Ending the pain of an insulin injection daily for diabetic patients, Niagara University researchers have developed a miracle pill for oral administration to deliver insulin where it needs to go. The faculty members and undergraduate student from Niagara University are now sharing their in vivo testing results.
Mary McCourt, Lawrence Mielnicki, and rising senior Jamie Catalano presented their work on Wednesday at the 252nd National Meeting & Exposition of the American Chemical Society in Philadelphia.
“We have developed a new technology 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 biggest obstacle to delivering insulin orally is ushering it through the stomach intact. Insulin degrades often due to highly acidic environment of the stomach before it reaches the intestines and the bloodstream.
Some efforts to package insulin inside a protective polymer coating to shield the protein from stomach acids did not go well and another approach to develop inhalable insulin too proved futile. The Niagara University researchers have developed a new tactic.
Using the patented Cholestosomes developed in the B. Thomas Golisano Center for Integrated Sciences, the researchers have successfully encapsulated insulin. The novel vesicles are made of naturally occurring lipid molecules, which are normal building blocks of fats. But the researchers said that 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 degrading. When CholestosomesTM reach the intestines, the body recognizes them as something to be absorbed. The vesicles pass through the intestines, into the bloodstream, and then cells take them in and break them apart, releasing insulin.
The team has delivered multiple molecules with these vesicles into cells in the lab. To pack the most insulin into the CholestosomesTM, the 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 showed that certain formulations of CholestosomesTM 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.