MICROPARTICULATE DRUG DELIVERY SYSTEM FOR TOPICAL ADMINISTRATION OF ITRACONAZOLE

Abstract

The purpose of the present study was to formulate microemulsion based gel for topical delivery of water insoluble antifungal agent Itraconazole with an aim to increase its penetration through skin and thereby its flux. Pseudoternary phase diagrams were constructed to identify microemulsion existing region using various combinations of surfactant and cosurfactant with oil and water. Solubility of drug in various oils was determined to select the suitable oil having maximum solubilizing capacity for I t raconazole. Different formulations so formed were evaluated for phase separation, isotropic nature, clarity and part icle size analysis and opt imized formulat ions were selected for formulat ing microemulsion based gel using 0.75% w/ w of carbopol 934P NF. The microemulsion-based gels were evaluated for rheological behavior , in- vit ro permeat ion studies and in- vit ro ant ifungal act ivit y. The in- vit ro permeat ion studies was carried out on human cadaver skin, mounted on Keshary-Chien diffusion cell using 10% v/v methanolic solut ion of pH 1.2 phosphate buffer as diffusion medium and Candida albicans as a model fungus to evaluate the ant ifungal act ivity of I t raoconazole through the opt imized formulat ions using cup plate method. Stat ist ically significant increase in in- vit ro permeat ion rate was found among the laboratory microemulsion based gel formulated when compared with convent ional cream formulat ion. The rheological behavior of the prepared systems showed pseudoplast ic ( shear thinning) flow pat tern. The invitro antifungal activity of Itraconazole was found to be significant with microemulsion based gel. Thus it can be concluded that microemulsion based gel is better choice of vehicle for delivery of Itraconazole as topical drug delivery system.