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Effect of an Excipient on the Formation of PLGA Particles Using Supercritical Fluid

초임계 유체를 이용한 PLGA 입자 제조에 첨가제가 미치는 영향

  • Jung, In-Il (Department of Chemical and Biomolecular Engineering, Yonsei University) ;
  • Haam, Seung-Joo (Department of Chemical and Biomolecular Engineering, Yonsei University) ;
  • Lim, Gio-Bin (Department of Chemical Engineering, The University of Suwon) ;
  • Ryu, Jong-Hoon (Department of Chemical Engineering, The University of Suwon)
  • 정인일 (연세대학교 화공생명공학과) ;
  • 함승주 (연세대학교 화공생명공학과) ;
  • 임교빈 (수원대학교 화학공학과) ;
  • 유종훈 (수원대학교 화학공학과)
  • Received : 2011.04.19
  • Accepted : 2011.07.26
  • Published : 2012.01.25

Abstract

In this study, we employed hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) as an excipient to produce poly(lactic-$co$-glycolic acid) (PLGA) fine particles by a supercritical fluid process, called aerosol solvent extraction system (ASES), and investigated the effect of HP-${\beta}$-CD content on the morphology of the particles. The influence of HP-${\beta}$-CD on the drug release characteristics of paclitaxel-loaded PLGA particles was also evaluated. Fine particles were obtained when the HP-${\beta}$-CD content in PLGA/HP-${\beta}$-CD mixtures was greater than 40% and 30%, respectively, for PLGA(75:25) and PLGA(50:50), whereas a film-like precipitate was obtained for lower HP-${\beta}$-CD content. The release rate for paclitaxel loaded PLGA(75:25)/HP-${\beta}$-CD particles was found to increase with HP-${\beta}$-CD content.

본 연구에서는 초임계 aerosol solvent extraction system(ASES) 공정을 이용하여 poly(lactic-$co$-glycolic acid)(PLGA) 미립자를 제조하기 위해 첨가제로 hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD)를 사용하였으며, HP-${\beta}$-CD의 첨가량이 PLGA 입자의 형상에 미치는 영향을 조사하였다. 또한 항암제인 파클리탁셀이 봉입된 미립자를 제조하여 HP-${\beta}$-CD의 함량에 따른 약물 방출 특성의 변화를 고찰하였다. PLGA(75:25)의 경우 HP-${\beta}$-CD를 고분자 중량 대비 약 40%까지, PLGA(50:50)의 경우 약 30%까지 첨가하였을 때 미립자가 형성되었으며, HP-${\beta}$-CD의 첨가량이 이보다 더 적은 경우에는 PLGA가 필름 형태로 형성되었다. 파클리탁셀이 봉입된 PLGA/HP-${\beta}$-CD 미립자의 경우 HP-${\beta}$-CD의 함량이 증가함에 따라 더 빠른 속도로 약물이 방출됨을 확인할 수 있었다.

Keywords

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