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叶酸靶向的纳米结构脂质载体增强表没食子儿茶素没食子酸酯的口服递送。

Folate-targeted nanostructured lipid carriers for enhanced oral delivery of epigallocatechin-3-gallate.

机构信息

UCIBIO, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.

UCIBIO, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.

出版信息

Food Chem. 2017 Dec 15;237:803-810. doi: 10.1016/j.foodchem.2017.06.019. Epub 2017 Jun 6.

DOI:10.1016/j.foodchem.2017.06.019
PMID:28764070
Abstract

The well-known pleiotropic health benefits of green tea are mainly attributed to epigallocatechin-3-gallate (EGCG), a polyphenolic compound from the group of catechins. EGCG's poor stability and intestinal permeability, however, can strongly impair its biological activities. In this work, EGCG-loaded nanostructured lipid carriers (NLC) functionalized with folic acid were optimized through a Box-Behnken design intended to provide an enhanced oral absorption and increased bioavailability of EGCG. Size, zeta potential and encapsulation efficiency (EE) of the produced spherical nanoparticles were evaluated. NLC were further characterized by Differential Scanning Calorimetry (DSC). An in vitro release study in simulated gastric and intestinal fluids was conducted and the storage stability of the nanoparticles was evaluated over a period of 8weeks. The overall results demonstrated the suitability of the developed formulation for the oral delivery of EGCG and its potential for applications in food industry.

摘要

绿茶的多种有益健康的功效主要归因于表没食子儿茶素没食子酸酯(EGCG),一种来自儿茶素类的多酚化合物。然而,EGCG 较差的稳定性和肠道通透性会严重影响其生物活性。在这项工作中,通过 Box-Behnken 设计优化了负载 EGCG 的纳米结构化脂质载体(NLC),该设计旨在提供增强的口服吸收和提高 EGCG 的生物利用度。评估了所制备的球形纳米粒子的粒径、Zeta 电位和包封效率(EE)。通过差示扫描量热法(DSC)对 NLC 进行了进一步表征。在模拟胃液和肠液中进行了体外释放研究,并在 8 周的时间内评估了纳米粒子的储存稳定性。总的来说,这些结果表明,所开发的配方适合 EGCG 的口服递送,并有潜力应用于食品工业。

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