P-糖蛋白抑制性纳米载体逆转肿瘤多药耐药的研究进展

Research progress of P-gp inhibitory nanocarriers for the reversal of multidrug resistance in tumors

P-糖蛋白(P-glycoprotein,P-gp)的过表达导致细胞外排泵活性增强,将抗肿瘤药物泵出胞外,从而导致多药耐药(multidrug resistance,MDR)的产生和化疗的失败。纳米药物载体的优势表现在减少药物外排、增加药物在肿瘤部位的蓄积、增强药物的靶向作用、下调P-gp的表达、协同逆转多药耐药等。本文就近年来纳米载体逆转P-gp介导的肿瘤多药耐药的研究进展进行综述,同时介绍了具有P-gp抑制特性的纳米材料的新进展,以期待将基础研究向临床应用转化提供一定参考。

The over-expression of P-glycoprotein leads to the enhanced activity of extracellular efflux pump,which pumps anti-tumor drugs out of the cell,leading to multidrug resistance(MDR)and failure of chemotherapy.The advantages of nanoparticle carriers include reducing drug efflux,increasing drug accumulation in tumor sites,enhancing drug targeting effect,downregulating the expression of P-gp,and synergistic reversal of multidrug resistance.This paper reviews the progress in the research on the reversal of P-gp-mediated multidrug resistance of nanocarrier drugs in the current stage of development,so as to provide some references for the transformation of basic research into clinical application.