PLoS ONE 2015-01-01

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

Zhuoyang Fan, Cheng Chen, Xiaoying Pang, Zhou Yu, Yang Qi, Xinyi Chen, Huihui Liang, Xiaoling Fang, Xianyi Sha

Index: PLoS ONE 10(4) , e0120129, (2015)

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Abstract

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.