OPTICORE™, an innovative and accurate colonic targeting technology

Abstract

Inflammatory bowel disease (IBD) is a debilitating condition, estimated to affect 7 million people worldwide. Current IBD treatment strategies are substandard, relying on colonic targeting using the pH gradient along the gastrointestinal tract. Here, we describe an innovative colonic targeting concept, OPTICORE™ coating technology. OPTICORE™ combines two release triggers (pH and enzyme: Phloral™) in the outer layer, with an inner layer promoting a release acceleration mechanism (Duocoat™). The technology comprises an inner layer of partially neutralized enteric polymer with a buffer agent and an outer layer of a mixture of Eudragit® S and resistant starch. 5-aminosalicylic acid (5-ASA) tablets were coated with different inner layers, where the type of polymer, buffer salt concentration and pH of neutralization, were investigated for drug release acceleration. Buffer capacity of polymethacrylate neutralized polymer significantly contributes to the buffer capacity of the inner layer formulation, while buffer salt concentration is a major contributor to dispersion buffer capacity in the case of hypromellose enteric polymer formulations. An interplay between buffer capacity, pH and ionic strength contributes to an accelerated drug release. Resistant starch does not impact the enteric properties but allows for drug release mediated by colonic bacterial enzymes, ensuring complete drug release. Therefore, OPTICORE™ technology is designed to offer significant advantages over standard enteric coatings, particularly allowing for more accurate colonic drug delivery in ulcerative colitis patients.

Keywords: Colon targeted oral drug products; Colonic drug delivery systems; Gastro resistant film coatings; Gut microbiome; Intestinal microbiota triggered drug release; Mesalazine.