Among different forms of plgabased drug delivery systems, microspheres or microparticles are the most common. Particles can be used as carriers by attaching drug or biologicalchemical entities to particle surface. Us6855331b2 us10165,975 us16597502a us6855331b2 us 6855331 b2 us6855331 b2 us 6855331b2 us 16597502 a us16597502 a us 16597502a us 6855331 b2 us6855331 b2 us 6855331b2 authority us united states prior art keywords taxol release paclitaxel hydrophobic microspheres prior art date 19940516 legal status the legal status is an assumption and is not a legal conclusion. Sem images of plga microspheres covered with ho8910 cells.
The wet microspheres obtained were collected by centrifugation followed by filtration and lyophillization 2,3,4,5. Studies of plga microspheres pharmaceutical technology. Preparation and in vitroin vivo evaluation of insulin. During some research on plga microspheres we found this interesting article published in european cells and materials vol 7 suppl 2. University of groningen protein delivery from polymeric. Microspheres are manufactured in both solid and hollow. Nalmefene was blended with poly lactidecoglycolide.
Novel preparation method for sustainedrelease plga microspheres using waterinoilinhydrophilicoilinwater emulsion xiaoyun hong,1,2, liangming wei,3, liuqing ma,2 yinghui chen,4 zhenguo liu,1. The loading efficiency, the encapsulation efficiency, and the release profile of the bsaloaded plga microspheres were measured and studied. In this study, porous plga microspheres were fabricated by an emulsionsolvent. A study of the microspheres stability at refrigerated temperatures is also examined. Plga microspheres loaded with kslw were prepared by using the doubleemulsification solvent evaporation method wow 1820, with plga 50.
In this article, the authors describe a study into the factorial effect of selected process parameters on the pharmaceutical characteristics of polydllactidecoglycolide microspheres containing methotrexate. Typically, drugloaded polymeric microspheres are prepared by oilinwater emulsification which yields a product with. The release characteristics of different model drugs from. Chapter 3 in combination with small sugars combine excellent stabilizing properties. Polylacticcoglycolic acid plga particles often serve as a biodegradable and biocompatible platform for drug delivery 1. Polymeric microspheres have gained widespread application as drug eluting depots. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Pdf plga microspheres containing minocycline as drug. Nov 25, 2014 polyd,llactidecoglycolide plga microspheres were prepared by emulsion solvent evaporation method. We offer degradex plga microspheres and nanoparticles from 100 nm to 50.
The aim of the present study was to investigate the morphology and function of a drug eluting metallic porous surface produced by the immobilization of poly lactidecoglycolide. Microspheres are manufactured in both solid and hollow form. Development of plga microspherepva hydrogel composite. Release of a woundhealing agent from plga microspheres in. The drug encapsulating efficiency of spllaibumicrospheres is high and release of ibuprofen. Protein encapsulation into plga nanoparticles by a novel phase separation method. Composite plga microspheres containing exenatideencapsulated lecithin nanoparticles exnpsplgams were obtained by initial fabrication. Pdf preparation of openclosed pores of plgamicrosphere for. The microspheres containing the sbm7462 peptide were prepared using the biodegradable plga copolymer 50. Implantable hydrogel beads entrapping plgapaclitaxel. In vitro and in vivo evaluations of plga microspheres. Jun 28, 2016 polylacticcoglycolic acid plga is the most widely used biomaterial for microencapsulation and prolonged delivery of therapeutic drugs, proteins and antigens. It was shown that the microspheres from double emulsion. Microspheres are made from polymeric, waxy or protective materials that is biodegradable synthetic polymers and modified natural products.
First, 1 ml of drug or water was dispersed in 5 ml of different concentrations of plga, pla, and dichloromethane solutions by stirring at a rotation speed of 2500 rpm for one minute using a homogenizer fa25, fluko, shanghai, peoples republic of china. Polylacticcoglycolic acid plga is the most widely used biomaterial for. We offer a full range of degradex plga microspheres and plga nanoparticles that are ideal for a variety of applications poly d,llactidecoglycolide or plga microspheres and nanoparticles are known to possess a unique ability to enable drug release in a controlled manner. Sem was used to determine the size of the microspheres by measuring the diameter of 50 microspheres in an sem. Two sustained release formulations, one incorporating 20% brij 98 and the other incorporating 3% mgco 3 in the oil phase. Polymer and microsphere blending to alter the release of a. Stability studies suggested that the microspheres we prepared had a very good stability. A fundamental understanding of the in vivo biodegradation phenomenon as well as an appreciation of cellular and tissue responses which determine the biocompatibility of biodegradable pla and plga microspheres are important components in the design and development of biodegradable microspheres containing bioactive agents for therapeutic application. Hollow microspheres are used as additives to lower the density of a material. Specific grade of polyethylene used in manufacturing of these microspheres is fdaapproved for food applications in chewing gum. Several publications describe alternative plga formulations for the controlled release of risperidone. Moreover, plga microspheres can be injected directly into the action site, where the sirna can be released in controlled manner, thus avoiding the need of frequent invasive administrations. Bioerodable plgabased microparticles for producing.
