• Korean Chemical Engineering Research
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• v.58 no.1
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• pp.36-43
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• 2020

A biliant stent was fabricated using a magnesium alloy wire, a biodegradable metal. In order to control the fast decomposition and corrosion of magnesium alloys in vivo, magnesium alloy wires were coated with biodegradable polymers such as polycaprolactone (PCL), poly(propylene carbonate) (PPC), poly (L-lactic acid) (PLLA), and poly (D, L-lactide-co-glycolide) (PLGA). In the case of PPC, which is a surface erosion polymer, there is no crack or peeling compared to other polymers (PCL, PLLA, and PLGA) that exhibit bulk erosion behavior. Also, the effect of biodegradable polymer coating on the axial force, which is the mechanical property of magnesium alloy stents, was investigated. Stents coated with most biodegradable polymers (PCL, PLLA, PLGA) increased axial forces compared to the uncoated stent, reducing the flexibility of the stent. However, the stent coated with PPC showed the axial force similar to uncoated stent, which did not reduce the flexibility. From the above results, PPC is considered to be the most efficient biodegradable polymer.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.511-520
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• 2000

Various bupivacaine-loaded microspheres were prepared from poly (d,l-lactide) (PLA) or poly (d,l-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. PLA and PLGA microspheres were prepared by w/o/w and w/o/o multiple emulsion solvent evaporation, respectively. The effects of process conditions such as emulsification speed, emulsifier type, emulsifier concentration and internal/external phase ratio on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency was higher in the microspheres prepared by w/o/o multiple emulsion than that by w/o/w multiple emulsion method, because the solubility of bupivacaine HCI was decreased in oil phase compared with water phase. The prepared microspheres had an average diameter between 1 and $2\;{\mu}M$ in all conditions of two methods. In morphology studies the PLA microspheres showed an irregular shape and smooth surface, but PLGA microspheres had a spherical shape and smooth surface. The release pattern of the drug from microspheres was evaluated on the basis of the burst effect and the extent of the release after 24h. The in vitro release of bupivacaine HCl from microspheres showed a large initial burst release and $60{\sim}80%$ release within one day in all conditions of two methods. The extents of the burst release against PLA and PLGA microspheres were $30{\sim}50%$ and $50{\sim}80%$ within 20min, respectively. This burst release seems to be due to the smaller size of microspheres and the solubility of drug in water.

• Archives of Pharmacal Research
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• v.29 no.8
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• pp.712-719
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• 2006

In this study, we prepared core-shell type nanoparticles of a poly(DL-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer with varying graft ratio of PLGA. The synthesis of the DexLG copolymer was confirmed by $^1H$ nuclear magnetic resonance (NMR) spectroscopy. The DexLG copolymer was able to form nanoparticles in water by self-aggregating process, and their particle size was around $50\;nm{\sim}300\;nm$ according to the graft ratio of PLGA. Morphological observations using a transmission electron microscope (TEM) showed that the nanoparticles of the DexLG copolymer have uniformly spherical shapes. From fluorescence probe study using pyrene as a hydrophobic probe, critical association concentration (CAC) values determined from the fluorescence excitation spectra were increased as increase of DS of PLGA. $^1H-NMR$ spectroscopy using $D_2O$ and DMSO approved that DexLG nanoparticles have core-shell structure, i.e. hydrophobic block PLGA consisted inner-core as a drug-incorporating domain and dextran consisted as a hydrated outershell. Drug release rate from DexLG nano-particles became faster in the presence of dextranase in spite of the release rate not being significantly changed at high graft ratio of PLGA. Core-shell type nanoparticles of DexLG copolymer can be used as a colonic drug carrier. In conclusion, size, morphology, and molecular structure of DexLG nanoparticles are available to consider as an oral drug targeting nanoparticles.

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.235.1-235.1
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• 2001

• Polymer(Korea)
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• v.26 no.1
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• pp.128-138
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• 2002

1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU, Carmustine)-loaded poly(D, L-lactide-co-glycolide) (PLGA, lactide/glycolide mole ratio 75 : 25) microparticles were prepared and fabricated into wafers in an attempt to study the possibility for the treatment of malignant glioma by direct inserting the wafers to the tumor or the cavity remained after surgical resection of the tumor. SEM observation of the microparticles prepared by spray drying method revealed that the microparticles were spherical, i. e. microspheres. Significant reduction of the crystallinity of BCNU encapsulated in PLGA was confirmed by X-ray diffraction and differential scanning calorimetry analyses of the BCNU-loaded PLGA microparticles. Release pattern of BCNU was dependent on several preparation parameters, such as the molecular weight and concentration of PLGA, and initial BCNU loading amount, etc. In vitro release of BCNU was prolonged over 8 weeks with close to zero-order release pattern after initial burst effect. Observations of morphological change of wafers and pH change of release media during release test period confirmed that hydration and degradation of PLGA would be facilitated with an increase of BCNU-loading amount.

