小檗碱纳米给药系统的制备及提高生物利用度研究进展

doi:10.5246/jcps.2026.03.015

中国药学(英文版) ›› 2026, Vol. 35 ›› Issue (3): 209-242.DOI: 10.5246/jcps.2026.03.015

• 【综述】 • 下一篇

小檗碱纳米给药系统的制备及提高生物利用度研究进展

邹时涛¹^,²^,^#, 侯智文²^,^#, 邹丽娜², 李烟雨², 林华清³^,^*(), 石孟琼¹^,^*(), 唐海明⁴, 李诗梅³, 许杰⁵, 张继红⁵^,^*()

^1. 三峡大学基础医学院&肿瘤微环境与免疫治疗湖北省重点实验室, 湖北宜昌 443002
^2. 三峡大学天然产物研究与利用湖北省重点实验室&药食同源大健康产品开发利用宜昌市重点实验室, 湖北宜昌 443002
^3. 湖北恒安芙林药业股份有限公司, 湖北宜昌 443103
^4. 华中农业大学食品科技学院, 湖北武汉 430070
^5. 三峡大学中医医院&湖北省功能性消化系统疾病中医临床医学研究中心, 湖北宜昌 443008

收稿日期:2025-09-18 修回日期:2025-10-16 接受日期:2026-01-12 出版日期:2026-04-04 发布日期:2026-04-03
通讯作者: 林华清, 石孟琼, 张继红

Research progress on the preparation of berberine nano-drug delivery system and the improvement of its bioavailability

Shitao Zou¹^,²^,^#, Zhiwen Hou²^,^#, Lina Zou², Yanyu Li², Huaqing Lin³^,^*(), Mengqiong Shi¹^,^*(), Haiming Tang⁴, Shimei Li³, Jie Xu⁵, Jihong Zhang⁵^,^*()

^1. Basic Medical College of China Three Gorges University & Hubei Provincial Key Laboratory of Tumor Microenvironment and Immunotherapy, Yichang 443002, Hubei, China
^2. Hubei Provincial Key Laboratory of Natural Product Research and Utilization of China Three Gorges University & Yichang Key Laboratory of Pharmaceutical and Edible Homologous Health Product Development and Utilization, Yichang 443002, Yichang 443002, Hubei, China
^3. Hubei Henganfulin Pharmaceutical Co., Ltd., Yichang 443103, Hubei, China
^4. College of Food Science and Technology, Huazhong Agricultural University, Wuhan 430070, Hubei, China
^5. China Three Gorges University Hospital of Traditional Chinese Medicine & Hubei Provincial Clinical Research Center of Traditional Chinese Medicine for Functional Digestive System Diseases, Yichang 443008, Hubei, China

Received:2025-09-18 Revised:2025-10-16 Accepted:2026-01-12 Online:2026-04-04 Published:2026-04-03
Contact: Huaqing Lin, Mengqiong Shi, Jihong Zhang
About author:
^# These authors contributed equally to this work.
Supported by:
Three Gorges University Open Fund of Hubei Key Laboratory for Tumor Microenvironment and Immunotherapy (Grant No. 2022KZL2-11)

摘要/Abstract

摘要：

小檗碱为毛茛科植物黄连(Coptis chinensis Franch.)、三角叶黄连(Coptis deltoidea C.Y. Cheng et Hsiao)或云连(Coptis teeta Wall.)、芸香科植物黄皮树(Phellodendron chinense Schneid.)的一种重要活性成分。研究表明, 小檗碱(Berberine, BBR)具有抗炎、抗氧化、抗肿瘤、降血糖、降血压、降血脂、抗菌等作用。然而由于BBR生物半衰期短、水溶性差和生物利用度低等不足使得其临床应用一直受到限制。近年来, 为了提高其应用效率, 对BBR纳米制剂的研究引起了研究人员的广泛关注。本文系统总结了BBR纳米制剂的分类、制备方法, 及其在增强药物靶向性、改善组织分布方面的应用, 并探讨了相关发展前景, 为BBR纳米给药系统的研发和临床应用提供参考。

关键词: 小檗碱, 纳米制剂, 靶向性, 药物递送, 组织分布

Abstract:

Berberine (BBR) is a major bioactive alkaloid found in Coptis chinensis Franch., Coptis deltoidea C.Y. Cheng et Hsiao, Coptis teeta Wall., and Phellodendron chinense Schneid. of the Rutaceae family, as well as in certain species of the Brassicaceae. Extensive studies have demonstrated that BBR exerts a broad spectrum of pharmacological activities, including anti-inflammatory, antioxidant, antitumor, hypoglycemic, antihypertensive, hypolipidemic, and antibacterial effects. Nevertheless, its clinical application has been hampered by intrinsic limitations such as a short biological half-life, poor water solubility, and low bioavailability. In recent years, nanotechnology-based delivery systems for BBR have attracted considerable attention as promising strategies to overcome these barriers. This review systematically summarizes the classification and preparation methods of BBR nanoformulations, highlights their potential in enhancing drug targeting and improving tissue distribution, and discusses future perspectives to inform the development and therapeutic applications of BBR-based nanomedicines.

Key words: Berberine, Nanoformulations, Targeting, Drug delivery, Tissue distribution

Supporting:

邹时涛, 侯智文, 邹丽娜, 李烟雨, 林华清, 石孟琼, 唐海明, 李诗梅, 许杰, 张继红. 小檗碱纳米给药系统的制备及提高生物利用度研究进展[J]. 中国药学(英文版), 2026, 35(3): 209-242.

Shitao Zou, Zhiwen Hou, Lina Zou, Yanyu Li, Huaqing Lin, Mengqiong Shi, Haiming Tang, Shimei Li, Jie Xu, Jihong Zhang. Research progress on the preparation of berberine nano-drug delivery system and the improvement of its bioavailability[J]. Journal of Chinese Pharmaceutical Sciences, 2026, 35(3): 209-242.

图/表 7

Figure 1. Structure of BBR.

Figure 2. Types of BBR preparations.

Table 1. Pharmacokinetic parameters of different dosage forms of BBR.

Table 2. Preparation details of BBR NP formulation.

Table 3. AUC enhancement of different nanoformulations.

Figure 3. Average values of drug loading rate (DLR) and entrapment efficiency (EE) of different nanoformulations.

Figure 4. The target mechanism of BBR NPs in the treatment of various diseases.

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小檗碱纳米给药系统的制备及提高生物利用度研究进展

Research progress on the preparation of berberine nano-drug delivery system and the improvement of its bioavailability

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