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Novel nanoparticles for pulmonary drug administration
P A Dickinson1, S W Howells, I W Kellaway
1Welsh School of Pharmacy, Cardiff University, Cathays Park, Cardiff, CF1 3XF, UK. paul.dickinson@astrazeneca.com
Journal of Drug Targeting
|November 8, 2001
Summary
This study presents a novel, low-energy method for creating hydrophilic drug nanoparticles for inhalers. Lecithin-based nanoparticles dispersed effectively in hydrofluoroalkane propellants, enabling targeted lung delivery.
Area of Science:
- Pharmaceutical Technology
- Nanotechnology
- Drug Delivery
Background:
- Developing effective drug delivery systems for pulmonary administration is crucial for systemic drug therapy.
- Traditional methods for nanoparticle production often involve harsh conditions and toxic chemicals.
- Hydrophilic drug nanoparticles require specific formulation strategies for stable dispersion in inhalant propellants.
Purpose of the Study:
- To investigate a novel, low-energy, one-step method for producing hydrophilic drug nanoparticles.
- To evaluate the suitability of these nanoparticles for dispersion in hydrofluoroalkane (HFA) propellants for pressurized metered dose inhalers (pMDIs).
- To assess the aerosol performance and lung deposition characteristics of the formulated nanoparticles.
Main Methods:
- Utilized reverse-phase microemulsions as templates for nanoparticle synthesis.
- Investigated two microemulsion systems: water/sodium bis(2-ethylhexyl) sulphosuccinate (AOT)/iso-octane and water/lecithin/propan-2-ol/iso-octane.
- Captured nanoparticles via snap freezing followed by freeze-drying and dispersed them in HFA-227 propellant for pMDI aerosol performance assessment using cascade impaction.
Main Results:
- Successfully produced spherical nanoparticles with sizes less than 300 nm.
- Nanoparticles formulated with AOT surfactant showed poor dispersibility in HFA-227.
- Lecithin-based nanoparticles demonstrated good dispersion in co-solvent modified HFA-227, yielding fine aerosols with a Mass Median Aerodynamic Diameter (MMAD) ≤ 1.5 microns and a fine particle fraction (FPF) > 58%.
Conclusions:
- The lecithin-based microemulsion method offers a viable, gentle approach for producing drug nanoparticles suitable for pMDIs.
- Effective dispersion in HFA-227 and favorable aerosol characteristics suggest targeted alveolar deposition for systemic drug delivery.
- This technique holds promise for improving pulmonary drug delivery efficiency and patient outcomes.