in the kidneys with very fast elimination. In conclusion, the phosphatidylserine-containing liposome showed to be a very useful tool to target antileishmanial agents to MPS and to sustain the drug levels for longer times. Besides, radiolabeled liposome is the easiest approach to perform biodistribution evaluation. (author)

  3. Probing mechanical properties of liposomes using acoustic sensors.

    Science.gov (United States)

    Melzak, Kathryn A; Bender, Florian; Tsortos, Achilleas; Gizeli, Electra

    2008-08-19

    Acoustic devices were employed to characterize variations in the mechanical properties (density and viscoelasticity) of liposomes composed of 1-oleoyl-2-palmitoyl- sn-glycero-3-phosphocholine (POPC) and cholesterol. Liposome properties were modified in three ways. In some experiments, the POPC/cholesterol ratio was varied prior to deposition on the device surface. Alternatively, the ratio was changed in situ via either insertion of cholesterol or removal of cholesterol with beta-cyclodextrin. This was done for liposomes adsorbed directly on the device surface and for liposomes attached via a biotin-terminated poly(ethylene glycol) linker. The acoustic measurements make use of two simultaneous time-resolved signals: one signal is related to the velocity of the acoustic wave, while the second is related to dissipation of acoustic energy. Together, they provide information not only about the mass (or density) of the probed medium but also about its viscoelastic properties. The cholesterol-induced increase in the surface density of the lipid bilayer was indeed observed in the acoustic data, but the resulting change in signal was larger than expected from the change in surface density. In addition, increasing the bilayer resistance to stretching was found to lead to a greater dissipation of the acoustic energy. The acoustic response is assessed in terms of the possible distortions of the liposomes and the known effects of cholesterol on the mechanical properties of the lipid bilayer that encloses the aqueous core of the liposome. To aid the interpretation of the acoustic response, it is discussed how the above changes in the lipid bilayer will affect the effective viscoelastic properties of the entire liposome/solvent film on the scale of the acoustic wavelength. It was found that the acoustic device is very sensitive to the mechanical properties of lipid vesicles; the response of the acoustic device is explained, and the basic underlying mechanisms of interaction are

  4. Peptide-Coated Liposomal Fasudil Enhances Site Specific Vasodilation in Pulmonary Arterial Hypertension

    OpenAIRE

    Nahar, Kamrun; Absar, Shahriar; Gupta, Nilesh; Kotamraju, Venkata Ramana; McMurtry, Ivan F.; Oka, Masahiko; Komatsu, Masanobu; Nozik-Grayck, Eva; Ahsan, Fakhrul

    2014-01-01

    This study sought to develop a liposomal delivery system of fasudil—an investigational drug for the treatment of pulmonary arterial hypertension (PAH)—that will preferentially accumulate in the PAH lungs. Liposomal fasudil was prepared by film-hydration method, and the drug was encapsulated by active loading. The liposome surface was coated with a targeting moiety, CARSKNKDC, a cyclic peptide; the liposomes were characterized for size, polydispersity index, zeta potential, and storage and neb...

  5. Size-Induced Enhancement of Chemical Exchange Saturation Transfer (CEST) Contrast in Liposomes

    OpenAIRE

    Zhao, Jason M.; Har-el, Yah-el; McMahon, Michael T.; Zhou, Jinyuan; Sherry, A. Dean; Sgouros, George; Bulte, Jeff W. M.; van Zijl, Peter C.M.

    2008-01-01

    Liposome-based chemical exchange saturation transfer (lipoCEST) agents have shown great sensitivity and potential for molecular magnetic resonance imaging (MRI). Here we demonstrate that the size of liposomes can be exploited to enhance the lipoCEST contrast. A concise analytical model is developed to describe the contrast dependence on size for an ensemble of liposomes. The model attributes the increased lipoCEST contrast in smaller liposomes to their larger surface-to-volume ratio, causing ...

  6. Nano- or Submicron-Sized Liposomes as Carriers for Drug Delivery

    OpenAIRE

    Jia-You Fang

    2006-01-01

    Liposomes are tiny spheres ranging in diameters from 50 nm to several microns. Thescope of this mini review is to introduce the concept of liposomes and to describe someaspects and mechanisms of stimulating topical and injectable products with liposomes. Twoexamples discussed in this article are topical delivery across skin and injectable formulationsfor anticancer drugs. Classic liposomes are of little value as carriers for drug delivery via theskin because they do not penetrate it deeply. O...

  7. Interaction of Colistin and Colistin Methanesulfonate with Liposomes: Colloidal Aspects and Implications for Formulation

    OpenAIRE

    WALLACE, STEPHANIE J.; Jian LI; Nation, Roger L; Prankerd, Richard J.; Boyd, Ben J.

    2012-01-01

    Interaction of colistin and colistin methanesulfonate (CMS) with liposomes has been studied with the view to understanding the limitations to the use of liposomes as a more effective delivery system for pulmonary inhalation of this important class of antibiotic. Thus, in this study, liposomes containing colistin or CMS were prepared and characterized with respect to colloidal behavior and drug encapsulation and release. Association of anionic CMS with liposomes induced negative charge on the ...

  8. Oxidative stability of Liposomes composed of docosahexaenoic acid-containing phospholipids

    DEFF Research Database (Denmark)

    Vikbjerg, Anders Falk; Andresen, Thomas Lars; Jørgensen, Kent;

    2007-01-01

    Oxidative stability of liposomes made of (Docosahexaenoic acid) DHA-containing phosphatidylcholine (PC) was examined during preparation and storage. After preparation of the liposomes, the concentration of primary (conjugated dienes) and secondary oxidation products (Thiobarbituric acid-reactive ......Oxidative stability of liposomes made of (Docosahexaenoic acid) DHA-containing phosphatidylcholine (PC) was examined during preparation and storage. After preparation of the liposomes, the concentration of primary (conjugated dienes) and secondary oxidation products (Thiobarbituric acid...

  9. The Immunological Enhancement Activity of Propolis Flavonoids Liposome In Vitro and In Vivo

    OpenAIRE

    Yang Tao; Deqing Wang; Yuanliang Hu; Yee Huang; Yun Yu; Deyun Wang

    2014-01-01

    The aim of this study was to investigate and assess the effects of propolis flavonoids liposome imposed on the immune system by comparing it to propolis flavonoids and blank liposome. In vitro, the effects of the above drugs on macrophages were assessed by measuring the phagocytic function and cytokine production. In vivo, the immunological adjuvant activity of propolis flavonoids liposome was compared with those of propolis flavonoids and blank liposome. The results showed that in vitro prop...

  10. In vivo and in vitro evaluation of octyl methoxycinnamate liposomes

    Directory of Open Access Journals (Sweden)

    de Carvalho Varjão Mota A

    2013-12-01

    Full Text Available Aline de Carvalho Varjão Mota,1 Zaida Maria Faria de Freitas,1 Eduardo Ricci Júnior,1 Gisela Maria Dellamora-Ortiz,1 Ralph Santos-Oliveira,2 Rafael Antonio Ozzetti,3 André Luiz Vergnanini,3 Vanessa Lira Ribeiro,4 Ronald Santos Silva,4 Elisabete Pereira dos Santos11Faculty of Pharmacy, Federal University of Rio de Janeiro, 2Nuclear Engineering Institute, National Nuclear Energy Commission, 3Allergisa Dermatocosmetic Research, University of Campinas, São Paulo, 4Pharmacology and Toxicology Department, National Insitute of Quality Control in Health, Oswaldo Cruz Foundation, Rio de Janeiro, BrazilAbstract: Solar radiation causes damage to human skin, and photoprotection is the main way to prevent these harmful effects. The development of sunscreen formulations containing nanosystems is of great interest in the pharmaceutical and cosmetic industries because of the many potential benefits. This study aimed to develop and evaluate an octyl methoxycinnamate (OMC liposomal nanosystem (liposome/OMC to obtain a sunscreen formulation with improved safety and efficacy by retaining OMC for longer on the stratum corneum.Methods: The liposome/OMC nanostructure obtained was tested for enzymatic hydrolysis with lipase from Rhizomucor miehei and biodistribution with liposomes labeled with technetium-99m. The liposome/OMC formulation was then incorporated in a gel formulation and tested for ocular irritation using the hen’s egg test-chorio-allantoic membrane (HET-CAM assay, in vitro and in vivo sun protection factor, in vitro release profile, skin biometrics, and in vivo tape stripping.Results: The liposome/OMC nanosystem was not hydrolyzed from R. miehei by lipase. In the biodistribution assay, the liposome/OMC formulation labeled with technetium-99m had mainly deposited in the skin, while for OMC the main organ was the liver, showing that the liposome had higher affinity for the skin than OMC. The liposome/OMC formulation was classified as nonirritating in

  11. Exploring the fate of liposomes in the intestine by dynamic in vitro lipolysis

    DEFF Research Database (Denmark)

    Parmentier, Johannes; Thomas, Nicky; Müllertz, Anette;

    2012-01-01

    Liposomes are generally well tolerated drug delivery systems with a potential use for the oral route. However, little is known about the fate of liposomes during exposure to the conditions in the gastro-intestinal tract (GIT). To gain a better understanding of liposome stability in the intestine, a...

  12. Albumin coated liposomes: a novel platform for macrophage specific drug delivery

    Directory of Open Access Journals (Sweden)

    Clément Vuarchey

    2011-07-01

    Full Text Available Here we report a new and efficient approach of macrophage specific drug delivery by coating liposomes with albumin. Activated albumin was reacted with liposomes containing polyethylene glycol (PEG as hydrophilic spacers to create a flexible layer of covalently bound albumin molecules on the liposome surface. Albumin coated liposomes were taken up faster and more efficiently than uncoated liposomes by murine macrophages. Liposome uptake was significantly higher in macropha - ges as compared to other cell types tested (endothelial cells, fibroblasts, tumor cells, suggesting specificity for macrophages. In vivo, splenic macrophages phagocytosed BSA coated liposomes (BSA-L at faster rates compared to conventional liposomes (L and PEG liposomes (PEG-L. To prove the effectiveness of this new macrophage specific drug carrier, the bisphosphonates clodronate and zoledronate were encapsulated in BSA-L and compared with conventional liposomes. In vitro, treatment of macrophages with clodronate or zoledronate in BSA-L led to cytotoxic activity within a very short time and to up to 50-fold reduced IC50 concentrations. In vivo, clodronate encapsulated in BSA-L depleted splenic macrophages at a 5-fold lower concentration as conventional clodronate-liposomes. Our results highlight the pharmaceutical benefits of albumin-coated liposomes for macrophage specific drug delivery.

  13. Nebulization of ultradeformable liposomes: the influence of aerosolization mechanism and formulation excipients.

    Science.gov (United States)

    Elhissi, Abdelbary M A; Giebultowicz, Joanna; Stec, Anna A; Wroczynski, Piotr; Ahmed, Waqar; Alhnan, Mohamed Albed; Phoenix, David; Taylor, Kevin M G

    2012-10-15

    Ultradeformable liposomes are stress-responsive phospholipid vesicles that have been investigated extensively in transdermal delivery. In this study, the suitability of ultradeformable liposomes for pulmonary delivery was investigated. Aerosols of ultradeformable liposomes were generated using air-jet, ultrasonic or vibrating-mesh nebulizers and their stability during aerosol generation was evaluated using salbutamol sulphate as a model hydrophilic drug. Although delivery of ultradeformable liposome aerosols in high fine particle fraction was achievable, the vesicles were very unstable to nebulization so that up to 98% drug losses were demonstrated. Conventional liposomes were relatively less unstable to nebulization. Moreover, ultradeformable liposomes tended to aggregate during nebulization whilst conventional vesicles demonstrated a "size fractionation" behaviour, with smaller liposomes delivered to the lower stage of the impinger and larger vesicles to the upper stage. A release study conducted for 2 h showed that ultradeformable liposomes retained only 30% of the originally entrapped drug, which was increased to 53% by inclusion of cholesterol within the formulations. By contrast, conventional liposomes retained 60-70% of the originally entrapped drug. The differences between ultradeformable liposomes and liposomes were attributed to the presence of ethanol or Tween 80 within the elastic vesicle formulations. Overall, this study demonstrated, contrary to our expectation, that materials included with the aim of making the liposomes more elastic and ultradeformable to enhance delivery from nebulizers were in fact responsible for vesicle instability during nebulization and high leakage rates of the drug. PMID:22796173

  14. Light- and temperature-responsive liposomes incorporating cinnamoyl Pluronic F127.

    Science.gov (United States)

    Wang, MinHui; Kim, Jin-Chul

    2014-07-01

    Light- and temperature-responsive liposomes were prepared by immobilizing cinnamoyl Pluronic F127 (CP F127) on the surface of egg phosphatidylcholine liposomes. CP F127 was prepared by a condensation reaction, and the molar ratio of cinnamoyl group to Pluronic F127 was calculated to be 1:1.4 on (1)H NMR spectrum. The cinnamoyl group of CP F127 was readily dimerized under the irradiation of a UV light (254 nm, 6 W). CP F127 decreased the absolute value of the zeta potential of liposome possibly because it can shift the hydrodynamic plane away from the liposome surface. The size of liposome decorated with CP F127, measured on a dynamic light scattering machine and observed on a TEM, was larger than that of bare liposome. The liposome bearing CP F127 seemed to fuse and aggregate each other. The liposome released calcein, a fluorescence dye, in response to a UV irradiation, possibly because the photo-dimerization of cinnamoyl group perturbs the liposomal membrane. Moreover, the liposome released the dye in response to a temperature change, possible due to the phase transition of Pluronic F127 layer on the liposomal surface or the hydrophobic interaction of the polymer with liposomal membrane. PMID:24709213

  15. Prednisolone-containing liposomes accumulate in human atherosclerotic macrophages upon intravenous administration

    NARCIS (Netherlands)

    Valk, van der Fleur M.; Wijk, van Diederik F.; Lobatto, Mark E.; Verberne, Hein J.; Storm, Gert; Willems, Martine C.M.; Legemate, Dink A.; Nederveen, Aart J.; Calcagno, Claudia; Mani, Venkatesh; Ramachandran, Sarayu; Paridaans, Maarten P.M.; Otten, Maarten J.; Dallinga-Thie, Geesje M.; Fayad, Zahi A.; Nieuwdorp, Max; Schulte, Dominik M.; Metselaar, Josbert M.; Mulder, Willem J.M.; Stroes, Erik S.G.

    2015-01-01

    Drug delivery to atherosclerotic plaques via liposomal nanoparticles may improve therapeutic agents’ risk–benefit ratios. Our paper details the first clinical studies of a liposomal nanoparticle encapsulating prednisolone (LN-PLP) in atherosclerosis. First, PLP’s liposomal encapsulation improved its

  16. Targeted Liposomal Drug Delivery to Monocytes and Macrophages

    Directory of Open Access Journals (Sweden)

    Ciara Kelly

    2011-01-01

    Full Text Available As the role of monocytes and macrophages in a range of diseases is better understood, strategies to target these cell types are of growing importance both scientifically and therapeutically. As particulate carriers, liposomes naturally target cells of the mononuclear phagocytic system (MPS, particularly macrophages. Loading drugs into liposomes can therefore offer an efficient means of drug targeting to MPS cells. Physicochemical properties including size, charge and lipid composition can have a very significant effect on the efficiency with which liposomes target MPS cells. MPS cells express a range of receptors including scavenger receptors, integrins, mannose receptors and Fc-receptors that can be targeted by the addition of ligands to liposome surfaces. These ligands include peptides, antibodies and lectins and have the advantages of increasing target specificity and avoiding the need for cationic lipids to trigger intracellular delivery. The goal for targeting monocytes/macrophages using liposomes includes not only drug delivery but also potentially a role in cell ablation and cell activation for the treatment of conditions including cancer, atherosclerosis, HIV, and chronic inflammation.

  17. Liposomes self-assembled from electrosprayed composite microparticles

    International Nuclear Information System (INIS)

    Composite microparticles, consisting of polyvinylpyrrolidone (PVP), naproxen (NAP) and lecithin (PC), have been successfully prepared using an electrospraying process and exploited as templates to manipulate molecular self-assembly for the synthesis of liposomes in situ. Field emission scanning electron microscope (FESEM) and transmission electron microscope (TEM) observations demonstrate that the microparticles have an average diameter of 960 ± 140 nm and a homogeneous structure. X-ray diffraction (XRD) patterns, differential scanning calorimetry (DSC) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) results verify that the building blocks NAP and PC are scattered in the polymer matrix in a molecular way owing to the very fast drying of the electrospraying process and the favorable secondary interactions among the components. FESEM, scanning probe microscope (SPM) and TEM observations demonstrate that the liposomes can be achieved through molecular self-assembly in situ when the microparticles contact water thanks to ‘like prefers like’ and by means of the confinement effect of the microparticles. The liposomes have an encapsulation rate of 91.3%, and 80.7% of the drug in the liposomes can be freed into the dissolution medium in a sustained way and by a diffusion mechanism over a period of 24 h. The developed strategy not only provides a new, facile, and effective method to assemble and organize molecules of multiple components into liposomes with electrosprayed microparticles as templates, but also opens a new avenue for nanofabrication in a step-by-step and controllable way. (paper)

  18. Crosslinked multilamellar liposomes for controlled delivery of anticancer drugs.

    Science.gov (United States)

    Joo, Kye-Il; Xiao, Liang; Liu, Shuanglong; Liu, Yarong; Lee, Chi-Lin; Conti, Peter S; Wong, Michael K; Li, Zibo; Wang, Pin

    2013-04-01

    Liposomes constitute one of the most popular nanocarriers for the delivery of cancer therapeutics. However, since their potency is limited by incomplete drug release and inherent instability in the presence of serum components, their poor delivery occurs in certain circumstances. In this study, we address these shortcomings and demonstrate an alternative liposomal formulation, termed crosslinked multilamellar liposome (CML). With its properties of improved sustainable drug release kinetics and enhanced vesicle stability, CML can achieve controlled delivery of cancer therapeutics. CML stably encapsulated the anticancer drug doxorubicin (Dox) in the vesicle and exhibited a remarkably controlled rate of release compared to that of the unilamellar liposome (UL) with the same lipid composition or Doxil-like liposome (DLL). Our imaging study demonstrated that the CMLs were mainly internalized through a caveolin-dependent pathway and were further trafficked through the endosome-lysosome compartments. Furthermore, in vivo experiments showed that the CML-Dox formulation reduced systemic toxicity and significantly improved therapeutic activity in inhibiting tumor growth compared to that of UL-Dox or DLL-Dox. This drug packaging technology may therefore provide a new treatment option to better manage cancer and other diseases. PMID:23375392

  19. Application of Liposomes in Treatment of Rheumatoid Arthritis: Quo Vadis

    Directory of Open Access Journals (Sweden)

    Bhupinder Kapoor

    2014-01-01

    Full Text Available The most common treatments for rheumatoid arthritis include nonsteroidal anti-inflammatory drugs (NSAIDs, corticosteroids, disease modifying antirheumatic drugs (DMARDs, and some biological agents. However, none of the treatments available is able to achieve the ultimate goal of treatment, that is, drug-free remission. This limitation has shifted the focus of treatment to delivery strategies with an ability to deliver the drugs into the synovial cavity in the proper dosage while mitigating side effects to other tissues. A number of approaches like microemulsions, microspheres, liposomes, microballoons, cocrystals, nanoemulsions, dendrimers, microsponges, and so forth, have been used for intrasynovial delivery of these drugs. Amongst these, liposomes have proven to be very effective for retaining the drug in the synovial cavity by virtue of their size and chemical composition. The fast clearance of intra-synovially administered drugs can be overcome by use of liposomes leading to increased uptake of drugs by the target synovial cells, which in turn reduces the exposure of nontarget sites and eliminates most of the undesirable effects associated with therapy. This review focuses on the use of liposomes in treatment of rheumatoid arthritis and summarizes data relating to the liposome formulations of various drugs. It also discusses emerging trends of this promising technology.

  20. Application of liposomes in treatment of rheumatoid arthritis: quo vadis.

    Science.gov (United States)

    Kapoor, Bhupinder; Singh, Sachin Kumar; Gulati, Monica; Gupta, Reena; Vaidya, Yogyata

    2014-01-01

    The most common treatments for rheumatoid arthritis include nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, disease modifying antirheumatic drugs (DMARDs), and some biological agents. However, none of the treatments available is able to achieve the ultimate goal of treatment, that is, drug-free remission. This limitation has shifted the focus of treatment to delivery strategies with an ability to deliver the drugs into the synovial cavity in the proper dosage while mitigating side effects to other tissues. A number of approaches like microemulsions, microspheres, liposomes, microballoons, cocrystals, nanoemulsions, dendrimers, microsponges, and so forth, have been used for intrasynovial delivery of these drugs. Amongst these, liposomes have proven to be very effective for retaining the drug in the synovial cavity by virtue of their size and chemical composition. The fast clearance of intra-synovially administered drugs can be overcome by use of liposomes leading to increased uptake of drugs by the target synovial cells, which in turn reduces the exposure of nontarget sites and eliminates most of the undesirable effects associated with therapy. This review focuses on the use of liposomes in treatment of rheumatoid arthritis and summarizes data relating to the liposome formulations of various drugs. It also discusses emerging trends of this promising technology. PMID:24688450

  1. Dextran sulfate-dependent fusion of liposomes containing cationic stearylamine.

    Science.gov (United States)

    Zschörnig, O; Arnold, K; Richter, W; Ohki, S

    1992-11-01

    The incorporation of the positively charged stearylamine into phosphatidylcholine liposomes was studied by measuring electrophoretic mobilities. Up to a molar ratio SA/PC = 0.5 an increase of the positive zeta potential can be observed. Addition of the negatively charged macromolecule dextran sulfate leads to a change of the sign of the surface potential of the PC/SA liposomes indicating binding of the macromolecule to the surface. This process is accompanied by an increase in turbidity, which is dependent on the molecular weight of the dextran sulfate and the SA concentration (measured by turbidimetry). Using the NBD/Rh and Pyr-PC fluorescence assays the fusion of SA containing liposomes was investigated. A strong influence of the SA content and molecular weight of dextran sulfate on the fusion extent was observed. The fusion extent is proportional to the SA content in the PC membrane and the molecular weight of dextran sulfate. PC/SA/PE liposomes exhibit a higher fusion extent after addition of dextran sulfate compared to PC/SA liposomes indicating that PE additionally destabilizes the bilayer. Freeze-fracture electron microscopy reveals that the reaction products are large complexes composed of multilamellar stacks of tightly packed, straight membranes and aggregated vesicles. The tight packing of the membranes in the stacks (and the narrow contact of the aggregated vesicles) indicates a strong adherence of opposite membrane surfaces induced by dextran sulfate. PMID:1486657

  2. Assembly of liposomes controlled by triple helix formation.

    Science.gov (United States)

    Jakobsen, Ulla; Vogel, Stefan

    2013-09-18

    Attachment of DNA to the surface of different solid nanoparticles (e.g., gold and silica nanoparticles) is well established, and a number of DNA-modified solid nanoparticle systems have been applied to thermal denaturation analysis of oligonucleotides. We report herein the noncovalent immobilization of oligonucleotides on the surface of soft nanoparticles (i.e., liposomes) and the subsequent controlled assembly by DNA triple helix formation. The noncovalent approach avoids tedious surface chemistry and necessary purification procedures and can simplify and extend the available methodology for the otherwise difficult thermal denaturation analysis of complex triple helical DNA assemblies. The approach is based on lipid modified triplex forming oligonucleotides (TFOs) which control the assembly of liposomes in solution in the presence of single- or double-stranded DNA targets. The thermal denaturation analysis is monitored by ultraviolet spectroscopy at submicromolar concentrations and compared to regular thermal denaturation assays in the absence of liposomes. We report on triplex forming oligonucleotides (TFOs) based on DNA and locked nucleic acid (LNA)/DNA hybrid building blocks and different target sequences (G or C-rich) to explore the applicability of the method for different triple helical assembly modes. We demonstrate advantages and limitations of the approach and show the reversible and reproducible formation of liposome aggregates during thermal denaturation cycles. Nanoparticle tracking analysis (NTA) and dynamic light scattering (DLS) show independently from ultraviolet spectroscopy experiments the formation of liposome aggregates. PMID:23885785

  3. Composition Influence on Pulmonary Delivery of Rifampicin Liposomes

    Directory of Open Access Journals (Sweden)

    Maria Letizia Manca

    2012-11-01

    Full Text Available The effects of lipid concentration and composition on the physicochemical properties, aerosol performance and in vitro toxicity activity of several rifampicin-loaded liposomes were investigated. To this purpose, six liposome formulations containing different amounts of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine, with and without cholesterol and oleic acid, were prepared and fully characterized. Uni- or oligo-lamellar, small (~100 nm, negatively charged (~60 mV vesicles were obtained. Lipid composition affected aerosol delivery features of liposomal rifampicin; in particular, the highest phospholipid concentration led to a better packing of the vesicular bilayers with a consequent higher nebulization stability. The retention of drug in nebulized vesicles (NER% was higher for oleic acid containing vesicles (55% ± 1.4% than for the other samples (~47%. A549 cells were used to evaluate intracellular drug uptake and in vitro toxicity activity of rifampicin-loaded liposomes in comparison with the free drug. Cell toxicity was more evident when oleic acid containing liposomes were used.

  4. CELECOXIB LOADED LIPOSOMES: DEVELOPMENT, CHARACTERIZATION AND IN VITRO EVALUATION

    Directory of Open Access Journals (Sweden)

    M. Yasmin Begum

    2012-01-01

    Full Text Available CLX (celecoxib is a highly hydrophobic non-steroidal anti-inflammatory drug with high plasma protein binding. We describe here the encapsulation of CLX in MLVs composed of SPC and variable amounts of cholesterol. The influence of drug – lipid ratio was studied and amount of the drug could be encapsulated was optimized. The effect of cholesterol and other process parameters were studied to obtain the liposomal vesicles with desired quality. All the prepared formulations were characterized for their physico chemical properties such as appearance, vesicle size, vesicle size distribution and percentage drug entrapment. Stability of the liposomes in terms of their drug leakage and drug retention behaviour was studied by storing the liposomal formulations under different conditions for the period of 30 days. The optimized formulation parameters and process parameters resulted the liposomes with mean vesicle diameter of 4.81μ. The maximum percentage drug entrapment was achieved with the formulation CL3 which contains the drug – lipid ratio of 1:10%W/W and the percentage drug entrapment is equal to 72.33±0.64 (%. In vitro release data showed that release profile follows zero order kinetics. Celecoxib liposomes with good stability and appreciable controlled drug release with good retention of the drug even after 24 hours were prepared successfully.

  5. Hemoglobin-mediated oxidation of marine liposomes

    OpenAIRE

    Škrabalová, Lada

    2012-01-01

    Cílem této práce bylo studium mechanismu oxidace lipidů katalyzované hovězím methemoglobinem a zhodnocení účinků různých experimentálních podmínek a antioxidantů (EDTA, askorbová kyselina, kávová kyselina, a-tokoferol, d-tokoferol, astaxanthin a L-askorbyl-6-palmitát) na methemoglobinem zprostředkovanou oxidaci lipidů v modelovém systému liposomů připravených z fosfolipidů. K monitorování oxidace lipidů při pH 5,5 a teplotě 30 °C bylo použito spotřeby kyslíku. Pro zhodnocení antioxidační akti...

  6. Preparation and Characterization of a Collagen-Liposome-Chondroitin Sulfate Matrix with Potential Application for Inflammatory Disorders Treatment

    Directory of Open Access Journals (Sweden)

    Oana Craciunescu

    2014-01-01

    Full Text Available Smart drug delivery systems with controllable properties play an important role in targeted therapy and tissue regeneration. The aim of our study was the preparation and in vitro evaluation of a collagen (Col matrix embedding a liposomal formulation of chondroitin sulfate (L-CS for the treatment of inflammatory disorders. Structural studies using Oil Red O specific staining for lipids and scanning electron microscopy showed an alveolar network of nanosized Col fibrils decorated with deposits of L-CS at both periphery and inner of the matrix. The porosity and density of Col-L-CS matrix were similar to those of Col matrix, while its mean pore size and biodegradability had significantly higher and lower values (P<0.05, respectively. In vitro cytotoxicity assays showed that the matrix system induced high cell viability and stimulated cell metabolism in L929 fibroblast cell culture. Light and electron micrographs of the cell-matrix construct showed that cells clustered into the porous structure at 72 h of cultivation. In vitro diffusion test indicated that the quantity of released CS was significantly lower (P<0.05 after embedment of L-CS within Col matrix. All these results indicated that the biocompatible and biodegradable Col-L-CS matrix might be a promising delivery system for local treatment of inflamed site.

  7. Study of surface cell Madelung constant and surface free energy of nanosized crystal grain

    Institute of Scientific and Technical Information of China (English)

    Zhang Wei-Jia; Wang Tian-Min; Rong Ai-Lun; Cui Min

    2006-01-01

    Surface cell Madelung constant is firstly defined for calculating the surface free energy of nanosized crystal grains,which explains the physical performance of small crystals and may be greatly beneficial to the analysis of surface states and the study of the dynamics of crystal nucleation and growth.A new approximative expression of the surface energy and relevant thermodynamic data are used in this calculation.New formula and computing method for calculating the Madelung constant α of any complex crystals are proposed,and the surface free energies and surface electrostatic energies of nanosized crystal grains and the Madelung constant of some complex crystals are theoretically calculated in this paper.The surface free energy of nanosized-crystal-grain TiO2 and the surface electrostatic energy (absolute value) of nanosized-crystal-grain α-A12O3 are found to be the biggest among all the crystal grains including those of other species.

  8. Liposomal delivery of radionuclides for cancer diagnostics and radiotherapy

    DEFF Research Database (Denmark)

    Petersen, Anncatrine Luisa

    loading experiments and isothermal titration calorimetry (ITC) measurements. Various chelators, ionophores and lipophilic chelators were tested at different pH and temperature conditions. Liposomes passively accumulate in tumors due to the enhanced permeability and retention (EPR) effect. In Article I...... of PEGylated 64Cu-liposomes with and without TATE, and their ability to image NE tumors in tumor-bearing mice using PET. Further, we compare the liposome tumor accumulation and imaging capability with that of the radiolabeled somatostatin analog 64Cu-DOTA-TATE. During the past 30 years, ionophores......, a so called “unassisted” loading, excluding any use of ionophores and lipophilic chelators. Project IV presents results from this invention (Patent II), where a presentation of various parameters affecting the efficiency of the unassisted loading method is given. Section 5 summarizes the regulatory...

  9. [A pharmacokinetic study of subconjunctival polyphase liposome 5-fluorouracil].

    Science.gov (United States)

    Ke, X F; Wei, H R; Yang, J X

    1994-03-01

    5-Fu polyphase liposome was prepared by fusing the drug with lecithin and cholesterol, the rate of encapsulation being 52%, and 97% of the particles were less than 2 microns in diameter and stable against heat and cold. 5 mg of tritiated 5-Fu in 0.5 ml of the polyphase liposome preparation was injected subconjunctivally in rabbits. The concentrations of 5-Fu in the conjunctiva, the sclera, and the conjunctiva-Tenen's capsule-sclera en bloc 180 degrees from the site of injection were measured by the scintillation method 12, 24, 48, 72 and 96 hours after injection to be no less than 0.2 microgram, the ID50 of fibroblast proliferation. These findings suggested that 5-Fu polyphase liposome preparation might be substituted for 5-Fu solution in the filtering operation to reduce the frequency of injections and to attenuate the side effects. PMID:8001446

  10. Biodistribution of liposomes after extradural administration in rodents.

    Science.gov (United States)

    Umbrain, V; Alafandy, M; Bourgeois, P; D'Haese, J; Boogaerts, J G; Goffinet, G; Camu, F; Legros, F J

    1995-09-01

    We have mapped over 24 h the biodistribution of 99mTc-labelled multilamellar and small unilamellar liposomes in rabbits and rats by scintigraphic imaging after extradural injection. Multilamellar vesicles formed a depot at the site of injection; small unilamellar vesicles spread immediately along the extradural space and entered the systemic compartment 30 min after injection. Well-delineated liver and kidney labellings were seen after 24 h. The use of 3H-cholesterol-labelled small unilamellar vesicles suggested hepatic capture of intact liposomes with sizes averaging 0.05 microns drained unmodified into the systemic circulation through the extradural lymphatics. These results have led to the selection of multilamellar vesicles (0.1-15 microns size range) for clinical trials using liposome-associated local anaesthetics. PMID:7547050

  11. Design and evaluation of liposomal formulation of pilocarpine nitrate

    Directory of Open Access Journals (Sweden)

    Rathod S

    2010-01-01

    Full Text Available Prolonged release drug delivery system of pilocarpine nitrate was made by optimizing thin layer film hydration method. Egg phosphatidylcholine and cholesterol were used to make multilamellar vesicles. Effects of charges over the vesicles were studied by incorporating dicetylphosphate and stearylamine. Various factors, which may affect the size, shape, encapsulation efficiency and release rate, were studied. Liposomes in the size range 0.2 to 1 ΅m were obtained by optimizing the process. Encapsulation efficiency of neutral, positive and negatively charged liposomes were found to be 32.5, 35.4 and 34.2 percent, respectively. In vitro drug release rate was studied on specially designed model. Biological response in terms of reduction in intraocular pressure was observed on rabbit eyes. Pilocarpine nitrate liposomes were lyophilized and stability studies were conducted.

  12. Novel methods for the encapsulation of meglumine antimoniate into liposomes

    Directory of Open Access Journals (Sweden)

    F. Frézard

    2000-07-01

    Full Text Available The antimonial drug, meglumine antimoniate, was successfully encapsulated in dehydration-rehydration vesicles and in freeze-dried empty liposomes (FDELs. High encapsulation efficiencies (from 28 to 58% and low weight ratios of lipids to encapsulated antimony (from 1:0.15 to 1:0.3 were achieved. These formulations, contrary to those obtained by conventional methods, can be stored as intermediate lyophilized forms and reconstituted just before use. The efficacy of FDEL-encapsulated meglumine antimoniate was evaluated in hamsters experimentally infected with Leishmania chagasi. A significant reduction of liver parasite burdens was observed in animals treated with this preparation, when compared to control animals treated with empty liposomes. In contrast, free meglumine antimoniate was found to be inefficient when administered at a comparable dose of antimony. This novel liposome-based meglumine antimoniate formulation appears to be promising as a pharmaceutical product for the treatment of visceral leishmaniasis.

  13. Studies on molecular interactions between puerarin and PC liposomes

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Fluorescence emission spectra, FTIR spectra, zeta potential measurements, and ab initio quantum calculation are used to study the interaction between puerarin and membranes composed of egg phosphatidylcholine (PC) liposome. The hydrophobic interactions cause the puerarin molecule to partition into lipid bilayers with its B-ring, and favor the displacement of acid-base equilibrium of puerarin towards the base form. Due to the hydrogen bond formation between the puerarin hydroxyl groups and polar groups of PC molecules on the water/membrane interface, puerarin can easily intercalate into the organized structure of phospholipids and modulate the membrane function. Our results reveal that the liposome membrane integrity is significantly higher compared with that of empty liposome.

  14. Lipophilic drug transfer between liposomal and biological membranes

    DEFF Research Database (Denmark)

    Fahr, Alfred; van Hoogevest, Peter; Kuntsche, Judith;

    2006-01-01

    is described as solubility of a drug in phospholipid membranes and the kinetics of transfer of a lipophilic drug between membranes. Finally, the consequences of these two factors on the design of lipid-based carriers for oral, as well as parenteral use, for lipophilic drugs and lead selection of oral......This review presents the current knowledge on the interaction of lipophilic, poorly water soluble drugs with liposomal and biological membranes. The center of attention will be on drugs having the potential to dissolve in a lipid membrane without perturbing them too much. The degree of interaction...... lipophilic drugs is described. Since liposomes serve as model-membranes for natural membranes, the assessment of lipid solubility and transfer kinetics of lipophilic drug using liposome formulations may additionally have predictive value for bioavailability and biodistribution and the pharmacokinetics of...

  15. Ultraviolet- and sunlight-induced lipid peroxidation in liposomal membrane

    International Nuclear Information System (INIS)

    Ultraviolet radiation and sunlight caused lipid peroxidation in the liposomal membrane (as detected by measurement of the oxidation index, A233/A215, and the amount of malondialdehyde formed) and made the membrane leaky (as revealed by the release of the trapped chromate anions). The oxidation index and the formation of malondialdehyde increased linearly with increasing dose of radiation and depended significantly on the dose rate. The effects were smaller in liposomes derived from Vibrio cholerae phospholipid than in those derived from egg lecithin. The effects of the radiation dose and dose rate on hemolysis and peroxidation (MDA formation) of the erythrocyte membrane followed a similar pattern. A direct correlation between the percentage leakage of chromate (Y) and the oxidation index (X) of the liposomal system was obtained as Y = 236.5 x X

  16. Nanosized patterns as reference structures for macroscopic transport properties and vortex phases in YBCO films

    OpenAIRE

    Mezzetti, E.; Chiodoni, A.; Gerbaldo, R.; Ghigo, G.; Gozzelino, L.; Minetti, B.; Camerlingo, C.; C. Giannini

    2000-01-01

    This paper studies the striking correlation between nanosized structural patterns in YBCO films and macroscopic transport current. A nanosized network of parallel Josephson junctions laced by insulating dislocations is almost mimicking the grain boundary structural network. It contributes to the macroscopic properties and accounts for the strong intergranular pinning across the film in the intermediate temperature range. The correlation between the two networks enables to find out an outstand...

  17. Nanosized Borides and Carbides for Electroplating. Metal-Matrix Coatings: Specifications, Performance Evaluation

    Science.gov (United States)

    Galevskiy, G. V.; Rudneva, V. V.; Galevskiy, S. G.; Il’yashchenko, D. P.; Kartsev, D. S.

    2016-04-01

    This paper summarizes experience of application of nano-sized carbides and borides of titanium and chromium, silicon carbide as components of electro-depositable coating compositions based on nickel, zinc, and chromium. Basic physical and mechanical properties of the coatings are determined. Technological and economic evaluation is completed; practicability of high-cost nano-diamonds substitution for nano-sized borides and carbides is justified.

  18. (99m)Tc-labeled therapeutic inhaled amikacin loaded liposomes.

