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

Abstract

The influence of beta-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 beta-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 beta-cyclodextrin concentration. The in vitro dissolution studies that were performed in phosphate buffer (pH 7.4) showed that celecoxib:beta-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:beta-cyclodextrin (1:2) binary mixture prepared by freeze-drying method showed significant improvement compared to pure drug.