Novel Chitosan-Coated Niosomal Formulation for Improved Management of Bacterial Conjunctivitis: A Highly Permeable and Efficient Ocular Nanocarrier for Azithromycin

In the present study, we aimed to formulate, optimize, and characterize azithromycin chitosan coated niosomes (AZM-CTS-NSM) as a novel colloidal system that increases precorneal residence period, eye permeation, and bioavailability. AZM-NSM was formulated via a modified thin-film hydration strategy and then coated with CTS. We assessed the influence of the cholesterol: surfactant molar ratio, CTS concentration, and surfactant type on particle diameter, entrapment, zeta potential, and NSM adhesion force to the corneal mucosal membrane and employed a central composite design (CCD). The resulting optimized AZM-CTS-NSM has a mean diameter of 376 nm, entrapment of 74.2%, surface charge of 32.1 mV, and mucoadhesion force of 3114 dyne/cm(2). The optimized AZM-CTS-NSM demonstrated a prolonged in vitro release behavior. When compared with commercial eye drops, the optimized AZM-CTS-NSM produced a 2.61-fold increase in the apparent permeability coefficient, significantly improving corneal permeability. Additionally, ocular irritation was assessed, with no major irritant effects found to be induced by the formulated NSM. Compared with AZM commercial drops, the optimized AZM-CTS-NSM revealed > 3-fold increase in AZM concentration in the rabbit eyes. Collectively, these findings indicate that CTS-NSM is a potentially valuable ocular nanocarrier that could augment the efficacy of AZM. (C) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.

Automated summary

In this study, azithromycin chitosan coated niosomes (AZM-CTS-NSM) were formulated, optimized, and characterized as a novel colloidal system to improve precorneal residence time, eye permeation, and bioavailability. The optimized AZM-CTS-NSM demonstrated prolonged in vitro release behavior and enhanced corneal permeability, with minimal ocular irritation effects and significantly increased AZM concentration in rabbit eyes compared to commercial drops.