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Preparation and Evaluation of Poly(Ethylene Glycol)–Poly(Lactide) Micelles as Nanocarriers for Oral Delivery of Cyclosporine A

Author(s): Zhang Yanhui | Li Xinru | Zhou Yanxia | Wang Xiaoning | Fan Yating | Huang Yanqing | Liu Yan

Journal: Nanoscale Research Letters
ISSN 1931-7573

Volume: 5;
Issue: 6;
Start page: 917;
Date: 2010;
Original page

Keywords: Monomethoxy poly(ethylene glycol)–poly(lactide) | Polymeric micelles | Cyclosporine A | Solubility parameter | In vitro release | Intestinal absorption

Abstract A series of monomethoxy poly(ethylene glycol)–poly(lactide) (mPEG–PLA) diblock copolymers were designed according to polymer–drug compatibility and synthesized, and mPEG–PLA micelle was fabricated and used as a nanocarrier for solubilization and oral delivery of Cyclosporine A (CyA). CyA was efficiently encapsulated into the micelles with nanoscaled diameter ranged from 60 to 96 nm with a narrow size distribution. The favorable stabilities of CyA-loaded polymeric micelles were observed in simulated gastric and intestinal fluids. The in vitro drug release investigation demonstrated that drug release was retarded by polymeric micelles. The enhanced intestinal absorption of CyA-loaded polymeric micelles, which was comparable to the commercial formulation of CyA (Sandimmun Neoral®), was found. These suggested that polymeric micelles might be an effective nanocarrier for solubilization of poorly soluble CyA and further improving oral absorption of the drug.

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