title: Self-assembled polymeric micellar nanoparticles as nanocarriers for poorly soluble anticancer drug ethaselen.
abstract: A series of monomethoxy poly(ethylene glycol)-poly(lactide) (mPEG-PLA) diblock copolymers were synthesized, and mPEG-PLA micelle was fabricated and used as a nanocarrier for solubilization and delivery of a promising anticancer drug ethaselen. Ethaselen was efficiently encapsulated into the micelles by the dialysis method, and the solubility of ethaselen in water was remarkably increased up to 82 μg/mL before freeze-drying. The mean diameter of ethaselen-loaded micelles ranged from 51 to 98 nm with a narrow size distribution and depended on the length of PLA block. In vitro hemolysis study indicated that mPEG-PLA copolymers and ethaselen-loaded polymeric micelles had no hemolytic effect on the erythrocyte. The enhanced antitumor efficacy and reduced toxic effect of ethaselen-loaded polymeric micelle when compared with ethaselen-HP-β-CD inclusion were observed at the same dose in H22human liver cancer cell bearing mouse models. These suggested that mPEG-PLA polymeric micelle nanoparticles had great potential as nanocarriers for effective solubilization of poorly soluble ethaselen and further reducing side effects and toxicities of the drug.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, 100191, Beijing, Haidian, People's Republic of China. yanliu@bjmu.edu.cn.
authors.forename: Xinru
authors.initials: X
authors.lastname: Li
authors.forename: Zhuoli
authors.initials: Z
authors.lastname: Yang
authors.forename: Kewei
authors.initials: K
authors.lastname: Yang
authors.forename: Yanxia
authors.initials: Y
authors.lastname: Zhou
authors.forename: Xingwei
authors.initials: X
authors.lastname: Chen
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Zhang
authors.forename: Fei
authors.initials: F
authors.lastname: Wang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Lijun
authors.initials: L
authors.lastname: Ren