This paper deals with various aspects of oral insulin delivery system. Insulin is used for the treatment of diabetes mellitus, which is characterized by the elevated glucose level (above the normal range) in the blood stream, that is, hyperglycemia. Oral route of administration of any drug is the most convenient route. Development of oral insulin is still under research. Oral insulin will cause the avoidance of pain during the injection (in subcutaneous administration), anxiety due to needle, and infections which can be developed. Different types of enzyme inhibitors, like sodium cholate, camostat, mesilate, bacitracin, leupeptin, and so forth, have been used to prevent insulin from enzymatic degradation. Subcutaneous route has been used for administration of insulin, but pain and itching at the site of administration can occur. That is why various alternative routes of insulin administration like oral route are under investigation. In this paper authors summarized advancement in insulin delivery with their formulation aspects. 1. Introduction Diabetes mellitus is a metabolic disorder which is characterized by the elevated glucose level (above the normal range) in the blood stream that is hyperglycemia. Millions of people in the world are affected by diabetes. It has been studied that approximately 7% of the people in US are affected by diabetes. Insulin is a polypeptide hormone required to be taken in patients suffering from diabetes mellitus. It is an anabolic hormone. Due to insulin glucose uptake by the cells of different organs (like muscle, liver, fat cells, etc.) from the blood can be possible. It stores the glucose in muscle and liver as glycogen. In the absence of insulin, cells of different organs cannot take the glucose through blood. In this condition fat is used as an energy source. Any imbalance in the level of insulin causes diabetes mellitus. It is produced by islets of Langerhans (clusters of cells that are embedded in exocrine portion of pancreas) [1]. Insulin which is very close to the human insulin is porcine insulin. Insulin controls the energy metabolism with the help of epinephrine and norepinephrine. It is the hormone which plays a very important role in use of fuels by tissues. Insulin is stored in cytosol and released by exocytosis. Metabolism of insulin takes place by enzyme Insulinase. Half-life of insulin is approximately 6 minutes. Insulin secretion is increased by an increase in glucose, amino acids, and gastrointestinal hormones. Release of insulin is decreased when there is a scarcity of dietary fuels, during stress
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