• Polymer(Korea)
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• v.31 no.1
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• pp.20-24
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• 2007

The preservation of biological activity of protein drugs in formulation is still a major challenge for successful drug delivery. Lipase was encapsulated in poly (D,L-lactide- co-glycolide) PLGA nano-particles using a w/o/w solvent evaporation technique. The lipase-containing PLGA/poly (vinyl alcohol) (PVA) nanoparticles were characterized with regard to morphology, size, size distribution, lipase-loading efficiency, in vitro lipase release, and stability of lipase activity. The size of nanoparticles increased as polymer concentration was increased. The size of particles was not significantly affected by the PVA concentration; on the other hand, the particle size distribution was the narrowest when 4% of PVA was used. In optimum conditions, we possessed nanoparticles that characterized 72.5% of encapsulation efficiency, $198.3{\pm}13.8 nm$ size diameter. During the initial burst phase, the in vitro release rate was very fast, reaching 83% within 12 days. Until days 6, enzyme activity increased as the amount of lipase released was increased.

• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.191-196
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• 2001

Biodegradable polymeric microspheres were studied for their usefulness as carriers for the delivery of vaccine antigens. However, protein antigen could be denatured during microencapsulation processes due to the exposure to the organic phase and stress condition of cavitation and shear force. Therefore this study was carried out to re-evaluate the degree of protein denaturation during microencapsulation with poly(lactide-co-glycolide) (PLGA) copolymer. PLGA microspheres containing ovalbumin (OVA), prepared by W/O/W multiple emulsification method, were suspended in pH 7.4 PBS and incubated with shaking at $37.5^{\circ}C$. Drug released medium was collected periodically and analyzed for protein contents by micro-BCA protein assay. In order to evaluate the protein integrity, release medium was subjected to the analyses of SDS-PAGE and size exclusion chromatography (SEC). And enzyme-linked immunosorbent assay (ELISA) was introduced to measure the immunoreactivity of entrapped OVA and to get an insight into the three-dimensional structure of epitope. The structures of entrapped protein were not affected significantly by the results of SDS-PAGE and SEC. However, immunoreactivity of released antigen was varied, revealing the possibility of protein denaturation in some microspheres when it was evaluate by ELISA method. Therefore, in order to express the degree of protein denaturation, antigenicity ratio (AR) was obtained as follows: amount of immunoreactivity of OVA/total amount of OVA released ${\times}100(%)$. ELISA method was an efficient tool to detect a protein denaturation during microencapsulation and the comparison of AR values resulted in more accurate evaluation for immunoreactivity of entrapped protein.

• Journal of Periodontal and Implant Science
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• v.31 no.1
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• pp.91-109
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• 2001

The purpose of this study is to evaluate histologically the resorption and tissue response of various resorbale membranes used for guided tissue regneration procedures, using a subcutaneous model on the dorsal surface of the rat. In this study, 12 Sprague-Dawley male rats(mean BW 150gm) were used and the commercially available materials included dense collagen membrane, freeze-dried bovine dura mater loos collagen membrane, PLA/PLGA membrane. Animals were sacrificed at 3, 6 and 8 weeks after implantation of various resorbable membranes. Specimens were prepared with Hematoxylin-Eosin stain for light microscopic evaluation. The results of this study were as follows: 1. Resorption : Loose collagen membrane group was resorbed most rapidly. Dense collagen membrane group and freeze-dried bovine dura mater group were rarely resorbed. 2. Inflammatory reactions : PLA/PLGA membrane group showed persistent and severe inflammatory reactions for 3 to 8 weeks. Moderate inflammatory reactions and the ectopic formation of calcified material were observed in dense collagen membrane group. Freeze-dried bovine dura mater group and loose collagen membrane group showed mild inflammatory reactions 3. In PLA/PLGA membrane group, multinucleated giant cells by foreign body reactions were observed. In conclusion, the resorption of freeze-dried bovine dura mater didn't happen for 3-6weeks, which showed the best bio-compatibility. Therefore, freeze-dried bovine dura mater was considered proper resorbable membrane for guided tissue regeneration.

