Stiff-Soft Hybrid Biomimetic Nano-Emulsion for Targeted Liver Delivery and Treatment of Early Nonalcoholic Fatty Liver Disease.

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Pharmaceutics Pub Date : 2024-10-07 DOI:10.3390/pharmaceutics16101303
Juan Li, Mingxing Yin, Maoxian Tian, Jianguo Fang, Hanlin Xu
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Abstract

Background: Nonalcoholic fatty liver disease (NAFLD) poses a risk for numerous metabolic diseases. To date, the U.S. Food and Drug Administration has not yet approved any medications for the treatment of NAFLD, for which developing therapeutic drugs is urgent. Dihydromyricetin (DMY), the most abundant flavonoid in vine tea, has been shown to be hepatoprotective. Its application was limited by low bioavailability in vivo; Methods: In order to improve the bioavailability of DMY and achieve liver-targeted delivery, we designed a DMY-loaded stiff-soft hybrid biomimetic nano drug delivery system (DMY-hNE). The in vivo absorption, distribution, pharmacokinetic profiles, and anti-NAFLD efficacy of DMY-hNE were studied; Results: DMY-hNE was composed of a stiff core and soft shell, which led to enhanced uptake by gastrointestinal epithelial cells and increased penetration of the mucus barrier, thus improving the in vivo absorption, plasma DMY concentration, and liver distribution versus free DMY. In an early NAFLD mouse model, DMY-hNE effectively ameliorated fatty lesions accompanied with reduced lipid levels and liver tissue inflammation; Conclusions: These findings suggested that DMY-hNE is a promising platform for liver drug delivery and treatment of hepatopathy.

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硬软混合仿生纳米乳液用于肝脏靶向输送和早期非酒精性脂肪肝的治疗
背景:非酒精性脂肪肝(NAFLD非酒精性脂肪肝(NAFLD)可引发多种代谢性疾病。迄今为止,美国食品和药物管理局尚未批准任何治疗非酒精性脂肪肝的药物。二氢杨梅素(DMY)是藤茶中含量最高的黄酮类化合物,具有保肝作用。但由于其在体内的生物利用度较低,其应用受到了限制:为了提高DMY的生物利用度并实现肝脏靶向给药,我们设计了一种DMY负载的软硬混合仿生纳米给药系统(DMY-hNE)。研究了DMY-hNE的体内吸收、分布、药代动力学特征和抗NAFLD的疗效:DMY-hNE由硬核和软壳组成,增强了胃肠道上皮细胞的摄取能力和粘液屏障的穿透力,因此与游离DMY相比,体内吸收、血浆DMY浓度和肝脏分布均有所改善。在早期非酒精性脂肪肝小鼠模型中,DMY-hNE 有效改善了脂肪病变,同时降低了血脂水平和肝组织炎症;结论:DMY-hNE 对非酒精性脂肪肝小鼠的治疗效果显著:这些研究结果表明,DMY-hNE 是一种很有前景的肝脏给药和肝病治疗平台。
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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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