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Release Properties (release + property)
Kinds of Release Properties Selected AbstractsFormation and Distribution of Silver Nanoparticles in a Functional Plasma Polymer Matrix and Related Ag+ Release PropertiesPLASMA PROCESSES AND POLYMERS, Issue 7 2010Enrico Körner Abstract Plasma polymer coatings with embedded Ag nanoparticles were deposited in a low pressure RF plasma reactor using an asymmetrical setup with an Ag electrode. The plasma polymer was deposited from a reactive gas/monomer mixture of CO2/C2H4 yielding a functional hydrocarbon matrix. In addition, Ar was simultaneously used to sputter Ag atoms from the Ag electrode, forming nanoparticles within the growing polymer matrix. The influence of the power input, gas ratio and coating thickness on both, the Ag content and the Ag nanoparticle morphology, as well as the distribution in the polymer matrix were investigated. It was found that both increasing the power input and the CO2 ratio result in a higher incorporation of Ag into the matrix. [source] Severely impaired neuromuscular synaptic transmission causes muscle weakness in the Cacna1a -mutant mouse rolling NagoyaEUROPEAN JOURNAL OF NEUROSCIENCE, Issue 7 2007Simon Kaja Abstract The ataxic mouse rolling Nagoya (RN) carries a missense mutation in the Cacna1a gene, encoding the pore-forming subunit of neuronal Cav2.1 (P/Q-type) Ca2+ channels. Besides being the predominant type of Cav channel in the cerebellum, Cav2.1 channels mediate acetylcholine (ACh) release at the peripheral neuromuscular junction (NMJ). Therefore, Cav2.1 dysfunction induced by the RN mutation may disturb ACh release at the NMJ. The dysfunction may resemble the situation in Lambert,Eaton myasthenic syndrome (LEMS), in which autoantibodies target Cav2.1 channels at NMJs, inducing severely reduced ACh release and resulting in muscle weakness. We tested neuromuscular function of RN mice and characterized transmitter release properties at their NMJs in diaphragm, soleus and flexor digitorum brevis muscles. Clinical muscle weakness and fatigue were demonstrated using repetitive nerve-stimulation electromyography, grip strength testing and an inverted grid hanging test. Muscle contraction experiments showed a compromised safety factor of neuromuscular transmission. In ex vivo electrophysiological experiments we found severely impaired ACh release. Compared to wild-type, RN NMJs had 50,75% lower nerve stimulation-evoked transmitter release, explaining the observed muscle weakness. Surprisingly, the reduction in evoked release was accompanied by an ,,3-fold increase in spontaneous ACh release. This synaptic phenotype suggests a complex effect of the RN mutation on different functional Cav2.1 channel parameters, presumably with a positive shift in activation potential as a prevailing feature. Taken together, our studies indicate that the gait abnormality of RN mice is due to a combination of ataxia and muscle weakness and that RN models aspects of the NMJ dysfunction in LEMS. [source] Photopolymerizable Hydrogels Made from Polymer-Conjugated Albumin for Affinity-Based Drug Delivery,ADVANCED ENGINEERING MATERIALS, Issue 1-2 2010Liat Oss-Ronen As a drug delivery vehicle, biodegradable albumin hydrogels can combine the high binding capacity of albumin with the structural stability of a polymeric hydrogel network to enable controlled release of small molecules based on both binding affinity and physical interactions. In the present study, we report on the development of a hybrid hydrogel composed of albumin conjugated to poly(ethylene glycol) (PEG) for drug delivery applications where controlled release is accomplished using the natural affinity of the drugs to the serum albumin. Bovine serum albumin was conjugated to PEG-diacrylate having a molecular weight of 1.5, 4, or 10,kDa to form a PEGylated albumin macromolecule (mono-PEGylated or multi-PEGylated). Biodegradable hydrogels were formed from the PEGylated albumin using photopolymerization. Two model drugs, Warfarin and Naproxen, were used for equilibrium dialysis and release experiments from the hydrogels, both having relatively low molecular weights and a known high affinity for albumin. Equilibrium dialysis experiments showed that multi-PEGylation of albumin significantly