School of Pharmaceutical Sciences of Ribeirao Preto, University of Sao Paulo, Ribeirao Preto, SP, Brazil.
Drug Deliv Transl Res. 2020 Dec;10(6):1584-1600. doi: 10.1007/s13346-020-00827-z.
Triptolide (TPL) is a natural compound and active component of Tripterygium wilfordii Hook F., an Asian native woody vine widely used for over 200 years in Chinese medicine. Hot water, ethanol-ethyl acetate, and chloroform-methanol extracts are the first reported TPL preparations in the literature, and since then, several studies for application in inflammation processes and cancer are described due to the antitumor, anti-inflammatory, and immunosuppressive characteristics of the molecule. However, physicochemical properties such as poor solubility and bioavailability are the main concerns regarding the TPL safety and efficacy in clinical studies since trials have reported adverse side effects alongside the excellent TPL therapeutic effects. Here, we review the main TPL applications and issues related to the drug usage, and a comprehensive summary of diseases is provided. Special emphasis is given to drug delivery systems designed to overcome the TPL physicochemical characteristics such as poor drug solubility, and how to increase efficacy and obtain a safe drug profile. Graphical abstract.
雷公藤红素（TPL）是一种天然化合物，也是亚洲本土木质藤本植物雷公藤的活性成分，在中国医学中已使用了 200 多年。热水、乙醇-乙酸乙酯和氯仿-甲醇提取物是文献中首次报道的 TPL 制剂，此后，由于该分子具有抗肿瘤、抗炎和免疫抑制特性，有几项关于在炎症过程和癌症中应用的研究。然而，由于 TPL 在临床研究中的安全性和疗效存在不良副作用，因此 TPL 的理化性质，如溶解度和生物利用度差，是人们关注的主要问题。在这里，我们综述了 TPL 的主要应用及与药物使用相关的问题，并对疾病进行了全面总结。特别强调了旨在克服 TPL 理化特性（如药物溶解度差）的药物传递系统，以及如何提高疗效和获得安全的药物特性。
