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综述坎尼汀在癌症治疗中的靶向药物传递系统。

Review targeted drug delivery systems for norcantharidin in cancer therapy.

机构信息

State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), Shaanxi Key Laboratory of Chinese Medicine Fundamentals and New Drugs Research, Shaanxi Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Shaanxi University of Chinese Medicine, Xi'an, 712046, China.

Xi'an Hospital of Traditional Chinese Medicine, Xi'an, 710021, China.

出版信息

J Nanobiotechnology. 2022 Dec 3;20(1):509. doi: 10.1186/s12951-022-01703-3.

Abstract

Norcantharidin (NCTD) is a demethylated derivative of cantharidin (CTD), the main anticancer active ingredient isolated from traditional Chinese medicine Mylabris. NCTD has been approved by the State Food and Drug Administration for the treatment of various solid tumors, especially liver cancer. Although NCTD greatly reduces the toxicity of CTD, there is still a certain degree of urinary toxicity and organ toxicity, and the poor solubility, short half-life, fast metabolism, as well as high venous irritation and weak tumor targeting ability limit its widespread application in the clinic. To reduce its toxicity and improve its efficacy, design of targeted drug delivery systems based on biomaterials and nanomaterials is one of the most feasible strategies. Therefore, this review focused on the studies of targeted drug delivery systems combined with NCTD in recent years, including passive and active targeted drug delivery systems, and physicochemical targeted drug delivery systems for improving drug bioavailability and enhancing its efficacy, as well as increasing drug targeting ability and reducing its adverse effects.

摘要

去甲斑蝥素(NCTD)是斑蝥素(CTD)的去甲基衍生物,CTD 是从传统中药芫青中分离得到的主要抗癌活性成分。NCTD 已获得国家食品药品监督管理局批准,用于治疗各种实体瘤,特别是肝癌。尽管 NCTD 大大降低了 CTD 的毒性,但仍存在一定程度的尿毒性和器官毒性,而且溶解度差、半衰期短、代谢快、静脉刺激性高以及肿瘤靶向能力弱,限制了其在临床上的广泛应用。为了降低其毒性并提高疗效,基于生物材料和纳米材料的靶向药物传递系统的设计是最可行的策略之一。因此,本综述重点介绍了近年来与 NCTD 结合的靶向药物传递系统的研究,包括被动和主动靶向药物传递系统,以及物理化学靶向药物传递系统,以提高药物的生物利用度和增强其疗效,增加药物的靶向能力并降低其不良反应。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cb/9719664/cc9a6671af33/12951_2022_1703_Fig1_HTML.jpg

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