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Formulation parameters of crystalline nanosuspensions on spray drying processing: a DoE approach
Sumit Kumar1, Xiaoming Xu1, Rajeev Gokhale2
1University of Connecticut, School of Pharmacy, Storrs, CT 06269, USA.
International Journal of Pharmaceutics
|January 23, 2014
Summary
Spray drying stabilizes nanocrystals for poorly soluble drugs. Lower drug-to-stabilizer ratios enhance dissolution and stability, crucial for pharmaceutical formulations.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Physical Chemistry
Background:
- Nanocrystalline suspensions enhance the dissolution of poorly soluble drugs (BCS Class II/IV).
- Spray drying is a key downstream process for improving the physical and chemical stability of dried nanocrystals.
- Understanding formulation variables is critical for successful spray drying of nanocrystals.
Purpose of the Study:
- To investigate the impact of nanocrystalline suspension formulation variables on spray-drying processing.
- To evaluate the effect of different stabilizers (Dowfax 2A1, HPMC E15) and drugs (naproxen, indomethacin) on spray-dried nanocrystal properties.
- To correlate formulation parameters with nanocrystal stability and dissolution.
Main Methods:
- Formulation of naproxen and indomethacin nanocrystals with varying stabilizers and drug-to-stabilizer ratios.
- Spray drying of nanocrystalline suspensions.
- Design of Experiments (DoE) approach to optimize critical formulation variables.
- Characterization of powders (particle size, moisture, XRD) and dissolution testing using a novel dialysis sac adapter.
- Accelerated storage stability testing.
Main Results:
- Nanocrystal aggregation was significantly influenced by the drug-to-stabilizer ratio.
- Glass transition temperature and charge effects were dominant factors in spray-dried powder yield.
- Formulations with lower drug-to-excipient ratios exhibited reduced aggregation and faster dissolution rates.
- The Flory-Huggins interaction parameter correlated with the stability of spray-dried nanocrystal formulations.
Conclusions:
- Spray drying is an effective method for producing stable nanocrystals with improved dissolution properties.
- Optimizing the drug-to-stabilizer ratio and considering drug-excipient interactions are crucial for stable nanocrystal formulations.
- The developed dialysis sac adapter effectively differentiates between aggregated and non-aggregated nanocrystal formulations.
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