decreased the drug affinity to the protein compared to non-PEGylated controls, irrespective of the PEG molecular weight. However, the results from drug release experiments showed that mono-PEGylation of albumin did not change its natural affinity to the drug. Comparing the release profiles with a Fickian diffusion model provided strong evidence that hydrogels containing mono-PEGylated albumin exhibited sub-diffusive drug release properties based on the affinity of the drug to the tethered protein. [source] Dextran Microgels for Time-Controlled Delivery of siRNA,ADVANCED FUNCTIONAL MATERIALS, Issue 7 2008Koen Raemdonck Abstract To apply siRNA as a therapeutic agent, appropriate attention should be paid to the optimization of the siRNA gene silencing effect, both in terms of magnitude and duration. Intracellular time-controlled siRNA delivery could aid in tailoring the kinetics of siRNA gene knockdown. However, materials with easily tunable siRNA release properties have not been subjected to thorough investigation thus far. This report describes cationic biodegradable dextran microgels which can be loaded with siRNA posterior to gel formation. Even though the siRNAs are incorporated in the hydrogel network based on electrostatic interaction, still a time-controlled release can be achieved by varying the initial network density of the microgels. To demonstrate the biological functionality of the siRNA loaded gels, we studied their cellular internalization and enhanced green fluorescent protein (EGFP) gene silencing potential in HUH7 human hepatoma cells. [source] Soluble Microcapsules Assembled Stepwise from Weak Polyelectrolytes Using Acid-Decomposable Cores,ADVANCED MATERIALS, Issue 11 2003C.-Y. Gao Decomposable microcapsules with tunable permeability, loading, and release properties,with potential applications as chemical reservoirs and for controlled drug release,have been fabricated by assembly of weak polyelectrolytes on melamine formaldehyde templates followed by removal of the cores at low pH by precise control of the time of acid treatment. The Figure shows capsules before (left) and after (right) treatment with 0.1 M HCl. [source] Calcium-carboxymethyl chitosan hydrogel beads for protein drug delivery systemJOURNAL OF APPLIED POLYMER SCIENCE, Issue 5 2007Zonghua Liu Abstract In this study, carboxymethyl chitosan (CMC) hydrogel beads were prepared by crosslinking with Ca2+. The pH-sensitive characteristics of the beads were investigated by simulating gastrointestinal pH conditions. As a potential protein drug delivery system, the beads were loaded with a model protein (bovine serum albumin, BSA). To improve the entrapment efficiency of BSA, the beads were further coated with a chitosan/CMC polyelectrolyte complex (PEC) membrane by extruding a CMC/BSA solution into a CaCl2/chitosan gelation medium. Finally, the release studies of BSA-loaded beads were conducted. We found that, the maximum swelling ratios of the beads at pH 7.4 (17,21) were much higher than those at pH 1.2 (2,2.5). Higher entrapment efficiency (73.2%) was achieved in the chitosan-coated calcium-CMC beads, compared with that (44.4%) in the bare calcium-CMC beads. The PEC membrane limited the BSA release, while the final disintegration of beads at pH 7.4 still leaded to a full BSA release. Therefore, the chitosan-coated calcium-CMC hydrogel beads with higher entrapment efficiency and proper protein release properties were a promising protein drug carrier for the site-specific release in the intestine. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 103: 3164,3168, 2007 [source] Characterization of the physicochemical, antimicrobial, and drug release properties of thermoresponsive hydrogel copolymers designed for medical device applicationsJOURNAL OF BIOMEDICAL MATERIALS RESEARCH, Issue 2 2008David S. Jones Abstract In this study, a series of hydrogels was synthesized by free radical polymerization, namely poly(2-(hydroxyethyl)methacrylate) (pHEMA), poly(4-(hydroxybutyl)methacrylate) (pHBMA), poly(6-(hydroxyhexyl)methacrylate) (pHHMA), and copolymers composed of N -isopropylacrylamide (NIPAA), methacrylic acid (MA), NIPAA, and the above monomers. The surface, mechanical, and swelling properties (at 20 and 37°C, pH 6) of the polymers were determined using dynamic contact angle