Amphotericin-B entrapped lecithin/chitosan nanoparticles for prolonged ocular application

Abstract

Fungal keratitis is the major cause of vision loss worldwide. Amphotericin-B is considered as the drug of choice for fungal infections. However, its use in ophthalmic drug delivery is limited by the low precorneal residence at ocular surface as a result of blinking reflex, tear turnover and nasopharyngeal drainage. We report Amphotericn-B loaded lecithin/chitosan nanoparticles for prolonged ocular application. The prepared nanoparticles were in the size range of 161.9–230.5 nm, entrapment efficiency of 70–75%, theoretical drug loading of 5.71% with positive zeta potential of 26.6–38.3 mV. As demonstrated by antifungal susceptibility against Candida albicans and Aspergillus fumigatus, nanoparticles were more effective than marketed formulation. They exhibited pronounced mucoadhesive properties. In-vivo pharmacokinetic studies in New Zealand albino rabbit eyes indicated improved bioavailablity (~2.04 fold) and precorneal residence time (~3.36 fold) of nanoparticles prepared from low molecular weight of chitosan as compared with marketed formulation.