    Science.gov (United States)

    Lee, Jae-Ho; Cheng, Kenneth T; Malinin, Vladimir; Li, Zhili; Yao, Zhengsheng; Lee, Sung-Jin; Gould, Christine M; Olivier, Kenneth N; Chen, Clara; Perkins, Walter R; Paik, Chang H

    2013-12-01

    The radiolabeling of the liposome surface can be a useful tool for in vivo tracking of therapeutic drug loaded liposomes. We investigated radiolabeling therapeutic drug (i.e. an antibiotic, amikacin) loaded liposomes with (99m)Tc, nebulization properties of (99m)Tc-labeled liposomal amikacin for inhalation ((99m)Tc-LAI), and its stability by size exclusion low-pressure liquid chromatography (LPLC). LAI was reacted with (99m)Tc using SnCl2 dissolved in ascorbic acid as a reducing agent for 10 min at room temperature. The labeled products were then purified by anion exchange resin. The purified (99m)Tc-LAI in 1.5% NaCl solution was incubated at 4 °C to assess its stability by LPLC. The purified (99m)Tc-LAI was subjected to studies with a clinically used nebulizer (PARI eFlow®) and the Anderson Cascade Impactor (ACI). The use of ascorbic acid at 0.91 mM resulted in a quantitative labeling efficiency. The LPLC profile showed that the liposomal peak of LAI detected by a UV monitor at both 200 nm and 254 nm overlapped with the radioactivity peak of (99m)Tc-LAI, indicating that (99m)Tc-LAI is suitable for tracing LAI. The ACI study demonstrated that the aerosol droplet size distribution determined gravimetrically was similar to that determined by radioactivity. The liposome surface labeling method using SnCl₂ in 0.91 mM ascorbic acid produced (99m)Tc-LAI with a high labeling efficiency and stability that are adequate to evaluate the deposition and clearance of inhaled LAI in the lung by gamma scintigraphy. PMID:23879241

  19. PEG minocycline-liposomes ameliorate CNS autoimmune disease.

    Directory of Open Access Journals (Sweden)

    Wei Hu

    Full Text Available BACKGROUND: Minocycline is an oral tetracycline derivative with good bioavailability in the central nervous system (CNS. Minocycline, a potent inhibitor of matrix metalloproteinase (MMP-9, attenuates disease activity in experimental autoimmune encephalomyelitis (EAE, an animal model of multiple sclerosis (MS. Potential adverse effects associated with long-term daily minocycline therapy in human patients are concerning. Here, we investigated whether less frequent treatment with long-circulating polyethylene glycol (PEG minocycline liposomes are effective in treating EAE. FINDINGS: Performing in vitro time kinetic studies of PEG minocycline-liposomes in human peripheral blood mononuclear cells (PBMCs, we determined that PEG minocycline-liposome preparations stabilized with CaCl(2 are effective in diminishing MMP-9 activity. Intravenous injections of PEG minocycline-liposomes every five days were as effective in ameliorating clinical EAE as daily intraperitoneal injections of minocycline. Treatment of animals with PEG minocycline-liposomes significantly reduced the number of CNS-infiltrating leukocytes, and the overall expression of MMP-9 in the CNS. There was also a significant suppression of MMP-9 expression and proteolytic activity in splenocytes of treated animals, but not in CNS-infiltrating leukocytes. Thus, leukocytes gaining access to the brain and spinal cord require the same absolute amount of MMP-9 in all treatment groups, but minocycline decreases the absolute cell number. CONCLUSIONS: Our data indicate that less frequent injections of PEG minocycline-liposomes are an effective alternative pharmacotherapy to daily minocycline injections for the treatment of CNS autoimmune diseases. Also, inhibition of MMP-9 remains a promising treatment target in EAE and patients with MS.

  20. Exchangeable pulmonary water space evaluation using giant liposomes

    International Nuclear Information System (INIS)

    The present work aims to study the potential use of liposomes for the evaluation of pulmonary exchangeable water space, important parameter in some pulmonary oedema situations. This study is based upon the delivery of a diffusible water radiotracer into pulmonary capillary network, which equilibrates with interstitial water space of the lung and returns to the blood circulation. The time constant of this phenomena depends on the magnitude of the water space under study. The release of the diffusible radiotracer in lung capillaries is performed using liposomes with specific formulation. The giant liposomes (15-30μm diameter) used in this study are instable at 37 deg. C. They are biocompatible, biodegradable, with low toxicity and showed no immunogenicity. A water tracer labelled with 99mTc, encapsulated in the aqueous phase of giant liposomes, has been used. Liposomes were prepared in sterile conditions and with apyrogenic materials. The lipid films composition is L-α-diestearoylphosphatidylcholine (DSPC), L-α-phosphatidyl-DL-glycerol (EPG) and cholesterol (CHOL) (60%/10%/30% mass ratio). After iv injection at +-20 deg. C in the femoral vein of Wistar rats (300g-600g) or albine rabbits (4.5-5Kg), the thermolabile liposomes will be entrapped in lung capillaries and release the radiotracer locally. When the radiodrug is diffusible we will evaluate the volume of the exchangeable pulmonary water analyzing the activity/time curves. These curves are slower for greater water spaces. When the radiotracer is non-diffusible, the disappearance curves are not influenced by the extravascular water space. (author)

  1. Delivery of siRNA Using Cationic Liposomes Incorporating Stearic Acid-modified Octa-Arginine.

    Science.gov (United States)

    Yang, Dongsheng; Li, Yuhuan; Qi, Yuhang; Chen, Yongzhen; Yang, Xuewei; Li, Yujing; Liu, Songcai; Lee, Robert J

    2016-07-01

    Cationic liposomes incorporating stearic acid-modified octa-arginine (StA-R8) were evaluated for survivin small interfering RNA (siRNA) delivery. StA-R8 was synthesized and incorporated into liposomes. The composition of liposomes was optimized. Physicochemical properties, cytotoxicity, cellular uptake and gene silencing activity of the liposomes complexed to survivin siRNA were investigated. The results showed that StA-R8-containing liposomes had reduced cytotoxicity and improved delivery efficiency of siRNA into cancer cells compared with StA-R8 by itself. PMID:27354583

  2. Permeability of iodide in multilamellar liposomes modeled by two compartments and a reservoir.

    Science.gov (United States)

    Schullery, S E

    1977-07-14

    A previously published rate law for the diffusion of iodide from multilamellar egg phosphatidylcholine liposomes (Schullery, S.E. (1975) Chem. Phys. Lipids 14, 49-58) is fitted to the relatively simple mathematical model of two compartments in series with a reservoir. All of the inner liposome compartments are assumed to behave as effectively one compartment in series with the liposome's outermost compartment. Based on this model, reasonable values are calculated for the fraction of the total solution trapped by liposomes which is in the outermost liposome compartment, 17%, and the permeability coefficient of iodide against isotonic, mixed iodide-chloride solution, 2-10(-9) cm/s. PMID:884087

  3. USE OF LIPOSOMES AND NANOPARTICLES FOR BRAIN DRUG TARGETING

    Directory of Open Access Journals (Sweden)

    Goutam Pal

    2012-08-01

    Full Text Available The Blood Brain Barrier (BBB poses a obstacle for a drugs, including antineoplastic agent, antibiotics, neuropeptides, CNS active agents, to be delivered to the brain for therapeutic reasons. The use of formulation dependent strategy such as the use of heterogenous pharmaceutical systems for its effective targeting to the brain is being explored recently. Liposomes and Nanoparticles are good possibilities to achieve the goal. Chemically modified liposomes and nanoparticles are tried in recent times to act as brain targeting aids, and this article tries to explain the possibilities and problems behind such an endeavor.KEY WORDS:

  4. Assembly of Liposomes Controlled by Triple Helix Formation

    DEFF Research Database (Denmark)

    Vogel, Stefan; Jakobsen, Ulla

    2013-01-01

    the otherwise difficult thermal denaturation analysis of complex triple helical DNA-assemblies. The approach is based on lipid modified triplex forming oligonucleotides (TFOs) which control the assembly of liposomes in solution in the presence of single- or double stranded DNA targets. The thermal...... denaturation analysis is monitored by ultraviolet spectroscopy at sub-micromolar concentrations and compared to regular thermal denaturation assays in the absence of liposomes. We report on triplex forming oligonucleotides (TFOs) based on DNA and locked nucleic acid (LNA)/DNA hybrid building blocks and...

  5. Local structure of nanosized tungstates revealed by evolutionary algorithm

    Energy Technology Data Exchange (ETDEWEB)

    Timoshenko, Janis; Anspoks, Andris; Kuzmin, Alexei [Institute of Solid State Physics, University of Latvia, Riga (Latvia); Kalinko, Alexandr [Institute of Solid State Physics, University of Latvia, Riga (Latvia); Synchrotron SOLEIL, l' Orme des Merisiers, Saint-Aubin, Gif-sur-Yvette (France)

    2015-02-01

    Nanostructured tungstates, such as CoWO{sub 4} and CuWO{sub 4}, are very promising catalytic materials, particularly for photocatalytic oxidation of water. The high catalytic activity of tungstate nanoparticles partially is a result of their extremely small sizes, and, consequently, high surface-to-volume ratio. Therefore their properties depend strongly on the atomic structure, which differ significantly from that of the bulk material. X-ray absorption spectroscopy is a powerful technique to address the challenging problem of the local structure determination in nanomaterials. In order to fully exploit the structural information contained in X-ray absorption spectra, in this study we employ a novel evolutionary algorithm (EA) for the interpretation of the Co and Cu K-edges as well as the W L{sub 3}-edge extended X-ray absorption fine structure (EXAFS) of nanosized CoWO{sub 4} and CuWO{sub 4}. The combined EA-EXAFS approach and simultaneous analysis of the W L{sub 3} and Co(Cu) K-edge EXAFS spectra allowed us for the first time to obtain a 3D structure model of the tungstate nanoparticles and to explore in details the effect of size, temperature and transition metal type. (copyright 2015 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  6. Protein interactions with nanosized hydrotalcites of different composition.

    Science.gov (United States)

    Bellezza, Francesca; Alberani, Alistella; Posati, Tamara; Tarpani, Luigi; Latterini, Loredana; Cipiciani, Antonio

    2012-01-01

    Nanosized hydrotalcite-like compounds (HTlc) with different chemical composition were prepared and used to study protein adsorption. Two soft proteins, myoglobin (Mb) and bovine serum albumin (BSA), were chosen to investigate the nature of the forces controlling the adsorption and how these depend on the chemical composition of the support. Both proteins strongly interact with HTlc exhibiting in most cases a Langmuir-type adsorption. Mb showed a higher affinity for Nickel Chromium (NiCr-HTlc) than for Nickel Aluminum (NiAl-HTlc), while for BSA no significant differences between supports were found. Adsorption experiments in the presence of additives showed that proteins exhibited different types of interactions onto the same HTlc surface and that the adsorption was strongly suppressed by the addition of disodium hydrogen phosphate (Na(2)HPO(4)). Atomic force microscopy images showed that the adsorption of both proteins onto nanoparticles was followed by the aggregation of biocomposites, with a more disordered structure for BSA. Fluorescence measurements for adsorbed Mb showed that the inorganic nanoparticles induced conformational changes in the biomolecules; in particular, the interactions with HTlc surface quenched the tryptophan fluorescence and this process was particularly efficient for NiCr-HTlc. The adsorption of BSA onto the HTlc nanoparticles induced a selective quenching of the exposed fluorescent residues, as indicated by the blue-shift of the emission spectra of tryptophan residues and by the shortening of the fluorescence decay times. PMID:22115829

  7. Refractive index modification of polymers using nanosized dopants

    Science.gov (United States)

    Hanemann, Thomas; Boehm, Johannes; Müller, Claas; Ritzhaupt-Kleissl, Eberhard

    2008-04-01

    The addition of nanosized inorganic or organic dopants to polymers allows the modification of the polymers physical properties enabling the realization of functionalized polymers with new application fields e.g. in microoptics. Exemplarily electron rich organic dopants, solved in polymers, cause a pronounced increase of the refractive index. Polymer based reactive resins like PMMA, solved in MMA, or unsaturated polyester, solved in styrene, can be cured to thermoplastic polymers. The resin's low viscous flow behaviour enables an easy composite formation by solving the organic dopants in the liquid up to a dopant content of 50 wt%, followed by solidification to a thermoplastic. The addition of simple organic molecules like phenanthrene or benzochinoline allows a refractive index elevation at 633 nm from 1.56 up to 1.60 retaining the good transmission properties. In comparison the refractive index of PMMA can be increased from the initial value of 1.49 up to values around 1.58 (@633 nm). All composites show an almost linear correlation between dopant content and refractive index. Using these composites devices like 3dB-couplers or an electrooptical modulator applying injection molded or hot embossed substrates have been realized.

  8. The Synthesis and Modification of Nanosized Clickable Latex Particles

    KAUST Repository

    Almahdali, Sarah

    2013-05-01

    This research aims to add to the current knowledge available for miniemulsion polymerization reactions and to use this knowledge to synthesize multifunctional nanosized latex particles that have the potential to be used in catalysis. The physical properties of the latex can be adjusted to suit various environments due to the multiple functional groups present. For this research, styrene, pentafluorostyrene, azidomethyl styrene, pentafluorostyrene with azidomethyl styrene and pentafluorostyrene with styrene latexes were produced, and analyzed by dynamic light scattering. The latexes were synthesized using a miniemulsion polymerization technique found through this research. Potassium oleate and potassium 1,1,2,2,3,3,4,4-nonafluorobutane-1-sulfonate were used as surfactants during the miniemulsion polymerization reaction to synthesize pentafluorostyrene with azidomethyl styrene latex. Transmission electron microscopy data and dynamic light scattering data have been collected to analyze the structure of this latex, and it has been synthesized using a number of conditions, differing in reaction time, surfactant amount and sonication methods. We have also improved the solubility of the latex through a copper(I) catalyzed 1,3-dipolar azide-alkyne reaction, by clicking (polyethylene glycol)5000 onto the azide functional groups.

  9. Nanotip analysis for dielectrophoretic concentration of nanosized viral particles

    International Nuclear Information System (INIS)

    Rapid and sensitive detection of low-abundance viral particles is strongly demanded in health care, environmental control, military defense, and homeland security. Current detection methods, however, lack either assay speed or sensitivity, mainly due to the nanosized viral particles. In this paper, we compare a dendritic, multi-terminal nanotip (‘dendritic nanotip’) with a single terminal nanotip (‘single nanotip’) for dielectrophoretic (DEP) concentration of viral particles. The numerical computation studies the concentration efficiency of viral particles ranging from 25 to 100 nm in radius for both nanotips. With DEP and Brownian motion considered, when the particle radius decreases by two times, the concentration time for both nanotips increases by 4–5 times. In the computational study, a dendritic nanotip shows about 1.5 times faster concentration than a single nanotip for the viral particles because the dendritic structure increases the DEP-effective area to overcome the Brownian motion. For the qualitative support of the numerical results, the comparison experiment of a dendritic nanotip and a single nanotip is conducted. Under 1 min of concentration time, a dendritic nanotip shows a higher sensitivity than a single nanotip. When the concentration time is 5 min, the sensitivity of a dendritic nanotip for T7 phage is 104 particles ml−1. The dendritic nanotip-based concentrator has the potential for rapid identification of viral particles. (paper)

  10. Preparation of nanosize polyaniline and its utilization for microwave absorber.

    Science.gov (United States)

    Abbas, S M; Dixit, A K; Chatterjee, R; Goel, T C

    2007-06-01

    Polyaniline powder in nanosize has been synthesized by chemical oxidative route. XRD, FTIR, and TEM were used to characterize the polyaniline powder. Crytallite size was estimated from XRD profile and also ascertained by TEM in the range of 15 to 20 nm. The composite absorbers have been prepared by mixing different ratios of polyaniline into procured polyurethane (PU) binder. The complex permittivity (epsilon' - jepsilon") and complex permeability (mu' - jmu") were measured in X-band (8.2-12.4 GHz) using Agilent network analyzer (model PNA E8364B) and its software module 85071 (version 'E'). Measured values of these parameters were used to determine the reflection loss at different frequencies and sample thicknesses, based on a model of a single layered plane wave absorber backed by a perfect conductor. An optimized polyaniline/PU ratio of 3:1 has given a minimum reflection loss of -30 dB (99.9% power absorption) at the central frequency 10 GHz and the bandwidth (full width at half minimum) of 4.2 GHz over whole X-band (8.2 to 12.4 GHz) in a sample thickness of 3.0 mm. The prepared composites can be fruitfully utilized for suppression of electromagnetic interference (EMI) and reduction of radar signatures (stealth technology). PMID:17655005

  11. Local structure of nanosized tungstates revealed by evolutionary algorithm

    International Nuclear Information System (INIS)

    Nanostructured tungstates, such as CoWO4 and CuWO4, are very promising catalytic materials, particularly for photocatalytic oxidation of water. The high catalytic activity of tungstate nanoparticles partially is a result of their extremely small sizes, and, consequently, high surface-to-volume ratio. Therefore their properties depend strongly on the atomic structure, which differ significantly from that of the bulk material. X-ray absorption spectroscopy is a powerful technique to address the challenging problem of the local structure determination in nanomaterials. In order to fully exploit the structural information contained in X-ray absorption spectra, in this study we employ a novel evolutionary algorithm (EA) for the interpretation of the Co and Cu K-edges as well as the W L3-edge extended X-ray absorption fine structure (EXAFS) of nanosized CoWO4 and CuWO4. The combined EA-EXAFS approach and simultaneous analysis of the W L3 and Co(Cu) K-edge EXAFS spectra allowed us for the first time to obtain a 3D structure model of the tungstate nanoparticles and to explore in details the effect of size, temperature and transition metal type. (copyright 2015 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  12. Quantitative analysis of the lamellarity of giant liposomes prepared by the inverted emulsion method.

    Science.gov (United States)

    Chiba, Masataka; Miyazaki, Makito; Ishiwata, Shin'ichi

    2014-07-15

    The inverted emulsion method is used to prepare giant liposomes by pushing water-in-oil droplets through the oil/water interface into an aqueous medium. Due to the high encapsulation efficiency of proteins under physiological conditions and the simplicity of the protocol, it has been widely used to prepare various cell models. However, the lamellarity of liposomes prepared by this method has not been evaluated quantitatively. Here, we prepared liposomes that were partially stained with a fluorescent dye, and analyzed their fluorescence intensity under an epifluorescence microscope. The fluorescence intensities of the membranes of individual liposomes were plotted against their diameter. The plots showed discrete distributions, which were classified into several groups. The group with the lowest fluorescence intensity was determined to be unilamellar by monitoring the exchangeability of the inner and the outer solutions of the liposomes in the presence of the pore-forming toxin α-hemolysin. Increasing the lipid concentration dissolved in oil increased the number of liposomes ∼100 times. However, almost all the liposomes were unilamellar even at saturating lipid concentrations. We also investigated the effects of lipid composition and liposome content, such as highly concentrated actin filaments and Xenopus egg extracts, on the lamellarity of the liposomes. Remarkably, over 90% of the liposomes were unilamellar under all conditions examined. We conclude that the inverted emulsion method can be used to efficiently prepare giant unilamellar liposomes and is useful for designing cell models. PMID:25028876

  13. Factorial design studies of antiretroviral drug-loaded stealth liposomal injectable: PEGylation, lyophilization and pharmacokinetic studies

    Science.gov (United States)

    Sudhakar, Beeravelli; Krishna, Mylangam Chaitanya; Murthy, Kolapalli Venkata Ramana

    2016-01-01

    The aim of the present study was to formulate and evaluate the ritonavir-loaded stealth liposomes by using 32 factorial design and intended to delivered by parenteral delivery. Liposomes were prepared by ethanol injection method using 32 factorial designs and characterized for various physicochemical parameters such as drug content, size, zeta potential, entrapment efficiency and in vitro drug release. The optimization process was carried out using desirability and overlay plots. The selected formulation was subjected to PEGylation using 10 % PEG-10000 solution. Stealth liposomes were characterized for the above-mentioned parameters along with surface morphology, Fourier transform infrared spectrophotometer, differential scanning calorimeter, stability and in vivo pharmacokinetic studies in rats. Stealth liposomes showed better result compared to conventional liposomes due to effect of PEG-10000. The in vivo studies revealed that stealth liposomes showed better residence time compared to conventional liposomes and pure drug solution. The conventional liposomes and pure drug showed dose-dependent pharmacokinetics, whereas stealth liposomes showed long circulation half-life compared to conventional liposomes and pure ritonavir solution. The results of statistical analysis showed significance difference as the p value is (<0.05) by one-way ANOVA. The result of the present study revealed that stealth liposomes are promising tool in antiretroviral therapy.

  14. Prolongation of residence time of liposome by surface-modification with mixture of hydrophilic polymers.

    Science.gov (United States)

    Shehata, Tamer; Ogawara, Ken-Ichi; Higaki, Kazutaka; Kimura, Toshikiro

    2008-07-01

    The objective of this study is to evaluate the biodistribution characteristics of liposomes surface-modified with the mixture of polyethylene glycol (PEG) and polyvinyl alcohol (PVA) as a drug carrier for passive targeting of drugs. The liposomes (egg phosphatidylcholine:cholesterol=55:40, molar ratio) modified with both PEG and PVA (4:1 molar ratio) (PEG4%/PVA1% liposome) provided the largest AUC, which could be attributed to the smallest hepatic clearance of the liposomes. The liver perfusion studies clearly indicated that lower hepatic disposition of PEG4%/PVA1% liposome was ascribed to the decrease in its hepatic uptake via receptor-mediated endocytosis. Furthermore, the amounts of whole serum proteins and of opsonins such as complement C3 and immunoglobulin G adsorbed on PEG4%/PVA1% liposome were significantly smaller than those on the liposome solely modified with PEG (PEG5% liposome). On the other hand, several proteins were adsorbed at larger amount on PEG4%/PVA1% liposome than PEG5% liposome, and the protein identification by LC-MS/MS suggested that some of those proteins including albumin might function as dysopsonins. The decrease in the adsorbed amount of several opsonins and the increase in the adsorbed dysopsonins would be responsible for its lower affinity to the liver and long residence in the systemic circulation of PEG4%/PVA1% liposome. PMID:18486370

  15. Preparation of human hepatocellular carcinoma-targeted liposome microbubbles and their immunological properties

    Institute of Scientific and Technical Information of China (English)

    Ai-Na Bian; Yun-Hua Gao; Kai-Bin Tan; Ping Liu; Gong-Jun Zeng; Xin Zhang; Zheng Liu

    2004-01-01

    AIM: To prepare the human hepatocellular carcinoma.(HCC)-targeted liposome microbubbles and to investigate their immunological properties.METHODS: Human hepatocarcinoma specific monoclonal antibody HAb18 was attached to the surface of home-made liposome microbubbles by static attraction to prepare the targeted liposome microbubbles. The combination of HAb18 with liposome microbubbles was confirmed by the slide agglutination test and immunofluorescent assay. Their immunological activity was measured by ELISA. Rosette formation test, rosette formation blocking test and immunofluorescent assay were used to identify the specific binding of targeted liposome microbubbles to SMMC-7721 hepatoma cells, and cytotoxicity assay was used to detect their effect on human hepatocytes.RESULTS: The targeted liposome microbubbles were positive in the slide agglutination test and immunofluorescent assay. ELISA indicated that the immunological activity of HAb18 on the liposome microbubbles was similar to that of free HAb18. SMMC-7721 cells were surrounded by the targeting liposome microbubbles to form rosettes, while the control SGC-7901 gastric cancer cells were not. Proliferation of SMMC-7721 cells and normal human hepatocytes was not influenced by the targeted liposome microbubbles.CONCLUSION: The targeted liposome microbubbles with a high specific biological activity have been successfully prepared, which specifically bind to human hepatocarcinoma cells, and are non-cytotoxic to hepatocytes. These results indicate that the liposome microbubbles can be used as a HCC-targeted ultrasound contrast agent that may enhance ultrasound images and thus improve the diagnosis of HCC,especially at the early stage.

  16. Characterization of biosurfactant-containing liposomes and their efficiency for gene transfection.

    Science.gov (United States)

    Ueno, Yoshinobu; Hirashima, Naohide; Inoh, Yoshikazu; Furuno, Tadahide; Nakanishi, Mamoru

    2007-01-01

    Recently we showed significance of biosurfactants in the field of non-viral vectors for gene transfection. There, a biosurfactant, mannosylerythritol lipid A (MEL-A), especially increased the efficiency of gene transfection mediated with cationic liposomes. However, the molecular mechanism has not been well-understood yet. Here, through the examination of the ability of cationic liposomes containing an MEL (MEL-A, MEL-B or MEL-C) for important transfectional processes of the DNA capsulation and the membrane fusion with anionic liposomes, we found that MEL-A-containing liposomes increased both processes, but that MEL-B and MEL-C-containing liposomes just increased either of them. The results indicated that these kinds of the physicochemical properties in MEL-A-containing liposomes are able to increase the efficiency of liposome-mediated gene transfection. PMID:17202680

  17. Delivery of negatively charged liposomes into the atherosclerotic plaque of apolipoprotein E-deficient mouse aortic tissue

    OpenAIRE

    Zhaorigetu, Siqin; Rodriguez-Aguayo, Cristian; Sood, Anil K.; Lopez-Berestein, Gabriel; Walton, Brian L.

    2014-01-01

    Liposomes have been used to diagnose and treat cancer and, to a lesser extent, cardiovascular disease. We previously showed the uptake of anionic liposomes into the atheromas of Watanabe heritable hyperlipidemic rabbits within lipid pools. However, the cellular distribution of anionic liposomes in atherosclerotic plaque remains undescribed. In addition, how anionic liposomes are absorbed into atherosclerotic plaque is unclear. We investigated the uptake and distribution of anionic liposomes i...

  18. Novel fluorescence method to visualize antibody-dependent hydrogen peroxide-associated "killing" of liposomes by phagocytes.

    OpenAIRE

    Petty, H R; Francis, J W

    1985-01-01

    We have developed a new methodology to examine effector-cell-mediated immune attack using liposomes as targets. Hydrogen-peroxide-associated killing of liposomes was observed with fluorescence intensification microscopy. Liposomes were composed of 98-99 mol % egg phosphatidylcholine and 1-2 mol % dinitrophenyl lipid hapten. Anti-dinitrophenyl IgG antibody was used to opsonize liposomes. Liposomes were loaded with dihydroxymandelic acid (DHMA) and peroxidase. Macrophage- or neutrophil-mediated...

  19. Length of hydrocarbon chain influences location of curcumin in liposomes: Curcumin as a molecular probe to study ethanol induced interdigitation of liposomes.

    Science.gov (United States)

    El Khoury, Elsy; Patra, Digambara

    2016-05-01

    Using fluorescence quenching of curcumin in 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) liposomes by brominated derivatives of fatty acids, the location of curcumin has been studied, which indicates length of hydrocarbon chain has an effect on the location of curcumin in liposomes. Change of fluorescence intensity of curcumin with temperature in the presence of liposomes helps to estimate the phase transition temperature of these liposomes, thus, influence of cholesterol on liposome properties has been studied using curcumin as a molecule probe. The cooperativity due to the interactions between the hydrocarbon chains during melting accelerates the phase transition of DPPC liposomes in the presence of high percentage of cholesterol whereas high percentage of cholesterol generates a rather rigid DMPC liposome over a wide range of temperatures. We used ethanol to induce interdigitation between the hydrophobic chains of the lipids and studied this effect using curcumin as fluorescence probe. As a result of interdigitation, curcumin fluorescence is quenched in liposomes. The compact arrangement of the acyl chains prevents curcumin from penetrating deep near the midplane. In the liquid crystalline phase ethanol introduces a kind of order to the more fluid liposome, and does not leave space for curcumin to be inserted away from water. PMID:26945646

  20. Imaging in rheumatoid arthritis using liposomes labelled with technetium

    International Nuclear Information System (INIS)

    The results are presented of a preliminary study showing that technetium-labelled liposomes are accumulated in clinically affected joints of patients with rheumatoid arthritis. Typical scintigraph scans are presented. This method offers an opportunity of determining the extent and activity of macrophages within synovial tissue. (UK)

  1. Enhancing Methotrexate Tolerance with Folate Tagged Liposomes in Arthritic Mice.

    Science.gov (United States)

    Nogueira, Eugénia; Lager, Franck; Le Roux, Delphine; Nogueira, Patrícia; Freitas, Jaime; Charvet, Celine; Renault, Gilles; Loureiro, Ana; Almeida, Catarina R; Ohradanova-Repic, Anna; Machacek, Christian; Bernardes, Gonçalo J L; Moreira, Alexandra; Stockinger, Hannes; Burnet, Michael; Carmo, Alexandre M; Gomes, Andreia C; Preto, Ana; Bismuth, Georges; Cavaco-Paulo, Artur

    2015-12-01

    Methotrexate is the first line of treatment of rheumatoid arthritis. Since many patients become unresponsive to methotrexate treatment, only very expensive biological therapies are effective and increased methotrexate tolerance strategies need to be identified. Here we propose the encapsulation of methotrexate in a new liposomal formulation using a hydrophobic fragment of surfactant protein conjugated to a linker and folate to enhance their tolerance and efficacy. In this study we aim to evaluate the efficiency of this system to treat rheumatoid arthritis, by targeting folate receptor β present at the surface of activated macrophages, key effector cells in this pathology. The specificity of our liposomal formulation to target folate receptor β was investigated both in vitro as in vivo using a mouse model of arthritis (collagen-induced arthritis in DBA/1J mice strain). In both systems, the liposomal constructs were shown to be highly specific and efficient in targeting folate receptor β. These liposomal formulations also significantly increase the clinical benefit of the encapsulated methotrexate in vivo in arthritic mice, together with reduced expression of CD39 and CD73 ectonucleotidases by joint-infiltrating macrophages. Thus, our formulation might be a promising cost effective way to treat rheumatoid arthritis and delay or reduce methotrexate intolerance. PMID:26510317

  2. Liposomal photosensitizers: potential platforms for anticancer photodynamic therapy

    Directory of Open Access Journals (Sweden)

    L.A. Muehlmann

    2011-08-01

    Full Text Available Photodynamic therapy is a well-established and clinically approved treatment for several types of cancer. Antineoplastic photodynamic therapy is based on photosensitizers, i.e., drugs that absorb photons translating light energy into a chemical potential that damages tumor tissues. Despite the encouraging clinical results with the approved photosensitizers available today, the prolonged skin phototoxicity, poor selectivity for diseased tissues, hydrophobic nature, and extended retention in the host organism shown by these drugs have stimulated researchers to develop new formulations for photodynamic therapy. In this context, due to their amphiphilic characteristic (compatibility with both hydrophobic and hydrophilic substances, liposomes have proven to be suitable carriers for photosensitizers, improving the photophysical properties of the photosensitizers. Moreover, as nanostructured drug delivery systems, liposomes improve the efficiency and safety of antineoplastic photodynamic therapy, mainly by the classical phenomenon of extended permeation and retention. Therefore, the association of photosensitizers with liposomes has been extensively studied. In this review, both current knowledge and future perspectives on liposomal carriers for antineoplastic photodynamic therapy are critically discussed.

  3. Some factors affecting the valinomycin-induced leak from liposomes

    NARCIS (Netherlands)

    Blok, M.C.; Gier, J. de; Deenen, L.L.M. van

    1974-01-01

    Experiments dealing with the valinomycin-induced K+ leak from egg lecithin liposomes have demonstrated the importance of the enclosed anion. Except when lipophilic anions are enclosed, the addition of both valinomycin and a uncoupler, e.g. carbonylcyanide p-trifluoromethoxyphenylhydrazone, is necess

  4. Liposomal extended-release bupivacaine for postsurgical analgesia

    Directory of Open Access Journals (Sweden)

    Lambrechts M

    2013-09-01

    Full Text Available Mark Lambrechts,1,2 Michael J O’Brien,2 Felix H Savoie,2 Zongbing You1–31Department of Structural and Cellular Biology, 2Department of Orthopaedic Surgery and Tulane Institute of Sports Medicine, 3Tulane Cancer Center, Louisiana Cancer Research Consortium, Tulane Center for Aging, Tulane Center for Stem Cell Research and Regenerative Medicine, Tulane University School of Medicine, New Orleans, Louisiana, USAAbstract: When physicians consider which analgesia to use postsurgery, the primary goal is to relieve pain with minimal adverse side effects. Bupivacaine, a commonly used analgesic, has been formulated into an aqueous suspension of multivesicular liposomes that provide long-lasting analgesia for up to 72 hours, while avoiding the adverse side effects of opioids. The increased efficacy of liposomal extended-release bupivacaine, compared to bupivacaine hydrochloride, has promoted its usage in a variety of surgeries including hemorrhoidectomy, bunionectomy, inguinal hernia repair, total knee arthroplasty, and augmentation mammoplasty. However, like other bupivacaine formulations, the liposomal extended-release bupivacaine does have some side effects. In this brief review, we provide an update of the current knowledge in the use of bupivacaine for postsurgical analgesia. Keywords: bupivacaine, liposome, analgesia, side effects, efficacy, patient satisfaction

  5. Incorporation of Amphiphilic Cyclodextrins into Liposomes as Artificial Receptor Units

    NARCIS (Netherlands)

    Kauscher, Ulrike; Stuart, Marc C. A.; Druecker, Patrick; Galla, Hans-Joachim; Ravoo, Bart Jan

    2013-01-01

    In this article, we describe the introduction of amphiphilic beta-cyclodextrins into liposomes to act as artificial receptor units. Using dynamic light scattering, dye encapsulation, and cryogenic transmission electron microscopy, we show that amphiphilic beta-cyclodextrins can be mixed in any propo

  6. Antimony to Cure Visceral Leishmaniasis Unresponsive to Liposomal Amphotericin B

    Science.gov (United States)

    Morizot, Gloria; Jouffroy, Romain; Faye, Albert; Chabert, Paul; Belhouari, Katia; Calin, Ruxandra; Charlier, Caroline; Miailhes, Patrick; Siriez, Jean-Yves; Mouri, Oussama; Yera, Hélène; Gilquin, Jacques; Tubiana, Roland; Lanternier, Fanny; Mamzer, Marie-France; Legendre, Christophe; Peyramond, Dominique; Caumes, Eric; Lortholary, Olivier; Buffet, Pierre

    2016-01-01

    We report on 4 patients (1 immunocompetent, 3 immunosuppressed) in whom visceral leishmaniasis had become unresponsive to (or had relapsed after) treatment with appropriate doses of liposomal amphotericin B. Under close follow-up, full courses of pentavalent antimony were administered without life-threatening adverse events and resulted in rapid and sustained clinical and parasitological cure. PMID:26735920

  7. Cerium-144 decorporation possibilities of liposome-incorporated EDTA

    International Nuclear Information System (INIS)

    The decorporation possibilities of EDTA, applied independently and liposome-incorporated, were the subject of comparative evaluation by physical, biophysical and biological criteria. It was found that the decorporating effect of EDTA was low and equal in either case of application of the complexone. 5 tabs., 14 refs

  8. Soft Interaction in Liposome Nanocarriers for Therapeutic Drug Delivery

    Directory of Open Access Journals (Sweden)

    Domenico Lombardo

    2016-06-01

    Full Text Available The development of smart nanocarriers for the delivery of therapeutic drugs has experienced considerable expansion in recent decades, with the development of new medicines devoted to cancer treatment. In this respect a wide range of strategies can be developed by employing liposome nanocarriers with desired physico-chemical properties that, by exploiting a combination of a number of suitable soft interactions, can facilitate the transit through the biological barriers from the point of administration up to the site of drug action. As a result, the materials engineer has generated through the bottom up approach a variety of supramolecular nanocarriers for the encapsulation and controlled delivery of therapeutics which have revealed beneficial developments for stabilizing drug compounds, overcoming impediments to cellular and tissue uptake, and improving biodistribution of therapeutic compounds to target sites. Herein we present recent advances in liposome drug delivery by analyzing the main structural features of liposome nanocarriers which strongly influence their interaction in solution. More specifically, we will focus on the analysis of the relevant soft interactions involved in drug delivery processes which are responsible of main behaviour of soft nanocarriers in complex physiological fluids. Investigation of the interaction between liposomes at the molecular level can be considered an important platform for the modeling of the molecular recognition processes occurring between cells. Some relevant strategies to overcome the biological barriers during the drug delivery of the nanocarriers are presented which outline the main structure-properties relationships as well as their advantages (and drawbacks in therapeutic and biomedical applications.

  9. Gemcitabine-loaded liposomes: rationale, potentialities and future perspectives

    Directory of Open Access Journals (Sweden)

    Federico C

    2012-11-01

    Full Text Available Cinzia Federico, Valeria M Morittu, Domenico Britti, Elena Trapasso, Donato CoscoDepartment of Health Sciences, Building of BioSciences, University “Magna Græcia” of Catanzaro, Campus Universitario “S Venuta”, Germaneto, ItalyAbstract: This review describes the strategies used in recent years to improve the biopharmaceutical properties of gemcitabine, a nucleoside analog deoxycytidine antimetabolite characterized by activity against many kinds of tumors, by means of liposomal devices. The main limitation of using this active compound is the rapid inactivation of deoxycytidine deaminase following administration in vivo. Consequently, different strategies based on its encapsulation/complexation in innovative vesicular colloidal carriers have been investigated, with interesting results in terms of increased pharmacological activity, plasma half-life, and tumor localization, in addition to decreased side effects. This review focuses on the specific approaches used, based on the encapsulation of gemcitabine in liposomes, with particular attention to the results obtained during the last 5 years. These approaches represent a valid starting point in the attempt to obtain a novel, commercializable drug formulation as already achieved for liposomal doxorubicin (Doxil®, Caelyx®.Keywords: gemcitabine, liposomes, multidrug, poly(ethylene glycol, tumors

  10. Drug delivery by phospholipase A(2) degradable liposomes

    DEFF Research Database (Denmark)

    Davidsen, Jesper; Vermehren, C.; Frøkjær, S.; Mouritsen, Ole G.; Jørgensen, Kent

    The effect of poly(ethylene glycol)-phospholipid (PE-PEG) lipopolymers on phospholipase A(2) (PLA(2)) hydrolysis of liposomes composed of stearoyl-oleoylphosphatidylcholine (SOPC) was investigated. The PLA(2) lag-time, which is inversely related to the enzymatic activity, was determined by...

  11. Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release

    DEFF Research Database (Denmark)

    Pedersen, Palle Jacob; Adolph, Sidsel Kramshøj; Subramanian, Arun Kumar;

    2010-01-01

    The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A(2) IIA and have potential in liposomal drug delivery targeting tumors. We have synthesi...

  12. In vivo toxicity of cationic micelles and liposomes

    DEFF Research Database (Denmark)

    Knudsen, Kristina Bram; Northeved, Helle; Ek, Pramod Kumar;

    2015-01-01

    This study investigated toxicity of nanocarriers comprised of cationic polymer and lipid components often used in gene and drug delivery, formulated as cationic micelles and liposomes. Rats were injected intravenously with 10, 25 or 100 mg/kg and sacrificed after 24 or 48 h, or 24 h after the las...

  13. In ovo transfection of chicken embryos using cationic liposomes.

    Science.gov (United States)

    Rosenblum, C I; Chen, H Y

    1995-05-01

    It is reported that cationic liposomes are capable of transfecting embryos in unincubated fertile chicken eggs and that the cationic liposome, TransfectAce, has superior properties to Lipofectin. In order to determine the duration of expression of genes introduced in this way, embryos were transfected with an expression vector encoding the firefly luciferase cDNA under the control of the Rous sarcoma virus long terminal repeat (LTR). Luciferase activity could be observed consistently in day 3 embryos and activity was detectable up to day 8 of incubation. The relative expression of luciferase under the control of different viral promoters was compared in transfected chicken embryo fibroblasts and day 3 embryos. The cytomegalovirus immediate early promoter and the SV40 early promoter directed the highest amount of expression in fibroblasts while the Rous sarcoma virus LTR caused the highest amount of expression in embryos. Chicken embryo fibroblasts were transfected with the luciferase vector in order to examine duration of reporter gene expression in vitro. Luciferase expression was decreased exponentially over a 24-day period after which point luciferase activity could no longer be detected. These data suggest that stable integration of transfected DNA using liposomes is a rare event. Nevertheless, liposome-mediated transfection of embryos is suitable for the examination of promoter activity in vivo and may be a useful method to transfect genes to study embryonic development. PMID:7795662

  14. Protein antigen adsorption to the DDA/TDB liposomal adjuvant

    DEFF Research Database (Denmark)

    Hamborg, Mette; Jorgensen, Lene; Bojsen, Anders Riber; Christensen, Dennis; Foged, Camilla

    2013-01-01

    Understanding the nature of adjuvant-antigen interactions is important for the future design of efficient and safe subunit vaccines, but remains an analytical challenge. We studied the interactions between three model protein antigens and the clinically tested cationic liposomal adjuvant composed...