analysis, tensile analysis, and thermogravimetry, respectively. The Tg and lower critical solution temperatures (LCST) were determined using modulated DSC and oscillatory rheometry, respectively. Drug loading of the hydrogels with chlorhexidine diacetate was performed by immersion in a drug solution at 20°C ( Role of Mn of PEG in the morphology and properties of electrospun PEG/CA composite fibers for thermal energy storageAICHE JOURNAL, Issue 3 2009Changzhong Chen Abstract As an aim toward developing novel class of form-stable polymer-matrix phase change materials for thermal energy storage, ultrafine composite fibers based on cellulose acetate and polyethylene glycol (PEG) with five different molecular weight (Mn) grades were prepared by electrospinning. The effects of Mn of PEG on morphology, thermal properties and mechanical properties of the composite fibers were studied by field emission scanning electron microscopy, differential scanning calorimetry, and tensile testing, respectively. It was found that the composite fibers were smooth and cylindrical shape, with the average diameters ranging from about 1000 to 1750 nm which increased with Mn of PEG. Thermal analysis results showed that the composite fibers imparted balanced thermal storage and release properties in different temperature ranges with the variation of Mn of PEG. Thermal cycling test indicated that the prepared composites had excellent thermal stability and reliability even they were subjected to 100 heating-cooling thermal cycles. © 2009 American Institute of Chemical Engineers AIChE J, 2009 [source] Drug release properties of polymer coated ion-exchange resin complexes: Experimental and theoretical evaluationJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 3 2007Seong Hoon Jeong Abstract Although ion-exchange resins have been used widely as drug delivery systems, their exact release kinetics has not been reported yet. Usually only the rate-limiting step has been taken into account and the rest of the steps have been ignored as instantaneous processes. To investigate the exact release kinetics of polymer-coated drug/ion-exchange resin complexes for sustained drug delivery, the results of new mathematical modeling were compared with experimental results. Drug/resin complexes with a model drug, dextromethorphan, were prepared and used as cores for fluid-bed coating. An aqueous colloidal dispersion of poly(vinyl acetate) was applied for the coating. A comprehensive mathematical model was developed using a mechanistic approach by considering diffusion, swelling, and ion-exchange processes solved by numerical techniques. The rate-limiting factor of the uncoated resin particles was diffusion through the core matrix. Similarly, in the coated particles the rate-limiting factor was diffusion through the coating membrane. The mathematical model has captured the phenomena observed during experimental evaluations and the release dynamics from uncoated and coated (at different coat levels) particles were predicted accurately (maximum RMSE 2.4%). The mathematical model is a useful tool to theoretically evaluate the drug release properties from coated ion-exchange complexes thus can be used for design purposes. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci [source] Acrylic polymers as thickening agents for tetraglycol cosolventJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2006Giulia Bonacucina Abstract This article evaluated the thickening properties of two different Eudragits, L and RS, in tetraglycol cosolvent in order to obtain high viscosity systems characterized by controlled release properties. Tetraglycol was chosen for its ability to dissolve a wide range of water insoluble drugs, while Eudragit RS and L for their specific dissolution and permeability properties under physiological conditions. Study of the rheological properties was performed to characterize elastic and viscous properties of Eudragit/tetraglycol samples in function of frequency and temperature. For all systems, the results outlined a liquid like behavior, as observed for dilute polymer solutions. In fact the fitting of the log G,-log G,, versus frequency curves showed a good agreement with the Rouse or Zimm models. So despite the increase in viscosity, samples still behaved like liquid systems. After the addition of paracetamol the release characteristics were defined pointing out the great release control properties of both Eudragit L and RS, which showed different release kinetics depending on the pH of the environment. Semisolid Eudragits/tetraglycol systems can be considered as a new alterative for the sustained release of insoluble or poorly water-soluble drugs. