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Oral insulin drops offer relief to diabetes patients

Diabetes rates continue to rise: 11.7 million Canadians live with diabetes or prediabetes. At UBC, scientists have created a painless medication delivery method to help people with diabetes more easily manage the disease and maintain their health.

Li Lab researchers have developed oral insulin drops that, when placed under the tongue, are quickly and efficiently absorbed by the body, potentially replacing the need for insulin injections.

The drops contain a mixture of insulin and a unique cell penetrating peptide (CPP) developed by Dr. Shyh-Dar Li and his colleagues.

A little help from a peptide guide.

“Insulin is a complicated molecule,” explains lead researcher Dr. Li, a professor in the Faculty of Pharmaceutical Sciences. “In pill form, it is easily destroyed in the stomach. Insulin also needs to be available quickly in the blood, but because it is a large molecule, it cannot pass through the cells easily on its own.” The peptide, obtained from fish byproducts, opens a pathway for insulin to cross.

Preclinical testing showed that insulin with the peptide effectively reaches the bloodstream, while without the peptide, insulin remains trapped in the inner lining of the mouth.

“Think of it as a guide that helps insulin navigate through a maze to quickly reach the bloodstream. This guide finds the best routes, making it easier for insulin to get where it needs to go,” Dr. Jiamin said. Wu, postdoctoral researcher. in the Li laboratory.

Two versions of the peptide are described in recent journal articles. Controlled Release Diary (here and here). The UBC team is working to license the technology to a commercial partner.

Keep medications up to date

Healthy people get their insulin naturally from the pancreas to regulate glucose after a meal. Patients with diabetes cannot produce enough insulin and need to obtain it from an external source.

Unregulated glucose can be very dangerous, so patients with diabetes should monitor their glucose levels and take insulin to lower them when necessary. While injections are the fastest way to get insulin into the blood, patients typically need at least three or four injections per day, which can affect their quality of life. Adherence to this regimen is challenging and over time this can cause serious complications such as eye, kidney and nerve damage, which could lead to limb amputations.

“My lab has been working on needle-free alternatives to insulin for the past three years,” Dr. Li said. “We tried nasal sprays before opting for oral drops, which are easy and convenient. Hopefully, oral drops open up a new possibility for diabetes patients, making it easier to take their medications and regulate blood glucose to maintain your health in the long term.”

Two inhalable insulin products (Exubera, Afrezza) were previously approved, but the effects were suboptimal and were shown to increase the risk of developing lung cancer. These products have been withdrawn. Dr. Li’s goal is to achieve rapid, painless insulin delivery without significant side effects. The new needle-free technology is expected to reduce the risk of cross-contamination, needle sticks, accidental infections and unsafe disposal of contaminated needles.