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Development of new targeted medicines for inflammatory bowel disease

The Basit group at the UCL School of Pharmacy has made significant contributions to enhancing therapeutic efficacy in targeted oral medicines, particularly for drug delivery to the large intestine.

Yellow pills in a pharmaceutical production line.

22 October 2024

The group's research has focused on understanding how the environment within the gastrointestinal (GI) tract, such as pH levels, fluid volumes, intestinal transit times, and the microbiota affect how medicines are absorbed. Contrary to previous beliefs, they demonstrated that intestinal pH alone cannot appropriately deliver the targeted release of medicines into specific parts of the intestine, such as the inflamed bowel. This demanded the development of more advanced drug delivery systems.

One of their major innovations is the Phloral™ system - a sophisticated, delivery technology that uses both pH changes and the presence of gut bacteria to ensure precise drug release in the colon. Additional advancements to Phloral™ led to the group’s development of OPTICORE™, an enhanced multilayer system with accelerated drug release shown above. Both technologies have since been patented, with OPTICORE™ further being licensed as the coating for Asacol™ 1600mg, a mesalazine tablet used to treat inflammatory bowel disease.

Following the success of Phase III clinical trials, this product is now commercially available in over 50 countries worldwide and taken by over 1 million patients daily. Notably, this tablet is the highest prescription strength mesalazine product for oral delivery available in the world, helping increase patient adherence and reducing medication burden.

 

A graphic showing an enteric coated mesazaline tablet and the chemical structure.

Image: An enteric-coated mesazaline tablet and a description of its chemical structure. 

These technologies represent a major advancement over the standard, enteric-coated mesalazine tablets, which had variable success due to the inconsistent nature of the GI tract. The Basit group’s work has had a profound impact on both patient outcomes and the pharmaceutical industry, driving innovation and leading to significant commercial successes.