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在模拟胃肠消化中具有缓释性能的磷脂酰胆碱-表没食子儿茶素没食子酸酯纳米粒的制备及其在Caco-2单层模型中的跨细胞通透性

Fabrication of phosphatidylcholine-EGCG nanoparticles with sustained release in simulated gastrointestinal digestion and their transcellular permeability in a Caco-2 monolayer model.

作者信息

Zhang Mengya, Su Yujie, Li Junhua, Chang Cuihua, Gu Luping, Yang Yanjun

机构信息

State Key Laboratory of Food Science and Resources, School of Food Science and Technology; Collaborative Innovation Center of Food Safety and Quality Control in Jiangsu Province, Jiangnan University, Wuxi, Jiangsu 214122, China.

State Key Laboratory of Food Science and Resources, School of Food Science and Technology; Collaborative Innovation Center of Food Safety and Quality Control in Jiangsu Province, Jiangnan University, Wuxi, Jiangsu 214122, China.

出版信息

Food Chem. 2023 Sep 25;437(Pt 1):137580. doi: 10.1016/j.foodchem.2023.137580.

DOI:10.1016/j.foodchem.2023.137580
PMID:39491254
Abstract

In this study, we prepared phosphatidylcholine (PC)-EGCG complex nanoparticles (P-E NPs) by solvent reflux method. The physicochemical properties, in vitro digestion, uptake in Caco-2 cells, and bidirectional permeability of P-E NPs were systematically investigated. The constructed P-E NPs had an average particle size of 118 nm, a ζ-potential of -37.8 mV, and a polymerization dispersion index (PDI) of 0.16. The encapsulation efficiency (EE) of EGCG was 85.0% and the loading capacity (LC) was 24.4%. UV spectra, FTIR, XRD and intermolecular force results indicated that hydrophobic, electrostatic and hydrogen bonding interactions contributed to formate P-E NPs. P-E NPs exhibited first-order kinetics sustained release properties in simulated gastrointestinal digestion. Furthermore, P-E NPs were able to enhance absorptive transport and inhibit efflux transport mediated by MRP2 and P-gp compared to EGCG. These results indicated that P-E NPs may be a potential strategy to ameliorate EGCG bioavailability.

摘要

在本研究中,我们采用溶剂回流法制备了磷脂酰胆碱(PC)-表没食子儿茶素没食子酸酯(EGCG)复合纳米粒(P-E NPs)。系统研究了P-E NPs的理化性质、体外消化、在Caco-2细胞中的摄取以及双向通透性。所构建的P-E NPs平均粒径为118 nm,ζ电位为-37.8 mV,聚合分散指数(PDI)为0.16。EGCG的包封率(EE)为85.0%,载药量(LC)为24.4%。紫外光谱、傅里叶变换红外光谱、X射线衍射和分子间作用力结果表明,疏水、静电和氢键相互作用有助于形成P-E NPs。P-E NPs在模拟胃肠消化中表现出一级动力学缓释特性。此外,与EGCG相比,P-E NPs能够增强吸收转运并抑制由多药耐药相关蛋白2(MRP2)和P-糖蛋白(P-gp)介导的外排转运。这些结果表明,P-E NPs可能是改善EGCG生物利用度的一种潜在策略。

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