Development and characterization of miconazole nitrate transfersomal gel

Abstract

Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm to 931 nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. In 24 hrs the drug release was observed ranging from 79.08% to 88.72%. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, Miconazole nitrate in the form of transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier. When the data subjected to zero order and first order kinetics model, a linear relationship was observed with high R2 values for zero order model as compared to first order model and suggested that the formulations followed zero order sustained release.