Design of a colonic delivery system based on cationic polymethacrylate (Eudragit E100)-mesalamine complexes

In this work, the design and evaluation of a colonic drug delivery system containing mesalamine (M) is presented. The main goal was to enable M to reach the first part of the colon, where the drug could then be released. To facilitate this, a tablet core was coated with two thin layers. The first compounded by chitosan, which was responsible for core protection in the small intestine until it reached the colon. Once at the colon, microbiological enzymatic activity of the caecal content would degrade the Ch layer, thus triggering drug release. The second layer, the outer one, was compounded with Eudragit L100 (EL), with its function being to avoid the dissolution of the Ch-covered core along the gastro intestinal tract (GIT). In order to achieve a modulated drug release, carbomer P934 (1%) was also included. Dissolution studies showed that the formulation seemed to behave as predicted. The amount of M released from the coated tablet was less than 10% at pH = 1.2 and 6.8. However, when the coated tablet was evaluated in a medium with a caecal content of pH = 7.4, the M delivery was immediately triggered owing to enzymatic activity of the microflora. In this medium, similar to 60% of M was released in a period of 3 h. Although these results are promising, further studies are still necessary to evaluate the possible in vitro/in vivo correlations.</.