Design and Evaluation of Eudragit RS-100 Based Itraconazole Nanosuspension for Ophthalmic Application

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 3<SUP>2</SUP> 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.

Itraconazole; eudragit RS-100; ex-vivo transconeal permeation; nanosuspension; pertinent; solvent evaporation.