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Self-Assembled Polymeric Micellar Nanoparticles as Nanocarriers for Poorly Soluble Anticancer Drug Ethaselen

Xinru Li1, Zhuoli Yang2, Kewei Yang3, Yanxia Zhou1, Xingwei Chen1, Yanhui Zhang1, Fei Wang1, Yan Liu1* and Lijun Ren4

Author Affiliations

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

2 TEAM Academy of Pharmaceutical Sciences, Beijing, People’s Republic of China

3 Department of Pharmaceutical Technology, Institute of Pharmacy, University Jena, Jena, Germany

4 Department of Three, Institute of Chemical Defence, Beijing, People’s Republic of China

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Nanoscale Research Letters 2009, 4:1502-1511  doi:10.1007/s11671-009-9427-2

Published: 16 September 2009


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.

Monomethoxy poly(ethylene glycol)-poly(lactide); Polymeric micelles; Hemolysis; Ethaselen; Antitumor efficacy