  15. Carcinogenesis response modulation induced by gelonin encapsulated in liposome.

    Science.gov (United States)

    Alam, Anis; Nakhuru, K S; Singha, L I

    2008-08-01

    The effectiveness of gelonin to arrest protein synthesis, thereby limiting the growth of cancer cells was studied by encapsulating it into liposomes. The protein was extracted from the seeds of Indian plant Gelonium multiflorum by ammonium sulfate precipitation and purified using cation-exchange and gel-filtration chromatography. Biological activity of purified gelonin was determined using a rabbit reticulocyte lysate assay in the cell-free translational experiments. Gelonin was encapsulated in conventional liposomes prepared by the dry film method in order to retain biological activity of the entrapped protein. Carcinogenesis was induced in Swiss albino mice by intravenous administration of DBN (10 mg kg(-1) body weight) at weekly intervals. Marker enzyme assays (GGT, AChE, and GST), GSH levels, cell proliferation assay, hepatocyte DNA analysis, histological examination of micro sections of liver tissues were parameters used to monitor carcinogenesis induction, and regression in mice. From the in vitro experiments conducted, it was observed that gelonin upon its encapsulation into liposome, resulted in significant destruction of the transformed liver cells by its cytotoxic effects that arrest protein synthesis. Various parameters studied to monitor regression also suggested mass cell destruction to liver upon administration of liposomal gelonin in mice exposed to DBN. PMID:18500656

  16. Activity-Based Protein Profiling of Rhomboid Proteases in Liposomes

    Czech Academy of Sciences Publication Activity Database

    Wolf, E. V.; Seybold, M.; Hadravová, Romana; Stříšovský, Kvido; Verhelst, S. H. L.

    2015-01-01

    Roč. 16, č. 11 (2015), s. 1616-1621. ISSN 1439-4227 R&D Projects: GA MŠk(CZ) LK11206; GA MŠk LO1302 Institutional support: RVO:61388963 Keywords : activity -based protein profiling * chemical probes * inhibitors * intramembrane proteases * liposomes Subject RIV: CE - Biochemistry Impact factor: 3.088, year: 2014

  17. Compressibilities and volume fluctuations of archaeal tetraether liposomes.

    Science.gov (United States)

    Chong, Parkson Lee-Gau; Sulc, Michael; Winter, Roland

    2010-11-17

    Bipolar tetraether lipids (BTLs) are abundant in crenarchaeota, which thrive in both thermophilic and nonthermophilic environments, with wide-ranging growth temperatures (4-108°C). BTL liposomes can serve as membrane models to explore the role of BTLs in the thermal stability of the plasma membrane of crenarchaeota. In this study, we focus on the liposomes made of the polar lipid fraction E (PLFE). PLFE is one of the main BTLs isolated from the thermoacidophilic crenarchaeon Sulfolobus acidocaldarius. Using molecular acoustics (ultrasound velocimetry and densimetry), pressure perturbation calorimetry, and differential scanning calorimetry, we have determined partial specific adiabatic and isothermal compressibility, their respective compressibility coefficients, partial specific volume, and relative volume fluctuations of PLFE large unilamellar vesicles (LUVs) over a wide range of temperatures (20-85°C). The results are compared with those obtained from liposomes made of dipalmitoyl-L-α-phosphatidylcholine (DPPC), a conventional monopolar diester lipid. We found that, in the entire temperature range examined, compressibilities of PLFE LUVs are low, comparable to those found in gel state of DPPC. Relative volume fluctuations of PLFE LUVs at any given temperature examined are 1.6-2.2 times more damped than those found in DPPC LUVs. Both compressibilities and relative volume fluctuations in PLFE LUVs are much less temperature-sensitive than those in DPPC liposomes. The isothermal compressibility coefficient (β(T)(lipid)) of PLFE LUVs changes from 3.59 × 10(-10) Pa(-1) at 25°C to 4.08 × 10(-10) Pa(-1) at 78°C. Volume fluctuations of PLFE LUVs change only 0.25% from 30°C to 80°C. The highly damped volume fluctuations and their low temperature sensitivity, echo that PLFE liposomes are rigid and tightly packed. To our knowledge, the data provide a deeper understanding of lipid packing in PLFE liposomes than has been previously reported, as well as a molecular

  18. Simulation, microstructure and microhardness of the nano-SiC coating formed on Al surface via laser shock processing

    International Nuclear Information System (INIS)

    Highlights: • Nano-SiC coating is successfully fabricated on pure Al surface via LSPC. • Movement states of the nano-SiC particles are analyzed by FEM. • Formation mechanism of the nano-SiC coating is put forward and discussed. • Microhardness of the Al is significantly improved due to the nano-SiC coating. - Abstract: A novel method, laser shock processing coating (LSPC), has been developed to fabricate a particle-reinforced coating based on laser shock processing (LSP). In this study, a nano-SiC coating is successfully prepared on pure Al surface via LSPC. The surface and cross section morphologies as well as the compositions of nano-SiC coating are investigated. Moreover, a finite element method (FEM) is employed to clarify the formation process of nano-SiC coating. On the basis of the above analyzed results, a possible formation mechanism of the nano-SiC coating is tentatively put forward and discussed. Furthermore, the nano-SiC coating shows superior microhardness over the Al substrate

  19. Surface Grafting of Polymers onto Nano-Sized Particles in Solvent-Free Dry-System and in Ionic Liquid

    Institute of Scientific and Technical Information of China (English)

    Norio TSUBOKAWA

    2005-01-01

    @@ 1Introduction We have reported the grafting of various polymers onto the surface of inorganic nano-sized particles, such as silica, titanium oxide, and carbon black[1]. The polymer-grafted nano-sized particles are known to have excellent properties, such as a good dispersibility in solvents and polymer matrices[1,2]. However, scale-up production of polymer-grafted nano-sized particles was hardly achieved, because complicated procedures, such as centrifugation, filtration, and solvent extraction, are needed for the production of polymer-grafted nano-sized particles, and a lot of abolishing solvent comes out.

  20. Local Electronic And Dielectric Properties at Nanosized Interfaces

    Energy Technology Data Exchange (ETDEWEB)

    Bonnell, Dawn A. [Univ. of Pennsylvania, Philadelphia, PA (United States)

    2015-02-23

    Final Report to the Department of Energy for period 6/1/2000 to 11/30/2014 for Grant # DE-FG02-00ER45813-A000 to the University of Pennsylvania Local Electronic And Dielectric Properties at Nanosized Interfaces PI: Dawn Bonnell The behavior of grain boundaries and interfaces has been a focus of fundamental research for decades because variations of structure and composition at interfaces dictate mechanical, electrical, optical and dielectric properties in solids. Similarly, the consequence of atomic and electronic structures of surfaces to chemical and physical interactions are critical due to their implications to catalysis and device fabrication. Increasing fundamental understanding of surfaces and interfaces has materially advanced technologies that directly bear on energy considerations. Currently, exciting developments in materials processing are enabling creative new electrical, optical and chemical device configurations. Controlled synthesis of nanoparticles, semiconducting nanowires and nanorods, optical quantum dots, etc. along with a range of strategies for assembling and patterning nanostructures portend the viability of new devices that have the potential to significantly impact the energy landscape. As devices become smaller the impact of interfaces and surfaces grows geometrically. As with other nanoscale phenomena, small interfaces do not exhibit the same properties as do large interfaces. The size dependence of interface properties had not been explored and understanding at the most fundamental level is necessary to the advancement of nanostructured devices. An equally important factor in the behavior of interfaces in devices is the ability to examine the interfaces under realistic conditions. For example, interfaces and boundaries dictate the behavior of oxide fuel cells which operate at extremely high temperatures in dynamic high pressure chemical environments. These conditions preclude the characterization of local properties during fuel cell

  1. INTRANASAL LIPOSOMES : AN APPROACH FOR DRUG DELIVERY TO BRAIN

    Directory of Open Access Journals (Sweden)

    Mr. Jatin B. Trivedi

    2012-05-01

    Full Text Available Targeting drug molecules to brain is one of the most challenging research areas in pharmaceuticalsciences. Drugs that are effective against diseases in the CNS and reach the brain via the bloodcompartment must pass the BBB. The blood-brain barrier (BBB represents an insurmountable obstaclefor a large number of drugs, including antibiotics, anti-neoplastic agents, and a variety of central nervoussystem (CNS-active drugs. Therefore, various strategies have been proposed to improve the delivery ofdifferent drugs to this tissue which includes liposomes, colloidal drug carriers, micelles, chimericpeptide technology, intranasal and olfactory route of administration and nano technology. The discoveryof liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon hydration; liposomedrug delivery systems have played a significant role in formulation of potent drug to improvetherapeutics Liposomes have been investigated as carriers of various pharmacologically active agentssuch as antineoplastic, antimicrobial drugs, chelating agents, steroids, vaccines, and genetic materials.Liposomes provide an efficient drug delivery system because they can alter the pharmacokinetics andpharmacodynamics of the entrapped drugs. Liposomes have been widely used for brain delivery in vivo.Nowadays, the nasal route for systemic drug delivery has gained great interest. It provides severaladvantages over other routes of drug administrations, which includes rapid absorption, avoids intestinaland hepatic presystemic disposition and high potential for drug transfer to the CSF. Moreover, the nasalroute is a potential alternative route for systemic availability of drugs restricted to intravenousadministration, viz. peptide and protein drugs and vaccines. As well, intranasal route has also beensuccessfully exploited for bypassing the blood brain barrier [BBB] and subsequently delivering drugmolecules to central nervous system [CNS].

  2. Silica-based monolithic capillary columns modified by liposomes for characterization of analyte–liposome interactions by capillary liquid chromatography

    Czech Academy of Sciences Publication Activity Database

    Moravcová, Dana; Planeta, Josef; Wiedmer, S. K.

    2013-01-01

    Roč. 1317, SI (2013), s. 159-166. ISSN 0021-9673 R&D Projects: GA MV VG20112015021; GA ČR(CZ) GAP206/11/0138 Institutional support: RVO:68081715 Keywords : monolithic silica capillary column * immobilized liposomes * biomimicking stationary phase Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 4.258, year: 2013

  3. Silica-based monolithic capillary columns modified by liposomes for characterization of analyte-liposome interactions by capillary liquid chromatography

    Czech Academy of Sciences Publication Activity Database

    Moravcová, Dana; Planeta, Josef; Wiedmer, S. K.

    2013. P-269-W. [International Symposium on Capillary Chromatography /37./ and GC×GC Symposium /10./. 12.05.2013-16.05.2013, Palm Springs] R&D Projects: GA ČR(CZ) GAP206/11/0138; GA MV VG20112015021 Institutional support: RVO:68081715 Keywords : monolithic silica capillary column * immobilized liposomes * biomimicking stationary phase Subject RIV: CB - Analytical Chemistry, Separation

  4. A targeting drug-delivery model via interactions among cells and liposomes under ultrasonic excitation

    International Nuclear Information System (INIS)

    In our previous work, it was found that acoustic cavitation might play a role in improving the cell permeability to microparticles when liposomes were used in an in vitro experiment. The purpose of this project is to expand our study and to learn other possible mechanisms by which cells may interact with liposomes under ultrasound (US) excitation and become transiently permeable to microparticles. It is further hypothesized that two possible scenarios may be involved in in vitro experiments: (1) drug-carrying liposomes transiently overcome the cell membrane barrier and enter into a cell while the cell is still viable; (2) the liposomes incorporate with a cell at its membrane through a fusing process. To prove this hypothesis, liposomes of two different structures were synthesized: one has fluorescent molecules encapsulated into liposomes and the other has fluorescent markers incorporated into the shells of liposomes. Liposomes of each kind were mixed with human breast cancer cells (MCF7-cell line) in a suspension at 5 (liposomes) : 1 (cell) ratio and were then exposed to a focused 1 MHz ultrasound beam at its focal region for 40 s. The US signal contained 20 cycles per tone-burst at a pulse-repetition-frequency of 10 kHz; the spatial peak acoustic pressure amplitude was 0.25 MPa. It was found that the possible mechanisms might include the acoustic cavitation, the endocytosis and cell-fusion. Acoustic radiation force might make liposomes collide with cells effectively and facilitate the delivery process

  5. An evaluation of anti-tumor effect and toxicity of PEGylated ursolic acid liposomes

    International Nuclear Information System (INIS)

    Therapy of solid tumors mediated by nano-drug delivery has attracted considerable interest. In our previous study, ursolic acid (UA) was successfully encapsulated into PEGylated liposomes. The study aimed to evaluate the tumor inhibition effect and cytotoxicity of the PEGylated UA liposomes by U14 cervical carcinoma-bearing mice. The liposomes were spherical particles with mean particle diameters of 127.2 nm. The tumor inhibition rate of PEGylated UA liposomes was 53.60 % on U14 cervical carcinoma-bearing mice, which was greater than those of the UA solution (18.25 %) and traditional UA liposome groups (40.75 %). The tumor cells apoptosis rate of PEGylated UA liposomes was 25.81 %, which was significantly higher than that of the traditional UA liposomes (13.37 %). Moreover, the kidney and liver did not emerge the pathological changes in UA therapeutic mice by histopathological analysis, while there were significant differences on tumor tissues among three UA formulation groups. The PEGylated UA liposomes exhibited higher anti-tumor activity and lower cytotoxicity, and the main reason was that the coating PEG layer improved UA liposome properties, such as enhancing the stability of liposomes, promoting the effect of slow release, and prolonging the time of blood circulation. This may shed light on the development of PEGylated nano-vehicles.

  6. Superresolution and Fluorescence Dynamics Evidence Reveal That Intact Liposomes Do Not Cross the Human Skin Barrier.

    Directory of Open Access Journals (Sweden)

    Jes Dreier

    Full Text Available In this study we use the combination of super resolution optical microscopy and raster image correlation spectroscopy (RICS to study the mechanism of action of liposomes as transdermal drug delivery systems in human skin. Two different compositions of liposomes were applied to newly excised human skin, a POPC liposome and a more flexible liposome containing the surfactant sodium cholate. Stimulated emission depletion microscopy (STED images of intact skin and cryo-sections of skin treated with labeled liposomes were recorded displaying an optical resolution low enough to resolve the 100 nm liposomes in the skin. The images revealed that virtually none of the liposomes remained intact beneath the skin surface. RICS two color cross correlation diffusion measurements of double labeled liposomes confirmed these observations. Our results suggest that the liposomes do not act as carriers that transport their cargo directly through the skin barrier, but mainly burst and fuse with the outer lipid layers of the stratum corneum. It was also found that the flexible liposomes showed a greater delivery of the fluorophore into the stratum corneum, indicating that they functioned as chemical permeability enhancers.

  7. Superresolution and Fluorescence Dynamics Evidence Reveal That Intact Liposomes Do Not Cross the Human Skin Barrier.

    Science.gov (United States)

    Dreier, Jes; Sørensen, Jens A; Brewer, Jonathan R

    2016-01-01

    In this study we use the combination of super resolution optical microscopy and raster image correlation spectroscopy (RICS) to study the mechanism of action of liposomes as transdermal drug delivery systems in human skin. Two different compositions of liposomes were applied to newly excised human skin, a POPC liposome and a more flexible liposome containing the surfactant sodium cholate. Stimulated emission depletion microscopy (STED) images of intact skin and cryo-sections of skin treated with labeled liposomes were recorded displaying an optical resolution low enough to resolve the 100 nm liposomes in the skin. The images revealed that virtually none of the liposomes remained intact beneath the skin surface. RICS two color cross correlation diffusion measurements of double labeled liposomes confirmed these observations. Our results suggest that the liposomes do not act as carriers that transport their cargo directly through the skin barrier, but mainly burst and fuse with the outer lipid layers of the stratum corneum. It was also found that the flexible liposomes showed a greater delivery of the fluorophore into the stratum corneum, indicating that they functioned as chemical permeability enhancers. PMID:26751684

  8. Sorafenib and gadolinium co-loaded liposomes for drug delivery and MRI-guided HCC treatment.

    Science.gov (United States)

    Xiao, Yanan; Liu, Yongjun; Yang, Shaomei; Zhang, Bo; Wang, Tianqi; Jiang, Dandan; Zhang, Jing; Yu, Dexin; Zhang, Na

    2016-05-01

    To improve the poor water solubility of sorafenib and to monitor its distribution and the early feedback effects on its in vivo treatment efficacy in a precise manner, sorafenib (SF) and gadolinium (Gd) co-loaded liposomes (SF/Gd-liposomes) were prepared. The simultaneous imaging and therapy efficacies of the SF/Gd-liposomes were tested. The solubility of SF in SF/Gd-liposomes was significantly increased from 0.21μg/mL to 250μg/mL. The imaging capability of SF/Gd-liposomes were tested by in-vitro and the in-vivo imaging ability tests and the results confirmed that SF/Gd-liposomes could be served as an effective contrast agent. The design of SF/Gd-liposomes allowed the MRI-guided in vivo visualization of the delivery and biodistribution of liposome. In the in vivo antitumor studies, SF/Gd-liposomes had better antitumor effects in H22 tumor-bearing mice than SF solution (oral or i.v. administration) (P<0.05). These findings indicated that the SF/Gd-liposomes could be used as the promising nano-carriers for the MRI-guided in vivo visualization of the delivery and HCC treatment. PMID:26844644

  9. Effects of chitosan coating on physical properties and pharmacokinetic behavior of mitoxantrone liposomes.

    Science.gov (United States)

    Zhuang, Jie; Ping, Qineng; Song, Yunmei; Qi, Jianping; Cui, Zheng

    2010-01-01

    The objective of this work was to evaluate the physical properties and in vivo circulation of chitosan (CH)-coated liposomes of mitoxantrone (MTO). Changes in particle size and zeta potential confirmed the existence of a coating layer on the surface of liposomes. The in vitro release of adsorbed CH from the liposomes was significantly slower than CH solution, indicating the stable interaction between CH and liposomes. The physical stability of the CH-coated liposomes was evaluated by measuring the change in particle size before and after freeze-drying and rehydration. The smallest change was observed when saturated adsorption of CH occurred (0.3%). The sustained release in vitro of MTO from CH-coated liposomes confirmed the increased stability of liposomes. Systemic circulation of CH-coated MTO liposomes was examined. The 0.3% CH-coated liposomes showed the longest circulation time. It could be concluded that the prolonged retention time of the liposomes was closely related with CH coating and its stability effect. PMID:20957162

  10. Anti-Cancer Efficacy of Paclitaxel Loaded in pH Triggered Liposomes.

    Science.gov (United States)

    Jiang, Lei; He, Bin; Pan, Dayi; Luo, Kui; Yi, Qiangying; Gu, Zhongwei

    2016-01-01

    Smart liposomes that are responsive to the microenvironment of tumor tissue have been utilized to enhance chemotherapeutic efficiency. Here, we reported a novel liposome called Trojan horse liposome, which has a pH response, to enhance drug accumulation in tumor sites and intercellular uptake. L-lysine was used as a linker to connect 2,3-dimethylmaleic anhydride (DMA) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE) to yield a DSPE-Lys-DMA (DLD) lipid. The pH-responsive DLD was mixed with other commercially available lipids to form liposomes. The size, morphology and zeta potential of the DLD liposomes (DLD-Lip) were measured. Paclitaxel (PTX) was loaded in the liposomes. The release profile, cellular uptake, in vitro and in vivo anticancer activity of the PTX-loaded liposomes were investigated. The results showed that the mean diameter of the liposomes was less than 200 nm. The zeta potential of the liposomes was negative at pH 7.4. However, it was transferred to positive at weak acidic pH values with the cleavage of DMA amide. The charge reversion of DMA in acidic environments facilitated the cellular internalization and endosome escape of DLD-Lip, which inhibited the proliferation of 4T1 cancer cells in vitro. The pH-responsive "Trojan horse"-like liposomes also exhibited efficient anticancer activity in the xenograft breast cancer model in vivo. PMID:27301174

  11. Indocyanine Green-Loaded Liposomes for Light-Triggered Drug Release.

    Science.gov (United States)

    Lajunen, Tatu; Kontturi, Leena-Stiina; Viitala, Lauri; Manna, Moutusi; Cramariuc, Oana; Róg, Tomasz; Bunker, Alex; Laaksonen, Timo; Viitala, Tapani; Murtomäki, Lasse; Urtti, Arto

    2016-06-01

    Light-triggered drug delivery systems enable site-specific and time-controlled drug release. In previous work, we have achieved this with liposomes containing gold nanoparticles in the aqueous core. Gold nanoparticles absorb near-infrared light and release the energy as heat that increases the permeability of the liposomal bilayer, thus releasing the contents of the liposome. In this work, we replaced the gold nanoparticles with the clinically approved imaging agent indocyanine green (ICG). The ICG liposomes were stable at storage conditions (4-22 °C) and at body temperature, and fast near-infrared (IR) light-triggered drug release was achieved with optimized phospholipid composition and a 1:50 ICG-to-lipid molar ratio. Encapsulated small molecular calcein and FITC-dextran (up to 20 kDa) were completely released from the liposomes after light exposure for 15 s. Location of ICG in the PEG layer of the liposomes was simulated with molecular dynamics. ICG has important benefits as a light-triggering agent in liposomes: fast content release, improved stability, improved possibility of liposomal size control, regulatory approval to use in humans, and the possibility of imaging the in vivo location of the liposomes based on the fluorescence of ICG. Near-infrared light used as a triggering mechanism has good tissue penetration and safety. Thus, ICG liposomes are an attractive option for light-controlled and efficient delivery of small and large drug molecules. PMID:27097108

  12. An evaluation of anti-tumor effect and toxicity of PEGylated ursolic acid liposomes

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Qianqian; Zhao, Tingting; Liu, Yanping; Xing, Shanshan; Li, Lei; Gao, Dawei, E-mail: dwgao@ysu.edu.cn [Yanshan University, Applying Chemistry Key Lab of Hebei Province, Department of Bioengineer (China)

    2016-02-15

    Therapy of solid tumors mediated by nano-drug delivery has attracted considerable interest. In our previous study, ursolic acid (UA) was successfully encapsulated into PEGylated liposomes. The study aimed to evaluate the tumor inhibition effect and cytotoxicity of the PEGylated UA liposomes by U14 cervical carcinoma-bearing mice. The liposomes were spherical particles with mean particle diameters of 127.2 nm. The tumor inhibition rate of PEGylated UA liposomes was 53.60 % on U14 cervical carcinoma-bearing mice, which was greater than those of the UA solution (18.25 %) and traditional UA liposome groups (40.75 %). The tumor cells apoptosis rate of PEGylated UA liposomes was 25.81 %, which was significantly higher than that of the traditional UA liposomes (13.37 %). Moreover, the kidney and liver did not emerge the pathological changes in UA therapeutic mice by histopathological analysis, while there were significant differences on tumor tissues among three UA formulation groups. The PEGylated UA liposomes exhibited higher anti-tumor activity and lower cytotoxicity, and the main reason was that the coating PEG layer improved UA liposome properties, such as enhancing the stability of liposomes, promoting the effect of slow release, and prolonging the time of blood circulation. This may shed light on the development of PEGylated nano-vehicles.

  13. PEG modification on 111In-labeled phosphatidyl serine liposomes for imaging of atherosclerotic plaques

    International Nuclear Information System (INIS)

    Introduction: Previously, we reported a probe for imaging of atherosclerotic plaques: 111In-labeled liposomes. Liposomes were modified with phosphatidylserine (PS) because macrophages recognize PS and phagocytize apoptotic cells in plaques. PS modification was successful and we could visualize atherosclerotic plaques by single-photon emission computed tomography (SPECT). However, too-rapid blood clearance reduced accumulation of PS-liposomes in plaques in vivo. Therefore, in the present study, PS-liposomes were modified with polyethylene glycol (PEG) to retard the rate of blood clearance. Methods: PS-liposomes (size, 100 nm or 200 nm) were PEGylated with PEG2000 or PEG5000 at 1 or 5 mol%, and radiolabeled with 111In. For the study of uptake in vitro, liposomes were incubated with mouse peritoneal macrophages. Biodistribution studies in vivo were carried out in ddY mice. En face autoradiograms were obtained with apoE−/− mice upon intravenous injection of 111In-liposomes. Results: Uptake was decreased significantly at 5 mol% PEGylation in 100-nm PS-liposomes (*P < 0.05 vs. 0 mol%). All the PEGylated liposomes tested showed significantly lower uptake than the non-PEGylated control in 200-nm liposomes. In vivo results showed slower blood clearance in PEGylated liposomes. Autoradiograms in apoE−/− mice were well matched with Oil Red O staining. Additionally, 200-nm PS-liposomes modified with 5%PEG2000 ([111In]5%PEG2000PS200) showed the highest uptake to the region in vivo. Conclusions: As expected, PEGylation retarded the rate of blood clearance. In addition, it affected liposome uptake by macrophages in vitro. These results suggest that the balance between the rate of blood clearance and macrophage recognition is important, and [111In]5%PEG2000PS200 showed the best results in our investigation

  14. Resuscitation Using Liposomal Vasopressin in an Animal Model of Uncontrolled Hemorrhagic Shock.

    Directory of Open Access Journals (Sweden)

    Meng-Tse Gabriel Lee

    Full Text Available Current research suggests that administration of vasopressin to patients with uncontrolled hemorrhagic shock (UHS can avoid the detrimental effects associated with aggressive fluid resuscitation. However, vasopressin has a short half-life of 10~35 minutes in in vivo use and precludes its use in the pre-hospital setting. To increase the half-life of vasopressin, we proposed to synthesize liposome-encapsulated vasopressin and test it in a rat model of UHS.The film hydration method was used to prepare liposomal vasopressin consisting of: Dipalmitoylphosphatidylcholine, cholesterol, and dipalmitoyl phosphatidylethanolamine (20:20:1 mole ratio. 42 rats were subjected to UHS and randomly received 5 different treatments (vasopressin, liposomal vasopressin, lactate ringer (LR, liposome only and sham. Outcome of UHS were measured using 4 common prognostic tests: mean arterial pressure (MAP, serum lactate level, inflammatory profile and pulmonary edema.The dynamic light scattering results confirmed that we had prepared a successful liposomal vasopressin complex. Comparing the serum vasopressin concentration of liposomal vasopressin and vasopressin treated animals by ELISA, we found that the concentration of vasopressin for the liposomal vasopressin treated group is higher at 60 minutes. However, there was no significant difference between the MAP profile of rats treated with vasopressin and liposomal vasopressin in UHS. We also observed that animals treated with liposomal vasopressin performed indifferently to vasopressin treated rats in serum lactate level, inflammatory profile and edema profile. For most of our assays, the liposome only control behaves similarly to LR resuscitation in UHS rats.We have synthesized a liposomal vasopressin complex that can prolong the serum concentration of vasopressin in a rat model of UHS. Although UHS rats treated with either liposomal vasopressin or vasopressin showed no statistical differences, it would be worthwhile

  15. Nano-sized ceria particles prepared by spray pyrolysis using polymeric precursor solution

    International Nuclear Information System (INIS)

    Nano-sized ceria particles were prepared from the aqueous solution containing the polymeric precursors by ultrasonic spray pyrolysis at the severe preparation conditions such as high flow rate of carrier gas and short residence time. The key idea to produce nanoparticles was to prepare hollow ceria particles which are easily turned to aggregates of nano-sized primary particles during the post-thermal treatment and thereafter disintegrate such aggregates to nano-sized particles by a simple ball milling process. It was found that using the polymeric precursor strongly influences the crystallization characteristics and morphological changes of the as-prepared particles during the post-thermal treatment. The as-prepared particles prepared from the polymeric precursor solution had non-spherical shape and fractured structure with a thin shell, whereas the as-prepared and calcined ceria particles obtained from the aqueous solution had spherical shape and hollow morphology with a thick shell. Also, nano-sized ceria particles prepared from the polymeric precursor solution had less aggregated structure than those prepared from the aqueous solution. For the ceria particles prepared from the polymeric precursor solution, the degree of aggregation between the primary particles was reduced as increasing the calcination temperature. As a result, aggregation-free nano-sized ceria particles were obtained above 1200 deg. C without a milling process. The mean size of the primary particles increased from several tens nanometer to submicrometer size as the calcination temperature changed from 800 to 1300 deg. C

  16. Expansion of colloid and surface chemistry to an interdisciplinary field. Biosimulation by liposome; Koroido kaimen kagaku wa gakusai ryoiki ni hirogaru. Liposome wo mochiite saibo kino ni semaru

    Energy Technology Data Exchange (ETDEWEB)

    Akiyoshi, K. [Kyoto University, Kyoto (Japan)

    1998-07-01

    This paper presents the usefulness of an approach using liposome as cell surface model system (biosimulation by liposome) for clarifying the cell control function of glycolipid. The author and others systematically studied the influence of the aggregation state of ganglioside glycochains on a liposome surface on adhesion and stimulus to cells. Study was also made on the interaction between DPPC liposome including ganglioside and immunocyte, in particular, T cell including an acceptor for glycochains. The interaction was evaluated by laser fluorescence microscope, and an increase in Ca concentration in cells was detected and evaluated by fluorescence probe. An activating rate was also evaluated by counting the number of stimulated cells among nearly 200 cells. As the study result on a degree of adsorption of liposome as fluorescence marker to cells, active systems were strongly adsorbed on cell surfaces, suggesting that signals are transmitted in cells after coupling of active systems with acceptors on cell surfaces. 10 refs., 5 figs.

  17. Incrusting structure of nanosized Fe3O4 particles in magnetic fluids

    Institute of Scientific and Technical Information of China (English)

    张金升; 尹衍升; 吕忆农; 张银燕; 马来鹏; 张淑卿

    2003-01-01

    High-performance nanosized Fe3O4 magnetic fluids are prepared by chemical co-pre- cipitate method. The microstructure of magnetic fluids is characterized using a transmission electron microscope (TEM) and high-resolution electron microscope (HREM). The results are satisfactory. The nanosized magnetic particles have diameter of 8-10 nm and the minimum diameter is 4 nm, belonging to super-paramagnetic material. The nanosized magnetic particles crystallized completely and have clear crystal boundary. The surfactant used in the test coats the magnetic particles homogeneously and forms a uniform and complete elastic spherical shell of amorphous phase around the magnetic particles. The study proves that the incrusting layer of surfactant has the protective effect and stable effect on the magnetic particles. These effects can enhance and maintain the magnetic properties of the magnetic fluids effectively.

  18. Nanosized aluminum nitride hollow spheres formed through a self-templating solid-gas interface reaction

    International Nuclear Information System (INIS)

    Nanosized aluminum nitride hollow spheres were synthesized by simply heating aluminum nanoparticles in ammonia at 1000 deg. C. The as-synthesized sphere shells are polycrystalline with cavity diameters ranging from 15 to 100 nm and shell thickness from 5 to 15 nm. The formation mechanism can be explained by the nanoscale Kirkendall effect, which results from the difference in diffusion rates between aluminum and nitrogen. The Al nanoparticles served as both reactant and templates for the hollow sphere formation. The effects of precursor particle size and temperature were also investigated in terms of product morphology. Room temperature cathode luminescence spectrum of the nanosized hollow spheres showed a broad emission band centered at 415 nm, which is originated from oxygen related luminescence centers. The hollow structure survived a 4-h heat treatment at 1200 deg. C, exhibiting excellent thermal stability. - Graphical abstract: Nanosized aluminum nitride hollow spheres were synthesized by nitridation of aluminum nanoparticles at 1000 deg. C using ammonia

  19. Preparation and properties of nanosize MnZn ferrite from δ-FeOOH

    Institute of Scientific and Technical Information of China (English)

    HAO Shunli; WANG Xin; WEI Yu; Wang Yongming; Liu Chunjing

    2006-01-01

    Ferrous ion was transformed into feroxyhyte (δ-FeOOH) by oxidation. Then, manganese sulfate and zinc sulfate in some ratio were added to the feroxyhyte solution. The co-precipitation was boiling reflux conditions sometime under constant stirring. The nanosize MnZn ferrite powder was formed. The mechanism of preparation of the nanosize MnZn ferrite was discussed, and the formation of feroxyhyte which was playing a key role during the process was mentioned. The properties of powder was tested by means of X-ray diffraction, transmission electron microscopy and vibrating sample magnetometer. The results show that the samples of spherical particles about 20 nm, which have characteristics of ferrimagnetism, has larger saturation magnetization, but the remanent magnetization and coercivity are comparatively smaller. The spinel MnZn ferrite nanosize powder was successfully prepared from δ-FeOOH at low temperature, with low-carbon steel and peroxide as main material.

  20. Effects of nanosized metallic palladium loading and calcination on characteristics of composite silica

    Institute of Scientific and Technical Information of China (English)

    吴玉程; 吴侠; 李广海; 张立德

    2003-01-01

    In order to investigate the effects of nanosized metallic palladium loading and calcination on the characteristics of composite silica,the silica was prepared by sol-gel technique,leading to an amorphous solid with mesoporosity,and the pore size distribution is narrow,centered at 3-5 nm.The composite silica was formed by impregnating palladium precursor into the porous network with sequel calcination in hydrogen.The results show that the nanosized palladium as guest phase in the composite silica is subjected to the mesoporous structure and calcination,resulting in the changes of optical adsorption that red-shifted to higher wavelength with the palladium loading and the heating temperature.The tailoring of the optical properties can be ascribed to the effect of the nanosized metal particles and interactions occurred between palladium and silica.

  1. Study of Surface Cell Madelung Constant and Surface Free Energy of Nanosized Crystal Grain

    Institute of Scientific and Technical Information of China (English)

    ZHANG Wei-Jia; WANG Tian-Min; CUI Min

    2005-01-01

    Surface cell Madelung constant is firstly defined in calculating surface free energy of nanosized crystal grains, which explains the physical performance of small crystals and may be great benefit to make surface analysis and study dynamics of crystal nucleus growth. A new ap- proximative expression of surface energy and relevant thermodynamic data was used in this cal- culation. A new formula and computing method for calculating the Madelung constant α of any complex crystals is proposed, and surface free energies and surface electrostatic energies of nano- sized crystal grains as well as Madelung constant of some complex crystals are theoretically cal- culated in this paper. The surface free energy of nanosized crystal grain TiO2 and surface elec- trostatic energy(absolute value) of nanosized crystal grain α-Al2O3 are found to be the biggest among other crystal grains.

  2. Simple routes to synthesis and characterization of nanosized tin telluride compounds

    Energy Technology Data Exchange (ETDEWEB)

    Salavati-Niasari, Masoud, E-mail: salavati@kashanu.ac.ir [Institute of Nano Science and Nano Technology, University of Kashan, Kashan, P.O. Box. 87317-51167 (Iran, Islamic Republic of); Department of Inorganic Chemistry, Faculty of Chemistry, University of Kashan, Kashan, P.O. Box. 87317-51167 (Iran, Islamic Republic of); Bazarganipour, Mehdi [Department of Inorganic Chemistry, Faculty of Chemistry, University of Kashan, Kashan, P.O. Box. 87317-51167 (Iran, Islamic Republic of); Davar, Fatemeh [Institute of Nano Science and Nano Technology, University of Kashan, Kashan, P.O. Box. 87317-51167 (Iran, Islamic Republic of); Fazl, Alireza Amini [Institute for Colorants, Paint and Coatings (ICPC), Tehran, P.O. Box. 16765/654 (Iran, Islamic Republic of)

    2010-11-15

    Nanosized tin telluride compounds were prepared by chemical reduction process and hydrothermal methods. The nanosized SnTe compounds were characterized by means of X-ray diffraction (XRD), scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The SnTe nanoalloy prepared by chemical reduction process presented quasi-spherical morphology with aggregation. The sizes of particle were 40-50 nm. The powder prepared by hydrothermal process was nearly nanospheres, and the particle sizes were 30-40 nm with narrow distribution. The effect of capping agent, reductant sort, and reaction temperature on the morphology, the particle sizes and the phase of SnTe alloys have been investigated. Experimental results indicated that N{sub 2}H{sub 4}.H{sub 2}O plays a crucial role in the formation of nanosized rode-like SnTe compounds.

  3. Inhibitory effect of liposome-entrapped lemongrass oil on the growth of Listeria monocytogenes in cheese.

    Science.gov (United States)

    Cui, H Y; Wu, J; Lin, L

    2016-08-01

    Listeria monocytogenes infection in dairy products is of mounting public concern. To inhibit bacterial growth, we engineered stimuli-responsive liposomes containing lemongrass oil for this study. The controlled release of liposome-entrapped lemongrass oil is triggered by listerolysin O, secreted by L. monocytogenes. We investigated the antibiotic activities of lemongrass oil liposomes against L. monocytogenes in cheese. We also assessed their possible effects on the quality of the cheese. Liposomes containing lemongrass oil (5.0mg/mL) presented the optimal polydispersity index (0.246), zeta-potential (-58.9mV) and entrapment efficiency (25.7%). The liposomes displayed satisfactory antibiotic activity against L. monocytogenes in cheese over the storage period at 4°C. We observed no effects on the physical and sensory properties of the cheese after the liposome treatment. PMID:27265173

  4. Evaluation of skin viability effect on ethosome and liposome-mediated psoralen delivery via cell uptake.

    Science.gov (United States)

    Zhang, Yong-Tai; Shen, Li-Na; Wu, Zhong-Hua; Zhao, Ji-Hui; Feng, Nian-Ping

    2014-10-01

    This study investigated the effect of skin viability on its permeability to psoralen delivered by ethosomes, as compared with liposomes. With decreasing skin viability, the amount of liposome-delivered psoralen that penetrated through the skin increased, whereas skin deposition of psoralen from both ethosomes and liposomes reduced. Psoralen delivery to human-immortalized epidermal cells was more effective using liposomes, whereas delivery to human embryonic skin fibroblast cells was more effective when ethosomes were used. These findings agreed with those of in vivo studies showing that skin psoralen deposition from ethosomes and liposomes first increased and then plateaued overtime, which may indicate gradual saturation of intracellular drug delivery. It also suggested that the reduced deposition of ethosome- or liposome-delivered psoralen in skin with reduced viability may relate to reduced cellular uptake. This work indicated that the effects of skin viability should be taken into account when evaluating nanocarrier-mediated drug skin permeation. PMID:25070929

  5. Structure of liposome encapsulating proteins characterized by X-ray scattering and shell-modeling

    Energy Technology Data Exchange (ETDEWEB)

    Hirai, Mitsuhiro, E-mail: mhirai@gunma-u.ac.jp; Kimura, Ryota; Takeuchi, Kazuki; Hagiwara, Yoshihiko [Gunma University, 4-2 Aramaki, Maebashi, Gunma 371-8510 (Japan); Kawai-Hirai, Rika [Gunma University, 3-39-15 Shouwa, Maebashi 371-8512 (Japan); Ohta, Noboru [JASRI, 1-1-1 Kuoto, Sayo-cho, Sayo-gun, Hyogo 679-5198 (Japan); Igarashi, Noriyuki; Shimuzu, Nobutaka [KEK-PF, 1-1 Oho, Tsukuba, Ibaraki 305-0801 (Japan)

    2013-11-01

    Wide-angle X-ray scattering data using a third-generation synchrotron radiation source are presented. Lipid liposomes are promising drug delivery systems because they have superior curative effects owing to their high adaptability to a living body. Lipid liposomes encapsulating proteins were constructed and the structures examined using synchrotron radiation small- and wide-angle X-ray scattering (SR-SWAXS). The liposomes were prepared by a sequential combination of natural swelling, ultrasonic dispersion, freeze-throw, extrusion and spin-filtration. The liposomes were composed of acidic glycosphingolipid (ganglioside), cholesterol and phospholipids. By using shell-modeling methods, the asymmetric bilayer structure of the liposome and the encapsulation efficiency of proteins were determined. As well as other analytical techniques, SR-SWAXS and shell-modeling methods are shown to be a powerful tool for characterizing in situ structures of lipid liposomes as an important candidate of drug delivery systems.

