Aim: This investigation aimed to develop a voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat fungal keratitis. Methods: Microemulsions were prepared using water titration, and the optimized microemulsion was coated with chitosan to prepare CVME. The physicochemical parameters, ocular irritation potential, in vitro antifungal efficacy and in vitro release studies were performed. The in vivo antifungal efficacy study was conducted in a fungal infection-induced rabbit eye model. Results: The developed CVME displayed acceptable physicochemical properties and excellent mucoadhesive behavior and showed a sustained release profile. Ex vivo and in vivo studies concluded that higher permeability and improved antifungal efficacy were observed for CVME than drug suspension (DS). Conclusion: The prepared CVME7 is a viable alternative to treating fungal keratitis with existing approaches.
Keywords: anti-fungal; cationic microemulsion; chitosan-coated microemulsion; cremophore EL; fungal keratitis; linoleic acid; mucoadhesive; ocular irritation; propylene glycol; voriconazole.
Nanotechnology can help resolve problems that are currently associated with eye medications. Microemulsions (MEs) are mixtures containing tiny droplets of oil and water, which are made stable by ingredients called surfactants (meaning a type of soap) and co-surfactants. The ability for medications to be released slowly in MEs makes them suitable for eye medications because they reduce the number of times eye drops need to be used each day. This study wanted to create a medicine called voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat a fungal infection in the eye called keratitis. We made MEs by gradually adding a combination of oil, surfactant, and water together. Then, we coated the best MEs with a substance called chitosan to make CVME. We tested its physical and chemical properties, whether it irritated the eyes, how well it could fight fungus, and how it released medicine. We tested CVME on rabbits with a fungal eye infection. CVME had good physical and chemical properties and stuck well to the mucus on the surface of the eyes. It released the medicine slowly. The system created in this study is very important for treating fungal infections because it helps the medicine stay on the eye surface longer and allows it to better reach the infected areas of the eye. CVME7 might be a better option for treating fungal keratitis instead of other methods that are currently used.