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<p>Superficial candidiasis caused by <i>Candida albicans</i> is a common fungal infection, with rising resistance to conventional antifungals such as fluconazole. Luliconazole (LUL), a potent imidazole antifungal, exhibits limited skin penetration, necessitating novel delivery systems to overcome this limitation and enhance its therapeutic efficacy. The objective of this study was to develop and optimize a LUL-loaded proniosomal gel (LPG) to enhance topical delivery and antifungal activity against fluconazole-resistant <i>Candida albicans</i>. A D-optimal design was employed for the evaluation of the influence of lecithin amount, surfactant amount, and surfactant type (Cremophor RH40 vs. Brij 57) on vesicle size, zeta potential, polydispersity index, and the entrapment efficiency. Then the optimized LUL formulations were characterized by TEM and FTIR. In-vitro LUL release, ex-vivo skin permeation test, and in-vivo LUL antifungal activity were measured in comparison with the commercial LUL cream. The optimized formulation (300&#xa0;mg lecithin, 1200&#xa0;mg Brij 57) produced nanosized vesicles (89.12&#xa0;nm), with high entrapment efficiency (74.58%) and stable zeta potential (-23.15 mV). In vitro, LPG achieved 98.5% release within 24&#xa0;h, significantly higher than 19% from the commercial cream due to enhanced vesicular dispersion and surfactant-mediated diffusion. Ex vivo studies showed significantly higher permeation (Jss = 283.3&#xa0;µg/cm²/h; Er = 20.99) and good skin deposition. The in-vivo experiments demonstrated a superior antifungal activity of the optimized LPG with a minimum inhibitory concentration of 10.67 ng/mL versus 98.33 ng/mL for the commercial cream for fluconazole-resistant <i>Candida</i>. So, the optimized formulation exhibited significantly enhanced ex vivo permeation (<i>p</i> &lt; 0.05) and a markedly reduced MIC value (<i>p</i> &lt; 0.01) compared to the commercial formulation. Histopathological and biomarker analysis confirmed reduced inflammation and fungal burden in gel-treated rats.</p>

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Luliconazole-loaded Proniosomal Gel for Enhanced Topical Delivery Against Fluconazole-resistant Candida albicans

  • 期刊论文

  • 发表日期：

    2026年5月4日

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  • Dina F. El-Bahr,
  • Rania S. Abdel-Rashid,
  • Rana Elshimy,
  • Shereen S. El-Mancy

摘要

Superficial candidiasis caused by Candida albicans is a common fungal infection, with rising resistance to conventional antifungals such as fluconazole. Luliconazole (LUL), a potent imidazole antifungal, exhibits limited skin penetration, necessitating novel delivery systems to overcome this limitation and enhance its therapeutic efficacy. The objective of this study was to develop and optimize a LUL-loaded proniosomal gel (LPG) to enhance topical delivery and antifungal activity against fluconazole-resistant Candida albicans. A D-optimal design was employed for the evaluation of the influence of lecithin amount, surfactant amount, and surfactant type (Cremophor RH40 vs. Brij 57) on vesicle size, zeta potential, polydispersity index, and the entrapment efficiency. Then the optimized LUL formulations were characterized by TEM and FTIR. In-vitro LUL release, ex-vivo skin permeation test, and in-vivo LUL antifungal activity were measured in comparison with the commercial LUL cream. The optimized formulation (300 mg lecithin, 1200 mg Brij 57) produced nanosized vesicles (89.12 nm), with high entrapment efficiency (74.58%) and stable zeta potential (-23.15 mV). In vitro, LPG achieved 98.5% release within 24 h, significantly higher than 19% from the commercial cream due to enhanced vesicular dispersion and surfactant-mediated diffusion. Ex vivo studies showed significantly higher permeation (Jss = 283.3 µg/cm²/h; Er = 20.99) and good skin deposition. The in-vivo experiments demonstrated a superior antifungal activity of the optimized LPG with a minimum inhibitory concentration of 10.67 ng/mL versus 98.33 ng/mL for the commercial cream for fluconazole-resistant Candida. So, the optimized formulation exhibited significantly enhanced ex vivo permeation (p < 0.05) and a markedly reduced MIC value (p < 0.01) compared to the commercial formulation. Histopathological and biomarker analysis confirmed reduced inflammation and fungal burden in gel-treated rats.