  6. Cardanol as a replacement for cholesterol into the lipid bilayer of POPC liposomes.

    Science.gov (United States)

    De Maria, Paolo; Filippone, Paolino; Fontana, Antonella; Gasbarri, Carla; Siani, Gabriella; Velluto, Diana

    2005-01-15

    Large unilamellar liposomes were prepared by hydration of 1-palmitoyl-2-oleylphosphatydilcholine (POPC) films and subsequent extrusion of the obtained liposomal suspension. Inclusion of cholesterol and cardanol brings about a stabilization of the membranes of the liposomes, as determined by their rates of release of entrapped 5(6)-carboxyfluorescein. The liposome breakdown was promoted by a non-ionic surfactant (Triton X-100) and the kinetic measurements were carried out by fluorimetry in water at 25 degrees C. Morphological analyses of giant POPC liposomes in the presence and in the absence of both guests were also performed. The results obtained suggest the use of cardanol (an easy available natural product) as a replacement for cholesterol as a new possibility for stabilizing liposomes in drug targetting. PMID:15620834

  7. Tumor growth suppression by boron neutron capture therapy using PEG-liposomal boron delivery in vivo

    International Nuclear Information System (INIS)

    The tumor cell destruction in boron neutron-capture therapy (BNCT) is due to the nuclear reaction between 10B and thermal neutrons. We prepare a polyethylene glycol (PEG) binding liposome (DPPC/cholesterol/DSPC-PEG2000) entrapped 10B compound for the delivery system. We evaluated the cytotoxic effects of intravenously injected 10B-PEG-liposome on human pancreatic carcinoma (AsPC-1) xenografts in nude mice with thermal neutron irradiation. After thermal neutron irradiation of mice injected with 10B-bare liposome or 10B-PEG-liposome, AsPC-1 tumour growth was suppressed relative to controls. Injection of 10B-PEG-liposome caused the greatest tumour suppression with thermal neutron irradiation in vivo. These results suggests that intravenous injection of 10B-PEG-liposome can increase the retention of 10B atoms by tumor cells, causing tumor growth suppression in vivo upon thermal neutron irradiation. (author)

  8. Biodistribution and characterization of radiolabeled liposomal DTPA for heavy metal radionuclide decorporation

    International Nuclear Information System (INIS)

    Biodistribution of neutral and positively charged liposomes encapsulated with 99mTc-labeled DTPA was studied in experimental animal model. Unilamellar liposomes were prepared by thin film hydration method following sonication. 99mTc-labeled DTPA encapsulated in neutral and positively charged liposomes were composed of DPPC: cholestrol (molar ratio 7:3) and DPPC:cholestrol:stearylamine (molar ratio 7:2:0.5) respectively. The percentage encapsulation of 99mTc-labeled DTPA was found ∼ 8-9%. The average molecular dimension of these liposomes were about 180 nm as measured by dynamic light scattering method. Animals were randomized in three different groups each having 5 rats: free DTPA ii) positively charged liposomes encapsulated with 99mTc-labeled DTPA iii) neutral liposomes encapsulated with 99mTc-labeled DTPA

  9. Cancer gene therapy utilized ultrasound (US)-sensitive liposome as non-viral vector

    Science.gov (United States)

    Suzuki, Ryo; Oda, Yusuke; Namai, Eisuke; Nishiie, Norihito; Hirata, Keiichi; Taira, Yuichiro; Utoguchi, Naoki; Negichi, Yoichi; Maruyama, Kazuo

    2010-03-01

    Sonoporation is an attractive technique to develop non-invasive and non-viral gene delivery system. However, simple sonoporation using only ultrasound (US) is not enough to establish effective cancer gene therapy because of low efficiency of gene delivery. Therefore, we improved this problem by the combination of US and novel US-sensitive liposome (Bubble liposome) which was a liposome containing US imaging gas (perfluoropropane). This was an effective gene delivery system with collapse (cavitation) that was induced by US exposure to Bubble liposome. In this study, we assessed the ability of this system in cancer gene therapy using IL-12 cording plasmid DNA. The combination of Bubble liposomes and ultrasound was dramatically suppressed tumor growth. Therefore, we concluded that the combination of Bubble liposomes and ultrasound would be a good non-viral vector system in IL-12 cancer gene therapy.

  10. Physicochemical characterization of liposomes after ultrasound exposure - mechanisms of drug release

    DEFF Research Database (Denmark)

    Evjen, Tove J; Hupfeld, Stefan; Barnert, Sabine; Fossheim, Sigrid; Schubert, Rolf; Brandl, Martin

    -mediated drug release of liposomes (sonosensitivity) was shown to strongly depend on liposome membrane composition. In the current study the ultrasound-mediated drug release mechanism of liposomes was investigated. The results showed that differences in ultrasound drug release kinetics obtained for different......Ultrasound is investigated as a novel drug delivery tool within cancer therapy. Non-thermal ultrasound treatment of solid tumours post i.v.-injection of drug-carrying liposomes may induce local drug release from the carrier followed by enhanced intracellular drug uptake. Recently, ultrasound...... liposomal compositions were caused by distinctive release mechanisms of the carriers. Two types of liposomes composed of 1,2-dioleoyl-sn-glycero-3-phosphatidylethanolamine (DOPE) and hydrogenated soy L-α-phosphatidylcholine (HSPC) as main lipids, respectively, were recently shown to vary in sonosensitivity...

  11. Structure of liposome encapsulating proteins characterized by X-ray scattering and shell-modeling

    International Nuclear Information System (INIS)

    Wide-angle X-ray scattering data using a third-generation synchrotron radiation source are presented. Lipid liposomes are promising drug delivery systems because they have superior curative effects owing to their high adaptability to a living body. Lipid liposomes encapsulating proteins were constructed and the structures examined using synchrotron radiation small- and wide-angle X-ray scattering (SR-SWAXS). The liposomes were prepared by a sequential combination of natural swelling, ultrasonic dispersion, freeze-throw, extrusion and spin-filtration. The liposomes were composed of acidic glycosphingolipid (ganglioside), cholesterol and phospholipids. By using shell-modeling methods, the asymmetric bilayer structure of the liposome and the encapsulation efficiency of proteins were determined. As well as other analytical techniques, SR-SWAXS and shell-modeling methods are shown to be a powerful tool for characterizing in situ structures of lipid liposomes as an important candidate of drug delivery systems

  12. Lactosylated liposomes for targeted delivery of doxorubicin to hepatocellular carcinoma

    Directory of Open Access Journals (Sweden)

    Zhou X

    2012-10-01

    Full Text Available Xiaoju Zhou,1,2,* Mengzi Zhang,2,* Bryant Yung,2 Hong Li,2 Chenguang Zhou,2 L James Lee,3,4 Robert J Lee2,41State Key Laboratory of Virology, Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, Wuhan, People’s Republic of China; 2Division of Pharmaceutics, 3Department of Chemical and Biomolecular Engineering, 4NSF Nanoscale Science and Engineering Center for Affordable Nanoengineering of Polymeric Biomedical Devices, The Ohio State University, Columbus, OH, USA*These authors contributed equally to this workBackground: N-lactosyl-dioleoylphosphatidylethanolamine (Lac-DOPE was synthesized and evaluated as a liver-specific targeting ligand via asialoglycoprotein receptors for liposomal delivery of doxorubicin.Methods: Lactosylated liposomes encapsulating calcein (Lac-L-calcein or doxorubicin (Lac-L-DOX composed of egg phosphatidylcholine, cholesterol, monomethoxy polyethylene glycol 2000-distearoyl phosphatidylethanolamine, and Lac-DOPE at 50:35:5:10 (mol/mol were prepared by polycarbonate membrane extrusion and evaluated in human hepatocellular carcinoma HepG2 cells. Cellular uptake of Lac-L-calcein was monitored by confocal microscopy and by flow cytometry. The cytotoxicity of Lac-L-DOX was evaluated by MTT assay. The pharmacokinetic properties of Lac-L-DOX were studied in normal mice, and its biodistribution and antitumor activity were studied in nude mice with HepG2 xenografts.Results: The size of Lac-L-DOX was less than 100 nm and the liposomes demonstrated excellent colloidal stability. In vitro uptake of Lac-L-calcein by HepG2 cells was four times greater than that of non-targeted L-calcein. In the presence of 20 mM lactose, the uptake of Lac-L-calcein was inhibited, suggesting that asialoglycoprotein receptors mediated the observed cellular uptake. Lac-L-DOX exhibited enhanced in vivo cytotoxicity compared with the nontargeted liposomal doxorubicin (L

  13. In situ SAXS experiment during DNA and liposome complexation

    Energy Technology Data Exchange (ETDEWEB)

    Gasperini, A.A.; Cavalcanti, L.P. [Laboratorio Nacional de Luz Sincrotron (LNLS), Campinas, SP (Brazil); Balbino, T.A.; Torre, L.G. de la [Universidade Estadual de Campinas (UNICAMP), SP (Brazil); Oliveira, C.L.P. [Universidade de Sao Paulo (USP), Sao Paulo, SP (Brazil)

    2012-07-01

    Full text: Gene therapy is an exciting research area that allows the treatment of different diseases. Basically, an engineered DNA that codes a protein is the therapeutic drug that has to be delivered to the cell nucleus. After that, the DNA transfection process allows the protein production using the cell machinery. However, the efficient delivery needs DNA protection against nucleases and interstitial fluids. In this context, the use of cationic liposome/DNA complexes is a promising strategy for non-viral gene therapy. Liposomes are lipid systems that self-aggregate in bilayers and the use of cationic lipids allows the electrostatic complexation with DNA. In this work, we used SAXS technique to study the complexation kinetics between cationic liposomes and plasmid DNA and evaluate the liposome structural modifications in the presence of DNA. Liposomes were prepared according to [1] using as plasmid DNA vector model a modified version of pVAX1-GFP with luciferase as reporter gene [2]. The complexation was promoted in a SAXS sample holder containing a microchannel to get access to the compartment between two mica windows where the X-ray beam could cross through [3]. We obtained in situ complexation using such sample holder coupled to a fed-batch reactor through a peristaltic pump. The scattering curves were recorded each 30 seconds during the cycles. The DNA was added until a certain final ratio between surface charges previously determined. We studied the form and structure factor model for the liposome bilayer to fit the scattering curves [4]. Structural information such as the bilayer electronic density profiles, number of bilayers and fluidity were determined as a function of the complexation with DNA. These differences can reflect in singular in vitro and in vivo effects. [1] L. G. de la Torre et al. Colloids and Surfaces B: Biointerfaces, 73, 175 (2009) [2] A. R. Azzoni et al. The Journal of Gene Medicine, 9, 392 (2007) [3] L. P. Cavalcanti et al. Review of

  14. Tuftsin-bearing liposomes as rifampin vehicles in treatment of tuberculosis in mice.

    OpenAIRE

    Agarwal, A.; Kandpal, H; Gupta, H. P.; N. B. Singh; Gupta, C M

    1994-01-01

    The antitubercular activity of rifampin was considerably increased when it was encapsulated in egg phosphatidylcholine liposomes. A further increase in the activity was observed when the macrophage activator tetrapeptide tuftsin was grafted on the surface of the drug-loaded liposomes. Intermittent treatments (twice weekly) with these preparations were significantly more effective than the continuous treatments. Rifampin delivered twice weekly for 2 weeks in tuftsin-bearing liposomes was at le...

  15. Unilamellar liposomes modulate secretion of tumor necrosis factor by lipopolysaccharide-stimulated macrophages.

    OpenAIRE

    Brisseau, G F; Kresta, A; Schouten, D.; Bohnen, J M; P.N. Shek; Fok, E.; Rotstein, O D

    1994-01-01

    Liposomal encapsulation of antimicrobial agents has been used to improve drug delivery, particularly against intracellular pathogens. The effect of unilamellar liposomes on macrophage activation in response to Escherichia coli lipopolysaccharide was examined. Liposomes caused a dose- and time-dependent inhibition of tumor necrosis factor release by lipopolysaccharide-treated cells. The accumulation of tumor necrosis factor mRNA transcripts was unaffected, suggesting a posttranscriptional mech...

  16. On the formulation of pH-sensitive liposomes with long circulation times

    OpenAIRE

    Simões, Sérgio; Moreira, João Nuno; Fonseca, Cristina; Düzgünes, Nejat; Pedroso de Lima, Maria C

    2004-01-01

    Strategies used to enhance liposome-mediated drug delivery in vivo include the enhancement of stability and circulation time in the bloodstream, targeting to specific tissues or cells, and facilitation of intracytoplasmic delivery. pH-sensitive liposomes have been developed to mediate the introduction of highly hydrophilic molecules or macromolecules into the cytoplasm. These liposomes destabilize under acidic conditions found in the endocytotic pathway, and usually contain phosphatidylethano...

  17. Liposomes for Drug Delivery : from Physico-chemical Studies to Applications

    OpenAIRE

    Bergstrand, Nill

    2003-01-01

    Physico-chemical characterisation of structure and stability of liposomes intended for drug delivery is the central issue in this thesis. In addition, targeted liposomes to be used in boron neutron capture therapy (BNCT) were developed. Lysolipids and fatty acids are products formed upon hydrolysis of PC-lipids. The aggregate structure formed upon mixing lysolipids, fatty acids and EPC were characterised by means of cryo-TEM. A relatively monodisperse population of unilamellar liposomes was d...

  18. In vivo distributions of sup(99m)Tc-labelled liposomes

    International Nuclear Information System (INIS)

    Liposomes, carrying positive or negative charges, were prepared from combinations of phosphatidylcholine, cholesterol, phosphatidic acid, stearyl amines and dicetyl phosphate and treated with stannous chloride and labelled with technetium 99. The Liposomes were administered intravenously into rats and humans bearing carcinomas. Some patients with breast cancer were injected subcutaneously. The distribution of radioactivity, in various organs, was determined by scintiscanning at various time intervals. Differences between positively and negatively charged liposomes was observed. (U.K.)

  19. Transport and uptake effects of marine complex lipid liposomes in small intestinal epithelial cell models.

    Science.gov (United States)

    Du, Lei; Yang, Yu-Hong; Xu, Jie; Wang, Yu-Ming; Xue, Chang-Hu; Kurihara, Hideyuki; Takahashi, Koretaro

    2016-04-20

    Nowadays, marine complex lipids, including starfish phospholipids (SFP) and cerebrosides (SFC) separated from Asterias amurensis as well as sea cucumber phospholipids (SCP) and cerebrosides (SCC) isolated from Cucumaria frondosa, have received much attention because of their potent biological activities. However, little information is known on the transport and uptake of these lipids in liposome forms in small intestinal cells. Therefore, this study was undertaken to investigate the effects of these complex lipid liposomes on transport and uptake in Caco-2 and M cell monolayer models. The results revealed that SFP and SCP contained 42% and 47.9% eicosapentaenoic acid (EPA), respectively. The average particle sizes of liposomes prepared in this study were from 169 to 189 nm. We found that the transport of the liposomes across the M cell monolayer model was much higher than the Caco-2 cell monolayer model. The liposomes consisting of SFP or SCP showed significantly higher transport and uptake than soy phospholipid (soy-PL) liposomes in both Caco-2 and M cell monolayer models. Our results also exhibited that treatment with 1 mM liposomes composed of SFP or SCP for 3 h tended to increase the EPA content in phospholipid fractions of both differentiated Caco-2 and M cells. Moreover, it was also found that the hybrid liposomes consisting of SFP/SFC/cholesterol (Chol) revealed higher transport and uptake across the M cell monolayer in comparison with other liposomes. Furthermore, treatment with SFP/SFC/Chol liposomes could notably decrease the trans-epithelial electrical resistance (TEER) values of Caco-2 and M cell monolayers. The present data also showed that the cell viability of differentiated Caco-2 and M cells was not affected after the treatment with marine complex lipids or soy-PL liposomes. Based on the data in this study, it was suggested that marine complex lipid liposomes exhibit prominent transport and uptake in small intestinal epithelial cell models. PMID

  20. Surprising lack of liposome-induced complement activation by artificial 1,3-diamidophospholipids in vitro

    OpenAIRE

    Bugna, Simon; Buscema, Marzia; Matviykiv, Sofiya; Urbanics, Rudolf; Weinberger, Andreas; Meszaros, Tamas; Szebeni, Janos; Zumbuehl, Andreas; Saxer, Till; Müller, Bert

    2016-01-01

    Cardio-vascular diseases are the main cause of death, emphasizing the need to improve patient treatment and survival. One therapeutic approach is a liposome-based drug carrier system specifically targeting constricted arteries. The recently discovered mechano-sensitive liposomes use hemodynamic shear-stress differences between healthy and constricted blood vessels as trigger for drug release. Liposomes are promising delivery containers but are being recognized as foreign by the immune s...

  1. Targeting doxorubicin encapsulated in stealth liposomes to solid tumors by non thermal diode laser

    OpenAIRE

    Ghannam, Magdy M; El Gebaly, Reem; Fadel, Maha

    2016-01-01

    Background The use of liposomes as drug delivery systems is the most promising technique for targeting drug especially for anticancer therapy. Methods In this study sterically stabilized liposomes was prepared from DPPC/Cholesterol/PEG-PE encapsulated doxorubicin. The effect of lyophilization on liposomal stability and hence expiration date were studied. Moreover, the effect of diode laser on the drug released from liposomesin vitro and in vivo in mice carrying implanted solid tumor were also...

  2. Mechanism of Enhanced Activity of Liposome-Entrapped Aminoglycosides against Resistant Strains of Pseudomonas aeruginosa

    OpenAIRE

    Mugabe, Clement; Halwani, Majed; Azghani, Ali O.; Lafrenie, Robert M.; Omri, Abdelwahab

    2006-01-01

    Pseudomonas aeruginosa is inherently resistant to most conventional antibiotics. The mechanism of resistance of this bacterium is mainly associated with the low permeability of its outer membrane to these agents. We sought to assess the bactericidal efficacy of liposome-entrapped aminoglycosides against resistant clinical strains of P. aeruginosa and to define the mechanism of liposome-bacterium interactions. Aminoglycosides were incorporated into liposomes, and the bactericidal efficacies of...

  3. Effect of Cholesterol on the Properties of Spray-Dried Lysozyme-Loaded Liposomal Powders

    OpenAIRE

    Charnvanich, Dusadee; Vardhanabhuti, Nontima; Kulvanich, Poj

    2010-01-01

    The influence of cholesterol (Chol) in the liposomal bilayer on the properties of inhalable protein-loaded liposomal powders prepared by spray-drying technique was investigated. Lysozyme (LSZ) was used as a model protein. Feed solution for spray drying was prepared by direct mixing of aqueous solution of LSZ with mannitol solution and empty liposome dispersions composed of hydrogenated phosphatidylcholine and Chol at various molar ratios. The spray-dried powders were characterized with respec...

  4. Liposome-encapsulated superoxide dismutase prevents liver necrosis induced by acetaminophen.

    OpenAIRE

    Nakae, D.; Yamamoto, K; Yoshiji, H; Kinugasa, T.; Maruyama, H; Farber, J. L.; Konishi, Y

    1990-01-01

    Liposome-encapsulated human recombinant superoxide dismutase (LSOD) protected male rats that were pretreated with 3-methylcholanthrene from the liver necrosis produced by acetaminophen. By contrast, SOD-free liposomes, free SOD, or heat-denatured LSOD had no protective effect. Liposome-encapsulated SOD did not simply delay the onset of liver necrosis. A second dose of LSOD at 12 hours prevented the necrosis of the liver as assessed 24 hours after treatment with 500 mg/kg body weight of acetam...

  5. The Physical Characterization of Liposome Salicylic Acid Using Transmission Electron Microscope

    International Nuclear Information System (INIS)

    The physical characterization of liposome, formulated from salicylic acid using thin film hydration methods with cholesterol and soybean lecithin, has been done. The formula was characterized by optical microscopes and Transmission Electron Microscope (TEM). The observation result shows that the salicylic acid can be formulated to liposomes. Soybean lecithin combined with cholesterol (600 mg : 20 mg) was the best formula and the liposome was spherical vesicle like with dimension about 70 nm unit 800 nm. (author)

  6. Formulation and antifungal performance of natamycin-loaded liposomal suspensions: the benefits of sterol-enrichment.

    Science.gov (United States)

    Bouaoud, Clotilde; Lebouille, Jérôme G J L; Mendes, Eduardo; De Braal, Henriette E A; Meesters, Gabriel M H

    2016-06-01

    The aim of this study is to develop and evaluate food-grade liposomal delivery systems for the antifungal compound natamycin. Liposomes made of various soybean lecithins are prepared by solvent injection, leading to small unilamellar vesicles (Fine-tuning of sterol concentration allows preparation of liposomal suspensions presenting modulated in vitro release kinetics rates and enhanced antifungal activity against the model yeast Saccharomyces cerevisiae. PMID:26009272

  7. A simple route for renewable nano-sized arjunolic and asiatic acids and self-assembly of arjuna-bromolactone

    OpenAIRE

    Bag, Braja G; Dey, Partha P; Dinda, Shaishab K; Sheldrick, William S.; Iris M. Oppel

    2008-01-01

    While separating two natural nano-sized triterpenic acids via bromolactonization, we serendipitously discovered that arjuna-bromolactone is an excellent gelator of various organic solvents. A simple and efficient method for the separation of two triterpenic acids and the gelation ability and solid state 1D-helical self-assembly of nano-sized arjuna-bromolactone are reported.

  8. Phase transition of nano-sized amorphous tungsten to a crystalline state

    International Nuclear Information System (INIS)

    In this paper, some thermal properties of nano-sized amorphous W oxide and WO2 were measured. It was shown that amorphous nanoscale metal is crystallized at the temperature 1000-1370 degree C and this generates 170 ± 25 J/g energy substantially coincident, as expected, with a heat of phase transition point. As is typical for all nanosized amorphous material, phase transition temperature considerably less than half of the melting temperature of the material and does not have a strict threshold character observed for normal phase transition in crystalline materials

  9. Magnetic resonance lymphography of profundus lymph nodes with liposomal gadolinium-diethylenetriamine pentaacetic acid

    Energy Technology Data Exchange (ETDEWEB)

    Fujimoto, Yoshiko; Oku, Naoto [Univ. of Shizuoka (Japan). School of Pharmaceutical Sciences; Okuhata, Yoshitaka; Tyngi, Shia; Namba, Yukihiro

    2000-01-01

    Lymphography, especially imaging of profundus lymph nodes, is a useful tool for diagnosis of cancer metastases in lymph nodes. However, positive enhancement agents for magnetic resonance lymphography (MRL) have not been available, since the positive imaging agents so far introduced are low-molecular-weight materials that are not trapped in lymph nodes. For the purpose of improved positive enhanced MRL, we employed liposomes as carriers of a positive enhancer, gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA). Magnetic resonance (MR) imaging was performed after subcutaneous injection of Gd-liposomes into the hind feet of rabbits which had reactive enlarged retroperitoneal lymph nodes. As a result, not only popliteal but also profundus retroperitoneal lymph nodes were positively enhanced by Gd-liposomes, especially after 20 min massage of the injected sites. Gd-Liposomes containing dipalmitoylphosphatidylglycerol were more effective than Gd-liposomes containing palmityl-D-glucuronide, a type of long-circulating liposomes, suggesting that liposomal accumulation in lymph node is, at least partly, mediated by the trapping of liposomes by macrophages. These data show that liposomes modified with Gd-DTPA are effective for positive enhancement of both regional and profundus lymph nodes in MR lymphography. (author)

  10. Magnetic resonance lymphography of profundus lymph nodes with liposomal gadolinium-diethylenetriamine pentaacetic acid

    International Nuclear Information System (INIS)

    Lymphography, especially imaging of profundus lymph nodes, is a useful tool for diagnosis of cancer metastases in lymph nodes. However, positive enhancement agents for magnetic resonance lymphography (MRL) have not been available, since the positive imaging agents so far introduced are low-molecular-weight materials that are not trapped in lymph nodes. For the purpose of improved positive enhanced MRL, we employed liposomes as carriers of a positive enhancer, gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA). Magnetic resonance (MR) imaging was performed after subcutaneous injection of Gd-liposomes into the hind feet of rabbits which had reactive enlarged retroperitoneal lymph nodes. As a result, not only popliteal but also profundus retroperitoneal lymph nodes were positively enhanced by Gd-liposomes, especially after 20 min massage of the injected sites. Gd-Liposomes containing dipalmitoylphosphatidylglycerol were more effective than Gd-liposomes containing palmityl-D-glucuronide, a type of long-circulating liposomes, suggesting that liposomal accumulation in lymph node is, at least partly, mediated by the trapping of liposomes by macrophages. These data show that liposomes modified with Gd-DTPA are effective for positive enhancement of both regional and profundus lymph nodes in MR lymphography. (author)

  11. Massive targeting of liposomes, surface-modified with anionized albumins, to hepatic endothelial cells

    OpenAIRE

    Kamps, Jan A. A. M.; Morselt, Henriëtte W. M.; Swart, Pieter J.; Meijer, Dick K. F.; Scherphof, Gerrit L.

    1997-01-01

    Human serum albumin (HSA) derivatized with cis-aconitic anhydride was covalently coupled to liposomes with a size of approximately 100 nm [polyaconitylated HSA (Aco-HSA) liposomes]. Within 30 min after injection into a rat, Aco-HSA liposomes were completely cleared from the blood and almost exclusively taken up by the liver, whereas in control liposomes 80% was still present in the blood at that time. Endothelial cells were shown to account for almost two-thirds of the hepatic uptake of the A...

  12. Hepatocytes targeting of cationic liposomes modified with soybean sterylglucoside and polyethylene glycol

    Institute of Scientific and Technical Information of China (English)

    Xian-Rong Qi; Wen-Wei Yan; Jing Shi

    2005-01-01

    AIM: In this study, a hepatocyte-specific targeting technology was developed by modifying cationic liposomes with soybean sterylglucoside (SG) and polyethylene glycol (PEG) (C/SG/PEG-liposomes).METHODS: The liposomal transfection efficiencies in HepG22.2.15 cells were estimated with the use of fluorescein sodium (FS) as a model drug, by flow cytometry. The antisense activity of C/SG/PEG-liposomes entrapped antisense oligonucleotides (ODN) was determined as HBsAg and HBeAg in HepG2 2.2.15 cells by ELISA. The liposome uptake by liver and liver cells in mice was carried out after intravenous injection of 3H-labeled liposomes.RESULTS: C/SG-liposomes entrapped FS were effectively transfected into HepG2 2.2.15 cells in vitro. C/SG/PEGliposomes entrapped ODN, reduced the secretion of both HBsAg and HBeAg in HepG2 2.2.15 cells when compared to free ODN. After in vivo injection of 3H-labeled C/SG/PEG-liposomes, higher radiation accumulation was observed in the hepatocytes than non-parenchymal cells of the liver.CONCLUSION: C/SG/PEG-liposomes mediated gene transfer to the liver is an effective gene-delivery method for hepatocytes-specific targeting, which appears to have a potential for gene therapy of HBV infections.

  13. Hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration in mice

    Institute of Scientific and Technical Information of China (English)

    Zheng-hong WU; Qi-neng PING; Yi WEI; Jia-ming LAI

    2004-01-01

    AIM: To evaluate the hypoglycemic efficacy of insulin liposomes coated by chitosan with different molecular weights and concentrations after oral administration in mice. METHODS: Insulin-liposomes were prepared by reversed-phase evaporation. Chitosan coating was carried out by incubation of the liposomal suspensions with the chitosan solution. The hypoglycemic efficacies of chitosan-coated insulin liposomes were investigated by monitoring the blood glucose level using the glucose oxidase method after oral administration to healthy mice. RESULTS:In all the insulin liposomes, the insulin liposomes coated by 0.2 % chitosan (M. 1000 kDa) showed a better hypoglycemic efficacy as compared with the other liposomes coated by chitosan. The minimum blood glucose level was 15.1%±6.0 % of the initial (n=6). The hypoglycemic efficacy lasted for 4 h after oral administration to mice.CONCLUSION: Chitosan-coated liposomes could reduce tryptic digestion on insulin, and enhance enteral absorption of insulin. The molecular weights and concentrations of chitosan had significant effects on hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration to healthy mice.

  14. Formulation and Characterization of Tamoxifen Loaded Stealth Liposomes for Breast Cance

    Directory of Open Access Journals (Sweden)

    Mali Deepak

    2013-03-01

    Full Text Available The present study deals with the formulation and in-vitro characterization of tamoxifen loaded stealth liposomes. Passive targeting by stealth liposomes, once combined with efficient intracellular delivery, may be a very useful strategy to improve the antitumor efficacy for the anticancer agents. Stealth liposomes were prepared by using Cholesterol, DMPC, DSPC, and Polyethylene Glycol 4000 (PEG 4000 in order to achieve prolonged circulation time and sustained release. The prepared liposomes were evaluated for size, shape, profile, degree of drug entrapment, and in-vitro release efficiency. The effect of various formulation and drug release was investigated.

  15. Multifunctional liposomes for nasal delivery of the anti-Alzheimer drug tacrine hydrochloride

    DEFF Research Database (Denmark)

    Corace, Giuseppe; Angeloni, Cristina; Malaguti, Marco; Hrelia, Silvana; Stein, Paul C.; Brandl, Martin; Gotti, Roberto; Luppi, Barbara

    2014-01-01

    approach was chosen in order to obtain at the same time two positive results: an enhanced drug permeation through nasal mucosa and a concomitant neuroprotective effect. Several liposome formulations were prepared using the Reverse Phase Evaporation technique followed by membrane filter extrusion. In...... particular, liposome capacity to enhance drug permeation was evaluated by means of membrane permeation and cellular uptake studies. Furthermore, liposome effect on neuronal viability and intracellular ROS production was evaluated as well as their cytoprotective effect against oxidative stress. All liposome...

  16. Melittin liposomes surface modified with poloxamer 188: in vitro characterization and in vivo evaluation.

    Science.gov (United States)

    Tian, J L; Ke, X; Chen, Z; Wang, C J; Zhang, Y; Zhong, T C

    2011-05-01

    Melittin liposomes surface modified with poloxamer 188 were developed, and the effect of poloxamer 188 was investigated with regard to anti-cancer effect and vascular stimulation. Melittin liposomes surface modified with poloxamer 188 at different concentrations (0%, 2%, and 5%) were prepared using the adsorption method, followed by in vitro characterization, including entrapment efficiency, zeta potential, particle size, and morphology. Subsequently, the influence of repeated freeze-thawing on the liposomes was investigated, and the effect of poloxamer 188 on the repeated freeze-thawing process was explored. Vascular stimulation effects of MLT, and MLT liposome that surface coated with or without poloxamer were all studied. Pharmacokinetics of the different MLT preparations were determined and the anticancer activity of the MLT formulations was investigated. The particle size of the liposomes gradually increased with increasing poloxamer 188 content, while the entrapment efficiency did not change significantly. After the first freeze-thaw cycle, size and PDI were both markedly reduced, entrapment efficiency rose, and there was no significant change of zeta potential. The vascular irritation caused by MLT could be reduced to an extent by encapsulation in liposome, but not completely eliminated, while liposomes coated with poloxamer 188 can effectively abolish the phenomenon. Melittin liposomes with surface modified by poloxamer exhibit enhanced bioavailability, effective anticancer activity, and reduced side effects compared with melittin solution. Poloxamer plays an important role in melittin liposomes. PMID:21699070

  17. Selective partitioning of cholesterol and a model drug into liposomes of varying size

    DEFF Research Database (Denmark)

    Decker, Christiane; Fahr, Alfred; Kuntsche, Judith;

    2012-01-01

    The resistance of a lipid bilayer with respect to a bending deformation generally depends on the presence of membrane additives such as sterols, cosurfactants, peptides, and drugs. As a consequence, the partitioning of membrane additives into liposomes becomes selective with respect to liposome...... size; i.e., membrane rigidification depletes the membrane additives in the smaller (more strongly curved) liposomes. We have measured this liposome size-selective partitioning for two membrane additives - cholesterol and the porphyrin-based photosensitizer temoporfin - using asymmetrical flow field...

  18. Enhanced combination therapy effect on paclitaxel-resistant carcinoma by chloroquine co-delivery via liposomes

    Directory of Open Access Journals (Sweden)

    Gao MH

    2015-10-01

    Full Text Available Menghua Gao,1 Yuzhen Xu,1 Liyan Qiu2,3 1College of Pharmaceutical Sciences, 2Ministry of Education (MOE Key Laboratory of Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou, 3Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Chengdu, People’s Republic of China Abstract: A novel composite liposomal system co-encapsulating paclitaxel (PTX with chloroquine phosphate (CQ was designed for treating PTX-resistant carcinoma. It was confirmed that liposomal CQ can sensitize PTX by means of autophagy inhibition and competitively binding with multidrug-resistance transporters. Furthermore, according to the in vitro cytotoxicity and apoptosis assay, real-time observation of cellular uptake, and in vivo tissue distribution study, co-encapsulation of PTX and CQ in liposomes was validated as superior to the mixture of PTX liposome plus CQ liposome due to the simultaneous delivery and synergetic effect of the two drugs. Consequently, this composite liposome achieved significantly stronger anticancer efficacy in vivo than the PTX liposome plus CQ liposome mixture. This study helps to guide and enlighten ongoing and future clinical trials about the optimal administration modes for drug combination therapy. Keywords: paclitaxel, chloroquine, liposome, drug resistance, combination therapy

  19. Antibacterial activity of liposomal gentamicin against Pseudomonas aeruginosa: a time-kill study.

    Science.gov (United States)

    Rukholm, Gavin; Mugabe, Clement; Azghani, Ali O; Omri, Abdelwahab

    2006-03-01

    Cystic fibrosis (CF) is a common and lethal genetic disorder with a carrier frequency of 1 in 29 Caucasians. Chronic respiratory infections with Pseudomonas aeruginosa are the leading cause of morbidity and mortality in individuals with CF. Aminoglycoside antibiotics, including gentamicin, are highly effective against P. aeruginosa, but severe toxicity limits their use. One potential strategy for avoiding this problem is to encapsulate aminoglycosides in liposomes. In this study, we compared the bactericidal capacity of liposome-encapsulated gentamicin with that of free antibiotic against clinical isolates of P. aeruginosa. Liposome size, encapsulation efficiency and minimal inhibitory concentrations (MICs) of the free and liposomal gentamicin against gentamicin-sensitive and -resistant strains of P. aeruginosa were determined. In vitro time-kill studies were performed using free and liposomal gentamicin at 1, 2 or 4 times the MICs. The average liposomal size was 426.25 +/- 13.56 nm, with a gentamicin encapsulation efficiency of 4.51 +/- 0.54%. The MICs for liposomal gentamicin were significantly lower than those of corresponding free gentamicin. In addition, the time-kill values for liposomal gentamicin were either equivalent to or better than those of the free antibiotic. In conclusion, our liposomal gentamicin formulation is a more potent antipseudomonal drug with an improved killing time and prolonged antimicrobial activity. PMID:16472992

  20. FORMULATION AND DEVELOPMENT OF LIPOSOMAL GEL FOR TOPICAL DRUG DELIVERY SYSTEM

    Directory of Open Access Journals (Sweden)

    Suraj R. Wasankar*, Syed M. Faizi and Abhisek D. Deshmuk

    2012-11-01

    Full Text Available Aim: The aims of this study were to develop liposome enriched Dexibuprofen liposomal hydrogels for topical delivery, perform in vitro release studies and in vivo permeation studies through mice/rat skin, and evaluate the efficacy of liposomal gels against inflammation induced rats. The purpose was to provide the delivery of the topical drug at a sustained rate across intact skin to improve bioavailability and inflammation control for longer period from liposomal gels.Method: Phosphatidylcholine, Cholesterol and Dexibuprofen were dissolved in chloroform/methanol (2:1, v/v mixture and subsequently transferred into a pear-shaped flask connected to a Rotavapor (Büchi- type. Rotary evaporation method was used for the formulation of liposomes.Result: liposome prepared was evaluated for particle size measurement, percent drug entrapment, diffusion study, skin permeation study and in vivo study. F-7 batch found to be optimized batch having particle size 5.40 µm, % drug entrapment 61.70, % CDR 75.35 %. Hence F-7 batch further evaluated for skin permeation study, skin deposition study, in vivo study and stability study.Conclusion: The present study has been a satisfactory attempt to formulate and evaluate liposome of Dexibuprofen and liposomal gel with a providing sustained delivery of drug. From skin permeation study and in vivo study it was concluded that the prepared liposome of Dexibuprofen may prove to be potential candidate for safe and effective sustained drug delivery over an extended period of time which can reduce dosing frequency.

  1. Ultraviolet radiation-induced lipid peroxidation in liposomal membrane: modification by capsaicin

    International Nuclear Information System (INIS)

    Ultraviolet-radiation has been reported to cause lipid peroxidation in the liposomal membrane. In the present study, treatment with capsaicin, (8-methyl-n-vanillyl-6-nonenamide), the pungent principle of red hot pepper, was shown to modify UV-induced lipid peroxidation in the liposomal membrane. Treatment with low doses of capsaicin (less than 0.1 μg/mL of phosphatidyl choline liposome) produced a significant increase in UV-induced lipid peroxidation, while high doses (0.1-0.5 μg/mL of PC liposome) caused a significant decrease of UV-induced peroxidation

  2. PDT of tumor-bearing mice using liposome delivered texaphyrins

    International Nuclear Information System (INIS)

    The krypton ion laser (752.5 nm) induced photodynamic effects in bladder tumor-bearing nude mice after i.v. application of waterinsoluble cadmium texaphyrins were investigated. Liposomes using sojalecithin as phospholipid act as carriers. Cd-texaphyrin synthesized by Sessler, possesses strong absorption transitions at 765 nm and a high quantum efficiency of singlet oxygen production. The phototreatment 2 hours after i.v. injection of the photosensitizer led to significant tumor destruction, whereas the treatment 24 hours after administration shows no effect. This corresponds well to studies on the accumulation behaviour of the carriers in tumor, skin and inner organs using fluorophore-labeled liposomes. (author). 7 refs., 3 figs., 1 tab

  3. Liposomal delivery of benzoporphyrin derivative (BPD) to tumors

    International Nuclear Information System (INIS)

    A liposomal formulation of benzoporphyrin derivative, monoacid ring A (BPD), a potent lipophilic photosensitizer, was evaluated in a mouse tumor model. DBA/2 mice, bearing the M1 (rhabdomyosarcoma) tumor were injected intravenously with 14C-BPD (at 4 mg/kg) formulated in either liposomal suspension (L-14C-BPD) or 6% DMSO-PBS solution (A-14C-BPD) and the tumor accumulation of 14C-BPD and biodistribution in mouse tissues were determined and compared. Efficiency of photodynamic treatment was determined in the M1 tumor model in DBA/2 mice following intravenous injection of BPD in either formulation (0.5-3 mg/kg) 3 h prior to laser light (690 nm) treatment (150 or 210 J/cm2). Distribution of L and A-14C-BPD in human blood and plasma was determined in vitro. (author). 11 refs., 5 figs., 2 tabs

  4. Liposome-administered tetramethylhematoporphyrin (TMHP) as a photodynamic agent

    Science.gov (United States)

    Reich, Ella D.; Bachor, Ruediger; Miller, Kurt; Koenig, Karsten; Repassy, Denes; Hautmann, Richard E.

    1994-03-01

    The purpose of these studies was to determine whether liposomes can deliver the photo- sensitizer TMHP to human bladder carcinoma cells and fibroblast cells, and how effective the photodynamic activity of this photosensitizer is. TMHP was incorporated into small unilamellar liposomes of DPPC. Cellular uptake of TMHP was estimated after extraction with 0.1 N NaOH and by using a fluorescence microscope. Quantitative levels of TMHP in the three cell lines have been expressed in terms of (mu) g per 1.106 cells. PDT was performed for one hour after sensitization using an argon-pumped dye laser at 630 nm. Compared to the fibroblasts, neither a selective uptake of TMHP nor an increased effect of phototoxicity did occur in the tumor cell lines. PDT efficiency is dependent on cell line, dose and fluence rate.

