Preparation, In Vivo and In Vitro Evaluation, and Pharmacodynamic Study of DMY‐Loaded Self‐Microemulsifying Drug Delivery System

Abstract

AbstractHyperlipidemia has become a common disease in modern society with its prevalence becoming relatively high in the world. A series of complications that accompany hyperlipidemia are seriously threatening individuals’ health. Dihydromyricetin (DMY) is a kind of polyphenol hydroxy (OH) dihydroflavonol extracted from the stems and leaves of Ampelopsis grossedentata. It has a variety of pharmacological activities. This study aims to develop a self‐microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of DMY, and to evaluate its hypolipidemic activity. The self‐microemulsion drug delivery system is composed of medium chain triglyceride (MCT, oil phase), Tween 80 (emulsifier), and PEG 200 (coemulsifier). The prepared DMY‐SMEDDS has stable physical and chemical properties, small droplet size (15.49 ±0.15 nm), good polydispersity index (PDI = 0.160 ± 0.010), negative zeta potential (−17.37 ± 0.09 mV), and high encapsulation efficiency (98.04 ± 0.25%). The results of in vitro dissolution and in vivo pharmacokinetics show that the prepared DMY‐SMEDDS significantly improve the solubility of DMY in aqueous medium, while its oral bioavailability is 2.34 times higher than that of free drug. In conclusion, the DMY‐SMEDDS prepared in this study prospectively improves the solubility and oral bioavailability of DMY also enhance the therapeutic effect.Practical Applications: This study is relevant in the sense that SMEDDS may be used as a new strategy to improve the oral bioavailability of hydrophobic drugs. This novel nanocarrier could increase (by 2.34 times) the relative bioavailability of oral DMY‐SMEDDS in rats comparative to dihydromyricetin (DMY) suspension. Thus, DMY‐SMEDDS may prospectively be applied in food, nutraceutical, and pharmaceutical industries in view of its biocompatible excipients and good stability.