Bharadia, vikram pandya and darshan modi department of pharmaceutics, b. By default, the surfaces of plga microspheres are slightly negatively charged. Typically, drugloaded polymeric microspheres are prepared by oilinwater emulsification which yields a product with a broad size distribution. Novel preparation method for sustainedrelease plga microspheres using waterinoilinhydrophilicoilinwater emulsion xiaoyun hong,1,2, liangming wei,3, liuqing ma,2 yinghui chen,4 zhenguo liu,1 weien yuan2, 1department of neurology, xinhua hospital affiliated to shanghai jiaotong university, school of medicine, shanghai, peoples republic of china. The microspheres containing minocycline were prepared by the wow double.
Prepared using solvent evaporation methodibu could combine with splla well and part of plla were degraded after releasing. The aim of this study was to design and evaluate biodegradable plga microspheres for sustained delivery of risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Plga has excellent biodegradability and biocompatibility and is generally recognized as safe by international regulatory agencies including the united states food and drug administration and the european medicines agency. Fabrication of alginate beads entrapping plgapaclitaxel microspheres by electrospray. Polylacticcoglycolic acid plga is the most widely used biomaterial for microencapsulation and prolonged delivery of therapeutic drugs, proteins and antigens. The present disclosure provides, inter alia, formulation compositions comprising modified nucleic acid molecules which may encode a protein, a protein precursor, or a partially or fully processed form of the. The particle size of different lipid and plga hybrid mp was between 10 and 25. Use of biodegradable plga microspheres as a slow release. The aim of this study was to design and evaluate biodegradable plga microspheres for sustained delivery of risperidone, with an eventual goal of avoiding combination therapy for the treatment of. Magnetic microspheres18 this kind of delivery system is very much important which localizes the drug to the disease site.
Novel preparation method for sustainedrelease plga. Mar 22, 2012 spllaibuprofin microspheres 2010these are star shaped polyl lactideloaded ibuprofen spllaibu microspheres. Pdf biodegradation and biocompatibility of pla and plga. Plga microspheres are widely studied for controlled release drug delivery applications, and many models have been proposed to describe plga degradation and erosion and drug release from the bulk. Prepared using solvent evaporation methodibu could combine. The results showed that addition of porogen or surfactants to the inner aqueous phase, types of organic solvents and polymer concentration affected greatly the. The encapsulation efficiency and in vitro release profiles of different drugs with various water solubilities from medicated plga microspheres were investigated. Recent research and development of plgapla microspheres. Solid biodegradable microspheres incorporating a drug dispersed or dissolved throughout particle matrix have the potential for controlled release of the drug.
Preparation of polylactidecoglycolide microspheres and. The effect of addition of mgco 3, drug loading, and polymer blending on the release of fenretinide from plga microspheres was also investigated and observed to enhance the drug release. Poly lacticcoglycolic acid controlled release systems ncbi nih. The microspheres containing minocycline were prepared by the wow. The size of mp showed gaus distribution and 90% of the particles d0. Polyacryloyl hydroxyethyl starch plga composite microspheres ge jiang, 1wei qiu, and patrick p. Polyurethene, ureaformaldehyde, pmma, polystyrene 10 15 20 ncy % 0. Physicochemical characterization and pharmacokinetics of agomelatineloaded plga microspheres for intramuscular injection.
The release profile from the microspheres depends on the nature of the polymer used in the preparation as well as on the nature of the active drug. European journal of pharmaceutics and biopharmaceutics. For example, unpigmented or clear polyethylene microspheres supplied by cospheric in sizes from 10 micron to micron meet the quality requirements of the us fda as specified in 21 cfr 172. In an in vitro study of drug release, it can be concluded that the bdmc plga ms exhibited sustained and longterm release properties for 96 h. Preparation of plga microspheres with different porous.
