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<p>The present study aimed to develop and optimize bifonazole transethosomes (BFZ-TES) using a 3<sup>2</sup> factorial design to improve skin permeability, enhancing efficacy while addressing the limitations of conventional formulations by converting them into a transethosomal gel. BFZ-TES was formulated using a modified cold technique, and the 3<sup>2</sup> factorial design evaluated the effects of independent variables. The formulations underwent physicochemical characterization and were incorporated into a 1.5% Carbopol 934 gel base. Parameters such as homogeneity, spreadability, pH, viscosity, drug content, in vitro drug release, ex vivo drug permeation, goat skin histopathology, and in vitro antifungal activity were assessed, comparing the optimized formulation with a 1% conventional bifonazole cream. The BFZ-TES formulations exhibited encapsulation efficiency (66.0 ± 2.64% to 85.1 ± 1.01%), vesicle sizes (162 ± 1.30 to 281.9 ± 1.40&#xa0;nm), and a polydispersity index below 1. The optimized formulation showed a vesicle size of 162 ± 1.30&#xa0;nm, zeta potential of − 26.07&#xa0;mV, and %EE of 77.6 ± 0.72. TEM images confirmed uniform, spherical vesicles. The optimized BFZ gel demonstrated 91.2% in vitro drug release over 12&#xa0;h, significantly outperforming traditional cream (41.1%). Ex vivo studies revealed enhanced drug permeation, with a 1.56-fold increase in steady-state flux compared to the conventional gel and a 1.90-fold increase over marketed cream. Histopathology confirmed its safety for topical application. The optimized BFZ gel showed higher antifungal activity than marketed formulation as determined by zone of inhibition. The results of skin irritancy studies revealed that the BFZ-TES formulation (PDII = 0.49) is safe and non-toxic to the skin. These findings revealed that incorporating BFZ into a transethosomal gel effectively overcomes the stratum corneum barrier, improves drug permeability, prolongs release, and enhances antifungal efficacy.</p> Graphical Abstract <p></p>

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Formulation Optimization and Characterization of Bifonazole-Loaded Transethosomal Gel by 32 Factorial Design for the Treatment of Topical Fungal Infection

  • 期刊论文

  • 发表日期：

    2025年8月9日

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  • Umeshkumar Dinesh Patel,
  • Vinayak Shivamurthi Mastiholimath

摘要

The present study aimed to develop and optimize bifonazole transethosomes (BFZ-TES) using a 32 factorial design to improve skin permeability, enhancing efficacy while addressing the limitations of conventional formulations by converting them into a transethosomal gel. BFZ-TES was formulated using a modified cold technique, and the 32 factorial design evaluated the effects of independent variables. The formulations underwent physicochemical characterization and were incorporated into a 1.5% Carbopol 934 gel base. Parameters such as homogeneity, spreadability, pH, viscosity, drug content, in vitro drug release, ex vivo drug permeation, goat skin histopathology, and in vitro antifungal activity were assessed, comparing the optimized formulation with a 1% conventional bifonazole cream. The BFZ-TES formulations exhibited encapsulation efficiency (66.0 ± 2.64% to 85.1 ± 1.01%), vesicle sizes (162 ± 1.30 to 281.9 ± 1.40 nm), and a polydispersity index below 1. The optimized formulation showed a vesicle size of 162 ± 1.30 nm, zeta potential of − 26.07 mV, and %EE of 77.6 ± 0.72. TEM images confirmed uniform, spherical vesicles. The optimized BFZ gel demonstrated 91.2% in vitro drug release over 12 h, significantly outperforming traditional cream (41.1%). Ex vivo studies revealed enhanced drug permeation, with a 1.56-fold increase in steady-state flux compared to the conventional gel and a 1.90-fold increase over marketed cream. Histopathology confirmed its safety for topical application. The optimized BFZ gel showed higher antifungal activity than marketed formulation as determined by zone of inhibition. The results of skin irritancy studies revealed that the BFZ-TES formulation (PDII = 0.49) is safe and non-toxic to the skin. These findings revealed that incorporating BFZ into a transethosomal gel effectively overcomes the stratum corneum barrier, improves drug permeability, prolongs release, and enhances antifungal efficacy.

Graphical Abstract