  5. Treatment of lymphomatous and leukemic meningitis with liposomal encapsulated cytarabine

    Directory of Open Access Journals (Sweden)

    Melanie Kripp

    2008-09-01

    Full Text Available Melanie Kripp, Ralf-Dieter HofheinzOnkologisches Zentrum, III. Medizinische Klinik, Medizinische Fakultät Mannheim der Universität Heidelberg, GermanyAbstract: Liposomal encapsulated cytarabine (DepoCyte®, Mundipharma GmbH, Limburg/Lahn, Germany is a slow-release formulation of conventional cytarabine. It is licensed for intrathecal use in patients with lymphomatous and leukemic meningitis. DepoCyte® obtained superior response rates, improved patient quality of life and improved the time to neurological progression in a randomized albeit small clinical trial. In this review we briefly summarize the clinical data and discuss them in light of clinical problems and possible treatment scenarios.Keywords: liposomal cytarabine, leukemic meningitis, lymphomatous meningitis

  6. Engineering hybrid exosomes by membrane fusion with liposomes

    Science.gov (United States)

    Sato, Yuko T.; Umezaki, Kaori; Sawada, Shinichi; Mukai, Sada-atsu; Sasaki, Yoshihiro; Harada, Naozumi; Shiku, Hiroshi; Akiyoshi, Kazunari

    2016-01-01

    Exosomes are a valuable biomaterial for the development of novel nanocarriers as functionally advanced drug delivery systems. To control and modify the performance of exosomal nanocarriers, we developed hybrid exosomes by fusing their membranes with liposomes using the freeze–thaw method. Exosomes embedded with a specific membrane protein isolated from genetically modified cells were fused with various liposomes, confirming that membrane engineering methods can be combined with genetic modification techniques. Cellular uptake studies performed using the hybrid exosomes revealed that the interactions between the developed exosomes and cells could be modified by changing the lipid composition or the properties of the exogenous lipids. These results suggest that the membrane-engineering approach reported here offers a new strategy for developing rationally designed exosomes as hybrid nanocarriers for use in advanced drug delivery systems. PMID:26911358

  7. Octadecyl ferulate behavior in 1,2-Dioleoylphosphocholine liposomes.

    Science.gov (United States)

    Evans, Kervin O; Compton, David L; Whitman, Nathan A; Laszlo, Joseph A; Appell, Michael; Vermillion, Karl E; Kim, Sanghoon

    2016-01-15

    Octadecyl ferulate was prepared using solid acid catalyst, monitored using Supercritical Fluid Chromatography and purified to a 42% yield. Differential scanning calorimetry measurements determined octadecyl ferulate to have melting/solidification phase transitions at 67 and 39°C, respectively. AFM imaging shows that 5-mol% present in a lipid bilayer induced domains to form. Phase behavior measurements confirmed that octadecyl ferulate increased transition temperature of phospholipids. Fluorescence measurements demonstrated that octadecyl ferulate stabilized liposomes against leakage, maintained antioxidant capacity within liposomes, and oriented such that the feruloyl moiety remained in the hydrophilic region of the bilayer. Molecular modeling calculation indicated that antioxidant activity was mostly influenced by interactions within the bilayer. PMID:26332862

  8. Recurrent Candida albicans Ventriculitis Treated with Intraventricular Liposomal Amphotericin B

    Directory of Open Access Journals (Sweden)

    Demet Toprak

    2015-01-01

    Full Text Available Central nervous system (CNS infection with Candida is rare but significant because of its high morbidity and mortality. When present, it is commonly seen among immunocompromised and hospitalized patients. Herein, we describe a case of a four-year-old boy with acute lymphoblastic leukemia (ALL who experienced recurrent Candida albicans meningitis. The patient was treated successfully with intravenous liposomal amphotericin B at first attack, but 25 days after discharge he was readmitted to hospital with symptoms of meningitis. Candida albicans was grown in CFS culture again and cranial magnetic resonance imaging (MRI showed ventriculitis. We administered liposomal amphotericin B both intravenously and intraventricularly and favorable result was achieved without any adverse effects. Intraventricular amphotericin B may be considered for the treatment of recurrent CNS Candida infections in addition to intravenous administration.

  9. New nanosized technologies for dermal and transdermal drug delivery. A review.

    Science.gov (United States)

    Schroeter, Annett; Engelbrecht, Tanja; Neubert, Reinhard H H; Goebel, Alexandra S B

    2010-10-01

    Nanocarriers are promising dermal and transdermal drug delivery systems. The review recapitulates the most prominent nanocarriers such as microemulsions, liposomes and micro- and nanoparticles for the dermal and transdermal application. Microemulsions have a high solubilization capacity even for poorly soluble drugs and combined with their permeation enhancing effect high flux rates can be obtained. Liposomal carrier systems exhibit a high flexibility and mobility, whereas the follicular penetration of micro- and nanoparticular systems show an increase in the penetration depth. However, it is necessary to understand the particular mechanism of each transport system in order to limit undesired effects. PMID:21329045

  10. Synthetic liposomes are protective from bleomycin-induced lung toxicity

    OpenAIRE

    Gwinn, William M.; Kapita, Mayanga C.; Wang, Ping M.; Cesta, Mark F.; Martin, William J.

    2011-01-01

    Idiopathic pulmonary fibrosis is a devastating disease characterized by a progressive, irreversible, and ultimately lethal form of lung fibrosis. Except for lung transplantation, no effective treatment options currently exist. The bleomycin animal model is one of the best studied models of lung injury and fibrosis. A previous study using mouse tumor models observed that liposome-encapsulated bleomycin exhibited reduced lung toxicity. Therefore, we hypothesized that airway delivery of syntheti...

  11. Internalization of paramagnetic phosphatidylserine-containing liposomes by macrophages

    OpenAIRE

    Geelen Tessa; Yeo Sin; Paulis Leonie EM; Starmans Lucas WE; Nicolay Klaas; Strijkers Gustav J

    2012-01-01

    Abstract Background Inflammation plays an important role in many pathologies, including cardiovascular diseases, neurological conditions and oncology, and is considered an important predictor for disease progression and outcome. In vivo imaging of inflammatory cells will improve diagnosis and provide a read-out for therapy efficacy. Paramagnetic phosphatidylserine (PS)-containing liposomes were developed for magnetic resonance imaging (MRI) and confocal microscopy imaging of macrophages. Thes...

  12. Increased liposome extravasation in selected tissues: effect of substance P.

    OpenAIRE

    Rosenecker, J; Zhang, W; Hong, K; Lausier, J.; Geppetti, P.; Yoshihara, S.; Papahadjopoulos, D; Nadel, J A

    1996-01-01

    We have used a pharmacologic mediator to open intercellular connections in selected vessels to allow liposomes to escape from the blood stream and to extravasate into tissues that have appropriate receptors. We have examined the effects of substance P (SP), a peptide known to increase vascular permeability in selected tissues, such as trachea, esophagus, and urinary bladder in rats. We used quantitative fluorescence analysis of tissues to measure two fluorescent markers, one attached to the l...

  13. Ultrasonic radiation induced lipid peroxidation in liposomal membrane

    Energy Technology Data Exchange (ETDEWEB)

    Jana, A.K.; Agarwal, S.; Chatterjee, S.N.

    1986-12-01

    Ultrasonic radiation produced a dose dependent linear increase in lipid peroxidation (MDA formation) in the liposomal membrane. The yield of MDA was significantly inhibited by butylated hydroxytoluene (BHT), the antioxidant, sodium formate,the OH/sup ./ radical scavenger, and EDTA, the metal ion chelator. Ascorbic acid at low concentration increased the ultrasonic induced MDA formation while high concentrations inhibited lipid peroxidation. A mechanism of ultrasound induced lipid peroxidation is suggested.

  14. Development of liposomal curcumin for vaginal drug delivery

    OpenAIRE

    Hussain, Haider

    2010-01-01

    Curcumin (I), demethoxy curcumin (II) and bisdemethoxy curcumin (III) are commonly called curcuminoids, and derived products from the spice, turmeric. It has reported numerous of therapeutic activities including, anti-inflammatory, and anticancer properties. The aim of the current study was to develop a formulation which can overcome the limitation of curcumin being so poorly soluble in aqueous medium. Our approach has been directed toward investigating the potential of using liposomal for...

  15. Shrinkage of pegylated and non-pegylated liposomes in serum

    OpenAIRE

    Wolfram, Joy; Suri, Krishna; Yang, Yong; Shen, Jianliang; Celia, Christian; Fresta, Massimo; Zhao, Yuliang; Shen, Haifa; Ferrari, Mauro

    2013-01-01

    An essential requisite for the design of nanodelivery systems is the ability to characterize the size, homogeneity and zeta potential of nanoparticles. Such properties can be tailored in order to create the most efficient drug delivery platforms. An important question is whether these characteristics change upon systemic injection. Here, we have studied the behavior of phosphatidylcholine/cholesterol liposomes exposed to serum proteins. The results reveal a serum-induced reduction in the size...

  16. Radiation sterilization of antibiotic liposome formulations: A case study

    Science.gov (United States)

    Botelho, M. L.; Cabo Verde, S.; Alves, L.; Belchior, A.; Reymão, J.; Trabulo, S.; Gaspar, M. M.; Cruz, M. E. M.; Simões, S.

    2007-08-01

    New liposome formulations for antimycobacterial purpose are under development in Portugal. The drug must be submitted to a sterilization process. In order to find out if gamma radiation could be applied, microbiological and chemical studies were developed based on ISO standards. The bioburden was determined, the main critical points of line production were detected and the sterilization dose was determined based on a chart control for bioburden. A preliminary maximum acceptable dose for product was found out based on the main functional parameters.

  17. Radiation sterilization of antibiotic liposome formulations: A case study

    Energy Technology Data Exchange (ETDEWEB)

    Botelho, M.L. [Nuclear and Technological Institute, Estrada Nacional 10, Apartado 21, 2686-953 Sacavem (Portugal)]. E-mail: mlb@itn.pt; Cabo Verde, S. [Nuclear and Technological Institute, Estrada Nacional 10, Apartado 21, 2686-953 Sacavem (Portugal); Alves, L. [Nuclear and Technological Institute, Estrada Nacional 10, Apartado 21, 2686-953 Sacavem (Portugal); Belchior, A. [Nuclear and Technological Institute, Estrada Nacional 10, Apartado 21, 2686-953 Sacavem (Portugal); Reymao, J. [Instituto Nacional de Engenharia Tecnologia e Inovacao, IP, Estrada do Paco do Lumiar 22, 1649-048 Lisboa (Portugal); Trabulo, S. [Bluepharma, S.A., Rua da Bayer Sao Martinho do Bispo, Apartado 7003, 3045-016 Coimbra (Portugal); Gaspar, M.M. [Instituto Nacional de Engenharia Tecnologia e Inovacao, IP, Estrada do Paco do Lumiar 22, 1649-048 Lisboa (Portugal); Cruz, M.E.M [Instituto Nacional de Engenharia Tecnologia e Inovacao, IP, Estrada do Paco do Lumiar 22, 1649-048 Lisboa (Portugal); Simoes, S. [Bluepharma, S.A., Rua da Bayer Sao Martinho do Bispo, Apartado 7003, 3045-016 Coimbra (Portugal)

    2007-08-15

    New liposome formulations for antimycobacterial purpose are under development in Portugal. The drug must be submitted to a sterilization process. In order to find out if gamma radiation could be applied, microbiological and chemical studies were developed based on ISO standards. The bioburden was determined, the main critical points of line production were detected and the sterilization dose was determined based on a chart control for bioburden. A preliminary maximum acceptable dose for product was found out based on the main functional parameters.

  18. Radiation sterilization of antibiotic liposome formulations: A case study

    International Nuclear Information System (INIS)

    New liposome formulations for antimycobacterial purpose are under development in Portugal. The drug must be submitted to a sterilization process. In order to find out if gamma radiation could be applied, microbiological and chemical studies were developed based on ISO standards. The bioburden was determined, the main critical points of line production were detected and the sterilization dose was determined based on a chart control for bioburden. A preliminary maximum acceptable dose for product was found out based on the main functional parameters

  19. Strategies to improve intracellular drug delivery by targeted liposomes

    OpenAIRE

    Fretz, M.M.

    2007-01-01

    Biotechnological advances increased the number of novel macromolecular drugs and new drug targets. The latter are mostly found intracellular. Unfortunately, most of the new macromolecular drugs rely on drug delivery tools for their intracellular delivery because their unfavourable physicochemical properties hamper them to cross cellular barriers, like the plasma and endosomal membranes. The work described in this thesis aims to improve intracellular drug delivery by applying targeted liposome...

  20. DEVELOPMENT AND CHARACTARIZATION OF PERINDOPRIL ERBUMINE LOADED ETHANOLIC LIPOSOMES

    OpenAIRE

    Prakash Goudanavar; Manjunatha; Doddayya Hiremath

    2014-01-01

    The present work describes the preparation of Perindopril erbumine ethosomes and study of effect of alcohol and phospholipid on transdermal delivery. Perindopril erbumine is an ACE inhibitor which slowly inhibits the activity of the enzyme ACE, which decreases the production of angiotensin II, is being involved in the blood pressure regulation. Perindopril erbumine loaded ethanolic Liposomes were prepared by an hot - cold method using different concentrations of Alcohol and Soya lecithin in d...

  1. Liposomal voriconazole (VOR) formulation for improved ocular delivery.

    Science.gov (United States)

    de Sá, Fernando Augusto Pires; Taveira, Stephânia Fleury; Gelfuso, Guilherme Martins; Lima, Eliana Martins; Gratieri, Taís

    2015-09-01

    Treating infectious eye diseases topically requires a drug delivery system capable of overcoming the eye's defense mechanisms, which efficiently reduce the drug residence time right after its administration, therefore reducing absorption. In order to try to surpass such administration issues and improve life quality for patients with fungal keratitis, liposomal voriconazol (VOR) formulations were prepared. Formulations were composed of soy phosphatidylcholine (PC) containing or not 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) and cholesterol. Liposomes were characterized by their drug entrapment efficiency (EE), drug recovery (DR), average diameter (size) and polydispersivity index (PdI). In vitro mucosal interaction and irritancy levels, ex vivo permeation, as well as the short-term stability were also assessed. Liposomal VOR formulation produced with 7.2:40mM VOR:PC showed to be the most promising formulation: mean size of 116.6±5.9nm, narrow PdI (0.17±0.06), negative zeta potential (∼-7mV) and over 80% of EE and yield, remaining stable for at least 30 days in solution and 90 days after lyophilization. This formulation was classified as 'non-irritant' after HET-CAM's test and was able to deliver about 47.85±5.72μg/cm(2) of VOR into porcine cornea after 30min of permeation test. Such drug levels are higher than the minimal inhibitory concentrations (MIC) of several fungi species isolated from clinical cases of corneal keratitis. Overall results suggest VOR can be effectively incorporated in liposomes for potential topical treatment of fungal keratitis. PMID:26123854

  2. Normal and Frictional Interactions between Liposome-Bearing Biomacromolecular Bilayers.

    Science.gov (United States)

    Gaisinskaya-Kipnis, Anastasia; Klein, Jacob

    2016-08-01

    Highly efficient lubricating boundary layers at biosurfaces such as cartilage have been proposed to comprise phospholipids complexed with biomacromolecules exposed at the surfaces. To gain insight into this, a systematic study on the normal and frictional forces between surfaces bearing a sequentially deposited model alginate-on-chitosan bilayer, bearing different adsorbed phosphatidylcholine (PC) liposomes, was carried out using a surface force balance. Structures of the resulting surface complexes were determined using atomic force microscopy (AFM) and cryo-scanning electron microscopy (cryo-SEM). The liposome/lipid-polymer complexes could maintain their integrity up to high pressures in terms of both normal and shear interactions between the surfaces, which were repeatable, reproducible, and revealed very low friction (coefficient of friction μ down to 10(-3)-10(-4), depending on the PC used) up to pressures of hundreds of atm. We attribute this remarkable lubrication capability ultimately to hydration lubrication acting at the hydrated phosphocholine headgroups of the PC lipids, either exposed at the liposome surfaces or through complexation with the polyelectrolyte bilayer. Values of μ, while low, were roughly an order of magnitude higher than for the same PC vesicles adsorbed on bare mica, a difference attributed to their lower density on the bilayer; the bilayer, however, stabilized the PC-vesicles far better than bare mica against rupture and shear at high compressions and sliding. PMID:27409248

  3. Liposome-Based Delivery Systems in Plant Polysaccharides

    International Nuclear Information System (INIS)

    Plant polysaccharides consist of many monosaccharide by α or β glycosidic bond which can be extracted by the water, alcohol, lipophile liquid from a variety of plants including Cordyceps sinensis, astragalus, and mushrooms. Recently, many evidences illustrate that natural plant polysaccharides possess various biological activities including strengthening immunity, lowering blood sugar, regulating lipid metabolism, anti oxidation, anti aging, and antitumour. Plant polysaccharides have been widely used in the medical field due to their special features and low toxicity. As an important drug delivery system, liposomes can not only encapsulate small-molecule compound but also big-molecule drug; therefore, they present great promise for the application of plant polysaccharides with unique physical and chemical properties and make remarkable successes. This paper summarized the current progress in plant polysaccharides liposomes, gave an overview on their experiment design method, preparation, and formulation, characterization and quality control, as well as in vivo and in vitro studies. Moreover, the potential application of plant polysaccharides liposomes was prospected as well.

  4. Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin

    Science.gov (United States)

    Croci, Romina; Bottaro, Elisabetta; Chan, Kitti Wing Ki; Watanabe, Satoru; Pezzullo, Margherita; Mastrangelo, Eloise; Nastruzzi, Claudio

    2016-01-01

    RNA virus infections can lead to the onset of severe diseases such as fever with haemorrhage, multiorgan failure, and mortality. The emergence and reemergence of RNA viruses continue to pose a significant public health threat worldwide with particular attention to the increasing incidence of flaviviruses, among others Dengue, West Nile Virus, and Yellow Fever viruses. Development of new and potent antivirals is thus urgently needed. Ivermectin, an already known antihelminthic drug, has shown potent effects in vitro on Flavivirus helicase, with EC50 values in the subnanomolar range for Yellow Fever and submicromolar EC50 for Dengue Fever, Japanese encephalitis, and tick-borne encephalitis viruses. However ivermectin is hampered in its application by pharmacokinetic problems (little solubility and high cytotoxicity). To overcome such problems we engineered different compositions of liposomes as ivermectin carriers characterizing and testing them on several cell lines for cytotoxicity. The engineered liposomes were less cytotoxic than ivermectin alone and they showed a significant increase of the antiviral activity in all the Dengue stains tested (1, 2, and S221). In the current study ivermectin is confirmed to be an effective potential antiviral and liposomes, as drug carriers, are shown to modulate the drug activity. All together the results represent a promising starting point for future improvement of ivermectin as antiviral and its delivery. PMID:27242902

  5. Liposome-Based Delivery Systems in Plant Polysaccharides

    Directory of Open Access Journals (Sweden)

    Meiwan Chen

    2012-01-01

    Full Text Available Plant polysaccharides consist of many monosaccharide by α- or β-glycosidic bond which can be extracted by the water, alcohol, lipophile liquid from a variety of plants including Cordyceps sinensis, astragalus, and mushrooms. Recently, many evidences illustrate that natural plant polysaccharides possess various biological activities including strengthening immunity, lowering blood sugar, regulating lipid metabolism, antioxidation, antiaging, and antitumour. Plant polysaccharides have been widely used in the medical field due to their special features and low toxicity. As an important drug delivery system, liposomes can not only encapsulate small-molecule compound but also big-molecule drug; therefore, they present great promise for the application of plant polysaccharides with unique physical and chemical properties and make remarkable successes. This paper summarized the current progress in plant polysaccharides liposomes, gave an overview on their experiment design method, preparation, and formulation, characterization and quality control, as well as in vivo and in vitro studies. Moreover, the potential application of plant polysaccharides liposomes was prospected as well.

  6. Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin.

    Science.gov (United States)

    Croci, Romina; Bottaro, Elisabetta; Chan, Kitti Wing Ki; Watanabe, Satoru; Pezzullo, Margherita; Mastrangelo, Eloise; Nastruzzi, Claudio

    2016-01-01

    RNA virus infections can lead to the onset of severe diseases such as fever with haemorrhage, multiorgan failure, and mortality. The emergence and reemergence of RNA viruses continue to pose a significant public health threat worldwide with particular attention to the increasing incidence of flaviviruses, among others Dengue, West Nile Virus, and Yellow Fever viruses. Development of new and potent antivirals is thus urgently needed. Ivermectin, an already known antihelminthic drug, has shown potent effects in vitro on Flavivirus helicase, with EC50 values in the subnanomolar range for Yellow Fever and submicromolar EC50 for Dengue Fever, Japanese encephalitis, and tick-borne encephalitis viruses. However ivermectin is hampered in its application by pharmacokinetic problems (little solubility and high cytotoxicity). To overcome such problems we engineered different compositions of liposomes as ivermectin carriers characterizing and testing them on several cell lines for cytotoxicity. The engineered liposomes were less cytotoxic than ivermectin alone and they showed a significant increase of the antiviral activity in all the Dengue stains tested (1, 2, and S221). In the current study ivermectin is confirmed to be an effective potential antiviral and liposomes, as drug carriers, are shown to modulate the drug activity. All together the results represent a promising starting point for future improvement of ivermectin as antiviral and its delivery. PMID:27242902

  7. Susceptibility for hydroperoxide formation of phosphatidylcholine and phosphatidylethanolamine in liposomes.

    Science.gov (United States)

    Wang, J Y; Shibata, T; Ueki, T; Miyazawa, T

    1995-06-01

    To compare the peroxidative susceptibilities of phosphatidylcholine (PC) and phosphatidylethanolamine (PE) in liposomes, multilamellar vesicles (MLVs) were prepared with equimolar L-alpha-dilinoleoyl PC (DLPC) and L-alpha-dilinoleoyl PE (DLPE), and with soya PC and soya PE having a uniform constituent fatty acids. The hydroperoxide formation at 37 degrees C in the presence of a water-soluble radical initiator was examined by chemiluminescence-high-performance liquid chromatography (CL-HPLC), and the effect of heterogeneous distribution of PC and PE on peroxidation was investigated. No difference was found between the hydroperoxidation of PC and PE in MLVs systems, except that soya PC was more susceptible to peroxidation than soya PE in the L-alpha-dipalmitoyl PC (DPPC)-based liposomes. No correlation was found between the amount of phospholipids distributed in the external leaflet of MLVs and hydroperoxide formation. This result suggested that the unsaturation of constituent fatty acids in phospholipids is more important than the difference in the polar head group of phospholipids regarding their peroxidizabilities in liposomes. PMID:7472672

  8. Integration of {beta}-carotene molecules in small liposomes

    Energy Technology Data Exchange (ETDEWEB)

    Andreeva, Atanaska; Popova, Antoaneta, E-mail: andreeva@phys.uni-sofia.b

    2010-11-01

    The most typical feature of carotenoids is the long polyene chain with conjugated double bonds suggesting that they can serve as conductors of electrons, acting as 'molecular wires', important elements in the molecular electronic devices. Carotenoids are essential components of photosynthetic systems, performing different functions as light harvesting, photoprotection and electron transfer. They act also as natural antioxidants. In addition they perform structural role stabilizing the three-dimensional organization of photosynthetic membranes. Carotenoids contribute to the stability of the lipid phase, preserving the membrane integrity under potentially harmful environmental conditions. Carotenoids can be easily integrated into model membranes, facilitating the investigation of their functional roles. In carotenoid-egg phosphatidylcholine (EPC) liposomes ss-carotene is randomly distributed in the hydrocarbon interior of the bilayer, without any preferred, well defined orientation and retains a substantial degree of mobility. Here we investigate the degree of integration of ss-carotene in small unilamellar EPC liposomes and the changes in ss-carotene absorption and Raman spectra due to the lipid-pigment interaction. All observed changes in ss-carotene absorption and Raman spectra may be regarded as a result of the lipid-pigment interactions leading to the polyene geometry distortion and increasing of the environment heterogenety in the liposomes as compared to the solutions.

  9. Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin

    Directory of Open Access Journals (Sweden)

    Romina Croci

    2016-01-01

    Full Text Available RNA virus infections can lead to the onset of severe diseases such as fever with haemorrhage, multiorgan failure, and mortality. The emergence and reemergence of RNA viruses continue to pose a significant public health threat worldwide with particular attention to the increasing incidence of flaviviruses, among others Dengue, West Nile Virus, and Yellow Fever viruses. Development of new and potent antivirals is thus urgently needed. Ivermectin, an already known antihelminthic drug, has shown potent effects in vitro on Flavivirus helicase, with EC50 values in the subnanomolar range for Yellow Fever and submicromolar EC50 for Dengue Fever, Japanese encephalitis, and tick-borne encephalitis viruses. However ivermectin is hampered in its application by pharmacokinetic problems (little solubility and high cytotoxicity. To overcome such problems we engineered different compositions of liposomes as ivermectin carriers characterizing and testing them on several cell lines for cytotoxicity. The engineered liposomes were less cytotoxic than ivermectin alone and they showed a significant increase of the antiviral activity in all the Dengue stains tested (1, 2, and S221. In the current study ivermectin is confirmed to be an effective potential antiviral and liposomes, as drug carriers, are shown to modulate the drug activity. All together the results represent a promising starting point for future improvement of ivermectin as antiviral and its delivery.

  10. Mixing of nanosize particles by magnetically assisted impaction techniques

    Science.gov (United States)

    Scicolone, James V.

    Nanoparticles and nanocomposites offer unique properties that arise from their small size, large surface area, and the interactions of phases at their interfaces, and are attractive for their potential to improve performance of drugs, biomaterials, catalysts and other high-value-added materials. However, a major problem in utilizing nanoparticles is that they often lose their high surface area due to grain growth. Creating nanostructured composites where two or more nanosized constituents are intimately mixed can prevent this loss in surface area, but in order to obtain homogeneous mixing, de-agglomeration of the individual nanoparticle constituents is necessary. Due to high surface area, nano-particles form very large, fractal agglomerates. The structure of these agglomerates can have a large agglomerate composed of sub-agglomerates (SA), which itself consists of primary agglomerates (PA), that contain chain or net like nano-particle structures; typically sub-micron size. Thus the final agglomerate has a hierarchical, fractal structure, and depending upon the forces applied, it could break down to a certain size scale. The agglomerates can be fairly porous and fragile or they could be quite dense, based on primary particle size and its surface energy. Thus depending upon the agglomerate strength at different length scales, one could achieve deagglomeration and subsequent mixing at varying length scale. A better understanding of this can have a major impact on the field of nano-structured materials; thus the long term objective of this project is to gain fundamental understanding of deagglomeration and mixing of nano-agglomerates. Dry mixing is in general not effective in achieving desired mixing at nanoscale, whereas wet mixing suffers from different disadvantages like nanomaterial of interest should be insoluble, has to wet the liquid, and involves additional steps of filtration and drying. This research examines the use of environmentally friendly a novel

  11. Enhanced bactericidal potency of nanoliposomes by modification of the fusion activity between liposomes and bacterium

    Directory of Open Access Journals (Sweden)

    Ma YF

    2013-06-01

    Full Text Available Yufan Ma,1 Zhao Wang,1,2 Wen Zhao,1 Tingli Lu,1 Rutao Wang,1,2 Qibing Mei,1 Tao Chen1–3 1Key Laboratory for Space Bioscience and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, Xi'an, Shaanxi, People's Republic of China; 2Shaanxi Liposome Research Center, Xi'an, Shaanxi, People's Republic of China; 3Xi'an Libang Pharmaceuticals Co, Ltd, Xi'an, People's Republic of China Background: Pseudomonas aeruginosa represents a good model of antibiotic resistance. These organisms have an outer membrane with a low level of permeability to drugs that is often combined with multidrug efflux pumps, enzymatic inactivation of the drug, or alteration of its molecular target. The acute and growing problem of antibiotic resistance of Pseudomonas to conventional antibiotics made it imperative to develop new liposome formulations to overcome these mechanisms, and investigate the fusion between liposome and bacterium. Methods: The rigidity, stability and charge properties of phospholipid vesicles were modified by varying the cholesterol, 1,2-dioleoyl-sn-glycero-3-phosphatidylethanolamine (DOPE, and negatively charged lipids 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol sodium salt (DMPG, 1,2-dimyristoyl-sn-glycero-3-phopho-L-serine sodium salt (DMPS, 1,2-dimyristoyl-sn-glycero-3-phosphate monosodium salt (DMPA, nature phosphatidylserine sodium salt from brain and nature phosphatidylinositol sodium salt from soybean concentrations in liposomes. Liposomal fusion with intact bacteria was monitored using a lipid-mixing assay. Results: It was discovered that the fluid liposomes-bacterium fusion is not dependent on liposomal size and lamellarity. A similar degree of fusion was observed for liposomes with a particle size from 100 to 800 nm. The fluidity of liposomes is an essential pre-request for liposomes fusion with bacteria. Fusion was almost completely inhibited by incorporation of cholesterol into fluid liposomes. The increase in the

  12. Therapeutic Efficacy of Combining PEGylated Liposomal Doxorubicin and Radiofrequency (RF) Ablation: Comparison between Slow-Drug-Releasing, Non-Thermosensitive and Fast-Drug-Releasing, Thermosensitive Nano-Liposomes

    OpenAIRE

    Andriyanov, Alexander V.; Erez Koren; Yechezkel Barenholz; S Nahum Goldberg

    2014-01-01

    AIMS: To determine how the accumulation of drug in mice bearing an extra-hepatic tumor and its therapeutic efficacy are affected by the type of PEGylated liposomal doxorubicin used, treatment modality, and rate of drug release from the liposomes, when combined with radiofrequency (RF) ablation. MATERIALS AND METHODS: Two nano-drugs, both long-circulating PEGylated doxorubicin liposomes, were formulated: (1) PEGylated doxorubicin in thermosensitive liposomes (PLDTS), having a burst-type fast d...

  13. Silica-based monolithic capillary columns modified by liposomes for characterization of analyte-liposome interactions by capillary liquid chromatography

    Czech Academy of Sciences Publication Activity Database

    Wiedmer, S. K.; Moravcová, Dana; Planeta, Josef

    2013. s. 164-164. [HPLC 2013 AMSTERDAM. International Symposium on High Performance Liquid Phase Separations and Related Techniques /39./. 16.06.2013-20.06.2013, Amsterdam] R&D Projects: GA ČR(CZ) GAP206/11/0138; GA MV VG20112015021 Institutional support: RVO:68081715 Keywords : biomimicking stationary phase * immobilized liposomes * silica monolithic column Subject RIV: CB - Analytical Chemistry, Separation

  14. Incorporation of a selective sigma-2 receptor ligand enhances uptake of liposomes by multiple cancer cells

    Directory of Open Access Journals (Sweden)

    Zhang Y

    2012-08-01

    Full Text Available Yifei Zhang,1,* Yixian Huang,1,* Peng Zhang,1 Xiang Gao,1 Robert B Gibbs,2 Song Li1 1Center for Pharmacogenetics, 2Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, PA, USA*These authors contributed equally to this workBackground: The sigma-2 receptor is an attractive target for tumor imaging and targeted therapy because it is overexpressed in multiple types of solid tumors, including prostate cancer, breast cancer, and lung cancer. SV119 is a synthetic small molecule that binds to sigma-2 receptors with high affinity and specificity. This study investigates the utility of SV119 in mediating the selective targeting of liposomal vectors in various types of cancer cells.Methods: SV119 was covalently linked with polyethylene glycol-dioleyl amido aspartic acid conjugate (PEG-DOA to generate a novel functional lipid, SV119-PEG-DOA. This lipid was utilized for the preparation of targeted liposomes to enhance their uptake by cancer cells. Liposomes with various SV119 densities (0, 1, 3, and 5 mole% were prepared and their cellular uptake was investigated in several tumor cell lines. In addition, doxorubicin (DOX was loaded into the targeted and unmodified liposomes, and the cytotoxic effect on the DU-145 cells was evaluated by MTT assay.Results: Liposomes with or without SV119-PEG-DOA both have a mean diameter of approximately 90 nm and a neutral charge. The incorporation of SV119-PEG-DOA significantly increased the cellular uptake of liposomes by the DU-145, PC-3, A549, 201T, and MCF-7 tumor cells, which was shown by fluorescence microscopy and the quantitative measurement of fluorescence intensity. In contrast, the incorporation of SV119 did not increase the uptake of liposomes by the normal BEAS-2B cells. In a time course study, the uptake of SV119 liposomes by DU-145 cells was also significantly higher at each time point compared to the unmodified liposomes. Furthermore, the DOX-loaded SV119 liposomes

  15. Formulation, antileukemia mechanism, pharmacokinetics, and biodistribution of a novel liposomal emodin

    Directory of Open Access Journals (Sweden)

    Wang T

    2012-05-01

    Full Text Available Tiechuang Wang1, Xiaodong Yin2, Yaping Lu1, Weiguang Shan1, Subin Xiong11College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, People's Republic of China; 2Baxter International Inc, Shanghai, People's Republic of ChinaAbstract: Emodin is a multifunctional Chinese traditional medicine with poor water solubility. D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS is a pegylated vitamin E derivate. In this study, a novel liposomal-emodin-conjugating TPGS was formulated and compared with methoxypolyethyleneglycol 2000-derivatized distearoyl-phosphatidylethanolamine (mPEG2000–DSPE liposomal emodin. TPGS improved the encapsulation efficiency and stability of emodin egg phosphatidylcholine/cholesterol liposomes. A high encapsulation efficiency of 95.2% ± 3.0%, particle size of 121.1 ± 44.9 nm, spherical ultrastructure, and sustained in vitro release of TPGS liposomal emodin were observed; these were similar to mPEG2000–DSPE liposomes. Only the zeta potential of –13.1 ± 2.7 mV was significantly different to that for mPEG2000–DSPE liposomes. Compared to mPEG2000–DSPE liposomes, TPGS liposomes improved the cytotoxicity of emodin on leukemia cells by regulating the protein levels of myeloid cell leukemia 1 (Mcl-1, B-cell lymphoma-2 (Bcl-2 and Bcl-2-associated X protein, which was further enhanced by transferrin. TPGS liposomes prolonged the circulation time of emodin in the blood, with the area under the concentration–time curve (AUC 1.7 times larger than for free emodin and 0.91 times larger than for mPEG2000–DSPE liposomes. In addition, TPGS liposomes showed higher AUC for emodin in the lung and kidney than for mPEG2000–DSPE liposomes, and both liposomes elevated the amount of emodin in the heart. Overall, TPGS is a pegylated agent that could potentially be used to compose a stable liposomal emodin with enhanced therapeutics.Keywords: emodin, liposomes, TPGS, mPEG2000–DSPE, leukemia, transferrin

  16. Ultrafast synthesis of nano-sized zeolite SAPO-34 with excellent MTO catalytic performance.

    Science.gov (United States)

    Sun, Qiming; Wang, Ning; Guo, Guanqi; Yu, Jihong

    2015-11-25

    Nano-sized SAPO-34 zeolites with high crystallinity are obtained in 10 minutes by fast heating the reaction gel in a stainless steel tubular reactor combined with the seed-assisted method, which show outstanding performance in methanol-to-olefin (MTO) reaction. PMID:26412585

  17. NANOSIZE TITANIA STIMULATES REACTIVE OXYGEN SPECIES IN BRAIN MICROGLIA AND DAMAGES NEURONS.

    Science.gov (United States)

    Research that addresses the environmental impact and biological consequences of widely distributed, commonly used nanoparticles is needed. Nanosize titanium dioxide (i.e., titania, TiO2) is used in air and water remediation and in numerous products designed for direct human us...

  18. TRANSPORT AND DEPOSITION OF NANO-SIZE PARTICLES IN THE UPPER HUMAN RESPIRATORY AIRWAYS

    Science.gov (United States)

    TRANSPORT AND DEPOSITION OF NANO-SIZE PARTICLES IN THE UPPER HUMAN RESPIRATORY AIRWAYS. Zhe Zhang*, Huawei Shi, Clement Kleinstreuer, Department of Mechanical and Aerospace Engineering, North Carolina State University, Raleigh, NC 27695-7910; Chong S. Kim, National Health and En...

  19. Control of properties and performance of polymer gels and networks by structure of the nanosized precursors

    Czech Academy of Sciences Publication Activity Database

    Dušková-Smrčková, Miroslava; Dušek, Karel

    Pardubice : SYNPO, 2010. s. 16. [Workshop on Green Chemistry and Nanotechnologies in Polymer Chemistry /1./. 23.09.2010-24.09.2010, Pardubice] Institutional research plan: CEZ:AV0Z40500505 Keywords : polymer gels * nanosized precursors Subject RIV: CD - Macromolecular Chemistry

  20. Rapid solidification behavior of nano-sized Sn droplets embedded in the Al matrix by nanocalorimetry

    International Nuclear Information System (INIS)

    Al-10Sn (wt.%) melt-spun ribbons with nano-sized Sn droplets (20–400 nm in diameter) embedded in the Al matrix and bulk Sn distributed at Al grain boundaries were prepared. Differential fast scanning calorimetry (DFSC) based on nanocalorimetry and thin film technique was successfully applied to investigate the rapid solidification behavior of the embedded nano-sized Sn droplets at cooling rates ranging from 103 to 104 K s−1. Two broad exothermic peaks were observed in the DFSC curves. They were ascribed to the solidification of nano-sized Sn droplets with various catalytic activity factors f(θ). The cooling rate dependence of undercooling of nano-sized Sn droplets has been studied experimentally. The two series of undercooling which correspond to the two exothermic peaks increase slightly with the increases of cooling rate. Furthermore, a theoretical description of the experimental DFSC curves based on classical heterogeneous nucleation theory is developed. It is performed advancing a previously developed approach by assuming a smooth dependence of the droplet mass fraction on contact angle, m(θ), with a double Gaussian distribution during the nucleation process. This modified theoretical model is believed to be relevant also for other related rapid solidification processes. (paper)

  1. A top-down methodology for ultrafast tuning of nanosized zeolites.

    Science.gov (United States)

    Liu, Zhendong; Nomura, Naoki; Nishioka, Daisuke; Hotta, Yuusuke; Matsuo, Takeshi; Oshima, Kazunori; Yanaba, Yutaka; Yoshikawa, Takeshi; Ohara, Koji; Kohara, Shinji; Takewaki, Takahiko; Okubo, Tatsuya; Wakihara, Toru

    2015-08-14

    We herein present a top-down methodology to prepare nanosized zeolites with tunable size by combining post-synthesis milling and fast recrystallization of several minutes (10 min for SSZ-13 and 5 min for AlPO4-5). A continuous-flow recrystallization process is demonstrated to further enhance the overall product efficiency. PMID:26154841

  2. Nano-Sized Zero Valent Iron and Covalent Organic Polymer Composites for Azo Dye Remediation

    DEFF Research Database (Denmark)

    Mines, Paul D.; Byun, Jeehye; Hwang, Yuhoon;

    2014-01-01

    Having superior reductive properties and large surface areas, nanosized zero valent iron (nZVI) is ideal for the degradation of chemicals such as azo dyes and trichloroethylene (TCE). However, immobilization of nZVI is a key parameter in its effectiveness as a chemical degradation agent. In this...

  3. One-dimensional random walk of nanosized liquid Pb inclusions on dislocations in Al

    DEFF Research Database (Denmark)

    Johnson, E.; Levinsen, M.T.; Steenstrup, S.; Prokofjev, S.; Zhilin, V.; Dahmen, U.; Radetic, T.

    Migration of nanosized liquid Pb inclusions attached to dislocations in Al has been observed during in-situ transmission electron microscopy heating experiments and monitored by real-time video recordings. The movements of the inclusions can be separated into two independent components parallel to...

