Article
  • Preparation and Characterization of PEG-PLA(PLGA) Micelles for Solubilization of Rosiglitazone
  • Kim YH, Im JH, Min HS, Kim J, Lee YK, Park GE, Cho KJ, Huh KM
  • Rosiglitazone 가용화를 위한 PEG-PLA(PLGA) 고분자 미셀의 제조 및 특성분석
  • 김연환, 임정혁, 민현수, 김준기, 이용규, 박고은, 조광재, 허강무
Abstract
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-Npicolylnitinamide 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.

본 실험에서는 일련의 poly(ethylene glycol)-poly(D,L-lactide)(또는 -poly(D,L-lactide-co-glycolide)) 이중블록 공중합체들을 D,L-lactide(또는 glycolide)의 고리열림 중합에 의해 합성하고, 당뇨병 치료제 일종인 rosiglitazone의 가용화를 위한 고분자 미셀 제형으로서의 특성을 평가하였다. 고체분산법을 이용하여 높은 봉입률의 약물함유 미셀 제형을 효과적으로 제조하였고, 미셀 제형의 수용액 내 안정성을 hydrotropic agent의 일종인 2-hydroxy-N-picolylnitinamide(HPNA)의 사용으로 더욱 향상시킬 수 있었다. 생체 외 세포생존평가에서 생체적합성과 낮은 독성을 보였고, 쥐를 이용한 동물실험에서도 약물을 함유한 고분자 미셀이 약물 대조군보다 혈당을 보다 효과적으로 감소시켰다.

Keywords: PEG-PLA(PLGA) diblock copolymer; polymer micelle; rosiglitazone; hydrotropic agent

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  • Polymer(Korea) 폴리머
  • Frequency : Bimonthly(odd)
    ISSN 0379-153X(Print)
    ISSN 2234-8077(Online)
    Abbr. Polym. Korea
  • 2023 Impact Factor : 0.4
  • Indexed in SCIE

This Article

  • 2010; 34(3): 274-281

    Published online May 25, 2010

  • Received on Jan 12, 2010
  • Accepted on Feb 8, 2010