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Preparation of Functional Silica Using a Bioinspired Method
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Encapsulating insoluble antifungal drugs into oleic acid-modified silica mesocomposites with enhanced fungicidal

Ping Zhu1, Liuzhu Zhou1, Yiyan Song1

  • 1Center for Global Health, School of Public Health, Nanjing Medical University, Nanjing 211166, Jiangsu, China. okachen30@gmail.com jchen@njmu.edu.cn.

Journal of Materials Chemistry. B
|April 22, 2020
PubMed

Insights

A novel mesoporous silica nanocomposite effectively delivers the antifungal drug itraconazole (ITZ), enhancing its activity against resistant fungal infections. This formulation shows potential for topical therapies, offering a new approach in antifungal drug development.

Area of Science:

  • Materials Science
  • Nanotechnology
  • Mycology

Background:

  • Drug-resistant fungal infections pose a significant public health threat, especially in immunocompromised individuals.
  • Developing effective and safe antifungal agents is crucial for precision medicine.
  • Poor water solubility of many antifungal drugs limits their pharmaceutical efficacy and delivery.

Purpose of the Study:

  • To develop a novel drug delivery system for lipophilic antifungal agents.
  • To enhance the antifungal activity of itraconazole (ITZ) against resistant strains.
  • To investigate the mechanism of enhanced antifungal action.

Main Methods:

  • Synthesis of oleic acid (OA)-grafted mesoporous silica (SBA-15) modified with cetyltrimethylammonium bromide (CTAB).
  • Loading of itraconazole (ITZ) into the SBA-15-OA-CTAB matrix.
  • Physicochemical characterization of the nanocomposite.
  • Antifungal activity testing against Aspergillus fumigatus and Candida albicans.
  • Mechanism of action studies, including reactive oxygen species (ROS) detection.

Main Results:

  • A rod-like SBA-15-OA-CTAB/ITZ composite with retained mesostructural regularity was successfully synthesized.
  • The nanocomposite achieved a high loading amount of ITZ (approximately 18%) within the mesopores.
  • Enhanced antifungal activity was observed against Aspergillus fumigatus and Candida albicans.
  • The formulated ITZ induced reactive oxygen species (ROS) formation in fungal cells, unlike pure ITZ, suggesting a novel mechanism involving CTAB.

Conclusions:

  • The developed mesoporous silica nanocomposite serves as an effective drug matrix for itraconazole.
  • The formulation enhances antifungal activity, potentially through ROS generation mediated by CTAB.
  • This approach offers a promising alternative for improving lipophilic antifungal drugs, particularly for external applications like topical therapy.

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