  4. Thermal Stress Behavior of Micro- and Nano-Size Aluminum Films

    International Nuclear Information System (INIS)

    In-situ observation of thermal stresses in thin films deposited on silicon substrate was made by X-ray and synchrotron radiation. Specimens prepared in this experiment were micro- and nano-size thin aluminum films with and without passivation film. The thickness of the film was 1 micrometer for micro-size films and 10, 20 and 50 nanometer for nano-size films. The stress measurement in micro-size films was made by X-ray radiation whereas the measurement of nano-size films was made by synchrotron radiation. Residual stress measurement revealed tensile stresses in all as-deposited films. Thermal stresses were measured in a series of heating- and cooling-stage. Thermal stress behavior of micro-size films revealed hysteresis loop during a heating and cooling process. The width of a hysteresis loop was larger in passivated film that unpassivated film. No hysteresis loops were observed in nano-size films with SiO2 passivation. Strengthning mechanism in thin films was discussed on a passivation film and a film thickness

  5. Nano-sized polystyrene affects feeding, behavior and physiology of brine shrimp Artemia franciscana larvae

    NARCIS (Netherlands)

    Bergami, Elisa; Bocci, Elena; Vannuccini, Maria Luisa; Monopoli, Marco; Salvati, Anna; Dawson, Kenneth A; Corsi, Ilaria

    2016-01-01

    Nano-sized polymers as polystyrene (PS) constitute one of the main challenges for marine ecosystems, since they can distribute along the whole water column affecting planktonic species and consequently disrupting the energy flow of marine ecosystems. Nowadays very little knowledge is available on th

  6. Preparation and electrochemical properties of nanosized tin dioxide electrode material by sol-gel process

    Institute of Scientific and Technical Information of China (English)

    何则强; 李新海; 吴显明; 侯朝辉; 刘恩辉; 邓凌峰; 胡传跃; 田慧鹏

    2003-01-01

    Nanosized SnO2 powders were prepared by sol-gel process using inorganic salt as a precursor. The tin oxide powders obtained at different calcinating temperatures (300-700 ℃) were investigated by means of X-ray diffraction(XRD), infrared spectrum (IR), thermogravimetric analysis (TGA), differential thermal analysis (DTA) and transmission electron microscopy (TEM) as well. The results indicate that well-crystallized nanosized SnO2 powders with a structure of rutile and uniform size about 10 nm can be obtained when the calcinating is carried out at 550 ℃ for 3 h using the method. The electrochemical properties of nanosized SnO2 powders as anode material for lithium ion batteries were also studied in detail. The results show that nanosized SnO2 is a candidate of anode material for lithium ion batteries with reversible capacity more than 372 mA*h/g after ten cycles and low voltage for Li+ intercalation and de-intercalation.

  7. Effect of sodium citrate on preparation of nano-sized cobalt particles by organic colloidal process

    Institute of Scientific and Technical Information of China (English)

    Huaping ZHU; Hao LI; Huiyu SONG; Shijun LIAO

    2009-01-01

    Nano-sized cobalt particles with the diameter of 2 nm were prepared via an organic colloidal process with sodium formate, ethylene glycol and sodium citrate as the reducing agent, the solvent and the complexing agent, respectively. The effects of sodium citrate on the yield, crystal structure, particle size and size distribution of the prepared nano-sized cobalt particles were then investigated. The results show that the average particle diameter decreases from 200 nm to 2 nm when the molar ratio of sodium citrate to cobalt chloride changes from 0 to 6. Furthermore, sodium citrate plays a crucial role in the controlling of size distribution of the nano-sized particles. The size distribution of the particle without sodium citrate addition is in range from tens of nanometers to 300 or 400 nm, while that with sodium citrate addition is limited in the range of (2±0.25) nm. Moreover, it is found that the addition of sodium citrate as a complex agent could decrease the yield of the nano-sized cobalt particle.

  8. Creation of deep blue light emitting nitrogen-vacancy center in nanosized diamond

    Energy Technology Data Exchange (ETDEWEB)

    Himics, L., E-mail: himics.laszlo@wigner.mta.hu; Tóth, S.; Veres, M.; Koós, M. [Institute for Solid State Physics and Optics, Wigner Research Center for Physics, Hungarian Academy of Sciences, H-1525 Budapest, P.O. Box 49 (Hungary); Balogh, Z. [Uzhhorod National University, 88000 Uzhhorod (Ukraine)

    2014-03-03

    This paper reports on the formation of complex defect centers related to the N3 center in nanosized diamond by employing plasma immersion and focused ion beam implantation methods. He{sup +} ion implantation into nanosized diamond “layer” was performed with the aim of creating carbon atom vacancies in the diamond structure, followed by the introduction of molecular N{sub 2}{sup +} ion and heat treatment in vacuum at 750 °C to initiate vacancy diffusion. To decrease the sp{sup 2} carbon content of nanosized diamond formed during the implantation processes, a further heat treatment at 450 °C in flowing air atmosphere was used. The modification of the bonding properties after each step of defect creation was monitored by Raman scattering measurements. The fluorescence measurements of implanted and annealed nanosized diamond showed the appearance of an intensive and narrow emission band with fine structures at 2.98 eV, 2.83 eV, and 2.71 eV photon energies.

  9. Creation of deep blue light emitting nitrogen-vacancy center in nanosized diamond

    International Nuclear Information System (INIS)

    This paper reports on the formation of complex defect centers related to the N3 center in nanosized diamond by employing plasma immersion and focused ion beam implantation methods. He+ ion implantation into nanosized diamond “layer” was performed with the aim of creating carbon atom vacancies in the diamond structure, followed by the introduction of molecular N2+ ion and heat treatment in vacuum at 750 °C to initiate vacancy diffusion. To decrease the sp2 carbon content of nanosized diamond formed during the implantation processes, a further heat treatment at 450 °C in flowing air atmosphere was used. The modification of the bonding properties after each step of defect creation was monitored by Raman scattering measurements. The fluorescence measurements of implanted and annealed nanosized diamond showed the appearance of an intensive and narrow emission band with fine structures at 2.98 eV, 2.83 eV, and 2.71 eV photon energies

  10. Creation of deep blue light emitting nitrogen-vacancy center in nanosized diamond

    Science.gov (United States)

    Himics, L.; Tóth, S.; Veres, M.; Balogh, Z.; Koós, M.

    2014-03-01

    This paper reports on the formation of complex defect centers related to the N3 center in nanosized diamond by employing plasma immersion and focused ion beam implantation methods. He+ ion implantation into nanosized diamond "layer" was performed with the aim of creating carbon atom vacancies in the diamond structure, followed by the introduction of molecular N2+ ion and heat treatment in vacuum at 750 °C to initiate vacancy diffusion. To decrease the sp2 carbon content of nanosized diamond formed during the implantation processes, a further heat treatment at 450 °C in flowing air atmosphere was used. The modification of the bonding properties after each step of defect creation was monitored by Raman scattering measurements. The fluorescence measurements of implanted and annealed nanosized diamond showed the appearance of an intensive and narrow emission band with fine structures at 2.98 eV, 2.83 eV, and 2.71 eV photon energies.

  11. Spin-glass-like ordering of the magnetic moments of interacting nanosized maghemite particles

    DEFF Research Database (Denmark)

    Mørup, Steen; Bødker, Franz; Hendriksen, Peter Vang;

    1995-01-01

    Samples of interacting nanosized maghemite particles have been studied by Mössbauer spectroscopy and magnetization measurements. The apparent blocking temperatures obtained from Mössbauer spectroscopy and zero-field-cooled magnetization curves are nearly identical, but the values obtained from...

  12. Development and pharmacokinetic of antimony encapsulated in liposomes of phosphatidylserine using radioisotopes in experimental leishmaniasis

    International Nuclear Information System (INIS)

    Leishmaniasis are a complex of parasitic diseases caused by intra macrophage protozoa of the genus Leishmania, and is fatal if left untreated. Pentavalent antimonials, though toxic and their mechanism of action being unclear, remain the first-line drugs for treatment. Effective therapy could be achieved by delivering antileishmanial drugs to these sites of infection. Liposomes are phospholipid vesicles that promote improvement in the efficacy and action of drugs in target cell. Liposomes are taken up by the cells of mononuclear phagocytic system (MPS). The purpose of this study was to develop a preparation of meglumine antimonate encapsulated in liposomes of phosphatidylserine and to study its pharmacokinetic in healthy mice to establish its metabolism and distribution. Quantitative analysis of antimony from liposomes demonstrated that Neutron Activation Analysis was the most sensitive technique with almost 100 % of accuracy. All liposome formulations presented a mean diameter size of 150 nm. The determination of IC50 in infected macrophage showed that liposome formulations were between 10 - 63 fold more effective than the free drug, indicating higher selectivity index. By fluorescence microscopy, an increased uptake of fluorescent-liposomes was seen in infected macrophages during short times of incubation compared with non-infected macrophages. Biodistribution studies showed that meglumine antimonate irradiated encapsulated in liposomes of phosphatidylserine promoted a targeting of antimony for MPS tissues and maintained high doses in organs for a prolonged period. In conclusion, these data suggest that meglumine antimonate encapsulated in liposomes showed higher effectiveness than the non-liposomal drug against Leishmania infection. The development of liposome formulations should be a new alternative for the chemotherapy of infection diseases, especially Leishmaniasis, as they are used to sustain and target pharmaceuticals to the local of infection. (author)

  13. Functional coating of liposomes using a folate–polymer conjugate to target folate receptors

    Directory of Open Access Journals (Sweden)

    Watanabe K

    2012-07-01

    Full Text Available Kazuo Watanabe, Makoto Kaneko, Yoshie MaitaniInstitute of Medical Chemistry, Hoshi University, Tokyo, JapanAbstract: Folate-polymer-coated liposomes were developed for targeted chemotherapy using doxorubicin (DXR as a model drug. Folate-poly(L-lysine (F–PLL conjugates with a folate modification degree of 16.7 mol% on epsilon amino groups of PLL were synthesized. DXR-loaded anionic liposomes were coated with F–PLL, and the cellular association of F–PLL-coated liposomes was evaluated by flow cytometry, and confocal microscopy in human nasopharyngeal carcinoma KB cells overexpressing folate receptors (FRs, and human lung adenocarcinoma A549 cells [FR (-]. The existence of a polymer layer on the surface of F–PLL-coated liposomes was confirmed by zeta potential analysis. The KB cellular association of F–PLL-coated liposomal DXR was increased compared with that of PLL-coated liposomes and was inhibited in the presence of free folic acid. Twofold higher cytotoxicity of F–PLL-coated liposomal DXR was observed compared with that of the PLL-coated liposomal DXR in KB cells, but not in A549 cells, suggesting the presence of FR-mediated endocytosis. These results indicated that folate-targeted liposomes were prepared successfully by coating the folate–polymer conjugate F–PLL. This novel preparation method of folate-targeted liposomes is expected to provide a powerful tool for the development of a folate-targeting drug nanodevice as coating with ligand–polymer conjugates can be applicable to many kinds of particles, as well as to lipid-based particles.Keywords: cellular association, folate-targeting, liposome, poly-L-lysine, polymer coating, tumor targeting

  14. Retrospective analysis of quality improvement when using liposome bupivacaine for postoperative pain control

    Science.gov (United States)

    King, Nicole M; Quiko, Albin S; Slotto, James G; Connolly, Nicholas C; Hackworth, Robert J; Heil, Justin W

    2016-01-01

    Background/objective Liposome bupivacaine, a prolonged-release bupivacaine formulation, recently became available at the Naval Medical Center San Diego (NMCSD); before availability, postsurgical pain for large thoracic/abdominal procedures was primarily managed with opioids with/without continuous thoracic epidural (CTE) anesthesia. This retrospective chart review was part of a clinical quality initiative to determine whether postsurgical outcomes improved after liposome bupivacaine became available. Methods Data from patients who underwent laparotomy, sternotomy, or thoracotomy at NMCSD from May 2013 to May 2014 (after liposome bupivacaine treatment became available) were compared with data from patients who underwent these same procedures from December 2011 to May 2012 (before liposome bupivacaine treatment became available). Collected data included demographics, postoperative pain control methods, opioid consumption, perioperative pain scores, and lengths of intensive care unit and overall hospital stays. Results Data from 182 patients were collected: 88 pre-liposome bupivacaine (laparotomy, n=52; sternotomy, n=26; and thoracotomy, n=10) and 94 post-liposome bupivacaine (laparotomy, n=49; sternotomy, n=31; and thoracotomy, n=14) records. Mean hospital stay was 7.0 vs 5.8 days (P=0.009) in the pre- and post-liposome bupivacaine groups, respectively, and mean highest reported postoperative pain score was 7.1 vs 6.2 (P=0.007), respectively. No other significant between-group differences were observed for the overall population. In the laparotomy subgroup, there was a reduction in the proportion of patients who received CTE anesthesia post-liposome bupivacaine (22% [11/49] vs 35% [18/52] pre-liposome bupivacaine). Conclusion Surgeons and anesthesiologists have changed the way they manage postoperative pain since the time point that liposome bupivacaine was introduced at NMCSD. Our findings suggest that utilization of liposome bupivacaine may be a useful alternative

  15. Liposomal drug delivery system from laboratory to clinic.

    Science.gov (United States)

    Kshirsagar, N A; Pandya, S K; Kirodian, G B; Sanath, S

    2005-01-01

    The main objective of drug delivery systems is to deliver a drug effectively, specifically to the site of action and to achieve greater efficacy and minimise the toxic effects compared to conventional drugs. Amongst various carrier systems, liposomes have generated a great interest because of their versatility. Liposomes are vesicular concentric bilayered structures, which are biocompatible, biodegradable and nonimmumnogenic. They can control the delivery of drugs by targeting the drug to the site of action or by site avoidance drug delivery or by prolonged circulation of drugs. Amphotericin B (Amp B) remains the drug of choice in most systemic mycoses and also as a second line treatment for Kala azar. However, its toxic effects often limit its use. Although the liposome delivery system has been tried for several drugs, only a few have been used in patients due to the slow development of necessary large-scale pharmaceutical procedures. This paper reviews the development of the technique for liposomal Amphotericin B (L-Amp-LRC-1, Fungisome) drug delivery system in our laboratory in collaboration with the department of Biochemistry, Delhi University in India and proving the safety and efficacy of this preparation in clinical practice. It also attempts to compare the efficacy and benefits of our product for Indian patients with those of similar products and it includes facts from the publications that flowed from our work. As compared to conventional Amp B, Fungisome is infused over a much shorter period requiring a smaller volume and no premedication. It was found to be safe in patients who had developed serious unacceptable toxicity with conventional Amp B. In renal transplant patients, Fungisome did not produce any nephrotoxicity. Fungisome is effective in fungal infections resistant to fluconazole, conventional Amp B and in virgin and resistant cases of visceral leishmaniasis. The cost of any drug is of great significance, especially in India. We have therefore

  16. Liposomal drug delivery system from laboratory to clinic

    Directory of Open Access Journals (Sweden)

    Kshirsagar N

    2005-01-01

    Full Text Available The main objective of drug delivery systems is to deliver a drug effectively, specifically to the site of action and to achieve greater efficacy and minimise the toxic effects compared to conventional drugs. Amongst various carrier systems, liposomes have generated a great interest because of their versatility. Liposomes are vesicular concentric bilayered structures, which are biocompatible, biodegradable and nonimmumnogenic. They can control the delivery of drugs by targeting the drug to the site of action or by site avoidance drug delivery or by prolonged circulation of drugs. Amphotericin B (Amp B remains the drug of choice in most systemic mycoses and also as a second line treatment for Kala azar. However, its toxic effects often limit its use. Although the liposome delivery system has been tried for several drugs, only a few have been used in patients due to the slow development of necessary large-scale pharmaceutical procedures. This paper reviews the development of the technique for liposomal Amphotericin B (L-Amp-LRC-1, FungisomeTM drug delivery system in our laboratory in collaboration with the department of Biochemistry, Delhi University in India and proving the safety and efficacy of this preparation in clinical practice. It also attempts to compare the efficacy and benefits of our product for Indian patients with those of similar products and it includes facts from the publications that flowed from our work. As compared to conventional Amp B, Fungisome is infused over a much shorter period requiring a smaller volume and no premedication. It was found to be safe in patients who had developed serious unacceptable toxicity with conventional Amp B. In renal transplant patients, Fungisome did not produce any nephrotoxicity. Fungisome is effective in fungal infections resistant to fluconazole, conventional Amp B and in virgin and resistant cases of visceral leishmaniasis. The cost of any drug is of great significance, especially in India

  17. Liposomal clodronate selectively eliminates microglia from primary astrocyte cultures

    Directory of Open Access Journals (Sweden)

    Kumamaru Hiromi

    2012-05-01

    Full Text Available Abstract Background There is increasing interest in astrocyte biology because astrocytes have been demonstrated to play prominent roles in physiological and pathological conditions of the central nervous system, including neuroinflammation. To understand astrocyte biology, primary astrocyte cultures are most commonly used because of the direct accessibility of astrocytes in this system. However, this advantage can be hindered by microglial contamination. Although several authors have warned regarding microglial contamination in this system, complete microglial elimination has never been achieved. Methods The number and proliferative potential of contaminating microglia in primary astrocyte cultures were quantitatively assessed by immunocytologic and flow cytometric analyses. To examine the utility of clodronate for microglial elimination, primary astrocyte cultures or MG-5 cells were exposed to liposomal or free clodronate, and then immunocytologic, flow cytometric, and gene expression analyses were performed. The gene expression profiles of microglia-eliminated and microglia-contaminated cultures were compared after interleukin-6 (IL-6 stimulation. Results The percentage of contaminating microglia exceeded 15% and continued to increase because of their high proliferative activity in conventional primary astrocyte cultures. These contaminating microglia were selectively eliminated low concentration of liposomal clodronate. Although primary microglia and MG-5 cells were killed by both liposomal and free clodronate, free clodronate significantly affected the viability of astrocytes. In contrast, liposomal clodronate selectively eliminated microglia without affecting the viability, proliferation or activation of astrocytes. The efficacy of liposomal clodronate was much higher than that of previously reported methods used for decreasing microglial contamination. Furthermore, we observed rapid tumor necrosis factor-α and IL-1b gene induction in

  18. Tumor burden talks in cancer treatment with PEGylated liposomal drugs.

    Directory of Open Access Journals (Sweden)

    Yi-Yu Lin

    Full Text Available PURPOSE: PEGylated liposomes are important drug carriers that can passively target tumor by enhanced permeability and retention (EPR effect in neoplasm lesions. This study demonstrated that tumor burden determines the tumor uptake, and also the tumor response, in cancer treatment with PEGylated liposomal drugs in a C26/tk-luc colon carcinoma-bearing mouse model. METHODS: Empty PEGylated liposomes (NanoX and those encapsulated with VNB (NanoVNB were labeled with In-111 to obtain InNanoX and InVNBL in high labeling yield and radiochemical purity (all >90%. BALB/c mice bearing either small (58.4±8.0 mm(3 or large (102.4±22.0 mm(3 C26/tk-luc tumors in the right dorsal flank were intravenously administered with NanoVNB, InNanoX, InVNBL, or NanoX as a control, every 7 days for 3 times. The therapeutic efficacy was evaluated by body weight loss, tumor growth inhibition (using calipers and bioluminescence imaging and survival fraction. The scintigraphic imaging of tumor mouse was performed during and after treatment. RESULTS: The biodistribution study of InVNBL revealed a clear inverse correlation (r (2 = 0.9336 between the tumor uptake and the tumor mass ranged from 27.6 to 623.9 mg. All three liposomal drugs showed better therapeutic efficacy in small-tumor mice than in large-tumor mice. Tumor-bearing mice treated with InVNBL (a combination drug showed the highest tumor growth inhibition rate and survival fraction compared to those treated with NanoVNB (chemodrug only and InNanoX (radionuclide only. Specific tumor targeting and significantly increased tumor uptake after periodical treatment with InVNBL were evidenced by scintigraphic imaging, especially in mice bearing small tumors. CONCLUSION: The significant differences in the outcomes of cancer treatment and molecular imaging between animals bearing small and large tumors revealed that tumor burden is a critical and discriminative factor in cancer therapy using PEGylated liposomal drugs.

  19. Sphingomyelin-cholesterol liposomes significantly enhance the pharmacokinetic and therapeutic properties of vincristine in murine and human tumour models.

    OpenAIRE

    Webb, M S; Harasym, T. O.; Masin, D.; Bally, M. B.; Mayer, L. D.

    1995-01-01

    This study reports on the development of a liposomal formulation of vincristine with significantly enhanced stability and biological properties. The in vitro and in vivo pharmacokinetic, tumour delivery and efficacy properties of liposomal vincristine formulations based on sphingomyelin (SM) and cholesterol were compared with liposomes composed of distearoylphosphatidylcholine (DSPC) and cholesterol. SM/cholesterol liposomes had significantly greater in vitro stability than did similar DSPC/c...

  20. Preparation of novel capsosome with liposomal core by layer-by-Layer self-assembly of sodium hyaluronate and chitosan.

    Science.gov (United States)

    Yoo, Cha Young; Seong, Joon Seob; Park, Soo Nam

    2016-08-01

    Multi-compartmentalized capsosomes are polyelectrolyte capsules with liposomes as cargo, and are prepared by combining liposomes and polymer capsules. They offer additional functionality while maintaining the advantages and compensating for the weak points of both systems. In this study, a polyelectrolyte multilayered liposome was prepared by alternating adsorption of negatively charged sodium hyaluronate (HA) and positively charged chitosan (CH) on the surface of a cationic core liposome (CL) via layer-by-layer (LbL) deposition. Then, smaller sized liposomes (L) were coated onto the multilayered liposome. Lastly, the particle surfaces were coated with HA as a capping layer to obtain a novel type of capsosome with a liposomal core. The amount of adsorbed liposome was measured for different pH values (pH 2-10) and with liposome solutions of different concentrations (1-3%). The highest liposome adsorption occurred at pH 10 in the 3% solution, respectively. Finally, capsosomes in the size range of 500nm to 2μm were observed and the attached liposomes were located both on the surface and within the polymer shell. In conclusion, the cell-mimicking, liposome-based capsosomes could have infinite applications in the field of medicine, pharmaceuticals, and cosmetics as compartmentalized microreactors, multi-drug delivery systems with controlled release, or functional artificial cells in the future. PMID:27085041

  1. Neuroprotection against cerebral ischemia/reperfusion injury by intravenous administration of liposomal fasudil.

    Science.gov (United States)

    Fukuta, Tatsuya; Asai, Tomohiro; Sato, Akihiko; Namba, Mio; Yanagida, Yosuke; Kikuchi, Takashi; Koide, Hiroyuki; Shimizu, Kosuke; Oku, Naoto

    2016-06-15

    Fasudil, a Rho-kinase inhibitor, is a promising neuroprotectant against ischemic stroke; however, its low bioavailability is an obstacle to be overcome. Our previous study revealed that the liposomal drug delivery system is a hopeful strategy to increase the therapeutic efficacy of neuroprotectants. In the present study, the usefulness of intravenously administered liposomal fasudil for cerebral ischemia/reperfusion (I/R) injury treatment was examined in transient middle cerebral artery occlusion (t-MCAO) rats. The results showed that PEGylated liposomes of approximately 100nm in diameter accumulated more extensively in the I/R region compared with those of over 200nm. Confocal images showed that fluorescence-labeled liposomal fasudil was widely distributed in the I/R region, and was not noticeably taken up by microglia, which are well-known resident macrophages in the brain, and neuronal cells. These data indicated that liposomal fasudil mainly exerted its pharmacological activity by releasing fasudil from the liposomes in the I/R region. Moreover, liposomal fasudil effectively suppressed neutrophil invasion and brain cell damage in the t-MCAO rats, resulting in amelioration of their motor function deficits. These findings demonstrated both the importance of particle size for neuroprotectant delivery and the effectiveness of liposomal fasudil for the treatment of cerebral I/R injury. PMID:27107903

  2. Atomized paclitaxel liposome inhalation treatment of bleomycin-induced pulmonary fibrosis in rats.

    Science.gov (United States)

    Zhou, Y; Zhu, W P; Cai, X J; Chen, M

    2016-01-01

    We sought to determine the efficacy of atomized paclitaxel liposome inhalation treatment of pulmonary fibrosis in a bleomycin-induced rat model. Forty male Sprague-Dawley rats were randomly divided into four groups: healthy control, pulmonary fibrosis without treatment, paclitaxel liposome inhalation-treated, and intravenous paclitaxel liposome-treated. Fibrosis was induced by bleomycin injection. A total of 20 mg/kg paclitaxel liposome was administered by inhalation every other day for a total of 10 doses. The intravenous group received 5 mg/kg paclitaxel liposome on days 1, 7, 14, and 21. We observed the general condition, weight change, survival index, and pathological changes in the lung tissue of the rats. Quantitative analysis of collagen types I and III and transforming growth factor (TGF)-β1 expression in the lungs was also performed. The paclitaxel liposome inhalation and intravenous delivery methods improved survival index and pulmonary fibrosis Ashcroft score, and decreased the thickness of the alveolar interval. No obvious difference was found between the two groups. Compared with the untreated group, paclitaxel liposome inhalation and intravenous injection significantly reduced the levels of collagen types I and III and TGF-β1 expression equally. In conclusion, atomized paclitaxel liposome inhalation protects against severe pulmonary fibrosis in a bleomycin-induced rat model. This delivery method has less systemic side effects and increased safety over intravenous injection. PMID:27173212

  3. Kinetics of the valinomycin-induced potassium ion leak from liposomes with potassium thiocyanate enclosed

    NARCIS (Netherlands)

    Blok, M.C.; Gier, J. de; Deenen, L.L.M. van

    1974-01-01

    The kinetics of the valinomycin-induced K+ leak from egg lecithin liposomes with KCNS enclosed were studied by measuring the initial increase of the leak following the addition of the ionophore. Variation of liposome and valinomycin concentrations enabled a discrimination between the affinity of the

  4. In vitro and in vivo aspects of N-acyl-phosphatidylethanolamine-containing liposomes

    DEFF Research Database (Denmark)

    Vermehren, C.; Clausen-Beck, B.; Frøkjær, S.; Hansen, Harald S.

    2003-01-01

    Incorporation of the phospholipid, N-acyl-phosphatidylethanolamine (NAPE), has shown to increase the liposomal stability towards plasma components in vitro. Besides increasing the circulation-time, NAPE has been shown to contain fusiogenic properties. Hence, fusion between NAPE-liposomes and targ...

  5. FTIR Characterization of the Secondary Structure of Insulin Encapsulated within Liposome

    Institute of Scientific and Technical Information of China (English)

    ZHANGXuan; HUANGLi-xin; NIESong-qing; QIXian-rong; ZHANGQiang

    2003-01-01

    Aim:To determine the secondary structure of insulin encapsulated within liposome.Methods:The secondary structure of native insulin,mixture of insulin with liposome(sample I) and insulin encapsulated within liposome(sample Ⅱ) were determined by FTIR(Fourier Transform Infrared) spectroscopy.Results:The secondary structure of insulin encspsulated within liposome(Ⅱ) are similar with the secondary structure of native insulin.The difference existed in the amount of α-helices (from 36% of insulin to 31% of sample Ⅱ)and β-sheet(from 48% of insulin to 51% of sample Ⅱ).The content of α-helices and β-sheet of insulin in sample I was found to be very close to that of sample Ⅱ.The results revealed that the insulin encapsulated within liposome possibly spread on the surface of liposome,without inserting into the liposome membrane.Coclusion:The secondary structure of insulin encapsulated within liposome is similar with the native insulin.

  6. Intravenously delivered glucocorticoid liposomes inhibit osteoclast activity and bone erosion in murine antigen-induced arthritis

    NARCIS (Netherlands)

    Hofkens, Wouter; Grevers, Lilyanne C.; Walgreen, Birgitte; de Vries, Teun J.; Leenen, Pieter J. M.; Everts, Vincent; Storm, Gert; van den Berg, Wim B.; van Lent, Peter L.

    2011-01-01

    The objective of this study was to determine the effect of systemic delivery of prednisolone phosphate (PLP) encapsulated within long circulating 'stealth' liposomes on bone erosion and osteoclast activity during experimental antigen-induced arthritis (AIA). Liposomal PLP strongly suppressed knee jo

  7. Inhalational system for etoposide liposomes: Formulation development and in vitro deposition

    Directory of Open Access Journals (Sweden)

    J J Parmar

    2011-01-01

    Full Text Available Etoposide is a semisynthetic compound, widely used in treatment of non small cell lung cancer. However, frequent dosing and adverse effects remain a major concern in the use of etoposide. Liposomal systems for pulmonary drug delivery have been particularly attractive because of their compatibility with lung surfactant components. In the present investigation, pulmonary liposomal delivery system of etoposide was prepared by film hydration method. Various parameters were optimized with respect to entrapment efficiency as well as particle size of etoposide liposomes. For better shelf life of etoposide liposomes, freeze drying using trehalose as cryoprotectant was carried out. The liposomes were characterized for entrapment efficiency, particle size, surface topography, and in vitro drug release was carried out in simulated lung fluid at 37° at pH 7.4. The respirable or fine particle fraction was determined by using twin stage impinger. The stability study of freeze dried as well as aqueous liposomal systems was carried out at 2-8° and at ambient temperature (28±4° . The freeze dried liposomes showed better fine particle fraction and drug content over the period of six months at ambient as well as at 2-8° storage condition compared to aqueous dispersion of liposomes.

  8. Vibrating-mesh nebulization of liposomes generated using an ethanol-based proliposome technology.

    Science.gov (United States)

    Elhissi, Abdelbary; Gill, Hardyal; Ahmed, Waqar; Taylor, Kevin

    2011-06-01

    This is the first study that evaluates the influence of the compartmental design of the micropump Aeroneb Go nebulizer and the viscosity of a proliposome hydration medium on vibrating-mesh aerosolization of liposomes. Ethanol-based proliposomes comprising soya phosphatidylcholine and cholesterol (1:1 mole ratio) were hydrated by using isotonic NaCl (0.9%) or sucrose (9.25%) solutions to generate liposomes that entrapped approximately 61% of the hydrophilic drug, salbutamol sulphate. Liposomes were aerosolized by the nebulizer to a two-stage impinger. For both formulations, the aerosol mass output was higher than the phospholipid output, indicating some accumulation of large liposomes or liposome aggregate within the nebulizer. Using NaCl (0.9%) solution as the dispersion medium, aerosol droplet size was much smaller and aerosol mass and phospholipid outputs were higher. This was attributed to the lower viscosity of the NaCl solution, resulting in a reduced retention of the aerosols in the "trap" of the nebulizer. For the entrapped salbutamol sulphate, although the "fine particle fraction" was relatively high (57.44%), size reduction of the liposomes during nebulization caused marked losses of the drug originally entrapped. Overall, liposomes generated from proliposomes when using this nebulizer showed high nebulization output and small droplet size. However, further work is required to reduce the losses of the originally entrapped drug from liposomes. PMID:20684671

  9. Preparation and evaluation of mafenide acetate liposomal formulation as eschar delivery system

    Directory of Open Access Journals (Sweden)

    Behzad Sharif Makhmalzadeh

    2011-12-01

    Full Text Available Mafenide acetate is a commonly known antimicrobial agent for wound infection. Permeability of mafenide acetate through eschar is very high and it may lead to systemic toxicity after topical application. We wish to investigate whether topical use of mafenide acetate – including vesicles could result in drug trapping in rat skin, in comparison to mafenide acetate aqueous solution. In this study, liposomes were prepared with two techniques: Solvent evaporation and Microencapsulation vesicular (MCV. We applied full factorial design for experimental design and data analysis. Drug/lipid ratio, hydration time, aqueous phase volume and homogenizer rpm were considered as independent variable, on the other hand, liposome size, drug loading, stability, drug release and skin permeability parameters as responses. The results demonstrate that liposome were multilamellar and multivesicular. Particle size and drug loading percentage of MCV liposome indicated burst sustained release profile. Burst effect in solvent evaporation liposome was more than MCV liposome. In conclusion, solvent evaporation liposome improved mafenide acetate partitioning through rat skin and decrease diffusion coefficient with increase particle size of liposome.

  10. Silicone-stabilized liposomes as a possible novel nanostructural drug carrier.

    Science.gov (United States)

    Lewandowska-Łańcucka, Joanna; Mystek, Katarzyna; Gilarska, Adriana; Kamiński, Kamil; Romek, Marek; Sulikowski, Bogdan; Nowakowska, Maria

    2016-07-01

    Development of silicone stabilized liposomes which can serve as novel drug nanocarriers is presented. Silicone precursor 1,3,5,7-tetramethylcyclotetrasiloxane (D4(H)) was introduced into the bilayer of the cationic liposomes prepared from egg yolk phosphatidylocholine (PC) and double-tailed dimethyldioctadecylammonium bromide (DODAB). The silicone material was created inside of the liposomal bilayer in the base-catalyzed polycondensation process of the D4(H) what was confirmed employing (29)Si solid-state MAS NMR and FTIR measurements. Surfactant lysis experiments revealed that resulted systems can be effectively stabilized. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) measurements demonstrated that the silicone-stabilized liposomes have typical lipid vesicle's morphology and mean hydrodynamic diameters in the range of about 110nm. They have considerably lower tendency for aggregation than the pristine liposomes. The permeability of vesicles can be tuned by introducing various amounts of silicone precursor into the liposome bilayer, as confirmed in calcein-release studies. The effect of fetal bovine serum (FBS) on the stability of liposomes was also tested in in vitro studies. Biological studies revealed that resulted liposomes can be considered as possible drug nanocarriers because they are not toxic to human skin fibroblasts (HSFs) and mouse embryonic fibroblasts (MEFs). PMID:27022877

  11. Influence of microenvironment and liposomal formulation on secondary structure and bilayer interaction of lysozyme.

    Science.gov (United States)

    Witoonsaridsilp, Wasu; Panyarachun, Busaba; Sarisuta, Narong; Müller-Goymann, Christel C

    2010-02-01

    The conformation of peptide and protein drugs in various microenvironments and the interaction with drug carriers such as liposomes are of considerable interest. In this study the influence of microenvironments such as pH, salt concentration, and surface charge on the secondary structure of a model protein, lysozyme, either in solution or entrapped in liposomes with various molar ratios of phosphatidylcholine (PC):cholesterol (Chol) was investigated. It was found that entrapment efficiency was more pronounced in negatively charged liposomes than in non-charged liposomes, which was independent of Chol content and pH of hydration medium. The occurrence of aggregation, decrease in zeta potential, and alteration of 31P NMR chemical shift of negatively charged lysozyme liposomes compared to blank liposomes suggested that the electrostatic interaction plays a major role in protein-lipid binding. Addition of sodium chloride could impair the neutralizing ability of positively charged lysozyme on negatively charged membrane via chloride counterion binding. Neither lysozyme in various buffer solutions with sodium chloride nor that entrapped in liposomes showed any significant change in their secondary structures. However, significant decrease in alpha-helical content of lysozyme in non-charged liposomes at higher pH and salt concentrations was discovered. PMID:19880295

  12. Cross-linkable liposomes stabilize a magnetic resonance contrast-enhancing polymeric fastener.

    Science.gov (United States)

    Smith, Cartney E; Kong, Hyunjoon

    2014-04-01

    Liposomes are commonly used to deliver drugs and contrast agents to their target site in a controlled manner. One of the greatest obstacles in the performance of such delivery vehicles is their stability in the presence of serum. Here, we demonstrate a method to stabilize a class of liposomes that load gadolinium, a magnetic resonance (MR) contrast agent, as a model cargo on their surfaces. We hypothesized that the sequential adsorption of a gadolinium-binding chitosan fastener on the liposome surface followed by covalent cross-linking of the lipid bilayer would provide enhanced stability and improved MR signal in the presence of human serum. To investigate this hypothesis, liposomes composed of diyne-containing lipids were assembled and functionalized via chitosan conjugated with a hydrophobic anchor and diethylenetriaminepentaacetic acid (DTPA). This postadsorption cross-linking strategy served to stabilize the thermodynamically favorable association between liposome and polymeric fastener. Furthermore, the chitosan-coated, cross-linked liposomes proved more effective as delivery vehicles of gadolinium than uncross-linked liposomes due to the reduced liposome degradation and chitosan desorption. Overall, this study demonstrates a useful method to stabilize a broad class of particles used for systemic delivery of various molecular payloads. PMID:24635565

  13. Liposomes from mammalian liver mitochondria are more polyunsaturated and leakier to protons than those from reptiles.

    Science.gov (United States)

    Brand, M D; Couture, P; Hulbert, A J

    1994-06-01

    Liposomes were prepared from phospholipids extracted from liver mitochondria of the rat (Rattus norvegicus) and an agamid lizard, the bearded dragon (Amphibolurus vitticeps) and liposome proton conductance was measured at an imposed membrane potential of 160 mV as well as the fatty acid composition of the liposomes. Despite presumed changes in fatty acid composition during liposome preparation, the mammalian liposomes had a significantly lower content of the monounsaturated oleic acid and a significantly greater content of the omega-3 polyunsaturated docosahexaenoic acid. There were significant direct correlations between the liposome arachidonic and docosahexanoic acid content and bilayer proton flux and a significant inverse correlation between liposome oleic acid content and bilayer proton flux. "Apparent valinomycin-catalysed proton flux" was significantly directly correlated with liposome docosahexaenoic acid content and inversely correlated with oleic acid content. It is suggested that the high content of long-chain polyunsaturates in the mammalian mitochondrial membrane is responsible for an increased proton leak across the mitochondrial inner membrane and thus partly responsible for the high metabolic rate in endothermic mammals compared to their ectothermic reptilian predecessors. PMID:8055185

  14. Liposomal encapsulation of dexamethasone modulates cytotoxicity, inflammatory cytokine response, and migratory properties of primary human macrophages

    NARCIS (Netherlands)

    Bartneck, M.; Peters, F.M.; Warzecha, K.T.; Bienert, M.; Bloois, van L.; Trautwein, C.; Lammers, T.G.G.M.; Tacke, F.

    2014-01-01

    The encapsulation of drugs into liposomes aims to enhance their efficacy and reduce their toxicity. Corticosteroid-loaded liposomes are currently being evaluated in patients suffering from rheumatoid arthritis, atherosclerosis, colitis, and cancer. Here, using several different fluorophore-labeled f

  15. CHEMOIMMUNOTHERAPY OF MURINE LIVER METASTASES WITH 5-FLUOROURACIL IN COMBINATION WITH LIPOSOME-ENCAPSULATED MURAMYL DIPEPTIDE

    NARCIS (Netherlands)

    DAEMEN, T; DONTJE, BHJ; REGTS, J; SCHERPHOF, GL

    1993-01-01

    The therapeutic effect of a combination of liposomal muramyl dipeptide (MDP) and 5-fluorouracil (5FU) was studied in a murine tumor model of hepatic metastases of the tumor cell line C26, a colon adenocarcinoma. Liposomal MDP (250 mug/kg body wt) and a low, nontoxic, dose of 5FU (10 mg/kg body wt) w

  16. Surface functionalization of liposomes with proteins and carbohydrates for use in anti-cancer applications

    Science.gov (United States)

    Platt, Virginia M.

    Liposomes can be used to exploit the altered biology of cancer thereby increasing delivery of liposome-associated anti-cancer drugs. In this dissertation, I explore methods that utilize the unique cancer expression of the polymeric glycosaminoglycan hyaluronan (HA) and the HA receptor CD44 to target liposomes to tumors, using liposomes functionalized with proteins or oligosaccharides on their surface. To make it easier to prepare protein-functionalized liposomes, a non-covalent protein/liposome association method based upon metal chelation/his 6 interaction was devised and characterized. I evaluated non-covalent attachment of the prodrug converting enzyme yeast cytosine deaminase, the far-red fluorescent protein mKate, two antigens ovalbumin and the membrane proximal region of an HIV GAG and hyaluronidase, a HA-degrading enzyme. In Chapter 2, I describe the synthesis of hyaluronan-oligosaccharide (HA-O) lipid conjugates and their incorporation into liposomes to target CD44-overexpressing cancer cells. HA-O ligands of defined-length, up to 10 monosaccharides, were attached to lipids via various linkers by reductive amination. The HA-lipids were easily incorporated into liposomes but did not mediate binding of liposomes to CD44 overexpressing cells. In Chapter 3, I evaluate the capacity of tris-NTA-Ni-lipids incorporated within a liposome bilayer to associate with his6-tagged proteins. Tris-NTA-lipids of differing structures and avidities were used to associate yeast cytosine deaminase and mKate to the surface of liposomes. Two tris-NTA-lipids and a mono-NTA lipid associated his-tagged proteins to a 1:1 molar ratio in solution. The proteins remained active while associated with the liposome surface. When challenged in vitro with fetal calf serum, tris-NTA-containing liposomes retained his-tagged proteins longer than mono-NTA. However, the tris-NTA/his6 interaction was found to be in a dynamic state; free yeast cytosine deaminase rapidly competed with pre-bound m

  17. Liver contrast enhancement by iohexol carrying liposomes - experimental study using digital imaging X-ray methods

    International Nuclear Information System (INIS)

    Iohexol-carrying liposomes are obtained by the method of detergent dialysis. The maximum iodine content in liposomes is 64.4%. The liposome suspension has been injected into rabbit auricular vein at a dose of 2 ml/min. Images of animal hepar are obtained before injection and after it at min 10, 20 and 30 under comparative standard conditions. Liver images have been taken by DSA-apparatus and CT-unit of III generation. The results show that synthesized liposomes accumulate in the liver parenchyma and account for enhancement of its image. It is believed that liposomes of the kind represent potentially new contrast media and further studies along these lines are justified regardless of their time-consuming nature. 7 refs

  18. Liposome drugs' loading efficiency: a working model based on loading conditions and drug's physicochemical properties.

