Synthesis and evaluation of azo pro-drugs of flurbiprofen for colon targeting

This investigation for revealing the new synthsized azo prodrug of flurbiprofen which increase the potency of approach and decrease the associated adverse effects. Different class of amino acids which have synergestic effect with flurbiprofen for the treatment of UC and safely used in IBD, have been selected for synthesis of azo prodrug with fenoprofe. These azo prodrug of different classes has been further evaluated against physicochemical property, in vitro stability test and in vivo ulcer models in rats. The associated consequence reveals the successful synthesis of azo prodrug and also explored the significant therapeutic potential against TNBS induced UC model. Thin layer chromatography of all the intermediates and final compounds were performed on silica gel plates, using UV and iodine chamber for visualization of spots and single spots were obtained for the same,. Open capillary method was used to determine the melting points of the final products, which was found to be uncorrected. The objective of synthesizing such azo prodrugs of flurbiprofen which have improved aqueous solubility and lower log P values than that of flurbiprofen has been achieved. Such high values for aqueous solubility of these novel prodrugs confirm that they will reach intact into colon and will not get absorbed in the upper GIT. All physical and microscopical alteration has also been evaluated in standard (sulfasalazine) and all other azo prodrug groups, and significantly compared with colitis control. This evaluation confirmed that azo prodrugs significantly protect against TNBS induced colitis and show the similar results with sulfasalazine group. This finding proves the therapeutic potential of azo prodrug against ulcerative colitis as similar or better to sulfasalazine.