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Inhalable Clarithromycin Microparticles for Treatment of Respiratory Infections
Frantiescoli Dimer1, Cristiane de Souza Carvalho-Wodarz1, Jörg Haupenthal2
1Department of Drug Delivery (DDEL), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, 66123, Saarbrücken, Germany.
Purpose:
The aim of this work was to develop clarithromycin microparticles (CLARI-MP) and evaluate their aerodynamic behavior, safety in bronchial cells and anti-bacterial efficacy.
Methods:
Microparticles containing clarithromycin were prepared as dry powder carrier for inhalation, using leucine and chitosan. CLARI-MP were deposited on Calu-3 grown at air-interface condition, using the pharmaceutical aerosol deposition device on cell cultures (PADDOCC). Deposition efficacy, transport across the cells and cytotoxicity were determined. Anti-antibacterial effect was evaluated against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus.
Results:
Microparticles were of spherical shape, smooth surface and size of about 765 nm. Aerosolization performance showed a fine particle fraction (FPF) of 73.3%, and a mass median aerodynamic diameter (MMAD) of 1.8 μm. Deposition on Calu-3 cells using the PADDOCC showed that 8.7 μg/cm(2) of deposited powder were transported to the basolateral compartment after 24 h. The safety of this formulation is supported by the integrity of the cellular epithelial barrier and absence of toxicity, and the antimicrobial activity demonstrated for Gram positive and Gram negative bacteria.
Conclusions:
The appropriate aerodynamic properties and the excellent deposition on Calu-3 cells indicate that clarithromycin microparticles are suitable for administration via pulmonary route and are efficient to inhibit bacteria proliferation.
Insights
Developed clarithromycin microparticles (CLARI-MP) demonstrate suitable aerodynamic properties for pulmonary delivery. These microparticles exhibit excellent deposition on bronchial cells and potent antibacterial activity against common pathogens.
Area of Science:
- Pharmaceutical Sciences
- Biotechnology
- Drug Delivery Systems
Background:
- Antibiotic resistance necessitates novel drug delivery systems.
- Pulmonary drug delivery offers targeted treatment for respiratory infections.
- Clarithromycin is a macrolide antibiotic with broad-spectrum activity.
Purpose of the Study:
- To develop and characterize clarithromycin microparticles (CLARI-MP) for inhalation.
- To evaluate the aerodynamic performance of CLARI-MP.
- To assess the safety and antibacterial efficacy of CLARI-MP in bronchial cell models.
Main Methods:
- Clarithromycin microparticles were formulated using leucine and chitosan.
- Aerodynamic properties were assessed, including fine particle fraction (FPF) and mass median aerodynamic diameter (MMAD).
- Deposition, transport, and cytotoxicity were evaluated on Calu-3 bronchial cells using the pharmaceutical aerosol deposition device on cell cultures (PADDOCC).
Main Results:
- Spherical microparticles with a size of approximately 765 nm were obtained.
- CLARI-MP exhibited favorable aerosolization with an FPF of 73.3% and MMAD of 1.8 μm.
- Significant transport across Calu-3 cells was observed, with no cytotoxicity and demonstrated antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, and Staphylococcus aureus.
Conclusions:
- Clarithromycin microparticles possess optimal aerodynamic characteristics for pulmonary administration.
- The formulation demonstrates effective deposition and transport in bronchial cell models.
- CLARI-MP are safe and exhibit potent antibacterial activity, indicating suitability for treating respiratory bacterial infections.
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