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<p>The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across&#xa0;the skin by preparing&#xa0;the&#xa0;ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation &amp; hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 2<sup>3</sup> full factorial design was used&#xa0;using Design-Expert® software. The optimized batch exhibited a vesicle size (107.6&#xa0;nm), a polydispersity index (PDI) (0.248), entrapment efficiency (% EE) (76.9%), and a zeta potential (-33.7&#xa0;mV). Results from <i>ex vivo</i> skin permeation studies and <i>in vitro</i> drug release demonstrated enhanced improved skin permeation and drug release compared to other formulations. An <i>in vitro</i>&#xa0;antifungal and <i>in vivo</i>&#xa0;pharmacodynamic study, elucidated the enhanced effectiveness of the optimized formulation against <i>Candida albicans</i>. In summary, menthosomes could serve as a potent vehicle to enhance drug penetration via the skin to improve its antifungal activity.</p> Graphical Abstract <p></p>

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Menthol-based Novel Ultra-Deformable Vesicle: Formulation, Optimization and Evaluation of an Antifungal Drug

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年1月8日

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  • Hema Manjushree,
  • Devika Nayak,
  • Praveen Halagali,
  • Mahalaxmi Rathnanand,
  • Roshan Tawale,
  • Koteshwara Ananthmurthy,
  • Jesil Mathew Aranjani,
  • Vamshi Krishna Tippavajhala

摘要

The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across the skin by preparing the ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation & hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 23 full factorial design was used using Design-Expert® software. The optimized batch exhibited a vesicle size (107.6 nm), a polydispersity index (PDI) (0.248), entrapment efficiency (% EE) (76.9%), and a zeta potential (-33.7 mV). Results from ex vivo skin permeation studies and in vitro drug release demonstrated enhanced improved skin permeation and drug release compared to other formulations. An in vitro antifungal and in vivo pharmacodynamic study, elucidated the enhanced effectiveness of the optimized formulation against Candida albicans. In summary, menthosomes could serve as a potent vehicle to enhance drug penetration via the skin to improve its antifungal activity.

Graphical Abstract