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Encapsulation of esculetin into DSPE-MPEG2000 carrier was performed to improve its water solubility and oral bioavailability, as well as enhance its anti-inflammatory effect on a mouse model of ulcerative colitis that was induced with dextran sulphate sodium (DSS). We determined the in-vitro and in-vivo high-performance liquid chromatographic (HPLC) analysis method of esculetin; Esculetin-loaded nanostructure lipid carrier (Esc-NLC) was prepared using a thin-film dispersion method, wherein a particle size analyser was used to measure the particle size (PS) and zeta potential (ZP) of the Esc-NLC, while a transmission electron microscope (TEM) was employed to observe its morphology. Also, HPLC was used to measure its drug loading (DL), encapsulation efficiency (EE) and the in-vitro release of the preparation, as well as investigate the pharmacokinetic parameters. In addition, its anti-colitis effect was evaluated via histopathological examination of HE-stained sections and detection of the concentrations of tumour necrosis factor-alpha (TNF-α), interleukin (IL)-1 beta (β), and IL-6 in serum with ELISA kits. The PS of Esc-NLC was 102.29 ± 0.63 nm with relative standard deviation (RSD) of 1.08% (with poly-dispersity index-PDI of 0.197 ± 0.023), while the ZP was −15.67 ± 1.39 mV with RSD of 1.24%. Solubility of esculetin was improved coupled with prolonged release time. Its pharmacokinetic parameters were compared with that of free esculetin, wherein the maximum concentration of the drug in plasma was increased by 5.5 times. Of note, bioavailability of the drug was increased by 1.7 times, while the half-life was prolonged by 2.4 times. In the anti-colitis efficacy experiment, the mice in Esc and Esc-NLC groups exhibited significantly reduced levels of TNF-α, IL-1β, and IL-6 in their sera comparable to the DSS group. Colon histopathological examination revealed that mice with ulcerative colitis in both Esc and Esc-NLC groups displayed improved inflammation, amid the Esc-NLC groups having the best prophylactic treatment effect. Esc-NLC could ameliorate DSS-induced ulcerative colitis by improving bioavailability, prolonging drug release time and regulating cytokine release. This observation confirmed the potential of Esc-NLC to reduce inflammation in ulcerative colitis, albeit the need for follow-up research to verify the application of this strategy to clinical treatment of ulcerative colitis. [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]