Us6855331b2 sustained release hydrophobic bioactive plga. Plga microspheres are widely studied for controlled release drug delivery applications, and many models have been proposed to describe plga degradation and erosion and drug release from the bulk polymer. Aug 11, 2009 the aim of the present study was to investigate the morphology and function of a drug eluting metallic porous surface produced by the immobilization of poly lactidecoglycolide microspheres bearing dexamethasone onto plasma electrolytically oxidized ti6al7nb medical alloy. Plga particles are used for controlled release, sustained release and targeted drug delivery. The aim of the present study was to investigate the properties of different sizefractions of drugloaded microspheres, in order to delineate whether particle size. Three formulations having different organic to water ratio of the primary emulsion were prepared. Solid biodegradable microspheres incorporating a drug. Plga containing solvent acetone and the antisolvent water form an azeotropic mixture. Strategies for increasing drug loading in plgamicrospheres include modification of the classical solvent evaporation methods, preparation of multilayered microparticles, and development of novel methods for microparticle fabrication including hydrogel templates, coaxial electrospray, microfluidics, and scco 2. Design of controlled release plga microspheres for. In this article, the authors describe a study into the factorial effect of selected process parameters on the pharmaceutical characteristics of polydl.
However, commonly, the presence of lag times, sigmoidal release curves, and rather short release. Plga microspheres flexion therapeutics for musculoskeletal conditions. The formulation composition may further include a modified nucleic acid molecule and a delivery agent. Sem was used to determine the size of the microspheres by measuring the diameter of 50 microspheres in an sem picture and then taking an average value. Injectable and porous plga microspheres that form highly. To make our standard degradex plga nanospheres and microspheres, we use polyd,llactidecoglycolide with a lactic acid. Microencapsulation of inorganic nanocrystals into plga. Preparation of uniformsized pla microcapsules by combining shirasu porous glass membrane. The size of the plga microspheres was also measured by a bi240 laser scattering particle sizer brookhaven. Pla microcapsules by combining shirasu porous glass membrane. Among different forms of plga based drug delivery systems, microspheres or microparticles are the most common. The influences of inner aqueous phase, organic solvent, plga concentration on. Development of composite plga microspheres containing. Autocatalysis is known to have a complex role in the dynamics of plga erosion and drug transport and can lead.
The purpose of this study was to develop and evaluate a novel composite microsphere delivery system composed of polyd,l. The wet microspheres were then stirred at rpm for 2 hrs at 28c to permit evaporation of dcm and solidification of microspheres. Gastroretentive floating microspheres are lowdensity systems that have. This work focuses on the development of poly lacticcoglycolic acid plga microspherepolyvinyl alcohol pva hydrogel composite coatings to permit longterm glucose sensor. The release of drug from both biodegradable as well as nonbiodegradable microspheres is influenced by structure or micromorphology of the carrier and the properties of the polymer itself. It was shown that the microspheres from double emulsion had smaller particle sizes 350 m, a less porous structure, a poor loading efficiency 5. First, 1 ml of drug or water was dispersed in 5 ml of different concentrations of plga, pla, and dichloromethane solutions by stirring. Pharmaceutics free fulltext risperidoneloaded plga. Lipid and plga hybrid microparticles as carriers for. Biodegradation and biocompatibility of pla and plga. Polyd,llactidecoglycolide plga microspheres were prepared by emulsion solvent evaporation method. They are approved by the us food and drug administration fda to be used as drug delivery system in humans. Plain plga particles for testing system compatibility in drug delivery research. The present disclosure provides, inter alia, formulation compositions comprising modified nucleic acid molecules which may encode a protein, a protein precursor, or a partially or fully processed form of the protein or a protein precursor.
Pdf polyd,llacticcoglycolic acid has been extensively used as a controlled release carrier for drug. Effect of particle size on drug loading and release. However, monolithic or singlewalled plga microspheres and. The dolomite centre ltd continuous microfluidic synthesis. Plain degradex plga microspheres product data sheet. Plga micronanoparticles that combine plga particles with the beneficial. A longacting preparation may address these limitations. Pdf polyd,llacticcoglycolic acid plgapoly lactic acid pla. Porous plga microspheres effectively loaded with bsa. A fundamental understanding of the in vivo biodegradation phenomenon as well as an appreciation of cellular and tissue responses which determine the biocompatibility of biodegradable pla and plga. Plga itself is a moderate substrate for cell adhesion, and it was expected that presence of hydrophobic plga microspheres inside the scaffold may play a critical role in early phase of cell adhesion because.
Process for preparation of microcapsules and microspheres 67. Preparation of proteinloaded microspheres using the woo h w method. Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. The influences of inner aqueous phase, organic solvent, plga concentration on the morphology of microspheres were studied. Fabrication and characterization of controlled release. The plga particle formation takes place spontaneously at the nucleation spots that are distributed randomly. Plga microspheres were sieved by a 100mesh sieve before the millirod fabrication. Injectable and porous plga microspheres that form highly porous scaffolds at body temperature omar qutachia, jolanda r.