• Polymer(Korea)
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• v.32 no.2
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• pp.143-149
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• 2008

We synthesized PEG-PLA (or PLGA) amphiphilic di-block copolymers, which consist of PEG as biocompatible and hydrophilic block and PLA (or PLGA) as biodegradable and hydrophobic block, by ring opening polymerization of LA in the presence of methoxy PEG as a macroinitiator. The compositions and the molecular weights of the copolymers were controlled by changing the feed ratio of LA (and GA) to PEG initiator. The di-block copolymers could self-assemble in aqueous media to form micellar structure. A hydrophobic model drug, pioglitazone, was loaded into the polymer micelle using solid dispersion and dialysis methods, and the drug-loaded micelles were characterized by AFM, DLS and HPLC measurements. The drug loading capacity and in vitro release studies were performed and evaluated under various conditions. These results indicated that the amphiphilic di-block copolymers of PEG-PLA (or PLGA) could solubilize pioglitazone by solid dispersion method and the drug release was modulated according to micellar chemical compositions.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.13 no.11
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• pp.5595-5600
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• 2012

This paper is to review and study about the crystallization nucleating agent to improve the heat-resistance properties of poly(lactic acid). Four sub-micron sized nucleating agents, metallic salts of 2,2'-methylene bis(4,6-di-tert-butylphenol), were prepared and used as a crystallization nucleating agent. Thermal and mechanical properties of polymer compounds were investigated by DSC, HDT and UTM. As the results, While the heat-resistance properties of the polymer compound samples were increased linearly with the contents of nucleating agent as well as their smaller size. Among them, the highest heat-resistance property of compound was observed with 2 wt% of MPZ2. HDT values of PL98Z2 compound was $116^{\circ}C$ at 0.455Mpa.

• 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.

• Macromolecular Research
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• v.16 no.2
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• pp.139-148
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• 2008

Biodegradable and elastic poly(L-lactide-co-$\varepsilon$-caprolactone) (PLCL) was electrospun to prepare nanofibers, and N-isopropylacrylamide (NIPAAm) was then grafted onto their surfaces under aqueous conditions using $^{60}Co-{\gamma}$ irradiation. The graft yield increased with increasing irradiation dose from 5 to 10 kGy and the nanofibers showed a greater graft yield compared with the firms. SEM confirmed that the PLCL nanofibers maintained an interconnected pore structure after grafting with NIPAAm. However, overdoses of irradiation led to the excessive formation of homopolymer gels on the surface of thc PLCL nanofibers. The equilibrium swelling and deswelling ratio of the PNIPAAm-g-PLCL nanofibers (prepared with 10 kGy) was the highest among the samples, which was consistent with the graft yield results. The phase-separation characteristics of PNIPAAm in aqueous conditions conferred a unique temperature-responsive swelling behavior of PNIPAAm-g-PLCL nanofibers, showing the ability to absorb a large amount of water at < $32^{\circ}C$, and abrupt collapse when the temperature was increased to $40^{\circ}C$. In accordance with the temperature-dependent changes in swelling behavior, the release rate of indomethacin and FITC-BSA loaded in PNIPAAm-g-PLCL nanofibers by a diffusion-mediated process was regulated by the change in temperature. Both model drugs demonstrated greater release rate at $40^{\circ}C$ relative to that at $25^{\circ}C$. This approach of the temperature-controlled release of drugs from PNIPAAm-g-PLCL nanofibers using gamma-ray irradiation may be used to design drugs and protein delivery carriers in various biomedical applications.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1092-1096
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• 2005

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

• Macromolecular Research
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• v.8 no.2
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• pp.80-88
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• 2000

Biodegradable microspheres were prepared with poly(L-lactide-co-glycolide) (PLGA, 75 : 25 by mole ratio) by an oil/oil solvent evaporation method for the sustained release of anti-AIDS virus agent, AZT The microspheres of relatively narrow size distribution (7.6$\pm$ 3.8 ㎛) were obtained by controlling the fabrication conditions. The shape of microspheres prepared was smooth and spherical. The efficiency of AZT loading into the PLGA microsphere was over 93% compared to that below 15% for microspheres by a conventional water/oil/water method. The effects of Preparation conditions on the morphology and in vitro AZT release pattern were investigated. in vitro release studies showed that different release pattern and release rates could be achieved by simply modifying factors in the fabrication conditions such as the type and amount of surfactant, initial amount of loaded drug, the temperature of solvent evaporation, and so on. PLCA microspheres prepared by 5% of initial drug loading, 1.0% (w/w) of surfactant concentration, and 25$\^{C}$ of solvent evaporation temperature were free from initial burst effect and a near-zero order sustained release was observed. Possible mechanisms of the near-zero order sustained release for our system have been proposed.