• Journal of the Korean Society for Precision Engineering
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• v.26 no.1
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• pp.146-154
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• 2009

In recent tissue engineering field, it is being reported that the fabrication of 3D scaffolds having high porous and controlled internal/external architectures can give potential contributions in cell adhesion, proliferation and differentiation. To fabricate these scaffolds, various solid free-form fabrication technologies are being applied. The solid free-form fabrication technology has made it possible to fabricate solid free-form 3D microstructures in layer-by-layer manner. In this research, we developed a multi-head deposition system (MHDS) and used design of experiment (DOE) to fabricate 3D scaffold having an optimized internal/external shape, Through the organization of experimental approach using DOE, the fabrication process of scaffold, which is composed of blended poly-caprolactone (PCL), poly-lactic-co-glycolic acid (PLGA) and tricalcium phosphate (TCP), is established to get uniform line width, line height and porosity efficiently Moreover, the feasibility of application to the tissue engineering of MHDS is demonstrated by human bone marrow stromal cells (hBMSCs) proliferation test.

• Polymer(Korea)
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• v.24 no.6
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• pp.802-809
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• 2000

Counterion-specific helix formation and ion-selective transport of alkali metal chlorides (LiCl, NaCl, KCl, CsCl) were investigated for a poly(L-glutamic acid)(PLGA)/poly (vinyl alcohol)(PVA) blend membrane immersed in aqueous ethanol. The counterion specificity for helix formation of PLG alkali metal salts in the membrane was Li>Na>K>Cs. This specificity is ascribed to a contact ion-pair formation between the PLG carboxyl anion and the bound counterion, which depends on the energy balance between the electrostatic interaction and the desolvation. In aqueous ethanol, an appreciable ion-selectivity was observed for the permeability coefficient, i.e. Li$^{+}{\cdot}$Cl$^{-}$) formation between counterion and coion, and the latter to a specific interaction of diffusing counterions with polymer charges.

• Journal of Pharmaceutical Investigation
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• v.40 no.4
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• pp.231-236
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• 2010

This study was to fabricate the porous poly(lactide-co-glycolide) (PLGA) microparticles with anthocyanin (as a model antioxidant) for pulmonary drug delivery. The highly porous PLGA microparticles were prepared by the waterin-oil-in-water ($W_1/O/W_2$) multi-emulsion method, followed by the decomposition of ammonium bicarbonate (AB) in $W_1$ phase to the base of ammonia, carbon dioxide and water vapor at $50^{\circ}C$, making a porous structure in PLGA microparticles. Herein, hyaluronate (HA), a viscous polysaccharide, was incorporated in the porous microparticles for sustained anthocyanin release. In in vitro release studies, the anthocyanin release from the porous microparticles with HA continued up to 24 hours, while the porous microparticles without HA released 80 wt.% of encapsulated anthocyanin within 2 hours. In addition, these microparticle are expected to be effectively deposited at a lung epithelium due to its high porosity (low density) and avoid alveolar macrophage's uptake in the lung due to its large particle size. We believe that this system has a great pharmaceutical potential as a long acting antioxidant for relieving the oxidative stress in chronic obstructive pulmonary disease (COPD).

• Clean Technology
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• v.12 no.2
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• pp.53-61
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• 2006

A PGSS (Particles from Gas Saturated Solutions) process designed to generate nano-particles using supercritical fluids has been conducted for the fabrication of Poly(lactide-co-glycolide) (PLGA) microparticles that encapsulate a protein drug. It is demonstrated that the polymer and the dry powder of a protein can be mixed under supercritical carbon dioxide conditions and that the protein component retains its biological activity. In this experiment, the mixture of polymer which is plasticized and dry powder protein was sprayed to form solid polymer that encapsulate the protein. It is found that supercritical fluid process give fine tuning of particle size and particle size distribution by simple manipulations of the process parameters. Porous particles were formed with irregular shape. Protein encapsulated in the polymer was found to have enzymatic activity without significant loss of its initial value.

