文献类型：期刊文章

作　　者：王爱婷[1] 佟淑文[1,2] 胡新[1] 齐宪荣[3,1,4]

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]北京泰德制药股份有限公司,北京100176 [3]北京大学医学部分子药剂学与新释药系统北京市重点实验室,北京100191 [4]北京大学医学部天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：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);Doctoral Foundation of the Ministry of Education(Grant No.20130001110055)

年　　份：2015

卷　　号：24

期　　号：7

起止页码：419-426

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2015_2016、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：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 （TPGSIooo） 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 TPGSIooo 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.

关 键 词：Micelles  Multidrug resistance  PREPARATION DSPE-PEG  TPGS Folate  

分 类 号：R943] R96[药学类]