Department of Pharmaceutics, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, PR China.
Department of Pharmaceutics, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, PR China.
Colloids Surf B Biointerfaces. 2021 Sep;205:111914. doi: 10.1016/j.colsurfb.2021.111914. Epub 2021 Jun 8.
Currently, multidrug resistance (MDR) is one of the major reasons for failure in clinical cancer chemotherapy. Overexpression of the ATP binding cassette (ABC) transporter P-glycoprotein (P-gp), which significantly increases the efflux of anticancer drugs from tumor cells, enhances MDR. In the past few decades, four generations of P-gp inhibitors have appeared. However, they are limited in clinical application due to their severe toxic side effects. As a P-gp inhibitor and carrier for loading chemotherapy agents, TPGS has received increasing attention due to its advantages and unique properties of reversing MDR. TPGS is an amphipathic agent that increases the solubility of most chemotherapy drugs and decreases severe side effects. In addition, TPGS is an excellent carrier with P-gp-inhibiting ability. In this review, we summarize the latest articles on TPGS-based nanodelivery systems to prevent MDR.
目前，多药耐药（MDR）是临床癌症化疗失败的主要原因之一。三磷酸腺苷结合盒（ABC）转运蛋白 P-糖蛋白（P-gp）的过度表达显著增加了肿瘤细胞中抗癌药物的外排，增强了 MDR。在过去的几十年中，已经出现了四代 P-gp 抑制剂。然而，由于其严重的毒副作用，它们在临床应用中受到限制。作为 P-gp 抑制剂和载药体，TPGS 因其优势和逆转 MDR 的独特特性而受到越来越多的关注。TPGS 是一种两亲性物质，可提高大多数化疗药物的溶解度并降低严重的副作用。此外，TPGS 是一种具有 P-gp 抑制能力的优良载体。在这篇综述中，我们总结了基于 TPGS 的纳米递药系统预防 MDR 的最新研究进展。
