Nano Express

Nanoscale Research Letters

, Volume 5, Issue 6, pp 917-925

Open Access This content is freely available online to anyone, anywhere at any time.

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

  • Yanhui ZhangAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University
  • , Xinru LiAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University
  • , Yanxia ZhouAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University
  • , Xiaoning WangAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University
  • , Yating FanAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University
  • , Yanqing HuangAffiliated withPharmaceutical Teaching Experiment Center, School of Pharmaceutical Sciences, Peking University
  • , Yan LiuAffiliated withDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Email author 

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