Title:Nanosuspension as an Efficient Carrier for Improved Ocular Permeation of Voriconazole
Volume: 22
Issue: 2
Author(s): Tang Qin, Zhu Dai*, Xiaodi Xu, Zilin Zhang, Xiangyu You, Hongmei Sun, Mingxing Liu and Hongda Zhu*
Affiliation:
- Pharmaceutical Department, Hubei Cancer Hospital, Wuhan,China
- School of Food and Biological Engineering, National “111” Center for Cellular Regulation and Molecular Pharmaceutics, Key Laboratory of Fermentation Engineering (Ministry of Education), Hubei Key Laboratory of Industrial Microbiology, Hubei University of Technology, Wuhan,China
Keywords:
Ophthalmic formulation, fungal keratitis, nanosuspension, voriconazole, Pharmasolve®, Eudragit RS100.
Abstract:
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.