Aphios Corporation today announced that it received notification of allowance for a United States Patent entitled “Polymer Microspheres/Nanospheres and Encapsulating Therapeutic Proteins Therein” for the oral delivery of insulin.
With completion of the human genome sequence, the growth of the biotechnology marketplace is expanding rapidly. One of the major factors limiting the marketability and industrialization of biotechnology drugs is the method of delivery. These macromolecules are usually very effective when they can get to the disease site. They are also, for the most part, nontoxic since they mostly mimic human proteins. Unfortunately, these molecules, like insulin, are quite large and are most readily delivered by daily injections or intravenously in a hospital setting. These macromolecules are all candidates for improved oral, patch and pulmonary drug delivery.
“Aphios is enhancing the oral bioavailability of therapeutic proteins by encapsulating protein macromolecules and nanoparticles in biodegradable polymer nanospheres,” says Dr. Trevor P. Castor, President & CEO, Aphios Corporation. Nanoencapsulation is being used to protect the protein macromolecules/nanoparticles during the stomach passage; the residence time in the stomach will be short compared to the protein release rate from the polymer nanospheres. Animal data demonstrates that insulin, a labile peptide, being nanoencapsulated was protected in the stomach and then transported to the blood. When protein nanoparticles reach the gut, they are transported across the lining, which may be mediated by M cells in the lymphatic tissue of the gut. Alternatively, the protein can be mobilized from nanospheres and rapidly transported to systemic circulation by the epithelial cells. Both the polymer “shell” and the protein macromolecules/nanoparticles are intended to enable and regulate this stage of drug transport. With the optimal combination of the biodegradable polymer nanospheres shell properties and protein characteristics, we anticipate a significant improvement in oral bioavailability of protein therapeutics. We believe that our oral delivery nanotechnology will be applicable to large as well small protein molecules since we have demonstrated that our protein nanoparticles technology is independent of size and molecular weight (MW).