Preparation and in Vitro Evaluation of Inhalation Powder Containing Fluconazole Nanoparticles for the Treatment of Fungal Lung Infections

Document Type : Original Article(s)

Authors

1 Assistant Professor, Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran

2 Pharmacy Student, Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran

3 Assistant Professor, Department of Pharmaceutical Biotechnology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran

4 Professor, Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran

Abstract

Background: Immunocompromised persons are very susceptible to fungal infections. It is desirable to treat pulmonary fungal infections with specific delivery of drugs to the lungs.
Methods: Zein nanoparticles containing fluconazole were prepared by the anti-solvent method. Their physico-chemical properties were investigated. From the optimal formulation, the inhalation powder was prepared with lactose or mannitol using spray drying, and aerosolization characteristics of the dry powders were evaluated using Anderson's cascade impactor. Antifungal effect was investigated against candida albicans and minimum inhibitory concentration was determined. Cytotoxicity of free fluconazole, a dry powder inhaler containing drug loaded nanoparticles, and dry powder inhaler containing nanoparticles without a drug was also evaluated against the A549 cell line by the MTT method.
Findings: The size of nanoparticles was in the range of 88.70 ± 1.35 to 226.90 ± 5.40 nm, and the percentage of loading efficiency was in the range of 57.58 ± 3.61 to 92.94 ± 0.34. In the prepared dry powder samples, all the powder samples had a high emitted dose percentage. Cytotoxicity test showed that in general none of the groups had significant cytotoxic effects even at the highest studied concentration.
Conclusion: Using lactose as the carrier, can improve the aerodynamic properties of dry powder inhaler compared with mannitol. The prepared inhaled fluconazole powder has a suitable fine particle fraction % and a low median mass aerodynamic diameter and can be well deposited in the lung. In addition, powder containing fluconazole was safe and its effect was comparable with fluconazole.

Highlights

Somayeh Taymouri : PubMed, Google Scholar

Jaleh Varshosaz : PubMed, Google Scholar 

Keywords

Main Subjects

References

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Journal of Isfahan Medical School
Volume 41, Issue 728
4th Week, September
September and October 2023
Pages 604-614

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History

  • Receive Date: 31 May 2023
  • Revise Date: 09 August 2023
  • Accept Date: 09 August 2023

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