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

• Published in: Nanoscale research letters 2009, Vol.4 (12), p.1502-1511
• Main Authors: Li, Xinru, Yang, Zhuoli, Yang, Kewei, Zhou, Yanxia, Chen, Xingwei, Zhang, Yanhui, Wang, Fei, Liu, Yan, Ren, Lijun
• Format: Article
• Language: English
• Subjects: Antitumor efficacy; Ethaselen; Hemolysis; Monomethoxy poly(ethylene glycol)-poly(lactide); Polymeric micelles
• ISSN: 1931-7573; 1556-276X; 1556-276X
• DOI: 10.1186/1556-276X-4-1502

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 H₂₂ human 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.