Colonic targeting of the polypeptide drug nisin

摘要

Nisin is a peptide antimicrobial agent. It was found to be active against Clostridium difficile which causes severe repulsing diarrhea, and vancomycin resistant enterococci, which causes a large increase in the number of untreatable or difficult to treat bacterial infections. Both organisms colonize in the colon. Therefore, nisin must be formulated in a dosage form which immediately releases the intact antimicrobial agent in the colon. Nisin being a polypeptide is digested by the proteolytic enzymes in the small intestine. Therefore, protection of nisin through the gastrointestinal tract until it reaches the colon is essential. Developing colonic drug delivery system, using currently available materials, with potential to succeed should be based on utilization of pH and transit time of the different segments of the GIT. In this study EUDRAGIT L30D coating was used to target nisin to the colon.