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Nano- and Microstructured model carrier surfaces to alter dry powder inhaler performance
Niklas Renner1, Hartwig Steckel2, Nora Urbanetz3
1Department of Pharmaceutics and Biopharmaceutics, Kiel University, Grasweg 9a, 24118 Kiel, Germany.
International Journal of Pharmaceutics
|December 28, 2016
Summary
Surface modifications of inhalation carriers impact drug delivery. Hydrofluoric acid treatment reduced respirable fraction, while tungsten carbide milling enhanced aerosolisation performance for both budesonide and formoterol fumarate dihydrate.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Aerosol Science
Background:
- Optimizing carrier properties is crucial for effective inhaled drug delivery.
- Surface characteristics of carriers significantly influence drug-carrier interactions and aerosolisation.
- Understanding how surface modifications affect drug payload and aerodynamic performance is essential.
Purpose of the Study:
- To investigate the impact of different carrier surface modifications on aerosolisation performance.
- To evaluate the effect of surface modifications on the effective carrier payload (true surface coverage) of interactive blends.
- To assess these effects for two distinct active pharmaceutical ingredients (APIs): formoterol fumarate dihydrate (FF) and budesonide (BUD).
Main Methods:
- Model carriers (glass beads) were subjected to mechanical surface modifications: hydrofluoric acid (HF) treatment and milling with tungsten carbide (TC).
- Interactive blends were prepared using FF and BUD as APIs.
- In vitro aerodynamic characterisation was performed to assess respirable fraction and aerosolisation performance.
Main Results:
- HF treatment resulted in a significant decrease in respirable fraction (40.2-50.1%) due to particle sheltering in surface clefts.
- TC milling created nanoscale surface roughness, leading to increased aerodynamic performance (20.0-38.1%).
- These effects were consistent for both FF and BUD, irrespective of their chemical properties.
Conclusions:
- Carrier surface modification strategies profoundly influence aerosolisation performance and drug payload.
- Hydrofluoric acid treatment is detrimental to aerosolisation, while tungsten carbide milling enhances it.
- Surface engineering of carriers offers a viable approach to optimize inhaled drug delivery systems.
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