文献类型：期刊文献

英文题名：Use of 18β-glycyrrhetinic acid nanocrystals to enhance anti-inflammatory activity by improving topical delivery

作者：Quan, Weiyan[1];Kong, Songzhi[1];Ouyang, Qianqian[2];Tao, Jinlong[3];Lu, Sitong[1];Huang, Yongmei[2];Li, Sidong[1,2];Luo, Hui[2]

机构：[1]Guangdong Ocean Univ, Sch Chem & Environm Sci, Dept Appl Chem, Zhanjiang 524088, Peoples R China;[2]Marine Biomed Res Inst Guangdong Zhangjiang, Zhanjiang, Peoples R China;[3]Chinese Acad Trop Agr Sci, Agr Prod Proc Res Inst, Zhanjiang 524001, Peoples R China

年份：2021

卷号：205

外文期刊名：COLLOIDS AND SURFACES B-BIOINTERFACES

收录：SCI-EXPANDED(收录号：WOS:000703107600002)、、EI(收录号：20212110403579)、Scopus(收录号：2-s2.0-85106292586)、WOS

基金：This work supported by the National Natural Science Foundation of China (81803684), Natural Science Foundation of Guangdong Province (2018A030313416), the Scientific Research Fund of Guangdong Medical University (GDMUM202002) and the Science and technology program of Guangdong Province (2019B090905011), the public service platform of south China Sea for R&D marine biomedicine resources (2017C8A), the Fund of Southern Marine Science and Engineering Guangdong Laboratory (Zhanjiang) (ZJW-2019-007).

语种：英文

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

外文摘要：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.