title: Preparation and evaluation of poly(ethylene glycol)-poly(lactide) micelles as nanocarriers for oral delivery of cyclosporine a.
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.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Haidian District, Beijing, 100191, People's Republic of China. yanliu@bjmu.edu.cn.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xinru
authors.initials: X
authors.lastname: Li
authors.forename: Yanxia
authors.initials: Y
authors.lastname: Zhou
authors.forename: Xiaoning
authors.initials: X
authors.lastname: Wang
authors.forename: Yating
authors.initials: Y
authors.lastname: Fan
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Huang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu