Preparation of Ketoconazole-Loaded Nanoemulsions for Ophthalmic Delivery: Characterization and in-vitro Antifungal Activity Evaluation

Abstract

Background: Nanoemulsions (N.E.s) capable of ocular bioavailability elevation can be used for poor water-soluble drugs such as ketoconazole (K.Z.). The current investigation was designed for the purpose of overcoming this issue by developing K.Z. containing N.E.s for ophthalmic drug delivery with appropriate therapeutic efficiency. Methods: The preparation of ketoconazole N.E.s was performed by the low-energy technique. According to the phase diagram, three stable formulations were selected for more physicochemical analyses, including particle size, polydispersity index, pH, refractive index, osmolality, and viscosity. Finally, drug release patterns and in-vitro antifungal activity were assessed for the final selected formulation. Results: The developed N.E. formulations with droplet sizes less than 20nm showed appropriate physicochemical characteristics for ocular delivery. The selected formulation released 100% of the encapsulated drug during 24 h. Moreover, antifungal assessments showed that prepared N.E. had acceptable in vitro antifungal activity. Conclusions: Based on our findings, it can be concluded that N.E.s could be applied as effective carriers for the ophthalmic delivery of ketoconazole.