• Membrane Journal
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• v.24 no.2
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• pp.113-122
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• 2014

Porous poly(L-lactic acid)(PLLA) scaffold membranes were prepared via. phase separation process. Chloroform, dichloromethane and 1,4-dioxane were used as solvent and, ethyl alcohol was used as non-solvent. Morphologies, mechanical properties and mass transfer characteristics of the scaffold membranes were investigated through SEM, stress-strain test and glucose diffusion test. The scaffold membranes obtained from the casting solutions with chloroform and with dichloromethane showed similar morphologies. They showed sponge-like porous structure with the pore size in the range of $3-10{\mu}m$ and, their porosities were in 50-80% range. Using 1,4-dioxane as solvent, nano-fibrous scaffold membranes with porosities over 80% were fabricated. When the polymer content in the solution with 1,4-dioxane was lowered to 4%, highly porous, macroporous and nano-fibrous scaffold membranes were obtained. The size of the macropore was tens of the microns and the porosity was around 90%. These results indicate that the solvent has significant effect on the scaffold membrane structure and, that scaffold membranes with various structures can be fabricated through phase separation method by choosing solvent and by controlling polymer concentration in the casting solution.

• Membrane Journal
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• v.25 no.1
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• pp.48-59
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• 2015

This paper reports a fabrication of poly(L-lactic acid) (PLLA) scaffold membranes through phase separation process using pure and mixed solvents. Chloroform and 1,4-dioxane were used as pure solvents and mixed solvents were obtained by mixing the pure solvents together. Morphologies, mechanical properties and mass transfer characteristics of the scaffold membranes were investigated through SEM, stress-strain test and glucose diffusion test. Scaffold membranes from the solution with pure chloroform showed solid-wall pore structure. In contrast, nano-fibrous membranes were fabricated from the solution with pure 1,4-dioxane. In case of mixed solvents, the scaffold membranes showed various structures with changing composition of the solvents. When 1,4-dioxane content was lower than 20 wt% in the solvent, scaffold membrane showed solid-wall pore structure. When the content was 20 wt%, scaffold membranes with macropores with the maximum size of $100{\mu}m$ was obtained. In the concentration range of 1,4-dioxane over 25 wt%, the scaffold membranes showed nano-fibrous structures. In this range, the fibers showed different diameters with changing composition of the solvent. The minimum fiber diameter was about $15{\mu}m$, when 1,4-dioxane composition was 80 wt%. These results indicate that the composition of the solvent showed a significant effect on the structure of scaffold membrane.

• Polymer(Korea)
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• v.39 no.1
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• pp.40-45
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• 2015

Simple poor-cosolvent casting was used to surface treat biodegradable elastic poly(L-lactide-co-${\varepsilon}$-caprolactone) (PLCL; 50:50) copolymer films that presented lotus-leaf-like structures. We evaluated whether the lotus-leaflike-structured PLCL (L-PLCL) films could be used as a biomaterial for artificial vascular grafts. The surface morphology, hydrophobicity, and antithrombotic efficiency of the films were examined while immersed in platelet-rich plasma (PRP) using scanning electron microscopy (SEM) and a contact angle meter. The recovery and crystallinity of the films were measured using a tensile-strength testing machine and an X-ray diffractometer, respectively. The solvent containing acetic acid, as a poor co-solvent, and methylene chloride mixed in a 1:2 ratio produced an optimal PLCL film with a water contact angle of approximately $124^{\circ}$. Furthermore, the surface of the L-PLCL films immersed in PRP showed a lower rate of platelet adhesion (<10%) than that of the surface of an untreated PLCL film immersed in PRP.

• Polymer(Korea)
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• v.24 no.4
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• pp.505-512
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• 2000

The mixture density data for poly(lactide-co-glycolide) [PLGA] with supercritical $CO_2$, CHF$_3$ and CHClF$_2$ were obtained in the temperature range of 27 to 10$0^{\circ}C$ and at pressures as high as 3000 bar (PLGA$_{x}$, Where the molar concentration of glycolide in the backbone, x, range from 0 to 50 mol%). The PLA-$CO_2$, PLA-CHF$_3$, and PLA-CHClF$_2$ systems dissolve in the pressure less than 1430 below 700, and below 100 bar, respectively. The mixture density shows from 1.084 to 1.334 g/cm$^3$ at temperatures from 27 to 93$^{\circ}C$. The PLGA$_{15}$ -$CO_2$ mixture dissolves at pressures of below 1900 bar and the mixture density is in the range of 1.158 to 1.247 g/cm$^3$ at temperatures between 37 and 92$^{\circ}C$. The solubilities of the PLGA$_{25}$ for $CO_2$, CHF$_3$, and CHClF$_2$ are shown to pressure as high as 2390, 1470, and 118 bar, respectively, and the mixture density exhibits iron 1.154 to 1.535 g/cm$^3$ at temperatures from 29 to 81$^{\circ}C$. The PLGA$_{50}$-$CO_2$ system does not dissolve at 24$0^{\circ}C$ and 3000 bar while the PLGA$_{50}$-CHCIF$_2$ does easily at 5$0^{\circ}C$ and 100 bar. The mixture density for the PLGA-CHClF$_2$ system increases even at low pressures as the glycolide molar concentration increases.es.es.