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<p>Ketoconazole (KTZ) functions by suppressing the propagation of ergosterol, an essential element of the fungal cell membrane. However, its conventional topical delivery is often limited by less skin retention due to early drainage and washout. The objective of the present investigation was to fabricate a skin-targeting KTZ-loaded nanostructured lipid carriers (NLCs) with squalene, and thus the localized action. The NLCs were developed and characterized on various parameters like particle size, PDI, and %EE. The Box-Behnken design (BBD) was employed to effectively fabricate KTZ-loaded NLCs with squalene and Vitamin E TPGS for optimal formulation attributes. <i>In vitro</i> drug release of optimized KTZ NLCs exhibited sustained drug release with 45 ± 5% in 12&#xa0;h, while <i>ex vivo</i> drug permeation trials on goat skin confirmed improved penetration of drug when contrasted with conventional topical formulation. <i>In vitro</i> drug deposition studies revealed that the gel formulation could impede systemic absorption, offer a greater accumulative uptake of 31.36% after 24&#xa0;h, and be non-irritant to the skin compared to the conventional formulation. Further, <i>in vivo</i> studies showed that the optimized gel formulation had significantly improved antifungal effectiveness against <i>Candida albicans</i>. Results suggest that squalene-based NLCs are a promising drug delivery system for KTZ that can improve its skin penetration and therapeutic efficacy.</p>

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Novel Squalene Based Nanostructured Lipid Carriers of Ketoconazole for Enhanced Skin Penetration and Better Anti-Fungal Control: An In-Vitro, Ex-Vivo and In-Vivo Evaluation

  • 期刊论文

  • 发表日期：

    2025年8月12日

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  • Ravi Pratap Singh,
  • Raj Kumar Narang,
  • Nitin Sharma,
  • Maitrayee Ghosh,
  • Amisha,
  • Subheet Kumar Jain,
  • Amrinder Singh

摘要

Ketoconazole (KTZ) functions by suppressing the propagation of ergosterol, an essential element of the fungal cell membrane. However, its conventional topical delivery is often limited by less skin retention due to early drainage and washout. The objective of the present investigation was to fabricate a skin-targeting KTZ-loaded nanostructured lipid carriers (NLCs) with squalene, and thus the localized action. The NLCs were developed and characterized on various parameters like particle size, PDI, and %EE. The Box-Behnken design (BBD) was employed to effectively fabricate KTZ-loaded NLCs with squalene and Vitamin E TPGS for optimal formulation attributes. In vitro drug release of optimized KTZ NLCs exhibited sustained drug release with 45 ± 5% in 12 h, while ex vivo drug permeation trials on goat skin confirmed improved penetration of drug when contrasted with conventional topical formulation. In vitro drug deposition studies revealed that the gel formulation could impede systemic absorption, offer a greater accumulative uptake of 31.36% after 24 h, and be non-irritant to the skin compared to the conventional formulation. Further, in vivo studies showed that the optimized gel formulation had significantly improved antifungal effectiveness against Candida albicans. Results suggest that squalene-based NLCs are a promising drug delivery system for KTZ that can improve its skin penetration and therapeutic efficacy.