Intestinal inflammation, especially chronic (such as inflammatory bowel disease [IBD]), is an indispensable participant in the colonic neoplastic process, fostering the proliferation, survival, and migration of colonic tumor cells. Molecularly targeted therapeutics (e.g. anti-TNF-α agents) that exploit the targets involved in the pathophysiology of inflammatory responses in IBD are the most potent drugs currently available to treat IBD, which may also present anti-colon cancer effects. Unfortunately, most of these drugs were administered systemically in a high dose, and their use is limited by severe side effects.