摘要
肿瘤多药耐药性(multidrug resistance,MDR)严重影响了化疗药物的临床疗效。P-糖蛋白(P-glycoprotein, P-gp)过度表达则是引发肿瘤MDR的主要原因之一, P-gp抑制剂的应用可以达到逆转肿瘤MDR的效果,是一种增强化疗药物抗肿瘤作用的有效手段。近年来,由于聚乙二醇1000维生素E琥珀酸酯(D-α-tocopheryl polyethylene glycol 1000 succinate,TPGS)安全无毒,抑制P-gp效果出色,其在纳米递药系统的应用得到广泛研究。本文对P-gp及其抑制剂研究、TPGS及其抑制P-gp机制研究和TPGS在纳米载药系统中逆转肿瘤MDR应用进行综述。
Multidrug resistance（MDR） seriously affects the clinical efficacy of chemotherapeutic drugs.One of the main mechanisms of MDR is the overexpression of P-glycoprotein（P-gp） in tumor cells that reduces the intracellular drug concentrations and limits the effective use of chemotherapeutic drugs.Accordingly,application of P-gp inhibitors that can reverse tumor MDR is an effective strategy to enhance the anti-tumor effect of chemotherapeutic drugs.In recent years,D-α-tocopheryl polyethylene glycol 1000 succinate（TPGS） has been widely applied as the potential P-gp inhibitor for its excellent P-gp inhibition effect as well as good safety.In this paper,we reviewed the P-gp inhibitors,the mechanisms of TPGS in reversing P-gp-mediated MDR and the application of TPGS-based nano-drug delivery system.
作者
苏日娜
刘腾飞
朱秀梅
周建平
姚静
SU Ri-na, LIU Teng-fei, ZHU Xiu-mei, ZHOU Jian-ping, YAO Jing(China Pharmaceutical University, Nanjing 210009, China)
出处
《药学学报》
CAS
CSCD
北大核心
2018年第11期1797-1807,共11页
Acta Pharmaceutica Sinica
基金
江苏省第五期"333工程"培养基金资助项目(BRA2017432)
