Press Releases and News

United States Patent Office Issues Patent for Oral Delivery of Insulin
October 23, 2013
Woburn, Mass. – Aphios Corporation is pleased to announce that United States Patent Office issued US Patent No. 8,440,614 entitled "Polymer Microspheres/Nanospheres and Encapsulating Therapeutic Proteins Therein" for the oral delivery of insulin.

Oral insulin represents one of the holy grails of biotechnology and drug development. 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 unmet medical need to improve the delivery of insulin. While the oral delivery of proteins and peptides is 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.

Aphios' oral insulin product, APH-0907, being developed is a nanoencapsulation of insulin in biodegradable, hydrophobic polymer nanospheres (US Patent, 2013). The polymer, which is resistant to stomach acids, protects insulin from enzymatic degradation during the stomach passage. When protein nanoparticles reach the gut, they stick to the cell wall lining because of their hydrophobicity and are then transported across the lining. This transport may be mediated by M cells in the lymphatic tissue of the gut. The nanoparticles are rapidly transported to systemic circulation by the epithelial cells. As the biodegradable polymer shell degrades, insulin is released into the blood stream.

Dr. Trevor P. Castor, Inventor and CEO of Aphios Corporation states that "Our enabling technology platform to deliver proteins orally will be applicable to both small as well as large protein molecules."

ABOUT INSULIN AND DIABETES

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. Insulin accounts for about 50% of the diabetes market segment with a historic growth rate of 14% per annum.

ABOUT APHIOS CORPORATION

Aphios® Corporation, a clinical-stage biotechnology company, is developing enhanced therapeutics for chronic, debilitating diseases and improving quality of life. Using advanced scientific and engineering techniques, we are developing green, enabling technology platforms for improving drug discovery and manufacturing, nanotechnology drug delivery, viral vaccines, and virus-free human plasma and biologics. Based on these platforms, Aphios is developing quality-of-life medicines for health maintenance and disease prevention, and enhanced therapeutics for the treatment of certain cancers and supportive care, infectious disease such as HIV, CNS disorders such as Alzheimer's disease and metabolic diseases such as diabetes.