Flavopiridol has shown promising activities in hematologic and solid tumor models, as well as in clinical trials in chronic lymphocytic leukemia patients. Flavopiridol has relatively low solubility and high plasma protein-binding. To address these issues and to provide an alternative strategy to achieve clinical efficacy, we encapsulated flavopiridol into a liposomal carrier and characterized its physicochemical and pharmacokinetic properties. The liposomes, comprising hydrogenated soy phosphatidylcholine (HSPC), cholesterol and poly (ethylene glycol) 2000-distearoyl phosphatidylethanolamine (PEG-DSPE), were prepared by polycarbonate membrane extrusion and then loaded with flavopiridol by a pH-gradient driven remote loading procedure. The liposomes had a mean diameter of 120.7 nm and a flavopiridol entrapment efficiency of 70.4

作者：Xiaojuan, Yang；Xiaobin, Zhao；Mitch A, Phelps；Longzhu, Piao；Darlene M, Rozewski；Qing, Liu；L James, Lee；Guido, Marcucci；Michael R, Grever；John C, Byrd；James T, Dalton；Robert J, Lee

来源：International journal of pharmaceutics 2009 年 365卷 1-2期