Formulation and Antifungal Activity of Nanoliposomal Nystatin

Nystatin, a tatraene diene polyene antibiotic, has a broad spectrum of activity, but due to its low solubility in injectable solvents and toxicity limits its use in the treatment of systemic fungal infections. Liposome-based systems have been used to enhance efficacy and/or ameliorate toxicity of certain drugs [1,2]. Liposomes have been used to formulate a variety of hydrophobic, poorly soluble drugs [3,4]. Therefore formulation of nystatin in concentrated pharmaceutical delivery systems for parenteral administration is very difficult. One way of improving the solubility of drug is to formulate it into liposomes (Zhang et al. 2004). In this study, formulation of nystatin into liposome with or without cholesterol was prepared and characterized. The highest encapsulation efficacy of nystatin into liposomes was obtained with a cholesterol /DPPC. The encapsulation efficacy was decreased by DSPC and improved by addition of cholesterol. In liposomes composed of dipalmitoylphosphatidylcholine (DPPC)/cholesterol, the highest encapsulation efficiency of nystatin liposomes was achieved by the addition of cholesterol and hydration with 9% sucrose solution, as compared with lipid without cholesterol. The highest encapsulation efficiency is 70%. The best formulation contains liposomes of uniform size distribution (<400nm). Long term stability studied indicate that the lyophilized liposomal nystatin is physically and chemically stable for at least 8 month at -40°C. Anti fungal activity in vitro (MIT test) has shown liposomal nystatin was found to be more effective than free nystatin against candida

کلیدواژه ها:

Liposome ، stability ، lyophilization ، antifungal activity