Most oral medications release drugs in the stomach or small intestine, but a wealth of possibilities lie in delivering drugs further down the gastrointestinal tract, in the colon or rectum. Delivering drugs to these sites can facilitate more effective treatment of local diseases, such as inflammatory bowel disease and colorectal cancer, and limit adverse drug effects. The microbiome, which encompasses a myriad of emerging therapeutic targets, can also be targeted via the colon. Further, colorectal drug delivery may help to boost the bioavailability of certain drugs that are susceptible to interactions with specific enzymes and transporters abundantly found in the small intestine. Our latest review presents contemporary insights into colorectal drug delivery and the most effective techniques for developing new colorectal targeted medicines. The idiosyncrasies of colonic and rectal physiology are presented to enable design of new targeted formulations. Then, the most reliable formulations for colonic/rectal drug delivery are examined with mechanistic analysis of their drug release mechanisms. The review concludes with a detailed discussion of pertinent in vitro, in vivo, and in silico tools for streamlined development of new colorectal targeted medicines.

Read our open access research review here