Insulin is a polypeptide hormone (MW of ~ 6 KD (Kilo Daltons)) that regulates carbohydrate metabolism and blood glucose sugar levels. Patients with Type 1 diabetes mellitus, caused by autoimmune destruction of insulin-producing beta cells in the pancreas, depend on exogenous insulin usually injected subcutaneously. Patients with Type 2 diabetes mellitus, caused by genetic and environmental factors such as obesity, age, and physical inactivity, have either low insulin production or insulin resistance, or both. Approximately 20.8 million people in the United States have diabetes, an estimated 14.6 million are diagnosed and 6.2 million are undiagnosed. The estimated market size for insulin is about $13 billion worldwide and is estimated to grow to $20 billion by 2020. Insulins account for about 50% of the diabetes market segment with a historic growth rate of 14% per annum.

The Need for Change

Insulin is usually administered by subcutaneous injection since it is rapidly degraded into amino acids in the gastrointestinal tract by proteolytic enzymes. There is a significant amount of ongoing research on the oral, patch and pulmonary delivery of insulin. While the oral delivery of proteins and peptides are challenging because of enzymatic degradation in the GI tract and absorption through epithelial cells, oral administration is still more attractive in terms of ease of use and patient compliance. Currently, there are no insulin tablets for patients with diabetes.

Nanoencapsulated Insulin Can Help

Oral insulin represents one of the holy grails of biotechnology and drug development. We are developing:

• APH-0907 – a nanotechnology formulation of insulin in biodegradable polymers that makes insulin oral bioavailable through protection in the digestive tract and stomach, and delivery in the small intestine.