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 95:726,736, 2006 [source] Preparation, characterization and taste-masking properties of polyvinylacetal diethylaminoacetate microspheres containing trimebutineJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2002Yoshimi Hashimoto The objectives of this study were to produce acid soluble, polyvinylacetal diethylaminoacetate (AEA) microspheres containing trimebutine (as maleate), using a water-in-oil-in-water (w/o/w) emulsion solvent evaporation method, to characterize their in-vitro release properties, and to evaluate the taste-masking potential of this formulation in human volunteers. The pH of the external aqueous phase was the critical factor in achieving a high loading efficiency for trimebutine in the microencapsulation process; nearly 90% (w/w) loading efficiency was obtained at above pH 10. Trimebutine was completely released from AEA microspheres within 10 min in a dissolution test at pH 1.2, simulating conditions in the stomach, whereas at pH 6.8, the pH in the mouth, only small quantities of trimebutine were released in the initial 1,2 min. The results of a gustatory sensation test in healthy volunteers confirmed the taste-masking effects of the AEA microspheres. Finally, an attempt was made to encapsulate the salts of other basic drugs (lidocaine, imipramine, desipramine, amitriptyline, promethazine and chlorpheniramine) into AEA microspheres using the w/o/w emulsion evaporation method. The loading efficiencies were ranked in almost inverse proportion with the solubility of the drugs in the external aqueous phase. This study demonstrated the possibility of masking the taste of salts of basic drugs by microencapsulation with AEA using a w/o/w emulsion solvent evaporation method. [source] Synthesis and supramolecular self-assembly of thermosensitive amphiphilic star copolymers based on a hyperbranched polyether coreJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 2 2008Haiyan Hong Abstract A novel amphiphilic thermosensitive star copolymer with a hydrophobic hyperbranched poly (3-ethyl-3-(hydroxymethyl)oxetane) (HBPO) core and many hydrophilic poly(2-(dimethylamino) ethyl methacrylate) (PDMAEMA) arms was synthesized and used as the precursor for the aqueous solution self-assembly. All the copolymers directly aggregated into core,shell unimolecular micelles (around 10 nm) and size-controllable large multimolecular micelles (around 100 nm) in water at room temperature, according to pyrene probe fluorescence spectrometry and 1H NMR, TEM, and DLS measurements. The star copolymers also underwent sharp, thermosensitive phase transitions at a lower critical solution temperature (LCST), which were proved to be originated from the secondary aggregation of the large micelles driven by increasing hydrophobic interaction due to the dehydration of PDMAEMA shells on heating. A quantitative variable temperature NMR analysis method was designed by using potassium hydrogen phthalate as an external standard and displayed great potential to evaluate the LCST transition at the molecular level. The drug loading and temperature-dependent release properties of HBPO- star -PDMAEMA micelles were also investigated by using indomethacin as a model drug. The indomethacin-loaded micelles displayed a rapid drug release at a temperature around LCST. © 2007 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 46: 668,681, 2008 [source] Encapsulation and Controlled Release of a Hydrophobic Drug Using a Novel Nanoparticle-Forming Hyperbranched Polyester,MACROMOLECULAR BIOSCIENCE, Issue 7 2005Jianhua Zou Abstract Summary: An amphiphilic, hyperbranched polymer suitable for use in controlled drug delivery is reported. This polymer was obtained by modification of the hyperbranched aliphatic polyester BoltornÔ H20 (H20) with succinic anhydride and then glycidyl methacrylate, and formed nanoparticles in aqueous solution. The critical association