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Current Pharmaceutical Biotechnology


ISSN (Print): 1389-2010
ISSN (Online): 1873-4316

Research Article

Nanosuspension as an Efficient Carrier for Improved Ocular Permeation of Voriconazole

Author(s): Tang Qin, Zhu Dai*, Xiaodi Xu, Zilin Zhang, Xiangyu You, Hongmei Sun, Mingxing Liu and Hongda Zhu*

Volume 22, Issue 2, 2021

Published on: 20 August, 2020

Page: [245 - 253] Pages: 9

DOI: 10.2174/1389201021999200820154918

Price: $65


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.

Keywords: Ophthalmic formulation, fungal keratitis, nanosuspension, voriconazole, Pharmasolve®, Eudragit RS100.

Graphical Abstract
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