Niagara University faculty present groundbreaking research, new Insulin pill for diabetes patients.
The need for painful insulin injections by certain diabetes patients may be eliminated with the introduction of a new technique for oral insulin delivery developed by scientists at Niagara University in upstate New York.
Niagara faculty members, Mary McCourt, Ph.D., Lawrence Mielnicki, Ph.D., and undergraduate student Jamie Catalano, presented their development at the 252nd National Meeting & Exposition of the American Chemical Society, the world’s largest scientific society, in Philadelphia.
“The new technology is called a CholestosomeTM,” said Dr. McCourt, leader of the research team. “A CholestosomeTM is a neutral, lipid-based particle that is capable of doing some very interesting things.”
“The technology is a vesicle that carries the molecules intact to the GI tract, without the obstacles of prior versions that degraded the insulin in the harsh, highly acidic environment of the stomach. CholestosomeTM is resistant to pH and bile salts, which, when met with absorbing lipids, becomes picked up by that carrier and delivered intact,” said Dr. McCourt. “Cholestosomes also get into cells directly and move into the bloodstream where they’re needed.”
The patented CholestosomeTM, developed at Niagara University’s B. Thomas Golisano Center for Integrated Sciences, allowed the researchers to successfully encapsulate insulin. Dr. McCourt noted that the novel vesicles are comprised of naturally occurring lipid molecules, normal building blocks of fats. They are unlike other lipid-based drug carriers, called liposomes.
“Most liposomes need to be packaged in a polymer coating for protection,” said Dr. Mielnicki. “Here, we’re just using simple lipid esters to make vesicles with the drug molecules inside.”
Computer modeling showed that once the lipids are assembled into spheres, they form neutral particles resistant to attack from stomach acids. Drugs can be loaded inside and the tiny packages can pass through the stomach without breaking down. When CholestosomeTM reaches the intestines, the body recognizes it as something to be absorbed. The vesicles pass through the intestines, into the bloodstream where cells take them in and break them apart, releasing the needed insulin.
There have been other attempts at this process, said the Niagara research team. One approach, they reported, packages insulin inside a protective polymer coating to shield the protein from stomach acids and is being tested in clinical trials. Another is inhalable insulin, which drew positive reviews from some patients, but sales did not take off.
Another oral medication on the market, developed by the Israeli pharmaceutical company, Oramed, uses a stimulating absorption across the GI tract, but the delivery has a low rate of absorption.
To pack the most insulin into CholestosomeTM, the Niagara researchers determined the optimal pH and ionic strength of the drug-containing solution. They then moved the most promising candidates on to animal testing. Studies with rats demonstrated that certain formulations of CholestosomeTM loaded with insulin have high bioavailability, which means the vesicles travel into the bloodstream where the insulin needs to be.
Next, the team plans to further optimize the formulations, conduct more animal testing and develop new partnerships to move forward into human trials. They also say CholestosomeTM may be applicable for delivery of other medications.
The researchers were funded by Niagara University, CPL Associates and Theraholdings A.G.
Filed Under: Drug Discovery