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Inhalation powder development without carrier: How to engineer ultra-flying microparticles?
Anna Lechanteur1, Eva Gresse1, Luisa Orozco2
1Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, Liège 4000, Belgium.
Summary
Optimized spray drying created new inhaled powders for asthma, achieving over 55% fine particle fraction for superior deep lung drug delivery compared to existing products.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Respiratory Medicine
Background:
- Particle engineering enables advanced inhaled powders like PulmoSol™ and PulmoSphere™.
- Spray drying is a versatile technique for producing inhalable powders with tunable properties.
- Optimizing low-dose formulations is crucial for effective asthma management.
Purpose of the Study:
- To optimize the production of low-dose inhaled powders containing budesonide and formoterol.
- To maximize deep lung deposition of anti-asthmatic drugs using spray drying.
- To investigate the impact of excipients and process parameters on powder performance.
Main Methods:
- Utilized a Design of Experiments (DOE) approach to systematically vary formulation and process parameters.
- Produced 27 different powder batches with varying excipient mixes (cyclodextrins, raffinose, maltodextrins), concentrations, and spray drying conditions.
- Evaluated deep lung deposition using fine particle fraction (FPF) measurements with a next-generation impactor.
Main Results:
- Two optimized powders, one using hydropropyl-β-cyclodextrin and another with a blend including L-leucine, achieved FPF exceeding 55%.
- These FPF values significantly outperformed currently available commercial products.
- Deep lung deposition correlated with reduced particle size and lower inter-particular interactions, confirmed by laser diffraction and morphometry.
Conclusions:
- Developed novel carrier-free inhalation powders with highly efficient lung deposition capabilities.
- Demonstrated that inter-particular interactions significantly influence aerosolization behavior and drug delivery efficiency.
- The optimized powders promise uniform drug distribution in the lungs, essential for effective asthma symptom control.
