Solid-state flurbiprofen and methyl-β-cyclodextrin inclusion complexes prepared using a single-step, organic...

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Physical Chemistry

Background:

• Flurbiprofen exhibits poor aqueous solubility, limiting its therapeutic efficacy.
• Cyclodextrins, particularly methyl-β-cyclodextrin, are known to form inclusion complexes, potentially improving drug solubility.
• Supercritical fluid technology offers an environmentally friendly and efficient method for complex formation.

Purpose of the Study:

• To enhance the solubility and dissolution properties of flurbiprofen using methyl-β-cyclodextrin.
• To evaluate the efficacy of supercritical carbon dioxide technology for preparing these inclusion complexes.
• To characterize the formed inclusion complexes and assess their drug release profiles.

Main Methods:

• Preparation of flurbiprofen-methyl-β-cyclodextrin inclusion complexes using supercritical carbon dioxide processing.
• Characterization techniques including solubility studies, DSC, XRD, and SEM.
• In vitro dissolution studies to evaluate drug release.
• Computational molecular docking to predict complex formation and stoichiometry.

Main Results:

• Stable flurbiprofen-methyl-β-cyclodextrin inclusion complexes were formed with a 1:1 stoichiometry.
• Supercritical carbon dioxide processing significantly enhanced flurbiprofen dissolution, with 99.39% release within 30 minutes compared to 1.11% for pure flurbiprofen.
• Rapid drug release (>80% in 10 min) was observed for complexes prepared at 45°C, regardless of pressure.

Conclusions:

• Supercritical carbon dioxide technology is a viable, single-step, solvent-free method for preparing flurbiprofen-methyl-β-cyclodextrin inclusion complexes.
• The prepared inclusion complexes demonstrate markedly improved dissolution properties of flurbiprofen.
• This approach holds promise for developing advanced drug delivery systems with enhanced bioavailability.