College of Medicine, Hangzhou Normal University, Hangzhou, China.
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
J Liposome Res. 2020 Mar;30(1):12-20. doi: 10.1080/08982104.2019.1579838. Epub 2019 Mar 14.
Multidrug resistance (MDR) is the largest obstacle to the success of chemotherapy. The development of innovative strategies and safe sensitizers is required to overcome MDR. Paclitaxel (PTX) is a widely used chemotherapeutic drug, the application of which has been learn to understand MDR. However, the application and use are severely restricted because of this MDR. Cyclodextrins (CDs) of many carriers, additionally have shown anti-cancer capability in MDR cancer cells. In this study, novel paclitaxel/hydroxypropyl-β-cyclodextrin complex-loaded liposomes (PTXCDL) have been developed in an attempt to overcome MDR in a PTX-resistant human lung adenocarcinoma (A549/T) cell line. The application of PTXCDL exhibited pH-sensitive PTX release, potent cytotoxicity, and enhanced intracellular accumulation. In comparison to , PTXCDL also show a stronger inhibition of tumor growth. In comparison, these findings suggest that the PTXCDL provide a novel strategy for effective therapy of resistant cancers by overcoming the drug resistance.
多药耐药（MDR）是化疗成功的最大障碍。需要开发创新策略和安全增敏剂来克服 MDR。紫杉醇（PTX）是一种广泛使用的化疗药物，对其耐药性的研究已经取得了一定的成果。然而，由于这种多药耐药性，它的应用和使用受到了严重限制。许多载体的环糊精（CDs）已被证明在 MDR 癌细胞中具有抗癌能力。在本研究中，我们试图开发新型紫杉醇/羟丙基-β-环糊精复合物负载脂质体（PTXCDL）以克服 PTX 耐药的人肺腺癌细胞系（A549/T）中的 MDR。PTXCDL 的应用表现出 pH 敏感的 PTX 释放、强大的细胞毒性和增强的细胞内积累。与游离 PTX 相比，PTXCDL 还显示出更强的肿瘤生长抑制作用。这些发现表明，PTXCDL 通过克服耐药性为治疗耐药性癌症提供了一种新的策略。