    Science.gov (United States)

    Zucker, Daniel; Marcus, David; Barenholz, Yechezkel; Goldblum, Amiram

    2009-10-01

    Remote loading of liposomes by transmembrane gradients is one of the best approaches for achieving the high enough drug level per liposome required for the liposomal drug to be therapeutically efficacious. This breakthrough, which enabled the approval and clinical use of nanoliposomal drugs such as Doxil, has not been paralleled by an in-depth understanding that allows predicting loading efficiency of drugs. Here we describe how applying data-mining algorithms on a data bank based on Barenholz's laboratory's 15 years of liposome research experience on remote loading of 9 different drugs enabled us to build a model that relates drug physicochemical properties and loading conditions to loading efficiency. This model enables choosing candidate molecules for remote loading and optimizing loading conditions according to logical considerations. The model should also help in designing pro-drugs suitable for remote loading. Our approach is expected to improve and accelerate development of liposomal formulations for clinical applications. PMID:19508880

  19. Sucrose ester based cationic liposomes as effective non-viral gene vectors for gene delivery.

    Science.gov (United States)

    Zhao, Yinan; Zhu, Jie; Zhou, Hengjun; Guo, Xin; Tian, Tian; Cui, Shaohui; Zhen, Yuhong; Zhang, Shubiao; Xu, Yuhong

    2016-09-01

    As sucrose esters (SEs) are natural and biodegradable excipients with excellent drug dissolution and drug absorption/permeation in controlled release systems, we firstly incorporated SE into liposomes for gene delivery in this article. A peptide-based lipid (CDO14), Gemini-based quaternary ammonium-based lipid (CTA14), and mono-head quaternary ammonium lipid (CPA14), and SE as helper lipid, were prepared into liposomes which could enhance the interactions between liposomes and pDNA. Most importantly, the liposomes with helper lipid SE showed higher transfection and lower cytotoxicity than those without SE in Hela and A549 cells. It was also found that the transfection efficiency increased with the increase of SE content. The selected liposome, CDO14/SE, was able to deliver siRNA against luciferase for silencing gene in lung tumors of mice, with little in vivo toxicity. The results convincingly demonstrated SEs could be highly desirable candidates for gene delivery systems. PMID:27232309

  20. Aptamer-Modified Temperature-Sensitive Liposomal Contrast Agent for Magnetic Resonance Imaging.

    Science.gov (United States)

    Zhang, Kunchi; Liu, Min; Tong, Xiaoyan; Sun, Na; Zhou, Lu; Cao, Yi; Wang, Jine; Zhang, Hailu; Pei, Renjun

    2015-09-14

    A novel aptamer modified thermosensitive liposome was designed as an efficient magnetic resonance imaging probe. In this paper, Gd-DTPA was encapsulated into an optimized thermosensitive liposome (TSL) formulation, followed by conjugation with AS1411 for specific targeting against tumor cells that overexpress nucleolin receptors. The resulting liposomes were extensively characterized in vitro as a contrast agent. As-prepared TSLs-AS1411 had a diameter about 136.1 nm. No obvious cytotoxicity was observed from MTT assay, which illustrated that the liposomes exhibited excellent biocompatibility. Compared to the control incubation at 37 °C, the liposomes modified with AS1411 exhibited much higher T1 relaxivity in MCF-7 cells incubated at 42 °C. These data indicate that the Gd-encapsulated TSLs-AS1411 may be a promising tool in early cancer diagnosis. PMID:26212580

  1. On the phase diagram of reentrant condensation in polyelectrolyte-liposome complexation

    Science.gov (United States)

    Sennato, S.; Bordi, F.; Cametti, C.

    2004-09-01

    Complexation of polyions with oppositely charged spherical liposomes has been investigated by means of dynamic light scattering measurements and a well-defined reentrant condensation has been observed. The phase diagram of charge inversion, recently derived [T. T. Nguyen and B. I. Shklovskii, J. Chem. Phys. 115, 7298 (2001)] for the complexation of DNA with charged spherical macroions, has been employed in order to define the boundaries of the region where polyion-liposome complexes begin to condense, forming larger aggregates, and where aggregates dissolve again, towards isolated polyion-coated-liposome complexes. A reasonable good agreement is observed in the case of complexes formed by negatively charged polyacrylate sodium salt polyions and liposomes built up by cationic lipids (dioleoyltrimethylammoniumpropane), in an extended liposome concentration range.

  2. Activation of the human complement system by cholesterol-rich and pegylated liposomes - Modulation of cholesterol-rich liposome-mediated complement activation by elevated serum LDL and HDL levels

    DEFF Research Database (Denmark)

    Moghimi, S.M.; Hamad, I.; Bunger, R.; Andresen, Thomas Lars; Jørgensen, Kent; Hunter, A.C.; Baranji, L.; Rosivall, L.; Szebeni, J.

    2006-01-01

    liposome-mediated SC5b-9 generation considerably. While intravenous injection of cholesterol-rich liposomes into pigs was associated with an immediate circulatory collapse, the drop in systemic arterial pressure following injection of liposomes preincubated with human lipoproteins was slow and extended....... Therefore, surface-associated lipoprotein particles (or apolipoproteins) seem to lessen liposome-induced adverse haemodynamic changes, possibly as a consequence of suppressed complement activation in vivo. PEGylated liposomes were also capable of activating the human complement system, and the presence of......-mPEG conjugate seemed to play a critical role in activation of both the classical and alternative pathways of the complement system....

  3. Influence of polymer size, liposomal composition, surface charge, and temperature on the permeability of pH-sensitive liposomes containing lipid-anchored poly(2-ethylacrylic acid)

    OpenAIRE

    Lu T; Wang Z; Ma Y; Zhang Y; Chen T.

    2012-01-01

    Tingli Lu,1 Zhao Wang,2 Yufan Ma,1 Yang Zhang,2 Tao Chen1,21Key Laboratory for Space Bioscience and Biotechnology, School of Life Science, Northwestern Polytechnical University, 2Liposome Research Centre, Xi'an, ChinaBackground: Liposomes containing pH-sensitive polymers are promising candidates for the treatment of tumors and localized infection. This study aimed to identify parameters influencing the extent of contents release from poly(ethylacrylic acid) (PEAA) vesicles, focusing o...

  4. Gamma-irradiation of liposomes composed of saturated phospholipids: effect of bilayer composition, size, concentration and absorbed dose on chemical degradation and physical destabilization of liposomes.

    Science.gov (United States)

    Zuidam, N J; Versluis, C; Vernooy, E A; Crommelin, D J

    1996-04-01

    Liposomes composed of dipalmitoylphosphatidylcholine (DPPC), dipalmitoylphosphatidylglycerol (DPPG), or mixtures of these two phospholipids were exposed to gamma-irradiation in an air environment. Disappearance of the mother compounds was monitored by HPLC analysis. Plotting of the logarithmic values of residual DPPC or DPPG concentration versus irradiation dose resulted in straight lines. The slopes of these lines (overall degradation constants) depended on the type of phospholipids, concentration of the liposomes and the size of the liposomes. Under the chosen conditions, addition of DPPG in DPPC-liposomes did not affect the degradation rate constant of DPPC and vice versa. The presence of phosphate buffer (pH 7.4), pH or presence of sodium chloride did not affect the irradiation damage either. Minor changes were found upon analysis of total fatty acids by GLC and upon measurement of water soluble phosphate compounds. These changes were less pronounced than the changes monitored by HPLC of phospholipids, because the HPLC analysis monitored the overall degradation of the liposomal phospholipids. Thin-layer chromatography/fast atom bombardment mass spectrometry (TLC/FAB-MS) analysis of irradiated and non-irradiated DPPC or DPPG provided information on the structure of several degradation products. Degradation routes which include these degradation products are proposed. Gamma-irradiation neither affected the size of the liposomes nor the bilayer rigidity as determined by dynamic light scattering and fluorescence anisotropy of the probe 1,6-diphenyl-1,3,5-hexatriene (DPH), respectively. However, upon gamma-irradiation, changes in the melting characteristics of the liposomes were found by differential scanning calorimetry (DSC) measurements. The pre-transition melting enthalpy of the liposomal bilayer decreased or disappeared and the main-transition broadened. The changes found in DSC scans correlated qualitatively well with the changes recorded after HPLC analysis

  5. Transdermal Delivery of Small Interfering RNA with Elastic Cationic Liposomes in Mice

    Directory of Open Access Journals (Sweden)

    Yoshiyuki Hattori

    2013-01-01

    Full Text Available We developed elastic cationic liposomal vectors for transdermal siRNA delivery. These liposomes were prepared with 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP as a cationic lipid and sodium cholate (NaChol or Tween 80 as an edge activator. When NaChol or Tween 80 was included at 5, 10, and 15% (w/w into DOTAP liposomal formulations (C5-, C10-, and C15-liposomes and T5-, T10-, and T15-liposomes, C15- and T10-liposomes showed 2.4- and 2.7-fold-higher elasticities than DOTAP liposome, respectively. Although the sizes of all elastic liposomes prepared in this study were about 80–90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes were about 1,700–1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550–780 nm. Their elastic lipoplexes showed strong gene suppression by siRNA without cytotoxicity when transfected into human cervical carcinoma SiHa cells. Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution. These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.

  6. Prolonged hypoglycemic effect in diabetic dogs due to subcutaneous administration of insulin in liposomes

    International Nuclear Information System (INIS)

    The biologic action of insulin entrapped in liposomes (phospholipid vesicles) has been investigated following subcutaneous injection to dogs made diabetic with a combination of alloxan and streptozotocin. The fate of the liposomally entrapped material was determined by injecting rats subcutaneously with either 125I-insulin or the labeled polysaccharide 14C-inulin, incorporated in liposomes labeled with 3H-cholesterol. Injection of liposome insulin (0.75 U/kg) to five diabetic dogs resulted in a mean (+/- SEM) blood glucose fall from 16.4 +/- 0.8 to 2.9 +/- 0.4 mmol/L. The glucose level had still not returned to baseline after 24 h and, correspondingly, immunoreactive insulin (IRI) could still be detected in frozen and thawed plasma 24 h after injection. In contrast, the hypoglycemic effect of the same dose of free insulin with or without empty liposomes virtually ended within 8 h and IRI levels returned to baseline by 3 h after injection. In experiments on rats with liposomally entrapped 125I-insulin or 14C-inulin the proportion of the injected dose of tracer recoverable by excision of the injection site remained constant after about 1 h and 70% of the dose was still fixed in subcutaneous tissue for at least 5 h thereafter. When the plasma collected 3 h after subcutaneous injection of labeled liposomes containing 125I-insulin was passed through a column of Sepharose 6B, 50-75% of the 125I-activity was found in the fractions associated with intact liposomes. One possibility for the persistence of the hypoglycemic effect and of measurable IRI following injection of liposome insulin could be the presence of intact liposomes in the circulation for many hours after adsorption had ceased

  7. Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization

    Directory of Open Access Journals (Sweden)

    Jung IW

    2014-05-01

    Full Text Available Il-Woo Jung, Hyo-Kyung HanCollege of Pharmacy, Dongguk University-Seoul, Ilsan-Donggu, Goyang, Republic of KoreaAbstract: In this work, we aimed to develop chitosan-coated mucoadhesive liposomes ­containing risedronate to improve intestinal drug absorption. Liposomes containing risedronate were prepared with 1,2-distearoryl-sn-glycero-3-phosphocholine and distearoryl-sn-glycero-3-[phospho-rac-(1-glycerol] using the freeze-drying method, with subsequent coating of the anionic surfaces of the liposomes with chitosan. The in vitro characteristics of the chitosan-coated liposomes were investigated, including their stability, mucoadhesiveness, and Caco-2 cell permeability. This formulation was stable in simulated gastric and intestinal fluids, with the percentage of drug remaining in the liposomes being more than 90% after 24 hours of incubation. Chitosan-coated liposomes also showed strong mucoadhesive properties, implying potential electrostatic interaction with the mucous layer in the gastrointestinal tract. Compared with the untreated drug, chitosan-coated liposomes significantly enhanced the cellular uptake of risedronate, resulting in an approximately 2.1–2.6-fold increase in Caco-2 cells. Further, the chitosan-coated liposomes increased the oral exposure of risedronate by three-fold in rats. Taken together, the results of this study suggest that chitosan-coated liposomes containing risedronate should be effective for improving the bioavailability of risedronate.Keywords: cellular uptake, bioavailability, mucoadhesiveness, liposome, chitosan

  8. Mechanism of enhanced activity of liposome-entrapped aminoglycosides against resistant strains of Pseudomonas aeruginosa.

    Science.gov (United States)

    Mugabe, Clement; Halwani, Majed; Azghani, Ali O; Lafrenie, Robert M; Omri, Abdelwahab

    2006-06-01

    Pseudomonas aeruginosa is inherently resistant to most conventional antibiotics. The mechanism of resistance of this bacterium is mainly associated with the low permeability of its outer membrane to these agents. We sought to assess the bactericidal efficacy of liposome-entrapped aminoglycosides against resistant clinical strains of P. aeruginosa and to define the mechanism of liposome-bacterium interactions. Aminoglycosides were incorporated into liposomes, and the bactericidal efficacies of both free and liposomal drugs were evaluated. To define the mechanism of liposome-bacterium interactions, transmission electron microscopy (TEM), flow cytometry, lipid mixing assay, and immunocytochemistry were employed. Encapsulation of aminoglycosides into liposomes significantly increased their antibacterial activity against the resistant strains used in this study (MICs of > or =32 versus < or =8 microg/ml). TEM observations showed that liposomes interact intimately with the outer membrane of P. aeruginosa, leading to the membrane deformation. The flow cytometry and lipid mixing assays confirmed liposome-bacterial membrane fusion, which increased as a function of incubation time. The maximum fusion rate was 54.3% +/- 1.5% for an antibiotic-sensitive strain of P. aeruginosa and 57.8% +/- 1.9% for a drug-resistant strain. The fusion between liposomes and P. aeruginosa significantly enhanced the antibiotics' penetration into the bacterial cells (3.2 +/- 2.3 versus 24.2 +/- 6.2 gold particles/bacterium, P < or = 0.001). Our data suggest that liposome-entrapped antibiotics could successfully resolve infections caused by antibiotic-resistant P. aeruginosa through an enhanced mechanism of drug entry into the bacterial cells. PMID:16723560

  9. Preparation and Evaluation of Norcantharidin-encapsulated Liposomes Modified with a Novel CD19 Monoclonal Antibody 2E8

    Institute of Scientific and Technical Information of China (English)

    张晶樱; 汤永民; 钱柏芹; 沈红强

    2010-01-01

    In this study,norcanthridin(NCTD)-encapsulated liposomes were modified with a novel murine anti-human CD19 monoclonal antibody 2E8(2E8-NCTD-liposomes) and the targeting efficiency and specific cytotoxicity of 2E8-NCTD-liposomes to CD19+ leukemia cells were evaluated.BALB/c mice were injected with 2E8 hybridoma cells to obtain 2E8 monoclonal antibody(mAb).NCTD-liposomes were prepared by using film dispersion method.2E8 mAbs were linked to NCTD-liposomes using post-incorporation technology.Flow cytometry show...

  10. Liposomes and nanotechnology in drug development: focus on ocular targets

    Directory of Open Access Journals (Sweden)

    Honda M

    2013-02-01

    Full Text Available Miki Honda,1 Tomohiro Asai,2 Naoto Oku,2 Yoshihiko Araki,3 Minoru Tanaka,1 Nobuyuki Ebihara11Department of Ophthalmology, Juntendo University Urayasu Hospital, Chiba, Japan; 2Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan; 3Institute for Environmental and Gender-Specific Medicine, Juntendo University Graduate School of Medicine, Chiba, JapanAbstract: Poor drug delivery to lesions in patients' eyes is a major obstacle to the treatment of ocular diseases. The accessibility of these areas to drugs is highly restricted by the presence of barriers, including the corneal barrier, aqueous barrier, and the inner and outer blood–retinal barriers. In particular, the posterior segment is difficult to reach for drugs because of its structural peculiarities. This review discusses various barriers to drug delivery and provides comprehensive information for designing nanoparticle-mediated drug delivery systems for the treatment of ocular diseases. Nanoparticles can be designed to improve penetration, controlled release, and drug targeting. As highlighted in this review, the therapeutic efficacy of drugs in ocular diseases has been reported to be enhanced by the use of nanoparticles such as liposomes, micro/nanospheres, microemulsions, and dendrimers. Our recent data show that intravitreal injection of targeted liposomes encapsulating an angiogenesis inhibitor caused significantly greater suppression of choroidal neovascularization than did the injection of free drug. Recent progress in ocular drug delivery systems research has provided new insights into drug development, and the use of nanoparticles for drug delivery is thus a promising approach for advanced therapy of ocular diseases.Keywords: intravitreal injection, drug delivery system, age-related macular degeneration, APRPG-modified PEGylated liposome, DDS

  11. Hyaluronan synthase mediates dye translocation across liposomal membranes

    Directory of Open Access Journals (Sweden)

    Medina Andria P

    2012-01-01

    Full Text Available Abstract Background Hyaluronan (HA is made at the plasma membrane and secreted into the extracellular medium or matrix by phospolipid-dependent hyaluronan synthase (HAS, which is active as a monomer. Since the mechanism by which HA is translocated across membranes is still unresolved, we assessed the presence of an intraprotein pore within HAS by adding purified Streptococcus equisimilis HAS (SeHAS to liposomes preloaded with the fluorophore Cascade Blue (CB. Results CB translocation (efflux was not observed with mock-purified material from empty vector control E. coli membranes, but was induced by SeHAS, purified from membranes, in a time- and dose-dependent manner. CB efflux was eliminated or greatly reduced when purified SeHAS was first treated under conditions that inhibit enzyme activity: heating, oxidization or cysteine modification with N-ethylmaleimide. Reduced CB efflux also occurred with SeHAS K48E or K48F mutants, in which alteration of K48 within membrane domain 2 causes decreased activity and HA product size. The above results used liposomes containing bovine cardiolipin (BCL. An earlier study testing many synthetic lipids found that the best activating lipid for SeHAS is tetraoleoyl cardiolipin (TO-CL and that, in contrast, tetramyristoyl cardiolipin (TM-CL is an inactivating lipid (Weigel et al, J. Biol. Chem. 281, 36542, 2006. Consistent with the effects of these CL species on SeHAS activity, CB efflux was more than 2-fold greater in liposomes made with TO-CL compared to TM-CL. Conclusions The results indicate the presence of an intraprotein pore in HAS and support a model in which HA is translocated to the exterior by HAS itself.

  12. Mechanistic model and analysis of doxorubicin release from liposomal formulations.

    Science.gov (United States)

    Fugit, Kyle D; Xiang, Tian-Xiang; Choi, Du H; Kangarlou, Sogol; Csuhai, Eva; Bummer, Paul M; Anderson, Bradley D

    2015-11-10

    Reliable and predictive models of drug release kinetics in vitro and in vivo are still lacking for liposomal formulations. Developing robust, predictive release models requires systematic, quantitative characterization of these complex drug delivery systems with respect to the physicochemical properties governing the driving force for release. These models must also incorporate changes in release due to the dissolution media and methods employed to monitor release. This paper demonstrates the successful development and application of a mathematical mechanistic model capable of predicting doxorubicin (DXR) release kinetics from liposomal formulations resembling the FDA-approved nanoformulation DOXIL® using dynamic dialysis. The model accounts for DXR equilibria (e.g. self-association, precipitation, ionization), the change in intravesicular pH due to ammonia release, and dialysis membrane transport of DXR. The model was tested using a Box-Behnken experimental design in which release conditions including extravesicular pH, ammonia concentration in the release medium, and the dilution of the formulation (i.e. suspension concentration) were varied. Mechanistic model predictions agreed with observed DXR release up to 19h. The predictions were similar to a computer fit of the release data using an empirical model often employed for analyzing data generated from this type of experimental design. Unlike the empirical model, the mechanistic model was also able to provide reasonable predictions of release outside the tested design space. These results illustrate the usefulness of mechanistic modeling to predict drug release from liposomal formulations in vitro and its potential for future development of in vitro - in vivo correlations for complex nanoformulations. PMID:26310713

  13. Liposomal doxorubicin improves radiotherapy response in hypoxic prostate cancer xenografts

    International Nuclear Information System (INIS)

    Tumor vasculature frequently fails to supply sufficient levels of oxygen to tumor tissue resulting in radioresistant hypoxic tumors. To improve therapeutic outcome radiotherapy (RT) may be combined with cytotoxic agents. In this study we have investigated the combination of RT with the cytotoxic agent doxorubicin (DXR) encapsulated in pegylated liposomes (PL-DXR). The PL-DXR formulation Caelyx® was administered to male mice bearing human, androgen-sensitive CWR22 prostate carcinoma xenografts in a dose of 3.5 mg DXR/kg, in combination with RT (2 Gy/day × 5 days) performed under normoxic and hypoxic conditions. Hypoxic RT was achieved by experimentally inducing tumor hypoxia by clamping the tumor-bearing leg five minutes prior to and during RT. Treatment response evaluation consisted of tumor volume measurements and dynamic contrast-enhanced magnetic resonance imaging (DCE MRI) with subsequent pharmacokinetic analysis using the Brix model. Imaging was performed pre-treatment (baseline) and 8 days later. Further, hypoxic fractions were determined by pimonidazole immunohistochemistry of excised tumor tissue. As expected, the therapeutic effect of RT was significantly less effective under hypoxic than normoxic conditions. However, concomitant administration of PL-DXR significantly improved the therapeutic outcome following RT in hypoxic tumors. Further, the pharmacokinetic DCE MRI parameters and hypoxic fractions suggest PL-DXR to induce growth-inhibitory effects without interfering with tumor vascular functions. We found that DXR encapsulated in liposomes improved the therapeutic effect of RT under hypoxic conditions without affecting vascular functions. Thus, we propose that for cytotoxic agents affecting tumor vascular functions liposomes may be a promising drug delivery technology for use in chemoradiotherapy

  14. Treatment of lymphomatous and leukemic meningitis with liposomal encapsulated cytarabine.

    Science.gov (United States)

    Kripp, Melanie; Hofheinz, Ralf-Dieter

    2008-01-01

    Liposomal encapsulated cytarabine (DepoCyte, Mundipharma GmbH, Limburg/Lahn, Germany) is a slow-release formulation of conventional cytarabine. It is licensed for intrathecal use in patients with lymphomatous and leukemic meningitis. DepoCyte obtained superior response rates, improved patient quality of life and improved the time to neurological progression in a randomized albeit small clinical trial. In this review we briefly summarize the clinical data and discuss them in light of clinical problems and possible treatment scenarios. PMID:19337408

  15. Adjuvant Effect of Cationic Liposomes for Subunit Influenza Vaccine: Influence of Antigen Loading Method, Cholesterol and Immune Modulators

    Directory of Open Access Journals (Sweden)

    Alexander Kros

    2013-07-01

    Full Text Available Cationic liposomes are potential adjuvants for influenza vaccines. In a previous study we reported that among a panel of cationic liposomes loaded with influenza hemagglutinin (HA, DC-Chol:DPPC (1:1 molar ratio liposomes induced the strongest immune response. However, it is not clear whether the cholesterol (Chol backbone or the tertiary amine head group of DC-Chol was responsible for this. Therefore, in the present work we studied the influence of Chol in the lipid bilayer of cationic liposomes. Moreover, we investigated the effect of the HA loading method (adsorption versus encapsulation and the encapsulation of immune modulators in DC-Chol liposomes on the immunogenicity of HA. Liposomes consisting of a neutral lipid (DPPC or Chol and a cationic compound (DC-Chol, DDA, or eDPPC were produced by film hydration-extrusion with/without an encapsulated immune modulator (CpG or imiquimod. The liposomes generally showed comparable size distribution, zeta potential and HA loading. In vitro studies with monocyte-derived human dendritic cells and immunization studies in C57Bl/6 mice showed that: (1 liposome-adsorbed HA is more immunogenic than encapsulated HA; (2 the incorporation of Chol in the bilayer of cationic liposomes enhances their adjuvant effect; and (3 CpG loaded liposomes are more efficient at enhancing HA-specific humoral responses than plain liposomes or Alhydrogel.

  16. Effective transcutaneous immunization by antigen-loaded flexible liposome in vivo

    Directory of Open Access Journals (Sweden)

    Li N

    2011-12-01

    Full Text Available Ni Li1, Li-Hua Peng1, Xi Chen1, Shinsaku Nakagawa2, Jian-Qing Gao11Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China; 2Department of Biotechnology and Therapeutics, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, JapanBackground: Transcutaneous vaccines have received wide attention due to their easy-to-use, needle-free, noninvasive delivery. However, the novel barrier function of stratum corneum hinders the transport of antigen and adjuvant in transcutaneous immunization. Novel nanoscale delivery systems employing, for example, liposomes and nanoparticles, have been widely investigated to overcome the penetration barrier of stratum corneum for effective transcutaneous immunization.Objective: The objective of this study was to prepare two types of flexible liposomes and determine their efficacies for the transcutaneous delivery of antigen and the subsequent immune response induced in vivo.Methods: Ovalbumin (OVA liposome-based transcutaneous vaccines were prepared using reverse-phase evaporation and film-dispersion methods. Particle sizes and antigen encapsulating efficiency were then evaluated. After application to bare mouse skin, topical sites were examined for the presence of fluorescence-labeled liposome. The efficacy of the transcutaneously delivered OVA-loaded flexible liposome in activating the immune responses was investigated by detecting serum immunoglobulin G levels. The influence of an adjuvant, imiquimod, in the transcutaneous immunization was also tested.Results: Two flexible liposomes with well-encapsulated OVA were successfully prepared by film-dispersion or reverse-phase evaporation methods. The sizes of the prepared flexible liposomes ranged from 200 to 400 nm. In vivo, the fluorescence-labeled liposome was detected in hair-follicle ducts, indicating that the flexible liposome can penetrate the skin barrier through the hair

  17. Efficient intracellular drug-targeting of macrophages using stealth liposomes directed to the hemoglobin scavenger receptor CD163

    DEFF Research Database (Denmark)

    Etzerodt, Anders; Maniecki, Maciej Bogdan; Graversen, Jonas Heilskov;

    2012-01-01

    The hemoglobin scavenger receptor CD163 is exclusively expressed in the monocytic lineage and preferentially in tissue resident macrophages of the M2 phenotype and in macrophages in sites of inflammation and tumor growth. In the present study we have designed liposomes specifically targeting CD163...... by hydrophobic linkage of CD163-binding monoclonal antibodies to polyethylene glycol-coated liposomes ('stealth liposomes'). Targeting to the endocytic CD163 protein greatly increased the uptake of liposomes in CD163 transfected cells and macrophages as visualized by confocal microscopy and flow...... cytometry of cells exposed to CD163 targeting liposomes loaded with calcein. Strong cytotoxic effects were seen in CD163-expressing human monocytes by using the chemotherapeutic agent doxorubicin as cargo of the liposomes. In conclusion, the use of stealth liposomes modified to recognize CD163 is a...

  18. Ultrasound-targeted Bubble Liposome Destruction Enhances AG73-mediated Gene Transfer by Improvement of Intracellular Trafficking

    Science.gov (United States)

    Omata, Daiki; Negishi, Yoichi; Endo-Takahashi, Yoko; Suzuki, Ryo; Maruyama, Kazuo; Nomizu, Motoyoshi; Aramaki, Yukihiko

    2011-09-01

    For selective cancer gene therapy, we have developed AG73-labeled polyethyleneglycol-modified liposomes (AG73-PEG liposomes) capable of encapsulating a gene condensed by poly-l-lysine. The present study examined whether echo-contrast gas-entrapping liposomes, also known as Bubble liposomes (BLs), and ultrasound (US) exposure affect not only the cell membrane but also intracellular vesicles, and enhance the release of pDNA from endosomes into the cytoplasm to achieve efficient gene transfection. AG73-mediated liposomal gene transfection efficiency was enhanced when BLs and US exposure were used. Furthermore, confocal microscopic analysis revealed that the BLs and US exposure promoted intracellular trafficking of the AG73-PEG liposomes during gene transfection. Thus, the use of AG73-PEG liposomes together with BLs and US exposure may be a promising way to achieve selective and efficient gene delivery.

  19. Hierarchically micro-patterned nanofibrous scaffolds with a nanosized bio-glass surface for accelerating wound healing

    Science.gov (United States)

    Xu, He; Lv, Fang; Zhang, Yali; Yi, Zhengfang; Ke, Qinfei; Wu, Chengtie; Liu, Mingyao; Chang, Jiang

    2015-11-01

    A composite scaffold with a controlled micro-pattern, nano-sized fiber matrix and surface-modified nanobioglass component was successfully prepared for skin wound healing by combining the patterning electrospinning with pulsed laser deposition strategies, and the hierarchical micro/nano structures and nano-sized bioglass in the scaffolds could synergistically improve the efficiency and re-epithelialization of wound healing.A composite scaffold with a controlled micro-pattern, nano-sized fiber matrix and surface-modified nanobioglass component was successfully prepared for skin wound healing by combining the patterning electrospinning with pulsed laser deposition strategies, and the hierarchical micro/nano structures and nano-sized bioglass in the scaffolds could synergistically improve the efficiency and re-epithelialization of wound healing. Electronic supplementary information (ESI) available. See DOI: 10.1039/c5nr04802h

  20. Investigation on the red shift of charge transfer excitation spectra for nano-sized Y 2O 3:Eu 3+

    Science.gov (United States)

    Shang, Chunyu; Shang, Xiaohong; Qu, Yuqiu; Li, Meicheng

    2011-01-01

    Based upon the local structure data, the differences of energy bands between bulk and nano-sized Y2O3:Eu3+ have been presented. The volume expansion in nano-sized Y2O3:Eu3+ leads to the shrinkage of band gap and decrease of zero-phonon charge transfer (CT) energy; the enlargement of local disorder in nano-sized Y2O3:Eu3+ leads to the formation of impurity bands and further decrease of zero-phonon CT energy. On the basis of the differences in energy bands, the mechanisms for the decrease of CT energy, i.e., red shift of CT excitation spectra for nano-sized Y2O3:Eu3+ have been clarified.

  1. Manufacturing techniques and excipients used during the formulation of oil-in-water type nanosized emulsions for medical applications

    OpenAIRE

    Shunmugaperumal Tamilvanan; Sudalaimuthu Ramachandran Senthilkumar; Raj baskar; Thenrajan Raja Sekharan

    2010-01-01

    Medically, the oil-in-water nanosized emulsions are used mainly as delivery carriers for lipophilic drug molecules which show therapeutic activity when administered via parenteral, ocular andtransdermal routes. To extract multifunctional activities, the nanosized emulsions containing neutral, anionic and cationic charges over dispersed oil droplets are designed with the help of variety ofexcipients especially emulsifiers. This type of decoration on the dispersed oil droplet’s surface allows t...

  2. Influence of polymer size, liposomal composition, surface charge, and temperature on the permeability of pH-sensitive liposomes containing lipid-anchored poly(2-ethylacrylic acid

    Directory of Open Access Journals (Sweden)

    Lu T

    2012-09-01

    Full Text Available Tingli Lu,1 Zhao Wang,2 Yufan Ma,1 Yang Zhang,2 Tao Chen1,21Key Laboratory for Space Bioscience and Biotechnology, School of Life Science, Northwestern Polytechnical University, 2Liposome Research Centre, Xi'an, ChinaBackground: Liposomes containing pH-sensitive polymers are promising candidates for the treatment of tumors and localized infection. This study aimed to identify parameters influencing the extent of contents release from poly(ethylacrylic acid (PEAA vesicles, focusing on the effects of polymer size, lipid composition, vesicle surface charge, and temperature.Methods: Anchored lipid pH-sensitive PEAA was synthesized using PEAA with a molecular weight of 8.4 kDa. PEAA vesicles were prepared by insertion of the lipid-anchored PEAA into preformed large unilamellar vesicles. The preformed liposomes were manipulated by varying the phosphocholine and cholesterol content, and by adding negative or positive charges to the liposomes. A calcein release assay was used to evaluate the effects of polymer size, liposome composition, surface charge, and temperature on liposomal permeability.Results: The release efficiency of the calcein-entrapped vesicles was found to be dependent on the PEAA polymer size. PEAA vesicles containing a phosphatidylcholine to cholesterol ratio of 60:40 (mol/mol released more than 80% of their calcein content when the molecular weight of PEAA was larger than 8.4 kDa. Therefore, the same-sized polymer of 8.4 kDa was used for the rest of study. The calcein release potential was found to decrease as the percentage of cholesterol increased and with an increase in the phosphocholine acyl chain length (DMPC . DPPC . DSPC. Negatively charged and neutral vesicles released similar amounts of calcein, whereas positively charged liposomes released a significant amount of their contents. pH-sensitive release was dependent on temperature. Dramatic content release was observed at higher temperatures.Conclusion: The observed

  3. Preparation of Super Soft Granules from Nanosized Ceramic Powders by Spray Freezing

    International Nuclear Information System (INIS)

    Owing to their extremely high specific surfaces and their high surface-to-volume ratios nanosized ceramic powders show a strong tendency to agglomeration and poor flowability. For improved properties of these powders during storage, transport and shaping a granulation step is necessary. However, the granules must be completely destroyed during dry pressing or redispersion; otherwise, the advantages of nanoparticles in comparison to conventional powders will not be realized. Spray freezing is a new granulation technique which combines the advantages of a conventional granulation by spray drying and a sublimation drying process. Different suspensions of nanosized oxide powders were rapidly frozen by spray freezing and subsequently dried by freeze drying. Thus, capillary forces can be excluded by this process. The achieved granulates show spheric granules with very low strength, improved flowability and increased bulk density. They were redispersible and can be destroyed under very low pressures

  4. Current inversions induced by resonant coupling to surface waves in a nanosized water pump

    Science.gov (United States)

    Zhou, Xiaoyan; Wu, Fengmin; Liu, Yang; Kou, Jianlong; Lu, Hui; Lu, Hangjun

    2015-11-01

    We conducted a molecular dynamics simulation to investigate current inversions in a nanosized water pump based on a single-walled carbon nanotube powered by mechanical vibration. It was found that the water current depended sensitively on the frequency of mechanical vibration. Especially in the resonance region, the nanoscale pump underwent reversals of the water current. This phenomenon was attributed to the dynamics competition of the water molecules in the two sections (the left and right parts) divided by the vibrating atom and the differences in phase and decay between the two mechanical waves generated by mechanical vibration and propagating in opposite directions toward the two ends of the carbon nanotube. Our findings provide an insight into water transportation through nanosized pumps and have potential in the design of high-flux nanofluidic systems and nanoscale energy converters.

  5. Fabrication and microstructural characterization of porous silicon carbide with nano-sized powders

    International Nuclear Information System (INIS)

    Porous silicon carbide was fabricated by using nano-sized SiC powder additions and different cold isostatic pressing (CIP) conditions followed by sintering at 1500-1800 deg. C. The relationship between the processing conditions, pore size and microstructure was examined. The cold isostatic pressing conditions, sintering temperature and nano-sized additives were effective for controlling pore size and microstructure. The pore size and particle size increased with increasing sintering temperature, attributed to surface diffusion. However, no densification occurred because of pore enlargement. In addition, the compressive strength increased with sintering temperature and reached values as high as 513 MPa. This was due to the formation of well-developed neck areas. This study suggests that the promoted mass transfer can provide high strength due to increased neck area

  6. Preparation of nano-sized hydrophilic aluminum fins coating materials for air conditioner

    Institute of Scientific and Technical Information of China (English)

    陈志明; 韩峰; 邵利

    2002-01-01

    Semicontinuous seeded emulsion copolymerization of acrylic acid, acrylamide and divinylbenzene was carried out at 80℃ with ammonium persulphate as the initiator and the polyether with comb configuration as the emulsifier to prepare approximately mono-dispersed nano-sized polymer particles with average diameter 90nm. The particles were used to combine with special polyether and de-ionized water was added to obtain nano-sized hydrophilic aluminum fins coating materials with solid content of 10%. The aluminum fins were coated with the materials to get the film showing self-assembly properties in some degree. The obtained hydrophilic fins have contact angles <5° with de-ionized water, minimum value 0°, after 4 cycles of wet and dry, contact angles <10° with de-ionized water.

  7. Preparation of nanosized Fluticasone Propionate nasal spray with improved stability and uniformity

    OpenAIRE

    Dai Jiajia; Ruan Benfang H.; Zhu Ying; Liang Xianrui; Su Feng; Su Weike

    2015-01-01

    Transmucosal nasal delivery has been recognized as up-and-coming option for delivery of therapeutic compounds. However, the short residence time of the formulation within the nasal cavity coupled to its low permeability is regarded as the barrier to good bioavailability. To overcome those limitations, we developed a new formulation - nanosized Fluticasone Propionate (FP) nasal spray. High pressure homogenization (HPH) was employed to achieve effective parti...

  8. Comparison of freeze drying and spray drying to obtain porous nanostructured granules from nanosized suspensions

    OpenAIRE

    Vicent, Mónica; Sánchez Vilches, Enrique Javier; Molina, Tamara; Nieto, María Isabel; Moreno, Rodrigo

    2012-01-01

    This work studies the spray drying and freeze drying of different nanosized ceramic materials and the physicochemical characteristics of the obtained granules. Colloidal suspensions of alumina, titania, and a 87/13 mixture were studied. The influence of temperature, pressure, nozzle diameter, and solids loading on the morphology and characteristics of dried granules were evaluated. It was demonstrated that these processing parameters have practically no influence, and the only parameter deter...

  9. Mechanical properties of dental resin composites by co-filling diatomite and nanosized silica particles

    International Nuclear Information System (INIS)

    The aim of this study was to investigate the mechanical property effects of co-filling dental resin composites with porous diatomite and nanosized silica particles (OX-50). The purification of raw diatomite by acid-leaching was conducted in a hot 5 M HCl solution at 80 deg. C for 12 h. Both diatomite and nanosized SiO2 were silanized with 3-methacryloxypropyltrimethoxysilane. The silanized inorganic particles were mixed into a dimethacrylate resin. Purified diatomite was characterized by X-ray diffraction, UV-vis diffuse reflectance spectroscopy and an N2 adsorption-desorption isotherm. Silanized inorganic particles were characterized using Fourier transform infrared spectroscopy and a thermogravimetric analysis. The mechanical properties of the composites were tested by three-point bending, compression and Vicker's microhardness. Scanning electron microscopy was used to show the cross-section morphologies of the composites. Silanization of diatomite and nanosized silica positively reinforced interactions between the resin matrix and the inorganic particles. The mechanical properties of the resin composites gradually increased with the addition of modified diatomite (m-diatomite). The fracture surfaces of the composites exhibited large fracture steps with the addition of m-diatomite. However, when the mass fraction of m-diatomite was greater than 21 wt.% with respect to modified nanosized silica (mOX-50) and constituted 70% of the resin composite by weight, the mechanical properties of the resin composites started to decline. Thus, the porous structure of diatomite appears to be a crucial factor to improve mechanical properties of resin composites.

