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Synthesis and Characterization of Supramolecular Colloids
Published on: April 22, 2016
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A supramolecular synthon approach to design amorphous solid dispersions with exceptional physical stability
Naga Kiran Duggirala1, Jinghan Li, N S Krishna Kumar
1Department of Pharmaceutics, University of Minnesota, MN-55455, USA. surya001@umn.edu.
Chemical Communications (Cambridge, England)
|April 12, 2019
Summary
A novel supramolecular synthon approach created stable amorphous solid dispersions (ASDs) for drugs. This method enhances drug dissolution and physical stability through specific drug-polymer interactions.
Area of Science:
- Materials Science
- Pharmaceutical Sciences
- Physical Chemistry
Background:
- Amorphous solid dispersions (ASDs) are crucial for improving the bioavailability of poorly soluble drugs.
- Designing stable ASDs requires understanding and controlling drug-polymer interactions.
- Traditional methods may not fully exploit molecular interactions for optimal stability and dissolution.
Purpose of the Study:
- To develop amorphous solid dispersions (ASDs) using a supramolecular synthon approach.
- To investigate the specific interactions between drugs with an amino aromatic nitrogen moiety and polyacrylic acid.
- To evaluate the impact of these interactions on the physical stability and dissolution of the drug.
Main Methods:
- Supramolecular synthon strategy for ASD formulation.
- Characterization using differential scanning calorimetry (DSC).
- Spectroscopic analysis including Infrared (IR) and 15N Nuclear Magnetic Resonance (NMR) spectroscopy.
- X-ray crystallography for structural elucidation.
Main Results:
- Confirmation of drug-polymer interaction via DSC, IR, 15N NMR, and X-ray crystallography.
- Demonstrated decrease in molecular mobility within the ASD.
- Achieved exceptional physical stability of the amorphous drug.
- Significantly enhanced drug dissolution rates.
Conclusions:
- The supramolecular synthon approach effectively creates stable ASDs.
- Drug-polymer interactions are key to enhancing physical stability and dissolution.
- This strategy offers a promising route for formulating poorly soluble drugs.
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