Nanosuspension as an Efficient Carrier for Improved Ocular Permeation of Voriconazole.
BACKGROUND
The present limitations related to the ocular administration of antifungal drugs for the treatment of fungal keratitis include poor ocular bioavailability, limited retention time, and low ocular tissue penetration.


METHODS
This study aimed to prepare a novel ophthalmic voriconazole-loaded nanosuspension based on Eudragit RS 100. Pharmasolve® was explored as a corneal permeation enhancer in voriconazole ophthalmic formulation using in vitro and in vivo experiments. Briefly, 1% voriconazole-loaded nanosuspension was prepared using the quasi-emulsion solvent evaporation process.


RESULTS
Characterizations of the voriconazole-loaded nanosuspension by Zetasizer Nano ZS and Transmission Electron Microscope (TEM) showed a uniform spherical shape without any agglomeration. The well-discreted nanoparticle with a size of 138 ± 1.3 nm was achieved with high entrapment efficiency (98.6 ± 2.5%) and positive zeta potential in the range of 22.5-31.2mV, indicating excellent physical stability.


DISCUSSION
Voriconazole-loaded nanosuspension containing the penetration enhancer displayed good permeability both in vitro and in vivo compared with the commercial voriconazole injection. The voriconazole-loaded nanosuspension exhibited good antifungal activity, significantly inhibiting the growth of Candida albicans at a lower concentration of voriconazole (2.5μg/mL, p < 0.05).


CONCLUSION
In conclusion, the voriconazole-loaded nanosuspension containing Pharmasolve® can be used as an effective ophthalmic formulation for the topical ocular delivery of voriconazole.
['Qin|Tang|T|', 'Dai|Zhu|Z|', 'Xu|Xiaodi|X|', 'Zhang|Zilin|Z|', 'You|Xiangyu|X|', 'Sun|Hongmei|H|', 'Liu|Mingxing|M|', 'Zhu|Hongda|H|']
D060433:Administration, Ophthalmic D000818:Animals D000935:Antifungal Agents D002176:Candida albicans D003315:Cornea D004337:Drug Carriers D015821:Eye Infections, Fungal D005260:Female D008297:Male D053758:Nanoparticles D010316:Particle Size D010539:Permeability D051381:Rats D017207:Rats, Sprague-Dawley D065819:Voriconazole
nanosuspension voriconazole fungal keratitis Pharmasolve® Ophthalmic formulation Eudragit RS100