International Journal of Biological Macromolecules 2015-01-01

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

Yashpal S Chhonker, Yarra Durga Prasad, Hardik Chandasana, Akhilesh Vishvkarma, Kalyan Mitra, Praveen K Shukla, Rabi S Bhatta

Index: Int. J. Biol. Macromol. 72 , 1451-8, (2014)

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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 Amphotericin-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) by nanoparticles prepared from low molecular weight chitosan as compared with marketed formulation.Copyright © 2014. Published by Elsevier B.V.