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Pharmaceutics 2018, 10(1), 26; https://doi.org/10.3390/pharmaceutics10010026

Design, Optimization and Characterization of a Transfersomal Gel Using Miconazole Nitrate for the Treatment of Candida Skin Infections

1
Department of Pharmaceutics, Faculty of Pharmacy, Sinai University, Alarish, North Sinai 45511, Egypt
2
Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk 471, Saudi Arabia
3
Department of Pharmaceutics, Faculty of Pharmacy, Port Said University, Port Said 42511, Egypt
4
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Damanhour University, Damanhour 22511, Egypt
5
Department of Pharmaceutics, Faculty of Pharmacy, The British University in Egypt, Cairo 11837, Egypt
*
Authors to whom correspondence should be addressed.
Received: 19 January 2018 / Revised: 17 February 2018 / Accepted: 20 February 2018 / Published: 23 February 2018
(This article belongs to the Special Issue Lipid-Based Dosage Form)

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. View Full-Text
Keywords: Transfersomes; miconazole nitrate; antifungal activity; entrapment efficiency; Carbapol 934 Transfersomes; miconazole nitrate; antifungal activity; entrapment efficiency; Carbapol 934
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Qushawy, M.; Nasr, A.; Abd-Alhaseeb, M.; Swidan, S. Design, Optimization and Characterization of a Transfersomal Gel Using Miconazole Nitrate for the Treatment of Candida Skin Infections. Pharmaceutics 2018, 10, 26.

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