Eurofins CDMO helps solve the rising challenge of colon drug delivery for biologics

by Jody Voorspoels, Chief Scientific Officer, Eurofins CDMO Europe,  jodyvoorspoels@eurofins.com

Due to the increasing incidence of inflammatory bowel disease (IBD), most commonly Crohn’s disease and ulcerative colitis, colon delivery systems for oral administration have grown in popularity since the 1990s. Additionally, selective release of biologic drugs to the large bowel has been proposed as a viable strategy to enhance their oral bioavailability compared to gastric and/or small intestinal delivery via conventional peroral dosage forms.

Eurofins CDMO offers tailor-made solutions for biotech companies to deliver their biologic compound to the colon. Classical approaches are possible, which are based on pH-triggered polymeric coating of the dosage form (tablet, capsule or multiparticulate systems like pellets or minitablets). These coatings are resistant to acidic gastric pH and only dissolve and thus release the drug substance when the intestinal pH reaches a value of 6.5 to 7.0, typically in the ileocaecal region. Although this is a well-established technology, the drawback is that these coatings completely rely on the intestinal pH, which can vary from patient to patient, especially in those with IBD conditions. If the ileo-caecal or colonic pH does not reach the minimum value to dissolve the coating system, the drug release is incomplete or even zero. This results in a failure to deliver the drug as intended at the site of action.

Recently, more advanced systems can be offered. These are based on combining pH-triggered systems and enzymatically degradable systems, mostly polysaccharides. The dissolution of the coating is relying on two different mechanisms (pH or enzymatic), which results in a lower failure rate, compared to the single pH-triggered systems. These combinations are sometimes considered as fail-safe systems.

Research is currently underway at the Eurofins CDMO Ghent site (Belgium) to develop colon drug delivery systems for biologic drug substances. In addition to release characteristics, an extra challenge is the stability of the biologic drug substance, both in the dosage form and after release in the colon, where the biologic is often prone to enzymatic degradation.

For more information: www.eurofins.com/cdmo