concentration was 7.4,×,10,3 g,·,L,1, as determined by fluorescence spectroscopy using pyrene as a molecular probe. A static/dynamic laser light scattering (LLS) study revealed that the average particle size was 39.4 nm with a low particle size distribution (PDI = 0.04), and that each particle was composed of about 350 amphiphilic molecules. Daidzein, a hydrophobic traditional Chinese medicine, was encapsulated during particle formation and the release properties were determined. The optimal feeding concentration of daidzein to hyperbranched polyester was 4.9,×,10,5 g,·,mL,1 to 5.0,×,10,3 g,·,mL,1 with a loading efficiency of 76.1%. In the presence of the enzyme Lipase PS, the drug loaded nanoparticles degraded in a random one-by-one manner and released the drug over a few days. This system is therefore a novel controlled drug release system based on nanoparticles formed of hyperbranched polyester. Encapsulation of daidzein by hyperbranched polyester particles. [source] Synthesis and characterization of hydrogels containing biodegradable polymersPOLYMER INTERNATIONAL, Issue 7 2008Adina Cretu Abstract BACKGROUND: Amphiphilic block and graft copolymers constitute a very interesting class of polymers with potential for biomedical applications, due to their special characteristics, which derive from the combination of properties of hydrophilic and hydrophobic moieties. In this work, the synthesis and biodegradation of poly(2-hydroxyethyl methacrylate)- graft -poly(L -lactide) are studied. RESULTS: The graft copolymers were synthesized using the macromonomer technique. In a first step, methacryloyl-terminated poly(L -lactide) macromonomers were synthesized in a wide molecular weight range using different catalysts. Subsequently, these macromonomers were copolymerized with 2-hydroxyethyl methacrylate in order to obtain a graft copolymer. These new materials resemble hydrogel scaffolds with a biodegradable component. The biodegradation was studied in hydrolytic and enzymatic environments. The influence of different parameters (molecular weight, crystallinity, ratio between hydrophilic and hydrophobic components) on the degradation rate was investigated. CONCLUSION: Based on this study it will be possible to tailor the release properties of biodegradable materials. In addition, the materials will show good biocompatibility due to the hydrophilic poly(2-hydroxyethyl methacrylate) hydrogel scaffold. This kind of material has potential for many applications, like controlled drug-delivery systems or biodegradable implants. Copyright © 2008 Society of Chemical Industry [source] Preparation and properties of ionically cross-linked chitosan nanoparticlesPOLYMERS FOR ADVANCED TECHNOLOGIES, Issue 7 2009Hui Liu Abstract Chitosan nanoparticles were fabricated by a method of tripolyphosphate (TPP) cross-linking. The influence of fabrication conditions on the physical properties and drug loading and release properties was investigated by transmission electron microscopy (TEM), dynamic light scattering (DLS), and UV,vis spectroscopy. The nanoparticles could be prepared only within a zone of appropriate chitosan and TPP concentrations. The particle size and surface zeta potential can be manipulated by variation of the fabrication conditions such as chitosan/TPP ratio and concentration, solution pH and salt addition. TEM observation revealed a core,shell structure for the as-prepared nanoparticles, but a filled structure for the ciprofloxacin (CH) loaded particles. Results show that the chitosan nanoparticles were rather stable and no cytotoxicity of the chitosan nanoparticles was found in an in vitro cell culture experiment. Loading and release of CH can be modulated by the environmental factors such as solution pH and medium quality. Copyright © 2008 John Wiley & Sons, Ltd. [source] SURGICAL ADHESIONS: EVIDENCE FOR ADSORPTION OF SURFACTANT TO PERITONEAL MESOTHELIUMANZ JOURNAL OF SURGERY, Issue 6 2000Y. Chen Background: It has been speculated that the formation of surgical adhesions must be preceded by physical adhesion of the two surfaces, a process normally prevented by a lining of adsorbed surface-active phospholipid (surfactant) acting as both a superb boundary (solid-to-solid) lubricant and a release (antistick) agent. Animal trials administering exogenous surfactant