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Preparation and Drug Release of All-Trans Retinoic Acid-Loaded Poly(L-lactic acid) Nanoparticles

레티노산 함유 폴리락탄산 나노입자의 제조 및 약물 방출

  • Chae, Ji-Man (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Lee, Kyung-Man (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Kim, In-Sook (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Lee, Yong-Bok (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Shin, Sang-Chul (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Oh, In-Joon (College of Pharmacy and Research Institute of Drug Development, Chonnam National University)
  • 채지만 (전남대학교 약학대학 및 약품개발연구소) ;
  • 이경만 (전남대학교 약학대학 및 약품개발연구소) ;
  • 김인숙 (전남대학교 약학대학 및 약품개발연구소) ;
  • 이용복 (전남대학교 약학대학 및 약품개발연구소) ;
  • 신상철 (전남대학교 약학대학 및 약품개발연구소) ;
  • 오인준 (전남대학교 약학대학 및 약품개발연구소)
  • Published : 2004.10.20

Abstract

To develop an intravenous delivery system of all-trans retinoic acid (ATRA) for the cancer therapy, poly(L-lactic acid) nanoparticles were prepared and characterized. Emulsification-solvent evaporation method was chosen to prepare submicron sized nanoparticles. Spherical nanoparticles less than 200 nm in diameter with narrow size distribution were prepared, and the entrapment efficiency of drug was more than 95%. The endothermic peak at $183^{\circ}C$ and X-ray crystallographic peak of ATRA appeared in the nanoparticle system, suggesting the inhibition of crystallization of ATRA by polymer adsorption during the precipitation process. ATRA was released at $37^{\circ}C$ for 60 days and the release rate was dependent on the concentration of drug incorporated in the nanoparticles. While ATRA was unstable in the light, it was very stable at $4^{\circ}C$. These results suggest the usefulness of PLA nanoparticles as a sustained and prolonged release carrier for ATRA.

Keywords

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