Abstract
Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. 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 evaluated in comparison with a marketed product (Daktarin® cream 2%) for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro and in vivo antifungal activity. The prepared MIC Transfersomes had a high EE% ranging from (67.98 ± 0.66%) to (91.47 ± 1.85%), with small particle sizes ranging from (63.5 ± 0.604 nm) to (84.5 ± 0.684 nm). The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. 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). The prepared MIC transfersomal gel showed higher antifungal activity than Daktarin® cream 2%. Therefore, miconazole nitrate in the form of Transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier.
Highlights
Fungal infections are superficial infections which occur in the skin, nails, and mucous membranes
Topical treatment of fungal infections is usually preferred as opposed to systemic treatment, as the drug is delivered directly to the infected site, with decreased side effects and improved patient compliance [2]
The stratum corneum, which is the outermost layer of the skin, represents the main barrier for drug penetration
Summary
Fungal infections are superficial infections which occur in the skin, nails, and mucous membranes. Candidiasis is one of the most widespread types of superficial fungal infections, and can invade into deep tissue in cases of weakness in the immune system. It usually affects wet, warm, and furrowed areas such as the underarms and intergluteal areas [1]. Topical treatment of fungal infections is usually preferred as opposed to systemic treatment, as the drug is delivered directly to the infected site, with decreased side effects and improved patient compliance [2]. The stratum corneum, which is the outermost layer of the skin, represents the main barrier for drug penetration. It is necessary to design a drug delivery system for antifungal drugs which has the ability to overcome the barrier properties of the stratum corneum [2,3]
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