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Amorphous solid dispersion of ibuprofen: A comparative study on the effect of solution based techniques
Ahmad Ziaee1, Stephen O'Dea1, Aoise Howard-Hildige1
1Synthesis & Solid State Pharmaceutical Centre (SSPC), Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick, Ireland.
International Journal of Pharmaceutics
|November 4, 2019
Summary
Amorphous solid dispersions (ASDs) improve drug solubility. Processing techniques like electrospinning significantly impact ASD homogeneity and drug release rates, with HPMCAS proving a superior excipient for ASD formulation.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Amorphous solid dispersions (ASDs) enhance the solubility of poorly soluble drugs.
- Solvent-based techniques like electrospinning (ES), spray-drying (SD), and rotary evaporation (RE) are used for ASD formulation.
- The impact of these processing techniques on ASD homogeneity and quality is not well understood.
Purpose of the Study:
- To investigate the effect of ES, SD, and RE on the physicochemical properties and homogeneity of ibuprofen (IBU) ASDs.
- To compare the ASD forming capabilities of HPMCAS and HPMCP-HP55 excipients.
- To assess the influence of processing techniques on drug release and ASD stability.
Main Methods:
- Formulation of IBU ASDs with HPMCAS and HPMCP-HP55 using ES, SD, and RE.
- Evaluation of physicochemical, morphological, and dissolution properties.
- Differential Scanning Calorimetry (DSC) for assessing polymer ASD forming strength.
- Principal Component Analysis (PCA) of Raman spectra for ASD homogeneity analysis.
Main Results:
- ASD homogeneity is highly dependent on the processing technique, not solely the API:excipient ratio.
- Electrospun ASDs exhibited the highest drug release rates due to fibrous morphology and high surface area.
- Electrospun samples were the least homogenous, potentially affecting long-term stability.
- HPMCAS demonstrated superior performance as an ASD co-former compared to HPMCP-HP55.
Conclusions:
- Processing technique critically influences ASD homogeneity and drug release.
- Electrospinning yields rapid drug release but compromises homogeneity.
- HPMCAS is a more effective excipient for creating stable and high-performance amorphous solid dispersions.
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