UMN-Dow Research Yields Methods To Make Orally Administered Drugs More Absorbable

Patent filed for ‘smart’ polymer that could have big implications for pharma pipelines.

UMN-Dow Research Yields Methods To Make Orally Administered Drugs More Absorbable
The University of Minnesota won several U.S. patents over the years as the result of a long-standing research collaboration on plastics with Dow Chemical Co., including such inventions as flame-retardant epoxies, new polymers for use in nanotechnology and several other industry-changing advances.
Now, however, it’s the health care and pharmaceutical markets that stand to be impacted by their latest patent-pending collaboration: a new kind of biodegradable polymer that allows orally administered drugs which are now considered insoluble in the human digestive tract to be better absorbed.
The inventors at the U of M’s College of Science and Engineering and at Dow have hailed it as a breakthrough having the potential to make a major dent in the pharma industry.
The new patent covers the use of a certain kind of “smart polymer” – a type of advanced plastic specialized in by U of M researchers – as a first-of-its-kind excipient (excipients are substances added to drugs to make them more dissolvable in the stomach).
For decades, the most common type of excipient for oral drugs has been the polymer hypromellose acetate succinate. Its biggest drawback is that it often isn’t effective enough to make many kinds of early-pipeline drug candidates clinically useful. But now smart polymers are showing that even failed experimental compounds, initially rejected because of insolubility, can be repositioned successfully with more effective and inexpensive oral formulations.
What makes these advanced polymers “smart” is that they are designed to change their chemistry in response to environmental stimuli, such as the temperatures and conditions encountered within the human digestive tract.
 In a Dow-funded study performed on rats (published last month in the academic journal ACS Central Science), the researchers discovered that one kind of polymer tripled the “oral bioavailability” of the common anti-seizure drug phenytoin.
This could be huge news for the pharmaceutical industry, which continually struggles with the fact that many drugs (especially experimental ones) are ineffective because the doses needed to achieve efficacy are so high that they cause unsafe side effects. A technology that renders them soluble at lower doses could have a significant cost-reducing effect on the drug-discovery pipeline, one of the researchers asserted.
“It takes about $1 billion and 10 to 15 years for a pharmaceutical company to develop a new drug, but then they sometimes find marketable formulations are limited by solubility,” Dow R&D manager and study co-author Steven Guillaudeu said in an issued statement. “The methodology our team has created could help drug companies advance their pipeline compounds by using a better method to improve solubility and therefore bioavailability. The approach could have a major impact on the multibillion-dollar industry.”
Teresa Reineke, a U of M chemistry professor whose lab has been working on the human health aspects of plastics, added the key to the discovery’s commercial and clinical potential is that the inventors have succeeded in making it workable at industrial-scale levels that could be tapped for a wide range of drugs.
“While we were pleased with the results with (phenytoin), the most important thing is that we have developed a high-throughput methodology for excipient development that could be used by many companies to create other life-saving medicines,” Reineke said.
The U of M and Dow launched a $17 million research collaboration in 2011, with almost $2.3 million per year going toward the school’s researchers in chemical engineering and materials science, chemistry and mechanical engineering. Dow also contributed $5 million to help fund an expansion of Amundson Hall, which has completed last year.
Many of the U’s advances in the plastics field have come via its Center for Sustainable Polymers, which in 2014 received a five-year, $20 million grant from the National Science Foundation. Its mission is to “transform how plastics are made and unmade.”
Under the direction of Marc Hillmyer, a Distinguished McKnight Professor in the U’s chemistry department, the leaders of the multi-disciplinary collaborative say they have plans, among other things, to design plastics that are non-toxic, created in environmentally-friendly ways and don’t create toxic byproducts when recycled, composted or incinerated.
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