A long-held dream in the field of medicine is closer to reality as researchers at Kumamoto University have successfully developed insulin pills that bypass the digestive system, which could eliminate the need for daily injections for millions of people.
For years, scientists were unable to develop insulin pills due to the inability of the intestine to naturally absorb insulin into the bloodstream.
Additionally, enzymes in the digestive tract break down insulin immediately before it can work. Given the obstacles, the recent breakthrough could be a game-changer in diabetes treatment.
In a recent revolutionary approach, researchers used a cyclic peptide, known as the DNP peptide, which can pass through the small intestine, allowing insulin to be delivered orally in a way that was not previously possible.
The team developed two effective strategies, published in the journal molecular pharmaceutics, To ensure intestinal absorption of insulin.
mixing method
This approach relies on a physical interaction between the insulin molecule and the peptide without altering the chemical structure of insulin. When it comes to its efficacy, the mixture led to a faster return to healthy blood sugar levels when tested in chemically induced and genetic diabetes models.
This method proved to be quite effective in maintaining stable glucose control with just one dose per day over a three-day period.
conjugation method
This method is based on forming a permanent bond between the transport peptide and insulin. Using click chemistry, the team physically attached the DNP peptide directly to the insulin molecule to create a DNP-insulin conjugate.
This approach also achieved similar glucose-lowering success as the above method.
Limitations of oral insulin
Unlike injections, oral insulin requires extremely high doses, up to 10 times higher than injections. But, this new platform also reduces such requirements and ensures medicinal bioavailability of approximately 33-41 percent compared to subcutaneous injection.
future prospects
Given the significant medicinal bioavailability of oral insulin, it is not unreasonable to assume that oral insulin may be ready for real-world use in the near future.
“Insulin injections remain a daily burden for many patients. Our peptide-based platform provides a new route to deliver insulin orally and may be applicable to long-acting insulin formulations and other injectable biologics,” said Associate Professor Shingo Ito.
