Prodrug beats diclofenac
doi:10.1038/nindia.2011.7 Published online 26 January 2011
Researchers have identified one of the prodrugs of diclofenac ester as a better candidate for the treatment of chronic inflammatory diseases than its widely used parent drug diclofenac sodium. Pro drugs are forerunners or precursors to drugs.
The researchers synthesized pro drugs 4, 5 and 6 of diclofenac ester and evaluated them in vitro and in vivo for potential use by oral delivery. The idea was to obtain an enzymatically changeable (labile) and less ulcer-causing compound than diclofenac sodium.
They found these prodrugs to be anti-inflammatory and exhibiting lesser ulcerogenic potential in experimental mice. The prodrugs also underwent quick enzymatic hydrolysis to release the parent drug diclofenac within 30 minutes to an hour in rat liver microsomes and rat plasma.
Of the three, prodrug 4 was found to be a best for the treatment of chronic inflammatory diseases.
Bandgar, B. P. et al. Synthesis, Characterization, and Biological Evaluation of Novel Diclofenac Prodrugs. J. Med. Chem. doi: 10.1021/jm101095e (2011)