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BACKGROUND This study focused on the development of a self‐nanoemulsifying drug delivery system (SNEDDS) to improve, potentially, the solubility and oral bioavailability of liquiritin (LQ). METHODS: The solubility of LQ in different types of excipient, namely oils (OLs), emulsifiers (EMs), and co‐emulsifiers (CO‐EMs), was evaluated, and a pseudo‐ternary phase diagram (PTPD) and the formulation optimization were established. The prepared self‐nanoemulsifying drug delivery system of liquiritin (LQ‐SNEDDS) was assessed using droplet size (DS), zeta potential (ZP), polydispersity index (PDI), droplet morphology, drug release in vitro, and oral bioavailability. RESULTS: After the dilution of the LQ‐SNEDDS, a transparent nanoemulsion was obtained with an acceptable DS (24.70 ± 0.73 nm), ZP (−18.69 ± 1.44 mV), and PDI (0.122 ± 0.006). The LQ‐SNEDDS that was developed had a better release rate in vitro than the free LQ suspension. Pharmacokinetic evaluation showed that the relative oral bioavailability of LQ‐SNEDDS was increased by 5.53 times, and LQ‐SNEDDS exhibited a delayed half life and longer retention time in comparison with those of free LQ. Similarly, LQ‐SNEDDS had a better urate lowering effect and provided better organ protection than free LQ at the same dose (P < 0.05). CONCLUSIONS: The incorporation of LQ into SNEDDS could serve as a promising approach to improve the solubility, oral bioavailability, and anti‐hyperuricemic effect of LQ. © 2021 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Hyperlipidemia 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. [ABSTRACT FROM AUTHOR]