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

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• 作者：Xinru Li (1)
  Zhuoli Yang (2)
  Kewei Yang (3)
  Yanxia Zhou (1)
  Xingwei Chen (1)
  Yanhui Zhang (1)
  Fei Wang (1)
  Yan Liu (1)
  Lijun Ren (4)
  
• 关键词：Monomethoxy poly(ethylene glycol) ; poly(lactide) ; Polymeric micelles ; Hemolysis ; Ethaselen ; Antitumor efficacy
• 刊名：Nanoscale Research Letters
• 出版年：2009
• 出版时间：December 2009
• 年：2009
• 卷：4
• 期：12
• 页码：1502-1511
• 全文大小：302KB
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• 作者单位：Xinru Li (1)
  Zhuoli Yang (2)
  Kewei Yang (3)
  Yanxia Zhou (1)
  Xingwei Chen (1)
  Yanhui Zhang (1)
  Fei Wang (1)
  Yan Liu (1)
  Lijun Ren (4)
  
  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
  
• ISSN：1556-276X

文摘

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.