Background: Poor water soluble compounds are difficult to develop as drug products using
conventional formulation techniques.
Objective: In the present study, the potential of Eudragit RS-100 nanosuspension as a new vehicle
for the improvement of the delivery of drugs to the intraocular level was investigated.
Methods: Solvent evaporation technique has been employed for nanosuspension preparation. Surfactant
concentration and drug to polymer ratio has been optimized using 32 factorial design to
achieve desired particle size, entrapment efficiency and percent permeation responses as dependent
variables. All the formulations were characterized for particle size, zeta potential, polydispersity index
(PDI), Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetery (DSC),
X-ray Diffraction (XRD) analysis, viscosity, antifungal study and Transmission Electron Microscopy
(TEM). Secondly, itraconazole eye drop was prepared by using sulfobuty ether-β-cyclodextrin
and comparatively studying its antifungal efficacy.
Results: The nanosuspension had a particle size range of 332.7-779.2nm, zeta potential
+0.609-16.3, entrapment efficiency 61.32 ± 1.36%-76.34 ± 2.04%. Ex vitro corneal permeability
study showed that optimized itraconazole nanosuspension produced higher permeation as compared
to the market formulation and Itraconazole eye drop. Moreover, optimized nanosuspension
was found as more active against Candida albicans & Aspergillus flavus compared to the market
formulation and Itraconazole eye drop.
Conclusion: The nanosuspension approach could be an ideal, promising approach to increase the
solubility and dissolution of Itraconazole.