Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4

文献类型： 外文期刊

第一作者： Chen, Tingting

作者： Chen, Tingting;Dou, Yaoxing;Li, Qingguo;Huang, Ziwei;Su, Ziren;Zeng, Lingfeng;Dou, Yaoxing;Zeng, Lingfeng;Dou, Yaoxing;Liu, Jun;Liu, Jun;Zeng, Lingfeng;Dou, Yaoxing;Chen, Tingting;Ai, Gaoxiang

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关键词： Acute liver injury; Oxyberberine; Amorphous solid dispersions; Bioavailability

期刊名称：SCIENTIFIC REPORTS （ 影响因子：3.8； 五年影响因子：4.3 ）

ISSN： 2045-2322

年卷期： 2024 年 14 卷 1 期

页码：

收录情况： SCI

摘要： Oxyberberine (OBB) is a significant natural compound, with excellent hepatoprotective properties. However, the poor water solubility of OBB hinders its release and absorption thus resulting in low bioavailability. To overcome these drawbacks of OBB, amorphous spray-dried powders (ASDs) of OBB were formulated. The dissolution, characterizations, and pharmacokinetics of OBB-ASDs formulation were investigated, and its hepatoprotective action was disquisitive in the D-GalN/LPS-induced acute liver injury (ALI) mouse model. The characterizations of OBB-ASDs indicated that the crystalline form of OBB active pharmaceutical ingredients (API) was changed into an amorphous form in OBB-ASDs. More importantly, OBB-ASDs showed a higher bioavailability than OBB API. In addition, OBB-ASDs treatment restored abnormal histopathological changes, improved liver functions, and relieved hepatic inflammatory mediators and oxidative stress in ALI mice. The spray drying techniques produced an amorphous form of OBB, which could significantly enhance the bioavailability and exhibit excellent hepatoprotective effects, indicating that the OBB-ASDs can exhibit further potential in hepatoprotective drug delivery systems. Our results provide guidance for improving the bioavailability and pharmacological activities of other compounds, especially insoluble natural compounds. Meanwhile, the successful development of OBB-ASDs could shed new light on the research process of poorly soluble medicine.

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