Journal of Chinese Pharmaceutical Sciences ›› 2015, Vol. 24 ›› Issue (7): 419-426.DOI: 10.5246/jcps.2015.07.054

• Original articles •     Next Articles

Preparation and anti-MDR tumors study of folate and TPGS dual-modified DSPE-PEG micelles loaded with docetaxel

Aiting Wang2#, Shuwen Tong2,4#, Xin Hu2*, Xianrong Qi1,2,3*   

  1. 1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery System, Peking University Health Science Center, Beijing 100191, China
    2. School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    3. State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China
    4. Tide Pharmaceutical Co., Ltd., Beijing 100176, China
  • Received:2015-04-11 Revised:2015-04-17 Online:2015-07-28 Published:2015-05-08
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  • Supported by:

    National Natural Science Foundation of China (Grant No. 81273454 and 81473156), Beijing National Science Foundation (Grant No. 7132113), National Key Basic Research Program (Grant No. 2013CB932501), and Doctoral Foundation of the Ministry of Education (Grant No. 20130001110055).


Multidrug resistance (MDR) operated by P-glycoprotein (P-gp) is one of the major causes in the treatment failure of cancers. In this work,docetaxel-loaded mixed micelles comprised of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(polyethylene-glycol)2000 (DSPE-PEG2000),D-α-Tocopherylpolyethylene glycol 1000 succinate (TPGS1000) and DSPE-PEG2000-folate were developed to overcome MDR and reduce the side effect of docetaxel in cancer therapy. The diameters of micelles ranged from 13 to 26 nm and the encapsulation efficiencies were all above 85%. The influences of DSPE-PEG2000 and TPGS1000 ratios on the micellar characteristics and anti-resistant tumors effects were evaluated. Micelles with high TPGS1000 amount showed an increased cellular uptake and stronger cytotoxicity against MDR KBv cells. Moreover, the micelles modified by targeting ligand of folic acid exhibited better antitumor effect on folate receptor over-expressing KBv cells.The study provides a method for overcoming MDR in cancer therapy.

Key words: Micelles, Multidrug resistance, Preparation, DSPE-PEG, TPGS, Folate

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