Chen Yu, Pan Yue, Hu Danrong, Peng Jinrong, Hao Ying, Pan Meng, Yuan Liping, Yu Yongyang, Qian Zhiyong
Sichuan University West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, CHINA.
Sichuan University, Sichuan University, Chengdu, 610065, CHINA.
Biomed Mater. 2021 Feb 5. doi: 10.1088/1748-605X/abe396.
The antitumor efficacy of various paclitaxel (PTX) and docetaxel (DTX) formulations in clinical applications is seriously affected by drug resistance. Cabazitaxel, a second-generation taxane, exhibits greater anticancer activity than paclitaxel and docetaxel and has low affinity for the P-glycoprotein (P-gp) efflux pump because of its structure. Therefore, cabazitaxel has the potential to overcome taxane resistance. However, owing to the high systemic toxicity and hydrophobicity of cabazitaxel and the instability of its commercial preparation, Jevtana®, the clinical use of cabazitaxel is restricted to patients with metastatic castration-resistant prostate cancer (mCRPC) who show progression after docetaxel-based chemotherapy. Nanomedicine is expected to overcome the limitations associated with cabazitaxel application and surmount taxane resistance. This review outlines the drug delivery systems of cabazitaxel published in recent years, summarizes the challenges faced in the development of cabazitaxel nanoformulations, and proposes strategies to overcome these challenges.
各种紫杉醇（PTX）和多西他赛（DTX）制剂在临床应用中的抗肿瘤疗效受到耐药性的严重影响。卡巴他赛作为第二代紫杉烷，表现出比紫杉醇和多西他赛更强的抗癌活性，并且由于其结构，对P-糖蛋白（P-gp）外排泵的亲和力较低。因此，卡巴他赛有克服紫杉烷耐药性的潜力。然而，由于卡巴他赛具有高全身毒性和疏水性，以及其商业制剂Jevtana®的不稳定性，卡巴他赛的临床应用仅限于在基于多西他赛的化疗后出现进展的转移性去势抵抗性前列腺癌（mCRPC）患者。纳米药物有望克服与卡巴他赛应用相关的局限性并克服紫杉烷耐药性。本综述概述了近年来发表的卡巴他赛给药系统，总结了卡巴他赛纳米制剂开发中面临的挑战，并提出了克服这些挑战的策略。
