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Ketoconazole-loaded microspone film coating agent for superficial fungal infection: design, preparation and

Zhaowei Jin1, Danqing Wu1, Yangnan Chen1

  • 1Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, PR China.

Journal De Mycologie Medicale
|April 26, 2025
PubMed

Insights

This study developed ketoconazole (KCZ) microsponge film coating (KCZ-MSF) to improve topical antifungal treatment. KCZ-MSF demonstrated enhanced skin retention and bioavailability compared to conventional ketoconazole cream.

Area of Science:

  • Pharmaceutical Sciences
  • Dermatology
  • Drug Delivery Systems

Background:

  • Ketoconazole (KCZ) exhibits poor solubility and stability, limiting its transdermal absorption and bioavailability for treating fungal infections.
  • Developing advanced drug delivery systems is crucial to overcome KCZ's limitations and enhance therapeutic efficacy.
  • Microsponge technology offers a promising approach for improving the delivery of poorly soluble drugs like KCZ.

Purpose of the Study:

  • To develop and characterize a novel ketoconazole-loaded microsponge based film coating agent (KCZ-MSF) for enhanced transdermal delivery.
  • To optimize the formulation of KCZ-MSF for improved physical properties and topical skin application.
  • To evaluate the in vitro transdermal absorption and in vivo pharmacokinetic profile of KCZ-MSF compared to conventional formulations.

Main Methods:

  • Ketoconazole microspheres (KCZ-MS) were prepared using the emulsion solvent evaporation method and optimized via Box-Behnken design.
  • Characterization of KCZ-MS included SEM, FTIR, and DSC to assess morphology, drug-excipient compatibility, and thermal properties.
  • The optimized KCZ-MS was formulated into a film coating agent (KCZ-MSF) through orthogonal experimental design.
  • In vitro transdermal diffusion and in vivo pharmacokinetic studies were conducted to compare KCZ-MSF with ketoconazole cream and KCZ film.

Main Results:

  • Optimized KCZ-MS exhibited a spherical porous structure, mean particle size of 22.42 ± 8.45 µm, drug loading of 20.74%, and entrapment efficiency of 92.12%.
  • KCZ-MSF demonstrated good physical properties suitable for topical application.
  • In vitro studies showed superior skin retention of KCZ-MSF over commercial ketoconazole cream.
  • Pharmacokinetic analysis revealed KCZ-MSF had significantly higher AUC0-24 (420.71 ± 21.77 µg/(g·h)) compared to KCZ film and ketoconazole cream.

Conclusions:

  • Ketoconazole-loaded microsponge based film coating agent (KCZ-MSF) effectively enhances transdermal absorption and bioavailability.
  • KCZ-MSF presents a superior alternative to conventional ketoconazole formulations for treating superficial skin fungal infections.
  • The developed microsponge film coating platform holds significant potential for improving the therapeutic outcomes of topical antifungal treatments.
Keywords:
Film coating agentKetoconazoleMicrospongePharmacokineticsSuperficial fungal infectionTransdermal drug delivery

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