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Development of Amorphous Solid Dispersion Sustained-Release Formulations with Polymer Composite Matrix-Regulated
Lingwu Chen1,2, Enshi Hu3, Peiya Shen3
1School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.
Pharmaceutical Research
|May 14, 2024
Summary
Developing stable ibuprofen (IBU) amorphous solid dispersions (ASDs) using polymer composites created a consistent drug release plateau. This approach minimizes variations in drug release, enhancing formulation predictability.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Developing amorphous solid dispersions (ASDs) is crucial for improving the bioavailability of poorly soluble drugs like ibuprofen (IBU).
- Controlling drug release profiles from ASDs is essential for achieving sustained therapeutic effects and reducing dosing frequency.
Purpose of the Study:
- To develop ibuprofen (IBU) sustained-release amorphous solid dispersions (ASDs) utilizing polymer composite matrices.
- To achieve stable drug release plateaus and elucidate the relationship between polymer matrix ratios and drug release behavior.
Main Methods:
- Formulation of IBU ASDs using a combination of hydrophilic and hydrophobic polymers via hot melt extrusion.
- Analysis of drug dissolution curves, polymer swelling, and intermolecular forces to understand drug release mechanisms.
Main Results:
- IBU ASDs exhibited a 'dissolution plateau phenomenon' with stable release when poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP VA64) content ranged from 35% to 50%.
- Drug release was modulated by PVP VA64-mediated dissolution and RSPO-PVP VA64 assembly-mediated swelling.
- Similar intermolecular forces between RSPO and PVP VA64 were identified as key to the stable release plateau.
Conclusions:
- The study offers a strategy for developing ASD sustained-release formulations with predictable release profiles through polymer combinations.
- The developed ASDs offer advantages in terms of process simplicity, scalability, and favorable drug release characteristics.
Keywords:
amorphous solid dispersiondrug release plateauhot melt extrusion technologypolymer composite matrixsustained-release regulationMore Related Videos
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