Complexation of Amlodipine Besylate with β-Cyclodextrin

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Supramolecular Chemistry

Background:

• Amlodipine besylate is a widely used antihypertensive drug.
• β-cyclodextrin (β-CD) is a cyclic oligosaccharide known for its ability to form inclusion complexes with various molecules.
• Improving the stability and bioavailability of amlodipine besylate is crucial for its therapeutic efficacy.

Purpose of the Study:

• To prepare and structurally characterize inclusion compounds of amlodipine besylate with β-cyclodextrin.
• To investigate the effect of different preparation methods on the formation of these inclusion compounds.
• To assess the impact of β-CD complexation on the stability and bioavailability of amlodipine besylate.

Main Methods:

• Preparation of inclusion compounds using kneading, co-precipitation, and freeze-drying techniques.
• Structural characterization via Fourier-Transform Infrared (FTIR) spectroscopy, X-ray diffraction (XRD), and Differential Scanning Calorimetry (DSC).
• Molecular modeling using Density Functional Theory (DFT) to elucidate the inclusion complex's spatial architecture.

Main Results:

• Successful formation of amlodipine besylate-β-CD inclusion compounds was confirmed by FTIR, XRD, and DSC analyses.
• Molecular modeling indicated that the dihydropyridine dicarboxylate moiety of amlodipine besylate is encapsulated within the β-CD cavity.
• The inclusion complex formation was consistent across different preparation methods, with variations in structural details.

Conclusions:

• The preparation methods employed effectively yielded amlodipine besylate-β-CD inclusion compounds.
• The structural data and molecular modeling confirm the successful inclusion of amlodipine besylate within the β-CD cavity.
• Complexation with β-cyclodextrin significantly enhances the stability and bioavailability of amlodipine besylate, offering potential therapeutic advantages.