An overview on recent approaches for colonic drug delivery systems.

Colon-targeted drug delivery systems have garnered significant interest as potential solutions for delivering various medications susceptible to acidic and catalytic degradation in the gastrointestinal (GI) tract or as a means of treating colonic diseases naturally with fewer overall side effects. The increasing demand for patient-friendly drug administration underscores the importance of colonic drug delivery, particularly through noninvasive methods like nanoparticulate drug delivery technologies. Such systems offer improved patient compliance, cost reduction, and therapeutic advantages. This study places particular emphasis on formulations and discusses recent advancements in various methods for designing colon-targeted drug delivery systems and their medicinal applications.

OPTICORE™, an innovative and accurate colonic targeting technology.

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.