• Macromolecular Research
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• 제11권5호
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• pp.334-340
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• 2003

In order to fabricate new sustained delivery device of nerve growth factor (NGF), we developed NGF-loaded biodegradable poly(L-lactide-co-glycolide) (PLGA, the mole ratio of lactide to glycolide 75:25, molecular weight: 83,000 and 43,000 g/mole, respectively) film by novel and simple sandwich solvent casting method for the possibility of the application of neural tissue engineering. PLGA was copolymerized by direct condensation reaction and the molecular weight was controlled by reaction time. Released behavior of NGF from NGF-loaded films was characterized by enzyme linked immunosorbent assay (ELISA) and degradation characteristics were observed by scanning electron microscopy (SEM) and gel permeation chromatography (GPC). The bioactivity of released NGF was identified using a rat pheochromocytoma (PC-12) cell based bioassay. The release of NGF from the NGF-loaded PLGA films was prolonged over 35 days with zero-order rate of 0.5-0.8 ng NGF/day without initial burst and could be controlled by the variations of molecular weight and NGF loading amount. After 7 days NGF released in phosphate buffered saline and PC-12 cell cultured on the NGF-loaded PLGA film for 3 days. The released NGF stimulated neurite sprouting in cultured PC-12 cells, that is to say, the remained NGF in the NGF/PLGA film at 37 $^{\circ}C$ for 7 days was still bioactive. This study suggested that NGF-loaded PLGA sandwich film is released the desired period in delivery system and useful neuronal growth culture as nerve contact guidance tube for the application of neural tissue engineering.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.115.2-116
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• 2001

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.213.2-214
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.234.2-234.2
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• 2001

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.235.1-235.1
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• 2001

• Journal of Pharmaceutical Investigation
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• 제40권4호
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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).

• 한국재료학회:학술대회논문집
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• 한국재료학회 2009년도 추계학술발표대회
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• pp.38.2-38.2
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• 2009

Regeration of natural tissuesor to create biological substitutes for defective or lost tissues and organs through the use of cells. In addition to cells and their porous, drugs are required to promote tissue regeneration. Therefore, the present studies were prepared using simvastatim loaded porous poly(lactide-co-glycolide) (PLGA) by double emulsion solvent evaporation water-in-oil-in-water technique (W/O/W) as drug delivery system strategies for injuring tissue. The resulting microspheres were evaluated for morphology, particle size, encapsulation efficiency, degradation of PLGA microspheres in vitro drug release and in vitro cell viability. Scanning electronic microscopic (SEM) showed that the porosities of the particles was changed by experimental conditions and cultured cells were attached well on porous microspheres surface. The X-ray diffraction (XRD) and differential scanning calometry (DSC) analysis indicate thatsimvastatim was highly dipersed in the microsphere at amorphousstate.

• Journal of Pharmaceutical Investigation
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• 제40권3호
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• pp.193-200
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• 2010

The objective of this study was to investigate the effects of sample preparation, HPLC conditions and peak measurement methods upon determining progesterone content of poly-d,l-lactide-co-glycolide microspheres. A series of the microspheres with different formulations was first prepared. To determine their actual drug contents, the microspheres were dissolved in tetrahydrofuran and diluted with various amounts of methanol to precipitate the polymer. After removal of polymeric precipitates, the filtrates were subject to HPLC analysis under versatile experimental conditions. Interestingly, the composition of a sample solution (e.g., the ratio of methanol to tetrahydrofuran) affected the magnitudes of both peak fronting and peak broadening of progesterone. Its peak became broader and more asymmetrical at lower methanol:tetrahydrofuran ratios. Furthermore, its peak height was influenced by the proportion of tetrahydrofuran in a sample solution. Such problems encountered with tetrahydrofuran were exacerbated when a larger volume of the sample solution was injected onto an analytical column. Under our experimental conditions a peak area measurement provided more accurate and reliable determination of progesterone content in various microspheres than a peak height determination. Optimizing the composition of a sample solution, HPLC chromatographic conditions and peak analysis methods was a prerequisite to an accurate determination of progesterone encapsulated within microspheres.

• Journal of Pharmaceutical Investigation
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• 제41권2호
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• pp.91-94
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• 2011

The purpose of this study was to investigate the effect of peptide charge on the interaction between peptide and poly(D,L-lactide-co-glycolide) (PLGA) for evaluating mechanism of acylated peptide formation in PLGA matrix. As a model peptide, octreotide, a synthetic somatostatin analogue and active ingredient of commercial PLGA product, was used. The disulfide group of octreotide was reduced with dithiothreitol and the sulfhydryl groups were modified with N-${\beta}$-maleimidopropionic acid (BMPA) to neutralize octreotide with positive charge in physiological conditions. The BMPA-conjugated octreotide was identified by measuring the molecular mass with liquid chromatography-mass spectrometry. In the interaction study with PLGA, native octreotide showed initial adsorption to PLGA and substantial production of acylated peptides (56% of overall peptide), whereas BMPA-conjugated octreotide showed minimal adsorption to PLGA and no acylation products for 42 days. Consequently, the neutralization of octreotide completely inhibited the peptide acylation by preventing interaction of peptide with PLGA. In conclusion, this study demonstrates that the initial polymer interaction of peptide is important step for peptide acylation in PLGA matrix and suggests the modulation of peptide charge as strategy for inhibiting the formation of acylated peptide impurities.

• Bulletin of the Korean Chemical Society
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• 제23권11호
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• pp.1579-1584
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• 2002

Since surfactant or emulsifiers remained on the nanoparticle surface significantly affect the physicochemical properties, the biodegradation rate, the biodistribution, and the biocompatibility of nanoparticles, surfactant-free nanoparticles should be good candidate. surfactant-free PLGA nanoparticles were successfully prepared by both the dialysis method and the solvent diffusion method. The PLGA nanoparticles prepared using the solvent diffusion method has a smaller particle size than the dialysis method. The solvent diffusion method was better for a higher loading efficiency than the dialysis method but the nanoparticle yield was lower. Testosterone (TST) release from the PLGA nanoparticles was dependent on the particle size rather than the drug contents. Testosterone release from the PLGA nanoparticles prepared by the solvent diffusion method using acetone was faster than those prepared by the dialysis method. TST release from the PLGA nanoparticles prepared by the solvent diffusion method using acetone and the dialysis method using dimethylformamide (DMF) was completed for 4 days while the PLGA nanoparticles prepared by the dialysis method using acetone showed approximately 80% TST release after 4 days. Since the PLGA nanoparticle degradation ratio was below 20% within 5 days at all samples while TST release completed within 4 days, TST release was dependent on the diffusion mechanism rather than degradation.