Fluconazole-loaded liposomes for ocular delivery: characterization and antifungal activity

ABSTRACT

Fluconazole loaded liposomes were prepared using reverse phase evaporation technique for ocular delivery of the drug. Characterization of fluconazole liposomes including; particle size and physical morphology were studied. The effects of different variables [cholesterol weight ratio and charge type] on the loading efficiency of liposomes as well as particle size were determined. Inclusion of cholesterol in liposomal formulations improved the encapsulation of fluconazole into liposomes at certain Phosphatidylcholine Cholesterol [PC Ch] weight ratios further increase in cholesterol content resulted in a decrease in the encapsulation percent of the drug. A significant increase in the encapsulation at ratio 73 was noticed. At ratio 76, the encapsulation significantly decreased. Incorporation of stearylamine [SA] into liposomes decreased the loading efficiency of fluconazole at ratio [PC Ch SA] 5 5 0.25 followed by insignificant increase in the entrapment of the drug into liposomes at ratio 5 5 0.5. On the other hand, addition of dicetyl phosphate [DP] into liposomes resulted in a significant increase in fluconazole encapsulation into liposomes at all tested [PC Ch DP] ratios. The loading efficiency of the neutral liposomes was found to be in between those of positively and negatively charged liposomes. The particle size studies showed that, increasing cholesterol amount, led to an increase in the particle size. While increasing stearylamine and dicetyl phosphate led to decrease in the particle size of liposomes. An in-vitro study was done to know the effect of fluconazole loaded liposomes on different fungi isolated from eye