Shenyang Pharmaceutical University, Shenyang, China.
Mol Pharm. 2013 Apr 1;10(4):1465-9. doi: 10.1021/mp400022h. Epub 2013 Mar 19.
Multidrug resistance (MDR) is a major cause of failure in cancer chemotherapy. Tocopheryl polyethylene glycol 1000 succinate (TPGS) has been extensively explored for the treatment of MDR in cancer because of its ability to inhibit P-glycoprotein. Here, we have established multifunctional nanoparticles (MFNPs) using a single-molecule modification of TPGS, which can deliver a hydrophobic drug, paclitaxel (PTX), and a hydrophilic drug, fluorouracil (5-FU), and overcome MDR in cancer. Our data indicated that, when delivered into a PTX-resistant cell line using MFNPs, the combination of PTX and 5-FU was more cytotoxic than each agent individually.
多药耐药(MDR)是癌症化疗失败的主要原因。生育酚聚乙二醇 1000 琥珀酸酯(TPGS)因其能够抑制 P-糖蛋白而被广泛用于治疗癌症的多药耐药。在这里,我们使用 TPGS 的单分子修饰建立了多功能纳米颗粒(MFNPs),可以递送疏水性药物紫杉醇(PTX)和亲水性药物氟尿嘧啶(5-FU),并克服癌症中的多药耐药性。我们的数据表明,当使用 MFNPs 将其递送到 PTX 耐药细胞系中时,PTX 和 5-FU 的联合使用比单独使用每种药物的细胞毒性更强。