Intravenous itraconazole emulsions produced by SolEmuls technology

Abstract

Itraconazole is a drug which is poorly soluble in both the water and oil phases of emulsions. Incorporation in parenteral emulsions was performed applying the SolEmuls Technology, i.e. localising the drug in the interfacial lecithin layer of the emulsions by homogenising a hybrid dispersion of oil droplets and drug nanocrystals in water. The maximum loading capacity of the emulsion system was found to be 10 mg/ml; at 20 mg/ml the loading capacity was exceeded leading to remaining drug nanocrystals in the emulsion. Incorporation of itraconazole into the lecithin layer led to an enhanced dispersion effect, i.e. with increasing drug concentration the droplet size of the emulsions decreased. Physical long-term stability of the optimum emulsion with 10 mg/ml could be shown over a period of 3 months at room temperature.