Adding Vitamin E-TPGS to the Formulation of Genexol-PM: Specially Mixed Micelles Improve Drug-Loading Ability and Cytotoxicity against Multidrug-Resistant Tumors Significantly

被引：40

作者：

Fan, Zhuoyang ^{[1
]}

Chen, Cheng ^{[1
]}

Pang, Xiaoying ^{[1
]}

Yu, Zhou ^{[1
]}

Qi, Yang ^{[1
]}

Chen, Xinyi ^{[1
]}

Liang, Huihui ^{[1
]}

Fang, Xiaoling ^{[1
]}

Sha, Xianyi ^{[1
]}

机构：

[1] Fudan Univ, Sch Pharm, Dept Pharmaceut, Minist Educ & PLA,Key Lab Smart Drug Delivery, Shanghai 201203, Peoples R China

来源：

PLOS ONE | 2015年 / 10卷 / 04期

基金：

中国国家自然科学基金;

关键词：

CELL LUNG-CANCER; PHASE-II; COPOLYMER MICELLES; CREMOPHOR-FREE; IN-VITRO; PACLITAXEL; DELIVERY; GLYCOPROTEIN; PHARMACOKINETICS; BIODISTRIBUTION;

D O I：

10.1371/journal.pone.0120129

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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.

引用

页数：17

共 38 条

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