纳米载药系统逆转P-gp介导的肿瘤多药耐药的机制

多药耐药(MDR)是导致肿瘤化疗失败的重要原因,而引起MDR的主要原因为P-糖蛋白(P-gp)过度表达所致的肿瘤细胞内药物浓度下降.纳米载药系统具有靶向性、缓释性以及体内循环时间较长等特点,能通过非特异的胞吞作用、配体修饰的胞吞作用等机制,从蛋白质、基因水平抑制P-gp,有效弥补传统给药方法的不足,从而提高细胞内药物浓度,逆转MDR.

Mechanism of nano drug delivery systems in overcoming P-gp mediated multi-drug resistance

Multi-drug resistance (MDR) of cancer cells is a major cause of failure of chemotherapy in cancer treatment. Most MDRs are caused by overexpression of P-glycoprotein (P-gp) which effuses chemotherapeutic agents out of cells. Nano drug delivery systems (NDDS) have been valued for their characteristics including drug targeting, slow-releasing, and long circulation time in the body. Through mechanisms such as non-specific endocytosis and receptor-mediated endocytosis, NDDS can inhibit P-gp at the gene and protein level, leading to improved concentrations of chemotherapeutic drugs in cancer cells, and therefore reverse MDR.