Liposomes as an ocular delivery system for fluconazole: in-vivo study

ABSTRACT

The purpose of this study was to formulate topically effective controlled release ophthalmic fluconazole liposomal formulations using the reverse-phase evaporation technique. Soya bean phosphatidylcholine [PC] and cholesterol [Ch] in specific weight ratios were used. Selected formulations were tested for their in-vivo ocular antifungal effect. These included the neutral, the positively [using stearyl amine] and the negatively [using dicetyl phosphate] charged liposomes. A reproducible model of Candida keratitis in rabbits was performed and the effects of the prepared liposomes were better than a solution of fluconazole. The order of fluconazole liposomal formulations according to the time to achieve complete healing is arranged in a descending order negatively charged liposomes > positively charged liposomes > neutral liposomes [74] > neutral liposomes [55] > fluconazole solution. The frequency of instillation was decreased; also, the time of ulcer healing was decreased. It was concluded that the use of liposomes as a drug delivery system could contribute to the enhancement of the effect of fluconazole in the eye