Diabetes treatment may become ‘ouchless’ with the new insulin pill

An insulin pill that will spare millions of people with diabetes having to administer daily injections is a major step closer to reality.

Every day, millions of people with diabetes inject themselves with insulin to manage their blood-sugar levels. But scientists are developing less invasive alternatives such as, administering insulin orally with tiny vesicles that can deliver it where it needs to go without a shot.

"We have developed a new technology called a CholestosomeTM," says Mary McCourt, Ph.D., a leader author of the study.

"A CholestosomeTM is a neutral, lipid-based particle that is capable of doing some very interesting things."

The biggest hurdle to delivering insulin orally is escorting it through the stomach intact. The harsh and highly acidic environment of the stomach is very unfriendly for proteins such as insulin. They can degrade even before getting a chance to move into the intestines and then the bloodstream where they're needed. [Read more Type 2 Diabetes Cure? A Super Low-Calorie Diet May Be The Answer!]

Scientists have made some efforts to overcome or sidestep this barrier.One approach is packaging the insulin inside a protective polymer coating to guard the protein from stomach acids.

It is currently being tested in clinical trials.

Another form of insulin – the inhalable insulin – was developed and marketed by another company. But, despite rave reviews from some patients, it didn’t take off. [Read more Alarming new study: Alzheimer’s disease may spread through blood transfusions]

McCourt, Lawrence Mielnicki, Ph.D., and Jamie Catalano, an undergraduate student – all from Niagara University – came up with a new tactic. The researchers were able to successfully encapsulate insulin using the patented Cholestosomes^TM developed in the McCourt/Mielnicki lab. The novel vesicles are made of naturally occurring lipid molecules, which are normal building blocks of fats. But the researchers say that they are unlike other lipid-based drug carriers, called liposomes.

"Most liposomes need to be packaged in a polymer coating for protection," says Mielnicki.

"Here, we're just using simple lipid esters to make vesicles with the drug molecules inside."

Once the lipids are assembled into spheres, they form neutral particles resistant to attack from stomach acids, as shown by computer modeling. If the drugs are loaded inside the capsules, the small packages can travel through the stomach without degrading. When Cholestosomes^TM reach the intestines, the body thinks they are something to be absorbed. The vesicles thentravel through the intestines, into the bloodstream. Then they are taken by the cells, which break them apart and releases insulin.

In the lab, the researchers were able to deliver multiple molecules with these vesicles into cells. Theteam determined the optimal pH and ionic strength of the drug-containing solution in order to pack the most insulin into the Cholestosomes^TM. They then moved the most promising candidates on to animal testing. [Read more 7 Foods That Will Help You Lose Weight]

Studies with rats showed that certain formulations of Cholestosomes^TM 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. [জেনে নিন গাজরের অসংখ্য না জানা গুণাবলী]

The researchers presented their work at the 252nd National Meeting & Exposition of the American Chemical Society (ACS).

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