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.