US
scientists have developed an oral method of administering insulin that can be a
less painful alternative to millions of people worldwide with diabetes who have
to inject themselves with the drug to manage their blood-sugar levels.
The team has successfully encapsulated insulin
using Cholestosomes -- a neutral, lipid-based particle -- that can be
administered orally with tiny vesicles that can deliver insulin where it needs
to go without injecting.
The biggest obstacle to delivering insulin
orally is ushering it through the stomach intact. Proteins such as insulin are
no match for the harsh, highly acidic environment of the stomach. They degrade
before they get a chance to move into the intestines and then the bloodstream,
where they're needed, the study said.
However, the new vesicles that are made of
naturally occurring lipid molecules are normal building blocks of fats, the
researchers said, adding that they are unlike other lipid-based drug carriers,
called liposomes.
"Most liposomes need to be packaged in a
polymer coating for protection. Here, we are just using simple lipid esters to
make vesicles with the drug molecules inside," said lead researcher Mary
McCourt, Professor at Niagara University in New York, US.
Computer modelling 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
cholestosomes reach the intestines, the body recognises 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.
Studies
with rats showed that certain formulations of cholestosomes loaded with insulin
have high bioavailability, which means the vesicles travel into the bloodstream
where the insulin needs to be, the researchers concluded.
The results
were presented at the 252nd National Meeting and Exposition of the American
Chemical Society (ACS), in Philadelphia, recently.
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