Abstract 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 in vitro application of PTXCDL exhibited pH-sensitive PTX release, potent cytotoxicity, and enhanced intracellular accumulation. In comparison to in vivo, 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.

中文翻译：

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紫杉醇/羟丙基-β-环糊精复合脂质体克服癌症化疗中的多药耐药性

摘要 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敏化剂来克服 MDR。紫杉醇（PTX）是一种广泛使用的化疗药物，其应用已被了解了解MDR。但是，由于这种MDR，应用和使用受到严重限制。许多载体的环糊精 (CD) 在 MDR 癌细胞中也显示出抗癌能力。在这项研究中，开发了新型紫杉醇/羟丙基-β-环糊精复合脂质体 (PTXCDL)，试图克服 PTX 抗性人肺腺癌 (A549/T) 细胞系中的 MDR。PTXCDL 的体外应用表现出 pH 敏感的 PTX 释放、有效的细胞毒性和增强的细胞内积累。与体内相比，PTXCDL 还显示出更强的肿瘤生长抑制作用。相比之下，这些发现表明 PTXCDL 通过克服耐药性为有效治疗耐药癌症提供了一种新策略。