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Modification Tadalafil and Macitentan tablets to aerosol
Paul Zarogoulidis1,2, Dimitris Petridis3, Chrysa Sardeli4
1Pulmonary Department, "Bioclinic" Private Hospital, 115 24 Thessaloniki, Greece.
Pulmonary hypertension drugs, Tadalafil and Macitentan, can be effectively aerosolized. Both ultrasound nebulizers and specific jet-nebulizer setups produced optimal aerosol droplet sizes for delivery.
Area of Science:
- Pharmaceutical Sciences
- Respiratory Medicine
- Drug Delivery Systems
Background:
- Aerosolized medications are approved for conditions like cystic fibrosis and diabetes.
- Existing aerosol formulations are available for pulmonary hypertension treatment.
Purpose of the Study:
- To evaluate the aerosolization potential of Tadalafil and Macitentan for pulmonary hypertension.
- To determine optimal nebulizer and residual cup configurations for producing respirable aerosol particles.
Main Methods:
- Tadalafil and Macitentan tablets were milled into powders.
- Jet nebulizers with various residual cups and ultrasound nebulizers with different release methods were tested.
- Particle size distribution, specifically Mass Median Aerodynamic Diameter (MMAD), was analyzed.
Main Results:
- Nebulizer and residual cup design significantly influenced MMAD.
- Specific large residual cups (10 mL) with jet nebulizers yielded the smallest droplets.
- Both tested ultrasound nebulizers successfully generated aerosol droplets with MMAD ≤ 5 μm.
Conclusions:
- Tadalafil and Macitentan are suitable for aerosol administration.
- Further in vivo studies are warranted to confirm airway safety.
- Optimized nebulizer systems can achieve therapeutic aerosol particle sizes.
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