Synthesis, characterization and preliminary analysis of in vivo biological activity of chitosan/celecoxib microcapsules

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4147-51. doi: 10.1016/j.bmcl.2010.05.054. Epub 2010 Jun 9.

Abstract

The use of chitosan as the wall of microcapsule designed for delivery of encapsulated celecoxib is reported. Microcapsules were characterised with respect to size and encapsulation efficiency of celecoxib. In vivo animals demonstrated that both free celecoxib administration and chitosan/celecoxib microcapsules administration lead to a significant inhibition of cyclooxygenase-2 protein expression in the hepatocytes when compared with vehicle control mice. Interestingly, microcapsule containing celecoxib showed a better inhibition of cyclooxygenase-2 protein expression when compared with a simple oral administration of free celecoxib. Gas-chromatography-mass-spectrometry analysis showed that in mice treated with free celecoxib or chitosan/celecoxib microcapsules, their plasma concentration of celecoxib was similar. Microcapsules-based biomaterials as oral drug delivery vehicles may help to improve the absorption efficiency of therapeutic drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Celecoxib
  • Chitosan / chemical synthesis*
  • Chitosan / pharmacology*
  • Cyclooxygenase 2 Inhibitors / chemical synthesis*
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Gas Chromatography-Mass Spectrometry
  • Microscopy, Electron, Scanning
  • Microspheres
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology*
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology*

Substances

  • Cyclooxygenase 2 Inhibitors
  • Pyrazoles
  • Sulfonamides
  • Chitosan
  • Celecoxib