Studies on Polymeric and Lipid Nanoparticles of Ketoconazole for Ocular Administration

Abstract

The fungistatic molecule ketoconazole was incorporated into polymeric (Eudragit (R) RS 100) and solid lipid (Gelucire (R) 44/14) nanoparticles by quasi-emulsion solvent evaporation technique aiming ocular application. Characterization of ketoconazole nanoparticles were analyzed by particle size, polydispersity index, zeta potential, DSC, FT-IR and C-13 NMR, flow cytometry, entrapment efficacy and pH analyses. Nanoparticles were stored at 4 +/- 1 degrees C, 25 +/- 1 degrees C and 40 +/- 1 degrees C for the 3 months. During storage period, particle sizes were 111.93-802.57 nm except one formulation, polydispersity indexes were 0.42-0.90, pH values were 6.1-6.9 and zeta potential values were +42 mV, +65 mV for polymeric nanoparticles. High entrapment efficiencies were obtained for the formulation prepared (86.45-93.15%) except one formulation. Cytotoxicity analyses which are carried out 3T3 mouse fibroblast cells showed viability of 90.0-98.1%. As a result of the analyses polymeric nanoparticles could be better drug delivery systems for the ocular application of ketoconazole.