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用于提高绿茶表没食子儿茶素没食子酸酯生物利用度的纳米弹性体的配方与优化

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate.

作者信息

Mazyed Eman A, Helal Doaa A, Elkhoudary Mahmoud M, Abd Elhameed Ahmed G, Yasser Mohamed

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Kaferelsheikh University, Kaferelsheikh 33516, Egypt.

Department of Pharmaceutics, Faculty of Pharmacy, Fayoum University, Fayoum 63514, Egypt.

出版信息

Pharmaceuticals (Basel). 2021 Jan 15;14(1):68. doi: 10.3390/ph14010068.

DOI:10.3390/ph14010068
PMID:33467631
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7831059/
Abstract

The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate‎ (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 2 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted ‎for the estimation of EGCG‎. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.

摘要

本研究旨在探究纳米弹性体提升表没食子儿茶素没食子酸酯(EGCG)生物利用度的潜力。EGCG具有抗炎、抗氧化和抗肿瘤发生等重要作用。不幸的是,由于其渗透性有限且稳定性差,口服生物利用度较低。为克服这些缺陷,将EGCG制成纳米弹性体。纳米弹性体是由表面活性剂和边缘活化剂(EA)组成的柔性纳米囊泡。EA通过作为其囊泡膜的去稳定因子来提高弹性体的变形能力。根据二因素设计,采用乙醇注入法制备了负载EGCG的弹性体,以探究不同自变量对包封率(EE%)、12小时后药物释放百分比(Q)和粒径(PS)的影响。对优化配方进行了体外表征、离体肠道渗透试验和药代动力学研究。采用新开发的反相高效液相色谱(RP-HPLC)技术测定EGCG。优化配方(F4)显示出比相应的非离子型脂质体更长时间的药物释放,并且在EE%、渗透性、变形能力和稳定性方面有显著改善。药代动力学研究表明,F4比传统的非离子型脂质体和游离药物具有更持续的药物释放和更高的生物利用度。纳米弹性体可能是提高EGCG生物利用度的一种有前景的方法。

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