Sun Yuan, Wang Chengen, Li Xiaoguang, Lu Jun, Wang Maolin
Clinical Research Center, The First Affiliated Hospital of Shantou University Medical College, Shantou, China.
Department of Physiology, School of Basic Medical Sciences, Shenzhen University Health Sciences Center, Shenzhen, China.
Front Pharmacol. 2024 Feb 16;15:1137289. doi: 10.3389/fphar.2024.1137289. eCollection 2024.
Celastrol is a quinone methyl triterpenoid monomeric ingredient extracted from the root of . Celastrol shows potential pharmacological activities in various diseases, which include inflammatory, obesity, cancer, and bacterial diseases. However, the application prospect of celastrol is largely limited by its low bioavailability, poor water solubility, and undesired off-target cytotoxicity. To address these problems, a number of drug delivery methods and technologies have been reported to enhance the efficiency and reduce the toxicity of celastrol. We classified the current drug delivery technologies into two parts. The direct chemical modification includes nucleic acid aptamer-celastrol conjugate, nucleic acid aptamer-dendrimer-celastrol conjugate, and glucolipid-celastrol conjugate. The indirect modification includes dendrimers, polymers, albumins, and vesicular carriers. The current technologies can covalently bond or encapsulate celastrol, which improves its selectivity. Here, we present a review that focalizes the recent advances of drug delivery strategies in enhancing the efficiency and reducing the toxicity of celastrol.
雷公藤红素是从[植物名称缺失]根部提取的一种醌甲基三萜类单体成分。雷公藤红素在多种疾病中显示出潜在的药理活性，包括炎症、肥胖、癌症和细菌性疾病。然而，雷公藤红素的应用前景在很大程度上受到其低生物利用度、差的水溶性和不良的脱靶细胞毒性的限制。为了解决这些问题，已经报道了许多药物递送方法和技术来提高雷公藤红素的效率并降低其毒性。我们将当前的药物递送技术分为两部分。直接化学修饰包括核酸适配体 - 雷公藤红素缀合物、核酸适配体 - 树枝状大分子 - 雷公藤红素缀合物和糖脂 - 雷公藤红素缀合物。间接修饰包括树枝状大分子、聚合物、白蛋白和囊泡载体。当前技术可以将雷公藤红素共价结合或包裹起来，从而提高其选择性。在此，我们发表一篇综述，重点关注药物递送策略在提高雷公藤红素效率和降低其毒性方面的最新进展。
