Nanoemulsion improves hypoglycemic efficacy of berberine by overcoming its gastrointestinal challenge
Nanoemulsion improves hypoglycemic efficacy of berberine by overcoming its gastrointestinal challenge
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DOI：
10.1016/j.colsurfb.2019.06.006
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发表时间：
2019
期刊：
影响因子：
--
通讯作者：
Xiao-Ying Long
中科院分区：
文献类型：
--
作者：
Hong-Yu Xu;Chang-Shun Liu;Chuan-Li Huang;Li Chen;Yu-Rong Zheng;Si-Hang Huanga;Xiao-Ying Long
Berberine (BBR) is an important natural product with poor gastrointestinal behavior includes low permeability,.P-glycoprotein efflux, and mass elimination in the intestine. The aim of this study was to develop a novel.nanoemulsion (NE) to improve the hypoglycemic efficacy of BBR. NE was prepared and characterized by.morphology and droplet size detection, stored stability, in vitro intestinal lipolysis and metabolism, Caco-2 cells.transport, in situ single-pass intestinal perfusion, oral bioavailability in rats, and hypoglycemic efficacy in highfat diet and streptozocin-induced mice. BBR-loaded NE exhibits small droplet size (30.56 ± 0.35 nm) and good.stability. NE could remain intact after lipolysis and protect BBR against the intestinal metabolism mediated by.CYP2D6 and CYP3A4. Cells transport and intestinal perfusion studies revealed that NE decreases the P-glycoprotein efflux of BBR by 2-fold and enhances its permeability by 5.5-fold. Consequently, NE increased the oral.bioavailability of BBR in rats by 212.02%. Compared to BBR control, blood glucose level of diabetic mice by NE.was decreased by 3-fold. This novel NE provides a promising carrier to improve the hypoglycemic efficacy of.BBR by overcoming its gastrointestinal deficiency, which may offer a product for the therapy of diabet