as a dry powder (ALECÔ) have previously demonstrated a reduction of 80% in abdominal adhesions. Methods: Incubation of rat peritoneum (both live and excised) with radiolabelled dipalmitoyl phosphatidylcholine (DPPC) has been used to demonstrate adsorption; while the normal lining of surfactant in the human abdominal cavity has been confirmed by epifluorescence microscopy using Phosphin E as the hydrophobic probe. Aims: The overall aim is to confirm that peritoneal mesothelium has a lining of surfactant known for its lubricating and release properties, and that this lining can be enhanced by the adsorption of exogenous material. Results: Adsorption of DPPC to peritoneal mesothelium was 470 ng/cm 2 (n = 8) ex vivo and 598 ng/cm 2 (n = 18) in vivo, these rates being enhanced by EggPG by 62%ex vivo and 47%in vivo to reach the equivalent of almost three close-packed monolayers. Conclusions: These results can explain the reduction in surgical adhesions previously reported in animals by administering ALECÔ (7:3 DPPC:EggPG) as a highly surface-active dry powder, although it is now used in saline suspension to treat respiratory distress syndrome in newborns, in whom it has no side-effects. These findings would appear to justify clinical trials for dry ALECÔ in suppressing surgical adhesions with minimal risk of an adverse reaction. The results of these trials are also discussed and found to be compatible with the known ability of surfactant to resist physical adhesion by fibronectin, the tacky ,glue' by which fibroblasts attach to surfaces as the first step in formation of fibrinous adhesions. [source] 2261: Development and evaluation of PLGA nanoparticles with cyclosporine and the inclusion of HP,CD for ocular useACTA OPHTHALMOLOGICA, Issue 2010K HERMANS Ocular delivery of peptides requires new concepts in order to optimize the bioavailability and its therapeutic effect. The first peptide selected in present research project is Cyclosporine A (CyA) used in the treatment of the dry eye syndrome and against corneal graft rejection. The aim of the project is the development of nanoparticles with physicochemical properties for a suitable and prolonged release of CyA, using a factorial design. These drug delivery systems will be produced employing PLGA using the emulsification solvent evaporation method. Positively charged polymers as chitosan or Eudragit® will be incorporated to obtain nanoparticles with a positive particle charge. Electrostatic interactions with the negatively charged mucins lead to a prolonged residence time at the precorneal area. Nanoparticles will be evaluated on zeta potential, particle size and their in vitro drug release properties. CyA and CyA complexed with HP,CD will be compared. The most suitable preparations will be selected in a next phase of the project for an in vivo study using an animal model. [source] Synthesis of Magnetic, Up-Conversion Luminescent, and Mesoporous Core,Shell-Structured Nanocomposites as Drug CarriersADVANCED FUNCTIONAL MATERIALS, Issue 7 2010Shili Gai Abstract The synthesis (by a facile two-step sol,gel process), characterization, and application in controlled drug release is reported for monodisperse core,shell-structured Fe3O4@nSiO2@mSiO2@NaYF4: Yb3+, Er3+/Tm3+ nanocomposites with mesoporous, up-conversion luminescent, and magnetic properties. The nanocomposites show typical ordered mesoporous characteristics and a monodisperse spherical morphology with narrow size distribution (around 80,nm). In addition, they exhibit high magnetization (38.0,emu g,1, thus it is possible for drug targeting under a foreign magnetic field) and unique up-conversion emission (green for Yb3+/Er3+ and blue for Yb3+/Tm3+) under 980,nm laser excitation even after loading with drug molecules. Drug release tests suggest that the multifunctional nanocomposites have a controlled drug release property. Interestingly, the up-conversion emission intensity of the multifunctional carrier increases with the released amount of model drug, thus allowing the release process to be monitored and tracked by the change of photoluminescence intensity. This composite can act as a multifunctional drug carrier system, which can realize the targeting and monitoring of drugs simultaneously. [source]
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