• Polymer(Korea)
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• v.34 no.3
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• pp.274-281
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• 2010

In this study, PEG-PLA(or PLGA) amphiphilic di-block copolymers were synthesized by ring opening polymerization of D,L-lactide(or glycolide) and applied to polymeric micelle system for solubilization of a rosiglitazone as diabetes drug. The drug could be efficiently loaded into the polymer micelle by solid dispersion technique, and the drug-loaded micelles were characterized and evaluated as a drug delivery carrier by fluorescence spectrometer, DSC, and DLS measurements. The colloidal stability of drug loaded micelles in aqueous media could be enhanced by addition of 2-hydroxy-N-picolylnitinamide as a hydrotropic agent. The polymer micelles also showed biocompatible and nontoxic properties in vitro cell viability using MTT assay, and the drug loaded micelles were observed to be more effective than free drug for decreasing glucose in blood of rats.

• Polymer(Korea)
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• v.34 no.2
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• pp.178-183
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• 2010

Medical metal stents inserted to patients with a cardiovascular disease associated with coronary artery system have relatively increased the survival rate. The development of new stents is, however, urgently required due to restenosis and late thrombosis generated in metal stents. To solve these problems, the biodegradable polymers such as poly(lactide-co-glycolide) (PLGA), poly(L-lactide)(PLLA), and poly ($\varepsilon$-caprolactone)(PCL) were mixed with alpha lipoic acid (ALA), which is well known to inhibit the proliferation of neointimal hyperplasia. Subsequently, the ALA-loaded polymers were coated on stainless steel by electrospray. The drug-eluting behaviors from the coated polymers were investigated according to kinds and concentrations of polymers, spray rates, and kinds of solvents. The drug-eluting rate from PCL with the lowest glass transition temperature was the fastest among three polymers and followed by PLGA and PLLA. The surface roughness increased as the spray rate was increased and also the drug-eluting rate was affected by kinds of solvents with different boiling point. It is expected that drug-eluting stent (DES) coated with ALA-loaded polymers can be applied practically for clinical applications by controlling the behavior of drug release.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.20
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• pp.8693-8698
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• 2014

Background: Up-regulation of hsp90 gene expression occurs in numerous cancers such as lung cancer. D,L-lactic-co-glycolic acid-poly ethylene glycol-17-dimethylaminoethylamino-17-demethoxy geldanamycin (PLGA-PEG-17DMAG) complexes and free 17-DMAG may inhibit the expression. The purpose of this study was to examine whether nanocapsulating 17DMAG improves the anti cancer effect over free 17DMAG in the A549 lung cancer cell line. Materials and Methods: Cells were grown in RPMI 1640 supplemented with 10% FBS. Capsulation of 17DMAG is conducted through double emulsion, then the amount of loaded drug was calculated. Other properties of this copolymer were characterized by Fourier transform infrared spectroscopy and H nuclear magnetic resonance spectroscopy. Assessment of drug cytotoxicity on the grown of lung cancer cell line was carried out through MTT assay. After treatment, RNA was extracted and cDNA was synthesized. In order to assess the amount of hsp90 gene expression, real-time PCR was performed. Results: In regard to the amount of the drug load, IC50 was significant decreased in nanocapsulated(NC) 17DMAG in comparison with free 17DMAG. This was confirmed through decrease of HSP90 gene expression by real-time PCR. Conclusions: The results demonstrated that PLGA-PEG-17DMAG complexes can be more effective than free 17DMAG in down-regulating of hsp90 expression by enhancing uptake by cells. Therefore, PLGA-PEG could be a superior carrier for this kind of hydrophobic agent.