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Purpose <p>This study was undertaken to improve the treatment of deep seated fungal skin infection by formulation of setraconazole loaded invasome gels and films.</p> Method <p>Setraconazole invasomes were prepared by thin-film hydration method and optimized by factorial design. The entrapment efficiency of the invasomes were determined. Invasomes with highest entrapment efficiency were further evaluated for size, zeta potential and converted to gels and films. Films and gels were evaluated for antifungal activity, skin irritation and in vitro skin permeation. Additionally gels were evaluated for pH, viscosity and spreadability.</p> Results <p>The invasomes showed high entrapment of setraconazole up to 83.4%. Further, invasomes were successfully converted into gels and films. The gels showed good consistency and excellent spreadability. Setraconazole gel (F4) and films containing tween 60 exhibited maximum permeation up to 58.12% and 41.12% respectively through excised goat skin. The gel did not show any irritation (swelling, erythema) in the rabbit skin during the 24&#xa0;h of the study. The films showed higher antifungal activity than gels, containing invasome sespecially against <i>Aspergillus niger</i>. Invasome-loaded formulations were more effective due to better fungal cell penetration. The optimized invasome was found to have particle size (35.9&#xa0;nm) with high homogeneity (0.51 of PDI). The zeta potential was found to be negative (1.6 mV) revealing high stability and non-agglomeration of vesicles. The gels showed good consistency and excellent spreadability. Setraconazole loaded invasome (F4) gel and films containing tween 60 exhibited maximum permeation up to 58.12% and 41.12% respectively through excised goat skin. The gel did not show any signs of irritation in the rabbit skin. The films showed higher antifungal activity than gels, containing invasomes especially against <i>Aspergillus niger</i>. Invasome-loaded formulations were more effective due to better fungal cell penetration.</p> Conclusion <p>The study concluded that Sertaconazole invasome gels and films are effective carrier for transdermal delivery and topical treatment of fungal infections.</p>

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Development and Optimization of Setraconazole Invasomes, Gels, and Films for Enhanced Transdermal Delivery and Topical Fungal Treatment

  • 期刊论文

  • 发表日期：

    2025年7月16日

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  • Dibya Sundar Panda,
  • Deepak Kumar Dash,
  • Riya Vaiswade,
  • Gayatri Gupta,
  • Ranjan kumar Giri,
  • Ameeduzzafar zafar,
  • Omar Awad Alsaidan,
  • Shaliputra P. Magar

摘要

Purpose

This study was undertaken to improve the treatment of deep seated fungal skin infection by formulation of setraconazole loaded invasome gels and films.

Method

Setraconazole invasomes were prepared by thin-film hydration method and optimized by factorial design. The entrapment efficiency of the invasomes were determined. Invasomes with highest entrapment efficiency were further evaluated for size, zeta potential and converted to gels and films. Films and gels were evaluated for antifungal activity, skin irritation and in vitro skin permeation. Additionally gels were evaluated for pH, viscosity and spreadability.

Results

The invasomes showed high entrapment of setraconazole up to 83.4%. Further, invasomes were successfully converted into gels and films. The gels showed good consistency and excellent spreadability. Setraconazole gel (F4) and films containing tween 60 exhibited maximum permeation up to 58.12% and 41.12% respectively through excised goat skin. The gel did not show any irritation (swelling, erythema) in the rabbit skin during the 24 h of the study. The films showed higher antifungal activity than gels, containing invasome sespecially against Aspergillus niger. Invasome-loaded formulations were more effective due to better fungal cell penetration. The optimized invasome was found to have particle size (35.9 nm) with high homogeneity (0.51 of PDI). The zeta potential was found to be negative (1.6 mV) revealing high stability and non-agglomeration of vesicles. The gels showed good consistency and excellent spreadability. Setraconazole loaded invasome (F4) gel and films containing tween 60 exhibited maximum permeation up to 58.12% and 41.12% respectively through excised goat skin. The gel did not show any signs of irritation in the rabbit skin. The films showed higher antifungal activity than gels, containing invasomes especially against Aspergillus niger. Invasome-loaded formulations were more effective due to better fungal cell penetration.

Conclusion

The study concluded that Sertaconazole invasome gels and films are effective carrier for transdermal delivery and topical treatment of fungal infections.