与传统化疗药物相比，中药抗肿瘤活性成分具有多靶点、多层次及协同干预等独特的优势。然而，大部分中药抗肿瘤活性成分往往水溶性差、生物利用度低等，限制了其临床应用。纳米递送系统有望改善中药抗肿瘤活性成分的应用限制，与游离药物相比，纳米载药系统表现出改善的生物利用度、增强的组织靶向性、减轻的脱靶不良反应及更大的体内稳定性。综述了目前最常用的2种中药抗肿瘤活性成分纳米递送系统即包载递送系统和共价结合前药递送系统，并对其中存在的问题及未来发展进行讨论，旨在为促进中药抗肿瘤活性成分纳米递送系统在临床上的实际应用提供参考。

Compared with traditional chemotherapeutic drugs, antitumor active components of traditional Chinese medicine have unique advantages, such as multi-target, multi-level, and coordinated intervention. However, most active components of traditional Chinese medicine often have poor water solubility, low bioavailability and so on, which limit their clinical applications. Nano-delivery system is expected to improve the application limitations of antitumor components of traditional Chinese medicine. Compared with free drugs, nano-drug delivery system shows improved bioavailability, enhanced tissue targeting, reduced off-target side effects, and greater in vivo stability. The two most commonly used nano-delivery systems for antitumor active components of traditional Chinese medicine, namely, encapsulated delivery system and covalently bound prodrug system are reviewed in this article, the problems and future developments in them are discussed, in order to provide reference for promoting the clinical application of nano-drug delivery systems for antitumor active components of traditional Chinese medicine.

R283.69

国家自然科学基金资助项目（21907076）；天津市教委科研计划项目（2018KJ008）；天津市“131”创新型人才培养工程第三层次；天津市高校“青年后备人才支持计划”项目