Efficacy of Loteprednol Etabonate Drug Delivery System in Suppression of in vitro Retinal Pigment Epithelium Activation

Abstract

Choroidal neovascularization (CNV) is the growth of abnormal blood vessels in the choroid layer of the eye; it is a pathophysiological characteristic of wet age-related macular degeneration (AMD). Current clinical treatment utilizes frequent intravitreal injections, which can result in retinal detachment and increased ocular pressure. The purpose of the current study is to develop a novel drug delivery system of loteprednol etabonateencapsulated PEGylated PLGA nanoparticles incorporated into the PLGA-PEG-PLGA thermoreversible gel for treatment of AMD. The proposed drug delivery system was characterized for drug release, cytotoxicity studies and vascular endothelial growth factor (VEGF) suppression efficacy studies using ARPE-19 cells. The nanoparticles showed uniform size distribution with mean size of 168.60±23.18 nm and exhibited sustained drug release. Additionally, the proposed drug delivery system was non-cytotoxic to ARPE-19 cells and significantly reduced VEGF expression as compared to loteprednol etabonate solution. These results suggest the proposed drug delivery system can be used for further work in an animal model of experimental AMD with reduced intravitreal administration frequency. Keywords: Choroidal neovascularization, loteprednol etabonate, PLGA nanoparticles, thermoreversible gel, VEGF.