Open Access Nano Express

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

Yanhui Zhang1, Xinru Li1, Yanxia Zhou1, Xiaoning Wang1, Yating Fan1, Yanqing Huang2 and Yan Liu1*

Author affiliations

1 Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Haidian District, Beijing, 100191, People’s Republic of China

2 Pharmaceutical Teaching Experiment Center, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, People’s Republic of China

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Citation and License

Nanoscale Research Letters 2010, 5:917-925  doi:10.1007/s11671-010-9583-4

Published: 27 March 2010

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.

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