pulmicort and nitrobenzene

Celecoxib is a COX-2 inhibitor drug that can be used to reduce the risk of colorectal adenocarcinoma. Glucocorticoids are used in the treatment of inflammatory bowel disease. A limitation to the use of both drug types is that they undergo absorption from the intestinal tract with serious side effects. The prodrug systems introduced here involve forming a nitro-substituted acylsulfonamide group in the case of celecoxib and a nitro-substituted 21-ester for the glucocorticoids. Drug release is triggered by the nitro reductase action of the colonic microflora, liberating a cyclization competent species. The release of the active parent drugs was evaluated in vitro using Clostridium perfringens and epithelial transport through Caco-2 monolayer evaluation was carried out to estimate the absorption properties of the prodrugs compared to the parental drugs.

Topics: Antineoplastic Agents; Budesonide; Caco-2 Cells; Celecoxib; Cell Membrane Permeability; Clostridium perfringens; Colorectal Neoplasms; Cyclooxygenase 2 Inhibitors; Humans; Lactones; Nitrobenzenes; Nitroreductases; Prednisolone; Prodrugs; Pyrazoles; Sulfonamides