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

Sensoy D., Goenuellue U., Sagirli O., Yener G., Altug T.

ASIAN JOURNAL OF CHEMISTRY, vol.21, no.3, pp.1759-1768, 2009 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 21 Issue: 3
  • Publication Date: 2009
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1759-1768
  • Istanbul University Affiliated: Yes


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.