Oral delivery of biologics
Biologics are used to treat a variety of chronic diseases including diabetes and arthritis. Not surprisingly, they command a large share of the therapeutics market. Moreover, a large number of therapeutic proteins are currently in clinical development and the net present value of major biologics in the pipeline is estimated to be $129 billlion. Unfortunately, innovative approaches to delivery of biologics are still lagging behind. Current methods rely on either subcutaneous delivery (for small biologics) or intravenous delivery (for larger antibodies and proteins). Adherence and cost considerations associated with these two delivery methods continue to hamper the wider use of biologics.
As oral delivery is associated with high compliance and low cost, one potential solution would be to deliver biologics orally (while simultaneously preserving their systemic effects). The Mitragotri laboratory at Harvard has developed a novel platform technology to systemically deliver biologics after oral administration. The core technology features Ionic Liquids and utilizes GRAS ingredients that enable stabilization of biologics and enhance permeation across the intestinal epithelium.
This novel technology has been safely tested in rodents. Efficacy studies in rodents using Insulin, a widely used peptide within the diabetic population, revealed a very favorable glycemic response following oral administration. Pharmacokinetic measurements also revealed high level of systemic bioavailability that is well above the thresholds that were anticipated by current experts in this area of research. This technology is not limited to delivery of Insulin as the technology is highly tunable and thus adaptable to a wide range of therapeutics. Further development of this technology will allow for the oral delivery of additional high-value biologics. If successful, this technology will represent a paradigm shift in how biologics are administered.
Press release from Harvard SEAS (June 2018)
Publication in PNAS (July 10, 2018; published online June 25, 2018)