title: Adding vitamin E-TPGS to the formulation of Genexol-PM: specially mixed micelles improve drug-loading ability and cytotoxicity against multidrug-resistant tumors significantly.
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.
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Zhuoyang
authors.initials: Z
authors.lastname: Fan
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Cheng
authors.initials: C
authors.lastname: Chen
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Xiaoying
authors.initials: X
authors.lastname: Pang
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Zhou
authors.initials: Z
authors.lastname: Yu
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Qi
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Xinyi
authors.initials: X
authors.lastname: Chen
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Huihui
authors.initials: H
authors.lastname: Liang
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Xiaoling
authors.initials: X
authors.lastname: Fang
authors.affiliation: Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, China.
authors.forename: Xianyi
authors.initials: X
authors.lastname: Sha
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001692:Biological Transport; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003374:Coumarins / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D042541:Intracellular Space / Q000378:metabolism; D019344:Lactic Acid / Q000737:chemistry*; D008823:Micelles; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D010316:Particle Size; D011091:Polyesters; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D018874:Spheroids, Cellular / Q000187:drug effects; D013844:Thiazoles / Q000737:chemistry; D014810:Vitamin E / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D013844:Thiazoles; C517282:coumarin 6; D014810:Vitamin E; D019344:Lactic Acid; D011092:Polyethylene Glycols; C033616:poly(lactide); D017239:Paclitaxel
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