伊立替康（CPT-11）活性代谢物 7-乙基-10-羟基喜树碱的传递进展。
Advances in delivery of Irinotecan (CPT-11) active metabolite 7-ethyl-10-hydroxycamptothecin.
机构信息
Clinical Research Institute, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou 310014, China; Center for Cancer Biology and Innovative Therapeutics, Key Laboratory of Tumor Molecular Diagnosis and Individualized Medicine of Zhejiang Province, Hangzhou 310014, China.
Clinical Research Institute, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou 310014, China; Center for Cancer Biology and Innovative Therapeutics, Key Laboratory of Tumor Molecular Diagnosis and Individualized Medicine of Zhejiang Province, Hangzhou 310014, China; Second Clinical Medical College, Zhejiang Chinese Medical University, Hangzhou 310053, China.
出版信息
Int J Pharm. 2019 Sep 10;568:118499. doi: 10.1016/j.ijpharm.2019.118499. Epub 2019 Jul 9.
CPT-11 is a first-line chemotherapy for advanced or metastatic colorectal cancers. 7-Ethyl-10-hydroxycamptothecin (SN38), the active metabolite of CPT-11, has an anticancer efficacy 100-1000 folds more than CPT-11 in vitro. However, the drawbacks such as ultralow solubility and poor stability, greatly limit the clinical applications of SN38. Recently, SN38-based nanomedicines have greatly improved the pharmaceutical and therapeutic characteristics of SN38. In addition, these nanosized delivery systems can target tumor tissues via the EPR effect and/or active-targeting strategies, thereby significantly improving anticancer efficacy, reducing side effects and reversing drug resistance. This review focuses on the advances of nano-delivery systems for SN38. We categorize the published studies into two groups, physical encapsulation and chemical conjugation, for the development of SN38 nano-delivery systems, and particularly summarize those for active tumor targeting. The advantages and shortcomings of current SN38 nano-delivery systems, aiming to develop more potent SN38 nano-delivery systems, are also discussed.
CPT-11 是一种用于治疗晚期或转移性结直肠癌的一线化疗药物。伊立替康的活性代谢产物 7-乙基-10-羟基喜树碱（SN38）在体外的抗癌活性比 CPT-11 高 100-1000 倍。然而，其超低的溶解度和较差的稳定性等缺点，极大地限制了 SN38 的临床应用。最近，基于 SN38 的纳米药物极大地改善了 SN38 的药物学和治疗特性。此外，这些纳米级的给药系统可以通过 EPR 效应和/或主动靶向策略靶向肿瘤组织，从而显著提高抗癌疗效，降低副作用并逆转耐药性。本综述重点介绍了用于 SN38 的纳米递药系统的研究进展。我们将已发表的研究分为物理包封和化学偶联两类，用于开发 SN38 纳米递药系统，并特别总结了那些用于主动肿瘤靶向的研究。此外，还讨论了当前 SN38 纳米递药系统的优缺点，旨在开发更有效的 SN38 纳米递药系统。
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