Ulcerative colitis is an idiopathic, chronic and relapsing intestinal inflammatory disorder of digestive tract which is represented by bloody diarrhoea, tenesmus, anaemia, bowel distension. In Western Europe and in the USA, ulcerative colitis has a proportion of approximately 6 to 8 cases per 100,000 peoples and an approximated prevalence of around 70 to 150 per 100,000 peoples. Proper local targeting is the major challenge in the treatment of ulcerative colitis. To minimize these challenges oral controlled drug delivery system seem to be a promising approach for colon targeting. The main motive of this article is to explore the role of oral controlled drug delivery systems in ulcerative colitis for appropriate targeting of drug entities to the colon. The increased demand of these dosage forms is because of the alertness to toxicity and ineffectiveness of oral conventional approach in the form of capsules and tablets. Generally, conventional formulations create fluctuation in drug concentration in the tissues and bloodstream with ensuing undesirable toxicity and poor efficacy. These limitations of conventional treatment such as fluctuation in drug concentration, the inappropriate drug at the target site and repetitive dosing could be overcome by the oral controlled drug delivery system. The present article contains brief review on the pathophysiology of ulcerative colitis and several formulation approaches used for colon targeting by using the oral controlled drug delivery system.