Development, Optimization, and Antifungal Assessment of Ocular Gel Loaded With Ketoconazole Cubic Liquid Crystalline Nanoparticles

Ketoconazole is a drug that belongs to azole antifungal group. The current available marketed products of ketoconazole are accompanied with potential drawbacks such as short retention time at the eye surface and eye irritation. The aim of this research is to find a solution for the previously mentioned limitations through loading of ketoconazole within cubosomes (KZ-Cub) to be used as ophthalmic drug delivery systems. Cubosomes properties will help to keep the encapsulated drug in the solubilized form. Further incorporation of cubosomes into biodegradable polymer based gel could prolong the ocular retention time of the drug. Three studied independent variables included glyceryl-mono-oleate, Pluronic-F127 and Polyvinyl alcohol percentage with respect to the dispersion media, while particle size, entrapment efficiency and stability index were the dependent variables that have been evaluated. The optimized cubosomes was assessed for its in-vitro and in-vivo antifungal activity. The prepared gel loaded with KZ Cub formula had an enhanced permeability, ocular availability, antifungal activity and significant decrease in MIC values compared to commercial one, which reflected the strong impact on the activity of KZ in the management of eye infection. (C) 2021 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.

Automated summary

This research aims to address the limitations of current marketed ketoconazole products by developing a new ophthalmic drug delivery system using cubosomes. The inclusion of ketoconazole in cubosomes within a biodegradable gel resulted in enhanced drug permeability, ocular availability, and antifungal activity, showing promising potential for managing eye infections.