Use of 18 beta-glycyrrhetinic acid nanocrystals to enhance anti-inflammatory activity by improving topical delivery

文献类型： 外文期刊

第一作者： Quan, Weiyan

作者： Quan, Weiyan;Kong, Songzhi;Lu, Sitong;Li, Sidong;Ouyang, Qianqian;Huang, Yongmei;Li, Sidong;Luo, Hui;Tao, Jinlong

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关键词： 18 beta-Glycyrrhetinic acid; Nanocrystal; Topical delivery; Anti-inflammation activity

期刊名称：COLLOIDS AND SURFACES B-BIOINTERFACES （ 影响因子：5.268； 五年影响因子：4.957 ）

ISSN： 0927-7765

年卷期： 2021 年 205 卷

页码：

收录情况： SCI

摘要： 18 beta-Glycyrrhetinic acid (GA) is often topically applied in clinical treatment of inflammatory skin diseases. However, GA has poor solubility in water, which results in poor skin permeability and low bioavailability. Nanocrystallization of drugs can enhance their permeability and improve bioavailability. We prepared GA nanocrystals (Nano GA) by high-pressure homogenization. These nanocrystals were characterized by photon correlation spectroscopy, scanning electron microscopy, thermogravimetric analysis, and X-ray diffractometry. The ability of Nano GA to improve dermal permeability was investigated ex vivo using Franz diffusion vertical cells and mouse skin. The topical anti-inflammatory activity of Nano GA was assessed in vivo by a 12-O-tetradecanoyl phorbol-13-acetate (TPA)-induced model in mouse ears. The average particle size of a GA nanocrystalline suspension was 288.6 +/- 7.3 nm, with a narrow particle-size distribution (polydispersity index similar to 0.13 +/- 0.10), and the particle size of the lyophilized powder increased (552.0 +/- 9.8 nm). After nanocrystallization, the thermal stability and crystallinity decreased but solubility increased significantly. Nano GA showed higher dermal permeability than Coarse GA. Macroscopic and staining-based observations of mouse ears and the levels of proinflammatory factors and myeloperoxidase revealed that the Nano GA hydrogel exhibited better anti-edema ability and more strongly inhibited inflammation development than the Coarse GA hydrogel and indomethacin hydrogel (positive drug). These results suggest that Nano GA could be an efficacious topical therapeutic agent for skin inflammation.

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