<p>This study investigates the development and optimization of naftifine hydrochloride (Naf-HCl) loaded β-cyclodextrin-based nanosponges (Naf-NSs) for enhanced topical delivery and antifungal efficacy. Molecular docking showed Naf-HCl to be the most potent inhibitor of squalene epoxidase with a binding energy of − 11.0&#xa0;kcal/mol. Nanosponges formulated utilizing diphenyl carbonate (DPC) were optimized via a 3<sup>2</sup> factorial design, having a particle size of 327.5&#xa0;nm and entrapment efficiency of 92.57%. The Naf-NSs were incorporated into a hydrogel having a pH value of 6.3 ± 0.25, a viscosity of 1072 ± 0.65 cPs, and a spreadability of 34.2&#xa0;g·cm/s. In vitro release studies determined sustained release of the drug of 86.02% for 24&#xa0;h, whereas ex vivo analysis exhibited skin retention of 43.27%, which is superior to the marketed product. Antifungal activity against Trichophyton rubrum and <i>Candida albicans</i> indicated zones of inhibition of 21&#xa0;mm and 19&#xa0;mm, respectively. In vivo, the Naf-NSs-based hydrogel exhibited 82.35% recovery of lesions, suggesting its potential as a better option for the treatment of dermatophytosis by controlled release and improved efficacy.</p>

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In Silico Screening and β-Cyclodextrin Nanosponges: A Strategy for Optimizing Naftifine Hydrochloride Delivery for Effective Management of Dermatophytosis

  • Prashant Keshavrao Puranik,
  • Purvaja S. Patangray,
  • Ujban Md Hussain

摘要

This study investigates the development and optimization of naftifine hydrochloride (Naf-HCl) loaded β-cyclodextrin-based nanosponges (Naf-NSs) for enhanced topical delivery and antifungal efficacy. Molecular docking showed Naf-HCl to be the most potent inhibitor of squalene epoxidase with a binding energy of − 11.0 kcal/mol. Nanosponges formulated utilizing diphenyl carbonate (DPC) were optimized via a 32 factorial design, having a particle size of 327.5 nm and entrapment efficiency of 92.57%. The Naf-NSs were incorporated into a hydrogel having a pH value of 6.3 ± 0.25, a viscosity of 1072 ± 0.65 cPs, and a spreadability of 34.2 g·cm/s. In vitro release studies determined sustained release of the drug of 86.02% for 24 h, whereas ex vivo analysis exhibited skin retention of 43.27%, which is superior to the marketed product. Antifungal activity against Trichophyton rubrum and Candida albicans indicated zones of inhibition of 21 mm and 19 mm, respectively. In vivo, the Naf-NSs-based hydrogel exhibited 82.35% recovery of lesions, suggesting its potential as a better option for the treatment of dermatophytosis by controlled release and improved efficacy.