• Biomedical Science Letters
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• v.12 no.3
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• pp.177-183
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• 2006

To demonstrate the effect of formulation conditions and evaluations of structural integrity from ovalbumin containing poly lactide glycolide copolymer (PLGA) microspheres for Vaccine delivery, OVA microspheres were prepared by a W/O/W multiple emulsion solvent extraction technique. Dichloromethan (DCM) and Ethyl acetate (EA) were applied as an organic phase and poly vinyl alcohol (PVA) as a secondary emulsion stabilizer. Microspheres were characterized for particle size, morphology (optical microscopy and Scanning Electron Microscope (SEM)). Protein denaturation was evaluated by size exclusion chromatography (SEC), SDS-PAGE and isoelectric focusing (IEF). Residual organic solvent was estimated by gas chromatography (GC) and differential scanning calorimetry (DSC). Optical photomicrograph and SEM revealed that micro spheres were typically spherical but various morphologies were observed. Mean particle size $(d_{vs})$ of microspheres were in the range of $3{\sim}50{\mu}m$. Also, The protein stability was not affected by the fonnulation process and residual organic solvent was beyond the detection below 0.1ppm. These results demonstrated that micro spheres might be a good candidate for the parenteral vaccine delivery system.

• Polymer(Korea)
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• v.32 no.3
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• pp.246-250
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• 2008

Colloidal stability of the biodegradable nanoparticle was characterized by measuring the variation of particle size with time using photon correlation spectroscopy. Three kinds of polymers, namely, poly(D,L-lactide-co-glycolide)(PLGA), PLGA/poly(L-lactide) blends, and PLGA/poly(L-lactide)-g-poly(ethylene glycol) blends were used as matrix material for nanoparticle preparation. Nanoparticles were prepared with or without using poly(vinyl alcohol)(PVA) as suspension stabilizer to evaluate the condition of preparation. Nanoparticles from the blend of amphiphilic graft copolymer with short poly(ethylene glycol) chain and PLGA maintained suspension for 1 day when protein stock solution was introduced. This is somewhat improvement in colloidal stability against protein adsorption compared with that of nanoparticles without PEG moiety. Suspension stabilizer, PVA, had a significant effect on the colloidal stability against freezing and protein adsorption which led to coagulation of nanoparticles. It is important to consider effect of suspension stabilizer as well as materials used to prepare nanoparticle on the colloidal stability.

• 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.

• Polymer(Korea)
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• v.28 no.4
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• pp.335-343
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• 2004

Carmustine (l,3-bis(2-chloroethyI)-1-nitrosourea, BICNU) used as antineoplastic drug for the treatment of brain tumor is not appropriate for the long term delivery, because it has short biological half life. Therefore, poly(D,L-lactide-co-glycolide) (PLGA) is useful as drug carrier for the long term delivery due to bulk erosion property. Glycolide monomer is applied to release of BICNU owing to non-toxic and monomeric components after biodegradation of PLGA. In this study, BICNU-loaded PLGA wafers with or without glycolide monomer were fabricated by conventional direct compression method for the sustained release of BICNU. These wafers were observed for their release profiles of BICNU and degradation rates by SEM, NMR, and GPC. Furthermore, we make multi-layer wafers and compare them with release profiles of conventional wafer. From these results, drug release of BICNU-loaded PLGA wafers was increased with increasing the glycolid monomer contents. We confirmed that glycolide monomer and BICNU contents in barrier-layer influenced the drug release profiles and degradation rate.

• Archives of Pharmacal Research
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• v.26 no.2
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• pp.173-181
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• 2003

A polymeric micelle drug delivery system was developed to enhance the solubility of poorly-water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The block copolymers consisting of poly(D,L-lactide) (PLA) as the hydrophobic segment and methoxy poly(ethylene glycol) (mPEG) as the hydrophilic segment were synthesized and characterized by NMR, DSC and MALDI-TOF mass spectroscopy. The size of the polymeric micelles measured by dynamic light scattering showed a narrow monodisperse size distribution with the average diameter less than 50 nm. The MW of mPEG-PLA, 3000 (MW of mPEG, 2 K; MW of PLA, 1K), and the presence of hydrophilic and hydrophobic segments on the polymeric micelles were confirmed by MALDI-TOF mass spectroscopy and NMR, respectively. Polymeric micelle solutions of DDB were prepared by three different methods, i.e. the matrix method, emulsion method and dialysis method. In the matrix method, DDB solubility was reached to 13.29 mg/mL. The mPEG-PLA 2K-1K micelle system was compared with the poloxamer 407 micelle system for their critical micelle concentration, micelle size, solubilizing capacity, stability in dilution and physical state. DDB loaded-polymeric micelles prepared by the matrix method showed a significantly increased aqueous solubility (＞5000 fold over intrinsic solubility) and were found to be superior to the poloxamer 407 micelles as a drug carrier.