Nanoemulsion improves hypoglycemic efficacy of berberine by overcoming its gastrointestinal challenge

Colloids and Surfaces. B, Biointerfaces
Hong-Yu XuXiao-Ying Long

Abstract

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 high-fat 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 ...Continue Reading

Citations

Nov 14, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Xinmei XuGang Fan
Aug 4, 2021·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Oi Jin TanUsha Sundralingam
Jul 7, 2021·Journal of Biomaterials Science. Polymer Edition·Rakesh Kumar PaulKaisar Raza

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