  10. Nano-sized polystyrene affects feeding, behavior and physiology of brine shrimp Artemia franciscana larvae.

    Science.gov (United States)

    Bergami, Elisa; Bocci, Elena; Vannuccini, Maria Luisa; Monopoli, Marco; Salvati, Anna; Dawson, Kenneth A; Corsi, Ilaria

    2016-01-01

    Nano-sized polymers as polystyrene (PS) constitute one of the main challenges for marine ecosystems, since they can distribute along the whole water column affecting planktonic species and consequently disrupting the energy flow of marine ecosystems. Nowadays very little knowledge is available on the impact of nano-sized plastics on marine organisms. Therefore, the present study aims to evaluate the effects of 40nm anionic carboxylated (PS-COOH) and 50nm cationic amino (PS-NH2) polystyrene nanoparticles (PS NPs) on brine shrimp Artemia franciscana larvae. No signs of mortality were observed at 48h of exposure for both PS NPs at naplius stage but several sub-lethal effects were evident. PS-COOH (5-100μg/ml) resulted massively sequestered inside the gut lumen of larvae (48h) probably limiting food intake. Some of them were lately excreted as fecal pellets but not a full release was observed. Likewise, PS-NH2 (5-100µg/ml) accumulated in larvae (48h) but also adsorbed at the surface of sensorial antennules and appendages probably hampering larvae motility. In addition, larvae exposed to PS-NH2 undergo multiple molting events during 48h of exposure compared to controls. The activation of a defense mechanism based on a physiological process able to release toxic cationic NPs (PS-NH2) from the body can be hypothesized. The general observed accumulation of PS NPs within the gut during the 48h of exposure indicates a continuous bioavailability of nano-sized PS for planktonic species as well as a potential transfer along the trophic web. Therefore, nano-sized PS might be able to impair food uptake (feeding), behavior (motility) and physiology (multiple molting) of brine shrimp larvae with consequences not only at organism and population level but on the overall ecosystem based on the key role of zooplankton on marine food webs. PMID:26422775

  11. Nanoscale Design of Nano-Sized Particles in Shape-Memory Polymer Nanocomposites Driven by Electricity

    OpenAIRE

    Kai Yu; Fei Liang; Wei Min Huang; Haibao Lu

    2013-01-01

    In the last few years, we have witnessed significant progress in developing high performance shape memory polymer (SMP) nanocomposites, in particular, for shape recovery activated by indirect heating in the presence of electricity, magnetism, light, radio frequency, microwave and radiation, etc. In this paper, we critically review recent findings in Joule heating of SMP nanocomposites incorporated with nanosized conductive electromagnetic particles by means of nanoscale control via applying a...

  12. Microstructure and magnetic behavior of nanosized Fe sub 3 O sub 4 powders and polycrystalline films

    CERN Document Server

    Nedkov, I; Kolev, S; Krezhov, K; Niarchos, D; Moraitakis, E; Kusano, Y; Takada, J

    2002-01-01

    The object of investigation were the magnetic interactions in nanostructured Fe sub 3 O sub 4 assemblies of two kinds (powder and film) where particles of similar size present nearly uniform domains in a close to planar arrangement with spacings sufficient for magnetic interactions. We discuss the use of the soft-chemistry method, i.e. the modified 'ferrite plating' (MFP) technique, for the synthesis of polycrystalline films of magnetite with nanosized crystallites. (author)

  13. Preparation of Nano-Sized TiO2 Particles by Microemulsion Method

    Institute of Scientific and Technical Information of China (English)

    Shaohua Zhang; Bing Xie; Fengyi Li; Peng Xu

    2006-01-01

    Nano-sized titania powders have been prepared by hydrolysis of tetrabutyl titanate in the droplet of water/OP-7/pentanol/cyclohexane microemulsion system. The effects of ingredient change on the water drop size and particle size were investigated. The prepared TiO2 was in the form of anatase after annealing. TiO2 was characterized by TG-TGA,FTIR, XRD to measure the transformation temperature, surface adsorption and average size.

  14. One Step Encapsulation of Small Molecule Drugs in Liposomes via Electrospray-Remote Loading.

    Science.gov (United States)

    Duong, Anthony D; Collier, Michael A; Bachelder, Eric M; Wyslouzil, Barbra E; Ainslie, Kristy M

    2016-01-01

    Resiquimod is a Toll-like receptor (TLR) 7/8 agonist that has previously been used as a vaccine adjuvant, as a topical treatment of viral lesions and skin cancer, and as an antiviral treatment. We report on the combined application of remote loading and electrospray to produce liposomal resiquimod, with the broader goals of improving drug encapsulation efficiency and scalability of liposome production methods. Drug loading in liposomes increased from less than 1% to greater that 3% by mass when remote loading was used, whether the liposomes were generated by thin-film hydration or electrospray methods. Dynamic light scattering (DLS) determined mean vesicle diameters of 137 ± 11 nm and 103 ± 4 for the thin-film and electrospray methods, respectively. Transmission electron microscopy (TEM) images showed spherical vesicles with sizes consistent with the DLS measurements. In vitro drug release profiles found that most of the drug remained within the liposomes at both pH 5.5 and 7.4. The in vitro bioactivity of the liposomal drug was also demonstrated by the increase in nitrite production when RAW macrophages were exposed to the drug. Our findings indicate that the remotely loaded liposomes formed via the scalable electrospray method have characteristics comparable to those produced via conventional batch methods. The methods discussed here are not limited to the enhanced delivery of resiquimod. Rather, they should be readily adaptable to other compounds compatible with remote loading. PMID:26568143

  15. Transient effects of empty liposomes on hepatic macrophage populations in rats.

    Science.gov (United States)

    Pervin, Munmun; Golbar, Hossain M; Bondoc, Alexandra; Izawa, Takeshi; Kuwamura, Mitsuru; Yamate, Jyoji

    2016-04-01

    Liposomes have been used as a vehicle for encapsulating chemicals or toxins in toxicological studies. We investigated the transient effects of empty liposomes on hepatic macrophages by applying a single intravenous injection at a dose of 10 ml/kg body weight in 6-week-old male F344 rats. One day after injection, the numbers of hepatic macrophages reacting to CD163, CD68, Iba-1, MHC class II, Gal-3 and CD204 were significantly increased in liposome-treated rats. CD163(+) Kupffer cells and CD68(+) macrophages with increased phagocytic activity in hepatic lobules were most sensitive. The histological architecture of the liver was not changed following liposome injection; however, hepatocytes showed increased proliferating activity, demonstrable with proliferation marker immunostaining and by an increase in gene profiles related to the cell cycle. In the liposome-treated rats, interestingly, AST and ALT values were significantly decreased, and MCP-1, IL-1β and TGF-β1 mRNAs were significantly increased. Collectively, the present study found that hepatic macrophages activated by liposomes can influence liver homeostasis. This information would be useful for background studies on liposomes. PMID:27182120

  16. Efficiency of pH-Sensitive Fusogenic Polymer-Modified Liposomes as a Vaccine Carrier

    Directory of Open Access Journals (Sweden)

    Shinobu Watarai

    2013-01-01

    Full Text Available The usefulness of pH-sensitive fusogenic polymer-(succinylated poly(glycidol-(SucPG- modified liposomes as a vaccine carrier in the induction of immune responses was evaluated. Mice were intraperitoneally immunized with ovalbumin- (OVA- containing SucPG-modified liposomes. After immunization, significant OVA-specific antibodies were detected in the serum. When sera were analyzed for isotype distribution, OVA-specific IgG1 antibody responses were noted in mice immunized with OVA-containing polymer-unmodified liposomes, whereas immunization with OVA-containing SucPG-modified liposomes resulted in the induction of OVA-specific IgG1, IgG2a, and IgG3 Ab responses. In spleen lymphocytes from mice immunized with OVA-containing SucPG-modified liposomes, both IFN-γ-(Th1-type- and IL-4-(Th2 type- specific mRNA were detected. Moreover, substantial production of IFN-γ and IL-4 was demonstrated in spleen cells from OVA-containing SucPG-modified liposomes in vitro. These results suggest that the pH-sensitive fusogenic polymer-(SucPG- modified liposomes would serve effectively as an antigen delivery vehicle for inducing Th1 and Th2 immune responses.

  17. Labeling of preformed liposomes with Ga-67 and Tc-99m by chelation

    International Nuclear Information System (INIS)

    We have synthesized a long-chain hydrocarbon covalently coupled to diethylene-triaminepenta-acetic acid (stearylamine-DTPA) and have incorporated this compound in liposomes during their preparation. The lipophilic hydrocarbon chain anchors the molecule in the lipid bilayer, exposing the DTPA groups on the surface for chelation. Ethanolic solutions of the lipids are evaporated to dryness under nitrogen in multidose vials; the lipids are suspended in the vial by adding a small volume of distilled water followed by sonication. The liposomes are then labeled by transcomplexation in the case of Ga-67 and by conventional stannous reduction in the case of Tc-99m, by adding the activities directly to the vial. These liposomes bind 95 +/- 5% of Ga-67 and Tc-99m activity, as determined by paper chromatograph assay, eliminating the need for a purification step. The labeled liposomes release about 5% of their Ga-67 activity, and about 30% of their Tc-99m activity after 2 hr of incubation in 50% human plasma at 37 degrees C. Activity released from liposomes labeled with Ga-67 or Tc-99m oxine is much greater under the same conditions. In normal mice the labeled liposomes show biodistributions that are comparable with that obtained with liposomes labeled by conventional techniques

  18. Hyaluronic acid liposomal gel sustains delivery of a corticoid to the inner ear.

    Science.gov (United States)

    El Kechai, Naila; Mamelle, Elisabeth; Nguyen, Yann; Huang, Nicolas; Nicolas, Valérie; Chaminade, Pierre; Yen-Nicolaÿ, Stéphanie; Gueutin, Claire; Granger, Benjamin; Ferrary, Evelyne; Agnely, Florence; Bochot, Amélie

    2016-03-28

    The inner ear is one of the most challenging organs for drug delivery, mainly because of the blood-perilymph barrier. Therefore, local rather than systemic drug delivery methods are being developed for inner ear therapy. In this work, we have evaluated the benefit of a hyaluronic acid liposomal gel for sustained delivery of a corticoid to the inner ear after local injection into the middle ear in a guinea pig model. The liposomal gel was easily injectable as a result of the shear-thinning behavior of hyaluronic acid. A prolonged residence time at the site of injection as well as in the round window were achieved without any negative effect on the hearing thresholds of the animals. The presence of liposomes in the formulation resulted in sustained release of the drug in the perilymph for 30days and promoted the conversion of the prodrug loaded within the liposomes (dexamethasone phosphate) into its active form (dexamethasone). In this way, therapeutic doses were attained in the perilymph. A small amount of intact liposomes was visualized in the perilymph, whereas the main proportion of liposomes seemed to be trapped in the round window resulting in a reservoir effect. Thus, the administration of hyaluronic acid liposomal gel to the middle ear is an efficient strategy for delivering corticoids to the inner ear in a sustained manner. PMID:26860286

  19. Biophysical characterization of V3-lipopeptide liposomes influencing HIV-1 infectivity

    International Nuclear Information System (INIS)

    The V3-loop of the HIV-1 gp120 alters host cell immune function and modulates infectivity. We investigated biophysical parameters of liposome constructs with embedded lipopeptides from the principle neutralizing domain of the V3-loop and their influence on viral infectivity. Dynamic light scattering measurements showed liposome supramolecular structures with hydrodynamic radius of the order of 900 and 1300 nm for plain and V3-lipopeptide liposomes. Electron paramagnetic resonance measurements showed almost identical local microenvironment. The difference in liposome hydrodynamic radius was attributed to the fluctuating ionic environment of the V3-lipopeptide liposomes. In vitro HIV-1 infectivity assays showed that plain liposomes reduced virus production in all cell cultures, probably due to the hydrophobic nature of the aggregates. Liposomes carrying V3-lipopeptides with different cationic potentials restored and even enhanced infectivity (p < 0.05). These results highlight the need for elucidation of the involvement of lipid bilayers as dynamic components in supramolecular structures and in HIV-1 fusion mechanisms

  20. Interfacing Zwitterionic Liposomes with Inorganic Nanomaterials: Surface Forces, Membrane Integrity, and Applications.

    Science.gov (United States)

    Liu, Juewen

    2016-05-10

    Zwitterionic phosphocholine (PC) lipids are the main constituent of the mammalian cell membrane. PC bilayers are known for their antifouling properties, yet they are adsorbed by all tested inorganic nanoparticles. This feature article is focused on the developments in my laboratory in the past few years on this topic. The main experimental techniques include fluorescence-based liposome leakage assays, adsorption and desorption, and cryo-TEM. Different materials interact with PC liposomes differently. PC liposomes adsorb on SiO2, followed by membrane fusion with the surface forming supported lipid bilayers. TiO2 and other metal oxides adsorb only intact PC liposomes via lipid phosphate bonding; the steric effect from the choline group hinders subsequent liposome fusion onto the particles. Citrate-capped AuNPs are adsorbed very strongly via van der Waals forces, inducing local gelation. The result is transient liposome leakage upon AuNP adsorption or desorption and AuNP aggregation on the liposome surface. All carbon-based nanomaterials (graphene oxides, carbon nanotubes, and nanodiamond) are adsorbed mainly via hydrogen bonding. The oxidation level of graphene oxide strongly influences the outcome of the final hybrid material. In the context of inorganic nanoparticle adsorption, insights are given regarding the lack of protein adsorption by PC bilayers. These inorganic/lipid hybrid materials can be used for controlled release, drug delivery, and fundamental studies. A few examples of application are covered toward the end, and future perspectives are given. PMID:27093351

  1. Innovative bionanocomposite films of edible proteins containing liposome-encapsulated nisin and halloysite nanoclay.

    Science.gov (United States)

    Boelter, Juliana Ferreira; Brandelli, Adriano

    2016-09-01

    Films and coatings based on natural polymers have gained increased interest for food packaging applications. In this work, halloysite and phosphatidylcholine liposomes encapsulating nisin were used to develop nanocomposite films of gelatin and casein. Liposomes prepared with either soybean lecithin or Phospholipon(®) showed particle size ranging from 124 to 178nm and high entrapment efficiency (94-100%). Considering their stability, Phospholipon(®) liposomes with 1.0mg/ml nisin were selected for incorporation into nanocomposite films containing 0.5g/l halloysite. The films presented antimicrobial activity against Listeria monocytogenes, Clostridium perfringens and Bacillus cereus. Scanning electron microscopy revealed that the films had a smooth surface, but showed increased roughness with addition of liposomes and halloysite. Casein films were thinner and slightly yellowish, less rigid and very elastic as compared with gelatin films. Thermogravimetric analysis showed a decrease of the degradation temperature for casein films added with liposomes. The glass transition temperature decreased with addition of liposomes and halloysite. Gelatin and casein films containing nisin-loaded liposomes and halloysite represent an interesting alternative for development of active food packaging. PMID:27289315

  2. Enhanced Ehrlich tumor inhibition using DOX-NP™ and gold nanoparticles loaded liposomes

    Science.gov (United States)

    Mady, M. M.; Al-Shaikh, F. H.; Al-Farhan, F. F.; Aly, A. A.; Al-Mohanna, M. A.; Ghannam, M. M.

    2016-04-01

    Treatment with doxorubicin (DOX) is a common regime in treating various types of cancer. DOX-NP™ is one of a well established marketed liposomal formulation for DOX. It offers distinct advantages over conventional DOX in reducing the cardiac toxicity and increasing the tolerability and efficacy. Gold nanoparticles (GNPs), a typical biocompatible nanomaterial, have been widely used in biomedical engineering and bioanalytical applications such as biomedical imaging and biosensors. Ehrlich tumors were grown in female balb mice by subcutaneous injection of Ehrlich ascites carcinoma cells. Mice bearing Ehrlich tumor were injected with saline, free doxorubicin (DOX) in solution, gold nanoparticles loaded liposomes and commercial liposomal encapsulated doxorubicin (DOX-NP™). The results showed that GNPs loaded liposomes could enhance the antitumor activity of commercial liposomal formulation (DOX-NP™) and displayed significantly decreased systemic toxicity compared with free DOX and commercial liposomal formulation (DOX-NP™) at the equivalent dose. So the combination of GNPs and liposomes is expected to significantly increase the likelihood of cell killing and make it a promising new approach to cancer therapy.

  3. Preparation and properties of functional mixed-lipid liposomes by γ-ray irradiation

    International Nuclear Information System (INIS)

    The feature of mixed-lipid liposomes such as polymerization and polymerized liposomes stability were investigated to find means for producing red cells containing hemoglobin inside the liposomes. The surface pressure-area isotherm values of the mixed-lipid monolayer indicated 1-stearoyl-2-(2,4-octadecadienoyl)-glycero-3-phosphocholine (SOPC) to be immiscible in cholesterol (Chol) and stearic acid (SA), and each component to contain separate domains in the bilayer membrane of liposomes. Radiation induced polymerization of mixed-SOPC liposomes was carried out using γ-rays from 60Co at 4degC to stabilize lipid bilayers. The polymer yield increased significantly by adding Chol and SA to SOPC. The rate of polymerization of SOPC liposomes increased linearly with increasing of dose rate. The molecular weight of the polymer decreased with an increase in irradiation time. Irradiated SOPC/Chol/SA liposome vesicle size was affected by freeze-thawing. The vesicle size did not change when SOPC/Chol/SA was present in the system due to the addition of immiscible saturated 1,2-dipalmitoyl-glycero-3-phosphocholine (DPPC). (author)

  4. Encapsulation and release of a hydrophobic drug from hydroxyapatite coated liposomes.

    Science.gov (United States)

    Xu, Qingguo; Tanaka, Yasuhiro; Czernuszka, Jan T

    2007-06-01

    Hydroxyapatite (HA) coated liposomes (HACL) have been successfully manufactured and filled with a model hydrophobic (lipophilic) drug, indomethacin (IMC). These HACL particles have been characterized in terms of particle size and zeta-potential. The liposomes are formed from 1,2-dimyristoyl-sn-glycero-3-phosphate (DMPA) and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC). Altering their relative proportions caused the zeta-potential to change from -38.8 to -67.0 mV, with a concomitant change in phase transition temperature from 36.4 to 53.3 degrees C. These changes also affect the drug loading efficiency. The release profiles of IMC have been measured. HA coating of the liposome reduces the release rate of IMC over uncoated liposomes. Under the present experimental conditions 70% of the drug is released after approximately 5h from the liposome, but coating with HA changes this time to over 20 h. Perhaps most importantly, it has been observed that for uncoated liposomes, IMC is released at a greater rate at pH=7.4 than at pH=4. However, coating with HA reduced the rate at pH=7.4 compared to pH=4. This behaviour arises because IMC is more soluble under basic conditions, but HA is more soluble under acidic conditions. This behaviour shows that it is now possible to have environmental control over the release of drugs from HA-coated liposomes. PMID:17331574

  5. Preparation and quality evaluation of LHRHa-targeted Brucea javanica oil liposomes

    Directory of Open Access Journals (Sweden)

    Xiao-juan LIU

    2013-07-01

    Full Text Available Objective To prepare luteinizing hormone-releasing hormone a (LHRHa targeted Bruceajavanicaliposomes and evaluate its quality. Methods The LHRHa-targeted Bruceajavanicaliposome was prepared by thin layer dispersion together with biotin¬streptavidin bridge method. The optimum formation was selected by means of orthogonal design of experiment. The morphology of liposome was observed with transmission electron microscope. Zetasizer Nano ZS analyzer was used to measure the particle size and zeta potential. The entrapment efficiency was determined by ultra-violet spectroscopy and column chromatography. Centrifugal acceleration experiment and determination of leak rate were performed to prove the liposome stability. The targeting ability of liposome was appraised by cell experiment in vitro. Results The formed optimum formula was as follows: the ratio of lecithin to cholesterol was 4:1, Brucea javanicaoil:lipid was 3:10, DSPE-PEG (2000-Biotin:lecithin content was 3%, ultrasonic-homogenized for 8 minutes. Liposomes were round in shape, the average diameter and zeta potential of liposome were 155.1±14.5mm and –(24.1±0.54 mV, respectively. The average entrapment efficiency was 92.2%. Binding capacity with the A2780/DDP cell line in the LHRHa-targeted liposomes was 2.7 times higher than that in the non-targeting liposomes. Conclusion The technique of preparing LHRHa-targeted Bruceajavanicaliposome is suitable, and high in entrapment efficiency, with good stability and targeting ability.

  6. LIPOSOMAL ENCAPSULATION TECHNOLOGY A NOVEL DRUG DELIVERY SYSTEM DESIGNED FOR AYURVEDIC DRUG PREPARATION

    Directory of Open Access Journals (Sweden)

    M. Hemanth kumar

    2011-10-01

    Full Text Available Liposomal Encapsulation Technology (LET is the newest delivery method used by medical researchers to transfer drugs that act as healing promoters to the definite body organs. This form of delivery system offers targeted delivery of vital compounds to the body. It has been in existence since the early 70’s. Liposomal Encapsulation Technology is a state of the art method of producing sub-microscopic bubbles called liposomes, which encapsulate various substances. These phospholipids or “liposomes” form a barrier around their contents that is resistant to enzymes in the mouth and stomach, digestive juices, alkaline solutions, bile salts, and intestinal flora, found in the human body as well as free radicals. The contents of the liposomes are therefore shielded from degradation and oxidation. This protective phospholipid shield or barrier remains unharmed until the contents of the liposome are delivered right to the target organ, gland, or system where the contents will be utilized. Natural extracts are generally degraded because of oxidation and other chemical reactions before they delivered to the target site. Our research has shown liposomal encapsulated ayurvedic preparations have shown more stability and also more efficiency when compared to traditional preparations. Size of liposomes were measured around 85-200 nm.

  7. Acacia-gelatin microencapsulated liposomes: preparation, stability, and release of acetylsalicylic acid.

    Science.gov (United States)

    Dong, C; Rogers, J A

    1993-01-01

    Liposomes of dipalmitoylphosphatidylcholine (DPPC) containing acetylsalicylic acid (ASA) have been microencapsulated by acacia-gelatin using the complex coacervation technique as a potential oral drug delivery system. The encapsulation efficiency of ASA was unaltered by the microencapsulation process. The stability of the microencapsulated liposomes in sodium cholate solutions at pH 5.6 was much greater than the corresponding liposomes. The optimum composition and conditions for stability and ASA release were 3.0% acacia-gelatin and a 1- to 2-hr formaldehyde hardening time. Approximately 25% ASA was released in the first 6 hr from microencapsulated liposomes at 23 degrees C and the kinetics followed matrix-controlled release (Q varies; is directly proportional to t1/2). At 37 degrees C, this increased to 75% released in 30 min followed by a slow constant release, likely due to lowering of the phase transition temperature of DPPC by the acacia-gelatin to near 37 degrees C. At both temperatures, the release from control liposomes was even more rapid. Hardening times of 4 hr and an acacia-gelatin concentration of 5% resulted in a lower stability of liposomes and a faster release of ASA. It is concluded that under appropriate conditions the microencapsulation of liposomes by acacia-gelatin may increase their potential as an oral drug delivery system. PMID:8430052

  8. A novel cationic liposome formulation for efficient gene delivery via a pulmonary route

    Science.gov (United States)

    Li, Peng; Liu, Donghua; Sun, Xiaoli; Liu, Chunxi; Liu, Yongjun; Zhang, Na

    2011-06-01

    The clinical success of gene therapy for lung cancer is not only dependent on efficient gene carriers but also on a suitable delivery route. A pulmonary delivery route can directly deliver gene vectors to the lung which is more efficient than a systemic delivery route. For gene carriers, cationic liposomes have recently emerged as leading non-viral vectors in worldwide gene therapy clinical trials. However, cytotoxic effects or apoptosis are often observed which is mostly dependent on the cationic lipid used. Therefore, an efficient and safe cationic lipid, 6-lauroxyhexyl lysinate (LHLN), previously synthesized by our group was first used to prepare cationic liposomes. Physicochemical and biological properties of LHLN-liposomes were investigated. LHLN-liposome/DNA complexes showed positive surface charge, spherical morphology, a relatively narrow particle size distribution and strong DNA binding capability. Compared with Lipofectamine2000, the new cationic liposome formulation using LHLN exhibited not only lower cytotoxicity (P transfection efficiency in A549 and HepG2 lung cancer cells for in vitro tests. When administered by intratracheal instillation into rat lungs for in vivo evaluation, LHLN-liposome/DNA complexes exhibited higher pulmonary gene transfection efficiency than Lipofectamine2000/DNA complexes (P < 0.05). These results suggested that LHLN-liposomes may have great potential for efficient pulmonary gene delivery.

  9. A novel cationic liposome formulation for efficient gene delivery via a pulmonary route

    International Nuclear Information System (INIS)

    The clinical success of gene therapy for lung cancer is not only dependent on efficient gene carriers but also on a suitable delivery route. A pulmonary delivery route can directly deliver gene vectors to the lung which is more efficient than a systemic delivery route. For gene carriers, cationic liposomes have recently emerged as leading non-viral vectors in worldwide gene therapy clinical trials. However, cytotoxic effects or apoptosis are often observed which is mostly dependent on the cationic lipid used. Therefore, an efficient and safe cationic lipid, 6-lauroxyhexyl lysinate (LHLN), previously synthesized by our group was first used to prepare cationic liposomes. Physicochemical and biological properties of LHLN-liposomes were investigated. LHLN-liposome/DNA complexes showed positive surface charge, spherical morphology, a relatively narrow particle size distribution and strong DNA binding capability. Compared with Lipofectamine2000, the new cationic liposome formulation using LHLN exhibited not only lower cytotoxicity (P < 0.05) but also similar transfection efficiency in A549 and HepG2 lung cancer cells for in vitro tests. When administered by intratracheal instillation into rat lungs for in vivo evaluation, LHLN-liposome/DNA complexes exhibited higher pulmonary gene transfection efficiency than Lipofectamine2000/DNA complexes (P < 0.05). These results suggested that LHLN-liposomes may have great potential for efficient pulmonary gene delivery.

  10. Do plasma proteins distinguish between liposomes of varying charge density?

    KAUST Repository

    Capriotti, Anna Laura

    2012-03-01

    Cationic liposomes (CLs) are one of the most employed nonviral nanovector systems in gene therapy. However, their transfection efficiency is strongly affected by interactions with plasma components, that lead to the formation of a "protein corona" onto CL surface. The interactions between nanoparticles entering the body and biomolecules have an essential role for their biodistribution. Because the knowledge of proteins adsorbed onto vector surface could be useful in the screening of new, more efficient and more biocompatible liposomal formulations, the behavior of three CLs with different membrane charge densities was investigated. The proteins of the three coronas were identified by nano-liquid chromatography-tandem mass spectrometry, and quantified with label-free spectral counting strategy. Fibrinogen displayed higher association with CLs with high membrane charge density, while apolipoproteins and C4b-binding protein with CLs with low membrane charge density. These results are discussed in terms of the different lipid compositions of CLs and may have a deep biological impact for in vivo applications. Surface charge of nanoparticles is emerging as a relevant factor determining the corona composition after interaction with plasma proteins. Remarkably, it is also shown that the charge of the protein corona formed around CLs is strongly related to their membrane charge density. © 2012 Elsevier B.V.

  11. Liposomal Antioxidants for Protection against Oxidant-Induced Damage

    Directory of Open Access Journals (Sweden)

    Zacharias E. Suntres

    2011-01-01

    Full Text Available Reactive oxygen species (ROS, including superoxide anion, hydrogen peroxide, and hydroxyl radical, can be formed as normal products of aerobic metabolism and can be produced at elevated rates under pathophysiological conditions. Overproduction and/or insufficient removal of ROS result in significant damage to cell structure and functions. In vitro studies showed that antioxidants, when applied directly and at relatively high concentrations to cellular systems, are effective in conferring protection against the damaging actions of ROS, but results from animal and human studies showed that several antioxidants provide only modest benefit and even possible harm. Antioxidants have yet to be rendered into reliable and safe therapies because of their poor solubility, inability to cross membrane barriers, extensive first-pass metabolism, and rapid clearance from cells. There is considerable interest towards the development of drug-delivery systems that would result in the selective delivery of antioxidants to tissues in sufficient concentrations to ameliorate oxidant-induced tissue injuries. Liposomes are biocompatible, biodegradable, and nontoxic artificial phospholipid vesicles that offer the possibility of carrying hydrophilic, hydrophobic, and amphiphilic molecules. This paper focus on the use of liposomes for the delivery of antioxidants in the prevention or treatment of pathological conditions related to oxidative stress.

  12. Liposomes and nanotechnology in drug development: focus on ocular targets.

    Science.gov (United States)

    Honda, Miki; Asai, Tomohiro; Oku, Naoto; Araki, Yoshihiko; Tanaka, Minoru; Ebihara, Nobuyuki

    2013-01-01

    Poor drug delivery to lesions in patients' eyes is a major obstacle to the treatment of ocular diseases. The accessibility of these areas to drugs is highly restricted by the presence of barriers, including the corneal barrier, aqueous barrier, and the inner and outer blood-retinal barriers. In particular, the posterior segment is difficult to reach for drugs because of its structural peculiarities. This review discusses various barriers to drug delivery and provides comprehensive information for designing nanoparticle-mediated drug delivery systems for the treatment of ocular diseases. Nanoparticles can be designed to improve penetration, controlled release, and drug targeting. As highlighted in this review, the therapeutic efficacy of drugs in ocular diseases has been reported to be enhanced by the use of nanoparticles such as liposomes, micro/nanospheres, microemulsions, and dendrimers. Our recent data show that intravitreal injection of targeted liposomes encapsulating an angiogenesis inhibitor caused significantly greater suppression of choroidal neovascularization than did the injection of free drug. Recent progress in ocular drug delivery systems research has provided new insights into drug development, and the use of nanoparticles for drug delivery is thus a promising approach for advanced therapy of ocular diseases. PMID:23439842

  13. Experiments on Gene Transferring to Primary Hematopoietic Cells by Liposome

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    Liposomes have showed many advantages in mediating exogenous gene into many cell types in vitro and in vivo. But few data are available concerning gene transfer into hematopoietic cells. In this report, we described two-marker genes (Neo R and Lac Z) co-transferred into hematopoietic cells of human and mouse by using liposome in vitro. The efficiency of gene transfer was tested by Xgal staining and observation of colony formation. The X-gal blue staining rate of transduced cells was about (13.33±2. 68) % in human and about (16. 28±2.95) % in mouse without G418 selection. After G418 selection, the blue cell rate was (46. 06±3.47)%in human and (43. 45±4. 1) % in mouse, which were markedly higher than those before selection, suggesting that high-efficiency gene transfer and expression could be attained in primary hematopoietic cells using this easy and harmless transduction protocol. At the same time, this protocol provided experimental data for clinicians to investigate the biology of marrow reconstitution and trace the origin of relapse after autologous bone marrow transplantation for the patients with leukemia.

  14. Interaction of clonixin with EPC liposomes used as membrane models.

    Science.gov (United States)

    Ferreira, Helena; Lúcio, Marlene; Lima, José L F C; Matos, Carla; Reis, Salette

    2005-06-01

    In this work, an overall analysis of clonixin interaction with liposomes was achieved using different techniques, which allowed the evaluation of the change in different membrane's characteristics as well as the possible location of the drug in the membrane. Clonixin acidity constants were obtained and the values are 5.5 +/- 0.08 and 2.2 +/- 0.04. Clonixin partition coefficient (K(p)) between liposomes and water was also determined using derivative spectrophotometry, fluorescence quenching, and zeta-potential (zeta-potential). These three techniques yielded similar results. zeta-potential measurements were performed and an increase of the membrane negative charge with an increase of drug concentration was observed. Drug location within the bilayer was performed by fluorescence quenching using a set of n-(9-anthroyloxy) fatty acid probes (n = 2, 6, 9, and 12). The fluorescence intensity of all probes was quenched by the drug. This effect is more noticeable for the outer located probe, indicating that the drug is positioning in the external part of the membrane. These same probes were used for steady-state anisotropy measurements to determine the perturbation in membrane structure induced by clonixin. Clonixin increased membrane fluidity in a concentration dependent manner, with the highest perturbation occurring nearby the 2-AS probe, closely located to the bilayer surface. PMID:15858845

  15. Pegylated liposomal doxorubicin in the management of ovarian cancer

    Directory of Open Access Journals (Sweden)

    Gabriella Ferrandina

    2010-09-01

    Full Text Available Gabriella Ferrandina1,2, Giacomo Corrado1, Angelo Licameli1, Domenica Lorusso2, Gilda Fuoco1, Salvatore Pisconti3, Giovanni Scambia2 1Gynecologic Oncology Unit, Department of Oncology, Catholic University of Campobasso, Campobasso, Italy; 2Gynecologic Oncology Unit, Catholic University of Rome, Rome, Italy; 3Salvatore Pisconti, Oncology Unit, Taranto Hospital, Taranto, Italy Abstract: Among the pharmaceutical options available for treatment of ovarian cancer, much attention has been progressively focused on pegylated liposomal doxorubicin (PLD, whose unique formulation, which entraps conventional doxorubicin in a bilayer lipidic sphere ­surrounded by a polyethylene glycol layer, prolongs the persistence of the drug in the ­circulation and potentiates intratumor drug accumulation. These properties enable this drug to sustain its very favorable toxicity profile and to be used safely in combination with other drugs. PLD has been already approved for treatment of advanced ovarian cancer patients failing first-line platinum-based treatment. Moreover, phase III trials have been already completed, and results are eagerly awaited, which hopefully will expand the range of PLD clinical application in this neoplasia both in front-line treatment, and in the salvage setting in combination with other drugs. Moreover, attempts are continuing to enable this drug to be combined with novel cytotoxic drugs and target-based agents. This review aims at summarizing the available evidence and the new perspectives for the clinical role of PLD in the management of patients with epithelial ovarian cancer.Keywords: pegylated liposomal doxorubicin, ovarian cancer, clinical trials

  16. Nutrient Uptake by Protocells: A Liposome Model System

    Science.gov (United States)

    Monnard, Pierre-Alain; Deamer, David W.

    2001-02-01

    Over the past decade, several liposome-based models for protocells have been developed. For example, liposome systems composed of polymerase enzymes encapsulated with their substrates have demonstrated that complex compartmentalized reactions can be carried out under conditions in which polymeric products are protected from degradation by hydrolytic enzymes present in the external medium. However, such systems do not have nutrient uptake mechanisms, which would be essential for primitive cells lacking the highly evolved nutrient transport processes present in all contemporary cells. In this report, we explore passive diffusion of solutes across lipid bilayers as one possible uptake mechanism. We have established conditions under which ionic substrates as large as ATP can permeate bilayers at rates capable of supplying an encapsulated template-dependent RNA polymerase. Furthermore, while allowing the permeation of monomer substrates such as ATP, bilayer vesicles selectively retained polymerization products as small as dimers and as large as a transfer RNA. These observations demonstrate that passive diffusion could be used by the earliest forms of cellular life for transport of important nutrients such as amino acids, phosphate, and phosphorylated organic solutes.

  17. Nano-sized Fe3O4/carbon as anode material for lithium ion battery

    International Nuclear Information System (INIS)

    Nano-sized Fe3O4/carbon material is prepared via a simple citric-nitrate combustion method combining with a hydrothermal carbon coating technique. The synthesized Fe3O4/carbon composite shows a high reversible specific capacity (ca. 850 mAh g−1 at 100 mA g−1; ca. 600 mAh g−1 at 500 mA g−1), good rate-capability as well as superior cycling stability as anode for lithium-ion batteries. The ameliorated electrochemical performance of Fe3O4/carbon electrode is associated to the nano-sized particle feature and the continuous carbon coating layer. The former provides short lithium-ion/electron diffusion distance, while the latter enables the fast electron transport pathways. Besides, the carbon layer can act as a protective component to prevent the active particle Fe3O4 from aggregation and pulverization during the charge/discharge processes. - Highlights: • Nano-sized Fe3O4/C was prepared by a simple citric-nitrate combustion process. • Fe3O4/C particles show core–shell structure. • Fe3O4/C powder displays high specific capacity and good cycling stability. • Fe3O4/C composite exhibits a superior rate-capability

  18. Synthesis of nano-sized EuF3 hollow spheres via one step chemical conversion

    International Nuclear Information System (INIS)

    Highlights: → This method is simple and with well reproducibility. → Moreover it expels the usage of template in constructing the hollow structure. → This method could serve as a general route to prepare other rare earth fluorides hollow spheres. → In addition, the nano-sized hollow spheres could cut down the usage of expensive rare earth element for lower producing cost. → These well-crystallized EuF3 nano-sized hollow spheres could be used as a promising material to fabricate light-emitting device owing to the high efficiency and thermal stability. - Abstract: Monodisperse EuF3 hollow spheres with diameter of about 95 nm were firstly synthesized using Eu(OH)CO3 nanospheres as template. Control experiments indicated the morphology and crystal quality of the final products were greatly influenced by the synthesis parameters such as pH value, temperature and reactant concentration. Subsequently, a possible growth mechanism for the nano-sized hollow sphere was proposed and the photoluminescence (PL) properties of as-prepared EuF3 products were also intensively studied. Furthermore, this method could serve as a general route to prepare other rare earth fluorides hollow spheres.

  19. Nano-sized Y2O3:Eu phosphor particles prepared by spray pyrolysis

    International Nuclear Information System (INIS)

    Y2O3:Eu phosphor particles with nano-sized and non-aggregation characteristics were prepared by spray pyrolysis using spraying solution containing polymeric precursors and Li2CO3 flux material. The post-treated phosphor particles with fine size and high brightness were ball milled to reduce the aggregation degree of the nano-sized Y2O3:Eu phosphor particles. The mean particle size, morphology, and brightness of Y2O3:Eu phosphor particles were strongly affected by contents of the additives and post-treatment temperature. The Y2O3:Eu phosphor particles prepared from the solution containing 0.3 M citric acid, 0.3 M ethylene glycol and 5 wt.% Li2CO3 had fine size and good morphology after post-treatment. The Y2O3:Eu phosphor particles post-treated at 1000 deg. C for 3 h had the mean size of 300 nm. Nano-sized Y2O3:Eu phosphor particles prepared by spray pyrolysis had similar photoluminescence intensity to the micron-sized Y2O3:Eu commercial product prepared by solid state reaction method. The Y2O3:Eu phosphor particles had aggregation-free and regular morphology characteristics even after 30 min ball milling process

  20. Nano-sized precipitation and properties of a low carbon niobium micro-alloyed bainitic steel

    International Nuclear Information System (INIS)

    The present work focuses on microstructure evolution and precipitation strengthening during tempering at region of 550–680 °C to elucidate the structure–property relationship in the steel. The effect of tempering on the development of a 700 MPa grade high strength hot rolled cost-effective bainitic steel was studied for infrastructure applications. Granular bainite with dispersed martenisit–austenite (M–A) constituents in the bainitic ferrite matrix was obtained after hot rolling and air cooling to room temperature. The decomposition of M–A constituents to cementite carbides and the precipitation of nano-sized NbC carbides in bainitic matrix on tempering were characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Nano-sized precipitates of NbC precipitated during tempering were in average diameter of ~4.1–6.1 nm. There were ~86–173 MPa increases in yield strength after tempering at region of 550–680 °C. It is noticeable that those nano-sized NbC precipitates provide an effective way to significantly increase the strength of the low carbon bainitic steel. High yield strength of 716 MPa with high ductility (uniform elongation of 9.3% and total elongation of 22.4%), low yield to tensile ratio of 0.9 and good low temperature toughness of 47 J (half thickness) at –40 °C was obtained after tempering at 680 °C for 30 min