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Oral administration of insulin may be possible with Cholestosomes.
Patients with diabetes may no longer need to give themselves painful injections of insulin due to a novel delivery method of the treatment.
Researchers at Niagara University have developed a vesicle that delivers the medication, making the treatment “ouchless.” Their findings were presented at the 252nd National Meeting & Exposition of the American Chemical Society.
“The new technology is called a Cholestosome. A Cholestosome is a neutral, lipid-based particle that is capable of doing some very interesting things,” said lead researcher Mary McCourt, PhD. “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. Cholestosome is resistant to pH and bile salts, which, when met with absorbing lipids, becomes picked up by that carrier and delivered intact. Cholestosomes also get into cells directly and move into the bloodstream where they're needed.”
The vesicles containing the medication were developed with lipid molecules that occur naturally within the body, according to the university. However, this drug works differently than other liposome drugs.
“Most liposomes need to be packaged in a polymer coating for protection,” said researcher Lawrence Mielnicki, PhD. “Here, we're just using simple lipid esters to make vesicles with the drug molecules inside.”
Researchers used computer modeling to discover that lipids can form neutral particles that resist attacks from stomach acids when they are assembled in spheres. This means that drugs can be packaged inside the molecules and not break down in the stomach, allowing the medication to be as effective as possible.
Interestingly, the intestines will recognize Cholestosome as something that needs to be absorbed, despite it being unscathed from stomach acid. The vesicle passes through the intestines into the bloodstream, where it then is broken apart and releases the insulin, according to the study.
During initial stages, researchers said they determined optimal pH and ionic strength of the drug-containing solution, and tested the candidates in animal studies. In rat models, they found that Cholestosome with insulin had high bioavailability.
This new method also might have the ability to significantly reduce healthcare costs, since insulin needles are no longer needed. Researchers plan to optimize the formulations even further, and conduct additional animal trials before moving onto human trials.
This delivery method may be beneficial for other medications as well, according to the university.