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

Abstract

(-)-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.

Keywords

• EGCG
• Glucose-modified liposomes
• Brain targeting
• Antioxidant
• Neuroprotection