Ocular delivery systems for fluconazole: obtention, characterization and in vitro/in vivo passive and iontophoretic delivery

Abstract

According to the World Health Organization corneal diseases are, following cataract, the second cause of blindness. Fungal infections in the cornea tissue (keratites) are more common in tropical and subtropical regions, as Brazil. Fluconazol (FLU) is one of the most used drug on keratite’s treatment, although when it is administred topically it does not achieve therapeutic concentration. It is then often administered subconjuntively or intravitreal, that, besides offering great risk of complications, even more after repetitive doses, they provide pain and discomfort for patients. In this way, this project proposes the development and the characterization of topical formulations applied passively and by iontophoresis for ocular administration of FLU. Hydrophilic gels and particulated systems, as microparticles, will be evaluated. It is intended with those formulations and iontophoresis (appliance of a weak electric current) to improve FLU permeation in the corneal tissue, as well as its residence time, reducing consequently high dosages and repetitive administration. (AU)