Solubility enhancement of celecoxib using beta-cyclodextrin inclusion complexes

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Physical Chemistry

Background:

• Celecoxib exhibits poor water solubility, limiting its bioavailability.
• Beta-cyclodextrin (betaCD) is a known complexing agent capable of improving drug solubility.
• Inclusion complex formation is a strategy to enhance the dissolution rate of poorly soluble drugs.

Purpose of the Study:

• To investigate the complexation of celecoxib with beta-cyclodextrin in aqueous and solid states.
• To evaluate the impact of inclusion complex formation on celecoxib's solubility and dissolution rate.
• To characterize the solid inclusion complexes prepared by the kneading method.

Main Methods:

• Phase solubility studies and spectral shift analyses were employed to confirm 1:1 complex formation in solution.
• Apparent stability constants were determined using phase solubility and spectral shift data.
• Solid inclusion complexes were prepared via the kneading method at various molar ratios and characterized by differential scanning calorimetry (DSC).

Main Results:

• Complexation with betaCD significantly enhanced the solubility and dissolution rate of celecoxib.
• Phase solubility and spectral shift studies confirmed the formation of a 1:1 celecoxib-betaCD inclusion complex.
• DSC confirmed the formation of solid inclusion complexes, and dissolution rates increased with higher betaCD content, outperforming the pure drug and physical mixture.

Conclusions:

• Celecoxib-betaCD inclusion complexes effectively improve the solubility and dissolution characteristics of celecoxib.
• The kneading method is suitable for preparing solid inclusion complexes with enhanced drug release properties.
• This complexation strategy offers a promising approach for improving the oral bioavailability of celecoxib.