Purpose <p>Dermatophytosis is a ubiquitous superficial fungal infection, mostly caused by <i>Trichophyton rubrum</i>, and its effective treatment is frequently hindered by inadequate skin penetration, frequent dosing requirements, and increased antifungal resistance. This study aimed to formulate and assess morin hydrate-loaded nanostructured lipid carriers (MH-NLCs) as an innovative topical delivery system to enhance antifungal efficacy and skin penetration.</p> Methods <p>MH-NLCs were developed via hot-melt emulsification, followed by ultrasonication and optimization using a Box–Behnken experimental design. The lipid ratio, surfactant concentration, and sonication time were selected as independent variables, with particle size and entrapment efficiency as key responses. The optimized formulation was examined for its physicochemical properties and solid-state behaviour through various analyses, including DLS, FTIR, DSC, XRD, and TEM. Drug release was determined using a Franz diffusion cell, and antidermatophytosis activity was evaluated in a Wistar rat model of dermatophytosis induced by <i>T. rubrum</i>.</p> Results <p>The optimized MH-NLCs exhibited an average particle size of 143.06&#xa0;nm, a narrow size distribution (0.185), and satisfactory physical stability (-35.5 mV). The drug entrapment efficiency was 87 ± 4%. XRD and DSC showed that the drug was encapsulated in an amorphous form, and TEM confirmed that it was almost spherical, with a size of approximately 200&#xa0;nm. MH-NLCs exhibit a sustained drug release over 24&#xa0;h using a dialysis membrane. Stability studies indicated that the MHNLCs were more stable at refrigerated temperatures than at room temperature, and In vivo studies revealed that MH-NLCs were more effective against T. rubrum than conventional morin formulations. The MH-NLCs gel produced faster and more complete lesion clearance than the conventional morin gel, with a response comparable to that of standard luliconazole therapy.</p> Conclusion <p>Morin hydrate-loaded nanostructured lipid carriers are promising topical nanocarrier systems for the treatment of dermatophytosis. They exhibit improved stability, controlled drug release, and enhanced antifungal effects.</p>

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Development, Optimization, In-Vitro and In-Vivo Evaluation of Morin Hydrate-Loaded Nanostructured Lipid Carriers for the Treatment of Dermatophytosis

  • Dhanesh Kumar,
  • Rajesh Choudhary,
  • Swarnali Das Paul,
  • Jaya Shree

摘要

Purpose

Dermatophytosis is a ubiquitous superficial fungal infection, mostly caused by Trichophyton rubrum, and its effective treatment is frequently hindered by inadequate skin penetration, frequent dosing requirements, and increased antifungal resistance. This study aimed to formulate and assess morin hydrate-loaded nanostructured lipid carriers (MH-NLCs) as an innovative topical delivery system to enhance antifungal efficacy and skin penetration.

Methods

MH-NLCs were developed via hot-melt emulsification, followed by ultrasonication and optimization using a Box–Behnken experimental design. The lipid ratio, surfactant concentration, and sonication time were selected as independent variables, with particle size and entrapment efficiency as key responses. The optimized formulation was examined for its physicochemical properties and solid-state behaviour through various analyses, including DLS, FTIR, DSC, XRD, and TEM. Drug release was determined using a Franz diffusion cell, and antidermatophytosis activity was evaluated in a Wistar rat model of dermatophytosis induced by T. rubrum.

Results

The optimized MH-NLCs exhibited an average particle size of 143.06 nm, a narrow size distribution (0.185), and satisfactory physical stability (-35.5 mV). The drug entrapment efficiency was 87 ± 4%. XRD and DSC showed that the drug was encapsulated in an amorphous form, and TEM confirmed that it was almost spherical, with a size of approximately 200 nm. MH-NLCs exhibit a sustained drug release over 24 h using a dialysis membrane. Stability studies indicated that the MHNLCs were more stable at refrigerated temperatures than at room temperature, and In vivo studies revealed that MH-NLCs were more effective against T. rubrum than conventional morin formulations. The MH-NLCs gel produced faster and more complete lesion clearance than the conventional morin gel, with a response comparable to that of standard luliconazole therapy.

Conclusion

Morin hydrate-loaded nanostructured lipid carriers are promising topical nanocarrier systems for the treatment of dermatophytosis. They exhibit improved stability, controlled drug release, and enhanced antifungal effects.