• Title/Summary/Keyword: lactide

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Effect of Hydrophilic Polymers on the Release of BCNU from BCNU-loaded PLGA Wafer (친수성 고분자가 BCNU 함유 PLGA 웨이퍼로부터 BCNU의 방출에 미치는 효과)

  • 안태군;강희정;문대식;이진수;성하수
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.670-679
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    • 2002
  • 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine) is one of the effective chemotherapeutic agents which has been used clinically for treating malignant glioma. Poly(D,L-lactide-co-glycolide) (PLGA, molecular weight: 20000 g/mole. mole ratio of lactide to glycolide 75 : 15) is a well known biodegradable polymer used as a drug carrier for drug delivery system. In this study, we investigated the BCNU release behaviour of BCNU-loaded PLGA wafers containing poly (N-vinylpyrrolidone) (PVP) or polyethyleneoxide (PEO) and the effect of hydrophilic polymers incoporated in the wafers. BCNU-loaded PLGA microparticles with or without hydrophilic polymers were prepared by a spray drying method and fabricated into wafers by direct compression. Encapsulation efficiency of BCNU-loaded PLGA microparticles containing PVP and PEO was 85 ∼ 97% and crystallinity of BCNU encapsulated in PLGA decreased significantly initial release amount and release rate of BCNU increased with the increasing PVP or PEO amount. Morphological change and mass loss of wafers during the release test were confirmed that hydration and degradation of PLGA would be facilitated with an increase of hydrophilic polymers.

Surface Modification of Poly(L-lactide-co-ε-caprolactone) Nanofibers by Electron-beam Irradiation (전자선 조사 방법을 통한 생분해성고분자의 표면개질 특성 평가)

  • Kim, Woo-Jin;Shin, Young Min;Park, Jong-Seok;Gwon, Hui-Jeong;Nho, Young-Chang;Lim, Youn-Mook
    • Journal of Radiation Industry
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    • v.5 no.4
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    • pp.365-370
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    • 2011
  • Electrospun nanofibers prepared with synthetic biodegradable polymer have some limitations in regulating adhesion, proliferation, and spreading of cells because of their surface hydrophobicity and absence of cell-interaction. In this study, we functionalized the electrospun poly(L-lactide-co-${\varepsilon}$-caprolactone) (PLCL) nanofibers with acrylic acid (AAc) to modulate their surface hydrophilicity using electron-beam irradiation method and then measured grafting ratio of AAc, water contact angle, and ATR-FTIR of AAc-grafted nanofibers. A grafting ratio of AAc on the nanofibers was increased as irradiation dose and AAc concentration were increased. AAc-grafted nanofibers also have higher wettability than non-modified nanofibers. In conclusion, those surface-modified nanofibers may be an essential candidate to regulate cell attachment in tissue engineering applications.

Poly(DL-Lactide-co-Glycolide) Nanoparticles Used PEG-PPG Diblock Copolymer by Surfactant: Preparation and Loading of Water Insoluble Drug (유화제로서 PEG-PPG 블록 공중합체를 이용한 Poly(DL-Lactide-co-Glycolide) 나노입자: 제조 및 지용성 약물의 로딩)

  • Taek Kyu Jung;Sung Soo Kim;Byung Cheol Shin
    • Journal of the Korean Chemical Society
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    • v.47 no.5
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    • pp.479-486
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    • 2003
  • In this study, poly(DL-lactide-co-glycolide) nanoparticles loaded with water-insoluble vitamins such as vitamin A (Retinol) and vitamin E acetate were prepared by the emulsification diffusion method. Polymer solution was prepared by the two water-miscible organic solvent, such as ethanol and acetone. Because of its biocompatible property, polyethyleneglycol-polypropyleneglycol diblock copolymer was used as surfactant and stabilizer. The influence of some preparative variables on the nanoparticle formation and on the loading efficiency of active agents, such as the type and concentration of stabilizing agent, the stirring methods, the water/oil phase ratio and the polymer concentration were investigated in order to control and optimize the process. After preparation of nanoparticles loaded with active agent, particle size and distribution were evaluated by the light scattering particle analyzer. The loading efficiency of active agents was evaluated by the UV-visible spectroscopy. As the results, particle size were 50-200 nm and dispersibility was monodisperse. The optimum loading efficiency of active agents was observed 50-60%. It was found that the appropriate of selections of binary solvent mixtures and polymeric concentrations in both organic and aqueous phases could provide good yield and favorable physical properties of PLGA nanoparticles.

Preparation and Characterization of PEG-PLA(PLGA) Micelles for Solubilization of Rosiglitazone (Rosiglitazone 가용화를 위한 PEG-PLA(PLGA) 고분자 미셀의 제조 및 특성분석)

  • Kim, Yon-Hwan;Im, Jeong-Hyuk;Min, Hyun-Su;Kim, Jun-Ki;Lee, Yong-Kyu;Park, Go-Eun;Cho, Kwang-Jae;Huh, Kang-Moo
    • 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.

