Anti‐Atherogenic Effects of Lesion‐Targeted Epigallocatechin Gallate (EGCG) ‐ Loaded Nanoparticles

Objectives Macrophages are determinant cells for atherosclerotic lesion formation. The objectives of this study were to incorporate macrophage target ligands on the surface of biocompatible and biodegradable epigallocatechin gallate (EGCG)‐loaded nanoparticles (Enano), to evaluate their target specificity to macrophages and anti‐atherogenic effects in vitro and in vivo . Method The target specificity to macrophages ( in vitro ) and to atherosclerotic lesions in low density lipoprotein receptor knockout (LDLr‐/‐) mice was measured using a fluorescence microscopy and IVIS® in vivo imaging system, respectively. Macrophage cholesterol content was determined using a HPLC method, and macrophage monocyte chemoattractant protein 1 (MCP‐1) release was measured using an ELISA kit. After treating LDLr‐/‐ mice with EGCG, untargeted Enano, targeted Enano, void untargeted nano, void targeted nano, or saline via weekly intravenous injection for 20 weeks, atherosclerotic lesion area and inflammatory response were determined. Results As compared to untargeted Enano, targeted Enano significantly increased their binding affinity to THP‐1 macrophages, increased macrophage EGCG content and decreased macrophage cholesterol content and macrophage release of MCP‐1 image The targeted Enano improved the target specificity to atherosclerotic lesions, and decreased atherosclerotic lesion area and inflammatory response in LDLr‐/‐ mice image Conclusions Targeted nanoparticles represent a potential breakthrough in molecular imaging of atherosclerosis and have a potential for the prevention and treatment of atherosclerosis.