Current drug treatments are focused on pharmacological and chemotherapeutical treatment such as controlling the acute and chronic aggravation of diseases, maintaining remission, treating specific complications, and reducing the toxic effects. Several drugs are inappropriate for long-term therapy due to high toxicity levels and the inability to maintain remission of the therapy. An inflammatory bowel disease is a group of idiopathic, chronic, and pathological conditions which pursue protracted relapsing and remitting course cause prolonged inflammation in the gastrointestinal tract, including diarrhea, abdominal pain, bleeding, anemia, and weight loss due to dysregulated immune response. Several drugs have been come to the market to treat inflammatory bowel disease, but they are not potential to the patient due to their higher toxicity rate and low therapeutic activity. Ozanimod is an anti-inflammatory and neuroprotective oral selective modulator of sphingosine-1-phosphate selectively targeting inflammatory bowel disease like ulcerative colitis and Crohn’s disease and is also involved in the treatment of multiple sclerosis. There is no serious adverse effect, as well as adverse events such as cardiac events, serious infections, or macular edema, was found in the treatment of inflammatory bowel disease. The conventional drug delivery of ozanimod has severe adverse effects, which can be reduced by nanocarrier and stability and bioavailability can be enhanced. This review discusses the Pharmacological and therapeutical insight of Ozanimod for targeting inflammatory bowel diseases like Ulcerative colitis and Crohn’s disease as well as Multiple Sclerosis and the importance of nanocarriers for Ozanimod to target the colon region and recent advancement technology introduced to Ozanimod.