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<p>Fungal infections pose a significant global health challenge, especially in immunocompromised individuals. Luliconazole (LZL), a newly approved drug for topical fungal infections, faces limitations due to poor skin penetration, short skin retention time, and repeated administration. To address this, lipid nanocarrier-based ethosomal gel formulations at 1% w/w strength were developed and extensively characterized through <i>in vitro, ex vivo</i>, and <i>in vivo</i> studies, comparing them with conventional formulations. The optimized ethosomal formulations exhibited a vesicle size of 209.2 ± 8.52&#xa0;nm, encapsulation efficiency of 81.51 ± 3.62%, and PDI of 0.198 ± 0.001. These ethosomes were incorporated into a gel with adhesiveness of 1.012&#xa0;mJ, hardness of 0.17 N, and spreadability ranging from 7.9 to 0.52&#xa0;g·cm/sec. In vitro release studies showed 84.39 ± 1.5% release for the optimized ETs-gel formulation compared to 45.58 ± 0.9% for the LZL-conventional gel. <i>In-vitro</i> activity against <i>Candida albicans</i> demonstrated superior efficacy of the prepared ethosomal formulations over the conventional gel. <i>Ex vivo</i> studies on porcine ear skin indicated enhanced penetration and skin retention time for the optimized ETs-gel compared to the conventional gel. <i>In-vivo</i> antifungal activity on albino rats confirmed the safety, non-irritant nature, and efficacy of the optimized ETs-gel in topical fungal treatment, with no systemic drug circulation observed. Histopathology studies further supported the efficacy of the optimized ETs-gel formulation. Overall, squalene-based ethosomes emerge as promising carriers for enhancing the topical delivery and localized effectiveness of Luliconazole.</p> Graphical Abstract <p></p>

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Development and In Vivo Evaluation of QbD-Assisted Squalene-based Luliconazole Entrapped Ethosomal Gel for the Skin Fungal Infection

  • 期刊论文

  • 发表日期：

    2025年11月26日

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  • Taqdir Singh,
  • Akash Vikal,
  • Preeti Patel,
  • Ghanshyam Das Gupta,
  • Shubham Thakur,
  • Balak Das Kurmi

摘要

Fungal infections pose a significant global health challenge, especially in immunocompromised individuals. Luliconazole (LZL), a newly approved drug for topical fungal infections, faces limitations due to poor skin penetration, short skin retention time, and repeated administration. To address this, lipid nanocarrier-based ethosomal gel formulations at 1% w/w strength were developed and extensively characterized through in vitro, ex vivo, and in vivo studies, comparing them with conventional formulations. The optimized ethosomal formulations exhibited a vesicle size of 209.2 ± 8.52 nm, encapsulation efficiency of 81.51 ± 3.62%, and PDI of 0.198 ± 0.001. These ethosomes were incorporated into a gel with adhesiveness of 1.012 mJ, hardness of 0.17 N, and spreadability ranging from 7.9 to 0.52 g·cm/sec. In vitro release studies showed 84.39 ± 1.5% release for the optimized ETs-gel formulation compared to 45.58 ± 0.9% for the LZL-conventional gel. In-vitro activity against Candida albicans demonstrated superior efficacy of the prepared ethosomal formulations over the conventional gel. Ex vivo studies on porcine ear skin indicated enhanced penetration and skin retention time for the optimized ETs-gel compared to the conventional gel. In-vivo antifungal activity on albino rats confirmed the safety, non-irritant nature, and efficacy of the optimized ETs-gel in topical fungal treatment, with no systemic drug circulation observed. Histopathology studies further supported the efficacy of the optimized ETs-gel formulation. Overall, squalene-based ethosomes emerge as promising carriers for enhancing the topical delivery and localized effectiveness of Luliconazole.

Graphical Abstract