Efficient intra ocular delivery of polyphenols using nanoparticulate systems

Abstract

Glaucoma is the second most leading cause of blindness globally. Several studies were proved that free radicals are one of the major reasons for increasing glaucoma patient by increasing intra ocular pressure (IOP). Hence, potent anti-oxidants are suitable and focused for the prevention/ treatment of glaucoma. Resveratrol (RES) and quercetin (QUR) are the most attracting polyphenolic anti-oxidant molecules and also showed efficiency in reducing IOP. But they showed stumpy efficiency due to low solubility and permeability. Therefore, focused on novel approaches might improve the therapeutic efficacy of these compounds. Hence, the aim of the present study is to develop and characterize RES/QUR loaded polyethylene glycol (PEG) newlinemodified chitosan (CS) nanoparticles (NPs) and RES loaded biodegradable temperature-pH responsive pluronic F-127-grafted-peptide P11 nanodispersion (ND) to reduce the IOP for the treatment of glaucoma. Formulated PEG modified CS NPs showed controlled release, isoosmolar, and improved permeation of drugs. Ocular tolerance of the NPs was evaluated using Hen s egg test on the chorioallantoic membrane and it showed that the NPs were non-irritant. FITC loaded PEG modified CS NPs crossed the cornea and reached upto retinal choroid. RES/QUR loaded PEG modified CS NPs reduced the IOP by 4.3±0.5 mmHg and 3.7±0.5mmHg respectively upto 8hr in normotensive rabbits. The developed NPs have efficient delivery of RES/QUR for the treatment of glaucoma. newline newline