Preparation, Characterization and Antiinflammatory Activity of Celecoxib-?-Cyclodextrin Inclusion Complexes

Abstract

The influence of β-cyclodextrin on the in vitro dissolution rate, in vivo absorption and oral bioavailability of a poorly water soluble antiinflammatory agent, celecoxib was studied. For this purpose, celecoxib and β-cyclodextrin complexes were prepared in 1:1 and 1:2 molar ratios by the physical mixture, kneading and freeze-drying methods. The complexes were preliminary confirmed using differential scanning calorimetry, fourier transform-infrared spectroscopy and scanning electron microscopy. The solubility studies revealed a linear relationship between the increase in celecoxib solubility and the increase in β-cyclodextrin concentration. The in vitro dissolution studies that were performed in phosphate buffer (pH 7.4) showed that celecoxib:β-cyclodextrin (1:2) solid complexes prepared by freeze-drying method had highest celecoxib release compared to the other solid complexes. Pharmacological studies were performed with this complex in a carrageenan induced rat hind paw oedema model. Regarding to the inhibition of edema (%) and swelling (%) results, celecoxib:β-cyclodextrin (1:2) binary mixture prepared by freeze-drying method showed significant improvement compared to pure drug.