Preparation of a novel brain-targeted EGCG liposome and its antioxidative neuroprotection

作者：Xia Chen, Chunmei Gu, Gang Liu, Jiayuan Zhao, Siqi Wang, Chunyan Yang, Yongqing Zhu, Junlin Deng, Zuoya Xiang, Manyou Yu, Yi Guo, Yong Wu, Chen Jian · 发表于：Journal of Functional Foods · 年份：2023 · DOI：10.1016/j.jff.2023.105911 · 被引用次数：12 · 研究领域：Tea Polyphenols and Effects、Nanoparticle-Based Drug Delivery、Advanced Drug Delivery Systems

(-)-Epigallocatechin-3-gallate (EGCG) possesses potent antioxidant and neuroprotective properties. In this study, a novel glucose-modified EGCG encapsulated liposome (EGCG-Glu-Lip) was developed and characterized. EGCG-Glu-Lip liposome’s cytotoxicity, brain targeting ability, and its antioxidative neuroprotection were examined via bEnd.3 and PC12 cells testing. EGCG-Glu-Lip liposome particle mean size was 158.7 nm, with encapsulation efficiency 73.05 % under EGCG/lipid mass ratio 1:22 and soybean phospholipids (SPC) to cholesterol (Chol) mass ratio 3.84:1. EGCG-Glu-Lip exhibited less cytotoxicity, stronger protection to PC12 cells from H2O2 induced oxidative damage, keeping reactive oxygen species (ROS) level. Glucose modified liposome (Glu-Lip) cellular uptake in bEnd.3 and PC12 cells were 1.5-fold and 1.3-fold higher than that of Lip, supporting EGCG-Glu-Lip possessing enhanced blood–brain barrier (BBB) permeability mediated via glucose transporter protein 1 (GLUT1) and neuronal cell uptake for brain targeting. EGCG-Glu-Lip could provide an efficient nano delivery pathway to deliver sufficient EGCG to brain tissue exerting its antioxidative neuroprotection more efficiently.