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Purpose <p>Around the world, fungal infections are a major concern, and the most commonly used medication to treat them is fluconazole. Posaconazole (PCZ) is a BCS class II drug with low solubility and high permeability. Transfersomes are promising nanocarriers for enhancing drug solubility. This study aimed to create and evaluate transfersomal gels with PCZ incorporated to improve solubility and skin permeation for treating fungal infections.</p> Methods <p>Transfersomes were prepared by the thin film hydration method (formulations F1–F6) and incorporated into a carbopol 934 gel base. The compatibility of PCZ with different excipients was examined using DSC, XRD, and FTIR analyses. A characterization study, including vesicle size, PDI, zeta potential, and TEM, was used to analyze the transfersomes. The formulations were then incorporated into a carbopol 934 gel and evaluated for pH, viscosity, and antifungal activity.</p> Results <p>Formulations F2 and F5 showed high entrapment efficiencies of 82.1 ± 2.17% and 82.78 ± 2.92%, respectively. F5 exhibited the smallest vesicle size (210 ± 10&#xa0;nm), good spreadability (8.33 ± 0.21&#xa0;g·cm·s⁻¹), and sustained release (99.10 ± 0.51%). In antifungal studies, F5 demonstrated the highest inhibition against <i>C. albicans</i> (3.5 ± 0.11&#xa0;cm), while F2 showed slightly greater activity against <i>A. niger</i> (2.8 ± 0.15&#xa0;cm), both surpassing the free drug (~ 2.5 ± 0.06&#xa0;cm).</p> Conclusion <p>The present study demonstrated that F5 is a promising approach to enhance the solubility of the drug and increase skin permeability through the deeper skin layers as a topical gel formulation. Effective against fungal infections, PCZ-loaded transfersomal gel can be suited for clinical translation, broad-spectrum applications, combination therapy, commercialization, patient-centered formulations, and nanotoxicology research.</p> Graphical Abstract <p> Transfersomal Gel Loaded with Posaconazole for Improved Solubility and Antifungal Potency</p> <p></p>

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Design and Assessment of Posaconazole-Loaded Transfersomal Gel for Antifungal Efficacy Against Candida Albicans and Aspergillus Niger

  • 期刊论文

  • 发表日期：

    2026年1月9日

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  • Piyali Khamkat,
  • Snehamayee Mohapatra,
  • Swarupananda Mukherjee,
  • Gouranga Dutta,
  • Soumen Singh

摘要

Purpose

Around the world, fungal infections are a major concern, and the most commonly used medication to treat them is fluconazole. Posaconazole (PCZ) is a BCS class II drug with low solubility and high permeability. Transfersomes are promising nanocarriers for enhancing drug solubility. This study aimed to create and evaluate transfersomal gels with PCZ incorporated to improve solubility and skin permeation for treating fungal infections.

Methods

Transfersomes were prepared by the thin film hydration method (formulations F1–F6) and incorporated into a carbopol 934 gel base. The compatibility of PCZ with different excipients was examined using DSC, XRD, and FTIR analyses. A characterization study, including vesicle size, PDI, zeta potential, and TEM, was used to analyze the transfersomes. The formulations were then incorporated into a carbopol 934 gel and evaluated for pH, viscosity, and antifungal activity.

Results

Formulations F2 and F5 showed high entrapment efficiencies of 82.1 ± 2.17% and 82.78 ± 2.92%, respectively. F5 exhibited the smallest vesicle size (210 ± 10 nm), good spreadability (8.33 ± 0.21 g·cm·s⁻¹), and sustained release (99.10 ± 0.51%). In antifungal studies, F5 demonstrated the highest inhibition against C. albicans (3.5 ± 0.11 cm), while F2 showed slightly greater activity against A. niger (2.8 ± 0.15 cm), both surpassing the free drug (~ 2.5 ± 0.06 cm).

Conclusion

The present study demonstrated that F5 is a promising approach to enhance the solubility of the drug and increase skin permeability through the deeper skin layers as a topical gel formulation. Effective against fungal infections, PCZ-loaded transfersomal gel can be suited for clinical translation, broad-spectrum applications, combination therapy, commercialization, patient-centered formulations, and nanotoxicology research.

Graphical Abstract

Transfersomal Gel Loaded with Posaconazole for Improved Solubility and Antifungal Potency