D-Fructose Modification Enhanced Internalization of Mixed Micelles in Breast Cancer Cells via GLUT5 Transporters

作者：Zhou, Xu; Qin, Xianyan; Gong, Tao; Zhang, Zhi-Rong; Fu, Yao^*

来源：Macromolecular Bioscience, 2017, 17(7): 1600529.

DOI：10.1002/mabi.201600529

• D-fructose
• GLUT5
• mixed micelles
• poly(epsilon-caprolactone)
• self-assembly

D-Fructose modified poly(epsilon-caprolactone)-polyethylene glycol (PCL-PEG-Fru) diblock amphiphile is synthesized via Cu(I)-catalyzed click chemistry, which self-assembles with D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) into PCL-PEG-Fru/TPGS mixed micelles (PPF MM). It has been proven that glucose transporter (GLUT)5 is overexpressed in MCF-7 cells other than L929 cells. In this study, PPF MM exhibit a significantly higher uptake efficiency than fructose-free PCL-PEG-N-3/TPGS mixed micelles in both 2D MCF-7 cells and 3D tumor spheroids. Also, the presence of free D-fructose competitively inhibits the internalization of PPF MM in MCF-7 cells other than L929 cells. PPF MM show selective tumor accumulation in MCF-7 breast tumor bearing mice xenografts. Taken together, PPF MM represent a promising nanoscale carrier system to achieve GLUT5-mediated cell specific delivery in cancer therapy.

• 出版日期2017-7
• 单位四川大学