Adding vitamin E-TPGS to the formulation of Genexol-PM: specially mixed micelles improve drug-loading ability and cytotoxicity against multidrug-resistant tumors significantly.

Adding vitamin E-TPGS to the formulation of Genexol-PM: specially mixed micelles improve drug-loading ability and cytotoxicity against multidrug-resistant tumors significantly.
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DOI:
10.1371/journal.pone.0120129
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发表时间:
2015
期刊:
影响因子:
3.7
通讯作者:
Sha X
Sha X
中科院分区:
综合性期刊3区
文献类型:
--
作者:
Fan Z;Chen C;Pang X;Yu Z;Qi Y;Chen X;Liang H;Fang X;Sha X

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Genexol-PM, produced by Samyang Company (Korea) is an excellent preparation of paclitaxel (PTX) for clinical cancer treatment. However, it cannot resolve the issue of multidrug resistance (MDR)—a significant problem in the administration of PTX to cancer patients. To increase the efficacy of Genexol-PM against MDR tumors, a mixed micelle capable of serving as a vehicle for PTX was developed, and two substances were chosen as carrier materials: 1) Polyethylene glycol–polylactic acid (PEG-PLA), the original vehicle of Genexol-PM. 2) Vitamin E-TPGS, an inhibitor of P-glycoprotein (P-gp). P-gp has been proven to be the main cause of MDR. In vitro evaluation indicated that the mixed micelle was an ideal PTX delivery system for the treatment of MDR tumors; the mixed micelle also showed a significantly better drug-loading coefficient than Genexol-PM.
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