Metal Surface Coating Using Electrospray of Biodegradable Polymers and $\alpha$-Lipoic Acid Release Behavior for Drug-Eluting Stents (생분해성 고분자의 전기분사를 이용한 약물방출 스텐트용 금속표면 코팅 및 ALA방출 거동)

  • Kim, Dong-Min;Lee, Bong-Soo;Park, Cheol-Ho;Park, Kwi-Deok;Son, Tae-Il;Jeong, Myeong-Ho;Han, Dong-Keun
    • 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.

Surface Mmodification of Poly(DL-lactide-co-glycolide) Nanoparticle (Poly(DL-lactide-co-glycolide) 나노입자의 표면 수식)

  • Oh, Yu-Mi;Jung, Taek-Kyu;Chi, Sang-Cheol;Shin, Byung-Cheol
    • Journal of the Korean Chemical Society
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    • v.47 no.6
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    • pp.601-607
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    • 2003
  • We studied on preparation of nanoparticles modified surface using biodegradable polymer, poly(DL-lactide-co-glycolide) (PLGA). Two kinds of PLGA nanoparticles were prepared by a spontaneous emulsification solvent diffusion (SESD) method using cetyltrimethylammonium chloride (CTAC) and tetradecyltrimethylammonium bromide (TTAB) as a cationic surfactant and polyethylene glycol-block-polypropylene glycol copolymer (Lutrol F68) as a nonionic surfactant. Model protein was coated on the surface of nanoparticles by the ionic complexation. The model protein was that influenza vaccine ($H_3N_2,\;H_1N_1$, B strain) labeled with NHS-fluorescein. The sizes of cationic nanoparticles were 140-160 nm and the surface charges were 50-60 mV. The sizes of nonionic nanoprticles were 80-90 nm and the surface charge was -10 mV. After coating vaccine on the surface of nanoparticles, the sizes of cationic nanoparticles were increased to 380-400 nm and the size of nonionic nanoparticles was not increased. The amount of coated vaccine on the cationic nanoparticles was 22.73 ${\mu}g$/mg.

Synthesis of Methoxy Poly(ethylene glycol)/Polyesters Diblock Copolymers and Evaluation of Micellar Characterization as Drug Carrier (메톡시 폴리(에틸렌 글리콜)/폴리에스테르 블록공중합체의 합성 및 미셀 특성 비교)

  • Hyun, Hoon;Yang, Jae-Chan;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.30 no.6
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    • pp.464-470
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    • 2006
  • Diblock copolymers consisting of methoxy Poly (ethylene glycol) (MPEG) and poly (${\epsilon}-ca$ prolactone) (PCL), poly(${\delta}-valerolactone$) (PVL), poly(L-lactide) (PLLA), or poly(L-lactide-co-glycolide) (PLGA) were prepared to compare the characterization of diblock copolymers as a drug carrier. MPEG-PCL, MPEG-PVL, MPEG-PLLA, and MPEG-PLGA diblock copolymers were synthesized by the ring-opening polymerization of ${\epsilon}$-caprolactone or ${\delta}$-valerolactone in the presence of $HCl{\cdot}Et_2O$ as a monomer activator at room temperature and by the ring-opening polymerization of L-lactide or a mixture of L-lactide and glycolide in the presence of stannous octoate at $130^{\circ}C$, respectively. The synthesized diblock copolymers were characterized with $^1H-NMR$, GPC, DSC, and XRD. The micellar characterization of MPEG-polyester diblock copolymers in an aqueous phase was carried out by using NMR, dynamic light scattering, AFM, and fluorescence techniques. Most micelles exhibited a spherical shape in AFM. Thus, ore confirmed that the micelles formed with MPEG-polyester diblock copolymers have possibility as a potential hydrophobic drug delivery vehicle because a hydrophobic drug could be preferentially distributed in the micelle core.

Degradation Characteristics of Cross-linked Hyaluronic Acid Membrane (가교된 히아루론산 막의 분해 특성)

  • Cheong, Seong-Ihl;Cho, Gu-Hyun
    • Membrane Journal
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    • v.19 no.4
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    • pp.310-316
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    • 2009
  • The degradation characteristics of cross-linked lactide/hyaluronic acid (LA/HA) membranes were investigated for purpose of applying to tissue engineering. The lactide/hyaluronic acid cross-linked with 1,3-butadiene diepoxide (BD) and 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC) was degradated in deionized water in water bath at $37^{\circ}C$. As the LA/HA mole ratio or crosslinking agent concentration decreased, the degradation rate of the crosslinked membranes increased. In order to investigate the structure change of the membrane in the degradation process, the control sample and 3, 6, 9 days-degradated samples were analysed by the nuclear magnetic resonance spectroscopy. In case of the membranes crosslinked with EDC, the HA-EDC bonding structure was degradated slowly whereas the HA-LA bonding structure was degradated quickly and dissappeared completely after 6 days. In case of the membranes crosslinked with BD, all the crosslinked bonding structure degradated slowly. The HA-BD bonding structure maintained its original state about 89, 83% in case of 3, 6 days-degardated samples respectively whereas the HA-LA bonding structure maintained its original state about 83, 65%. The scanning electron microscopy of the degradated membranes showed that the pore density in the surface, and the structure in the surface and cross section, of the before and after-degradation membranes did not change greatly, so the membranes was shown to be applied to materials for tissue engineering.