Abstract
Purpose
To study the effect of the size of the surface-coated polycaprolactone (PCL) microparticle carriers on the aerosolization and dispersion of Salbutamol Sulfate (SS) from Dry Powder Inhaler (DPI) formulations.
Methods
The microparticles were fabricated using an emulsion technique in four different sizes (25, 48, 104 and 150 μm) and later coated with Magnesium stearate (MgSt) and leucine. They were characterized by laser diffraction and SEM. The Fine Particle Fraction (FPF) of SS from powder mixtures was determined by a Twin Stage Impinger (TSI).
Results
As the carrier size increased from 25 μm to 150 μm, the FPF of the SS delivered by the coated PCL particles increased approximately four fold. A linear relationship was found between the FPF and Volume mean Diameter (VMD) of the particles over this range.
Conclusions
The dispersion behaviour of SS from PCL carriers was dependent on the inherent size of the carriers and the increased FPF of SS with increased carrier size probably reflects the higher mechanical forces produced due to the carrier-carrier collisions or collisions between the carrier particles and the internal walls of the inhaler during aerosolization.
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Abbreviations
- d:
-
diameter
- DCM:
-
dichloromethane
- DPI:
-
dry powder inhaler
- ED:
-
emitted dose
- FPF:
-
fine particle fraction
- HPLC:
-
high performance liquid chromatography
- MgSt:
-
magnesium stearate
- MW :
-
molecular weight
- N:
-
particle number
- PCL:
-
polycaprolactone
- PVA:
-
polyvinyl alcohol
- RD:
-
recovered dose
- S1:
-
stage one
- S2:
-
stage two
- SEM:
-
scanning electron microscope
- SS:
-
salbutamol sulfate
- SX:
-
salmeterol xinafoate
- TSI:
-
twin stage impinger
- UV:
-
ultraviolet
- VMD:
-
volume median diameter
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Acknowledgments AND DISCLOSURES
This work has been financially supported through a PhD studentship and Rinku Tuli would like to acknowledge the scholarship support provided by the Faculty of Science and Technology, Queensland University of Technology.
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Tuli, R.A., George, G.A., Dargaville, T.R. et al. Studies on the Effect of the Size of Polycaprolactone Microspheres for the Dispersion of Salbutamol Sulfate from Dry Powder Inhaler Formulations. Pharm Res 29, 2445–2455 (2012). https://doi.org/10.1007/s11095-012-0772-y
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DOI: https://doi.org/10.1007/s11095-012-0772-y