Targeted delivery, safety, and efficacy of oral enteric-coated formulations of budesonide

Budesonide is a potent corticosteroid with a high first-pass metabolism rate. Two commercially available enteric-coated pH-dependent release formulations (Entocort™ EC and Budenofalk®) deliver budesonide to the ileum and proximal colon, regions most commonly affected in Crohn's disease. The drug's effectiveness in this disease has been proven in multiple, placebo-controlled trials, where it has been shown to be superior to mesalamine and placebo, and equivalent to prednisolone for the control of mild to moderately active right-sided Crohn's disease. This beneficial therapeutic effect comes with less adrenal suppression and a small improvement in the clinical adverse effect profile, as compared to prednisolone. However, budesonide provides no benefit over conventional therapy for left-sided colonic disease, and it is less effective for treatment of more severe disease activity and more distal colonic disease. Continuous budesonide does not prolong remission and is, therefore, best used in an intermittent fashion to treat acute exacerbations.