Formulation And Evaluation of Ketoconazole Microemulsion-Loaded Hydrogel with Olive Oil as a Penetration Enhancer

Abstract

The aim of the present research work was to develop ketoconazole microemulsion‐ loaded hydrogel formulation containing olive oil as permeation enhancer. Screening of oils, surfactants, and cosurfactants were done based on solubility studies. The microemulsion was characterized for optical transparency, Cannoning electron microscopy, zeta potential, % drug content, dilutability and Dispersion  Stability. In-vitro drug release studies were carried out using Franz diffusion cells using porcine skin membrane. The Carbopol 934P, Xanthan gum and HPMC-K100M as a gelling agent were used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. Three formulation were prepared of ketoconazole loaded microemulsion (KM1-KM3) with different concentration of olive oil. The SEM image of optimized best formulation showed that globules were spherical in shape and had smooth surface. Zeta potential result of optimized microemulsion (KM2) and its diluted form (100 times diluted with 0.1N HCl) was found to be -4.37mV. The medication content of KM-2 was 97.44±0.54% higher than that of other formulations. Out of all the formulations, formulation KM-2 had the highest penetration flux, measuring µg/cm2/hour. Over a 24-hour period, KM-2 tracked the zero-order release (r2 = 0.941). The KT-loaded microemulsion-based hydrogel gel formulation seemed to be a homogeneous, thick semisolid with the appropriate homogeneity and clarity upon visual inspection. Using an accelerated temperature investigation, the generated microemulsion formulations' stability was evaluated.  For up to three months, stability tests were conducted on the drug concentration, pH, and viscosity of the optimal formulation, KMG-3, at 40 °C/75% RH. The current work demonstrated significantly enhanced skin penetration of the microemulsion and enabled its use in transdermal medication delivery.  Considerable research has not yet been done to expand and examine its potential uses as a novel transdermal medication delivery technology.