Oral insulin may be available in 2-3 years

Scientists who have successfully created an oral insulin demonstrating efficacy in lowering blood glucose levels without inducing hypoglycemia in mice, rats, and baboons are poised to advance their drug to human clinical trials by 2025.

There is optimism among the researchers that the oral insulin could potentially be accessible to the general population within the next few years.

New Atlas has extensively reported on the evolution of oral insulin, spanning its creation to examinations in both animal and human trials. The dedication of scientists and researchers to the development of ingestible insulin is quite evident, particularly considering the global prevalence of diabetes.

READ MORE: BREAKING: Diabetes research lead to end of regular insulin injections

In 2021, 537 million adults, or one in 10 individuals worldwide, were living with diabetes, and projections indicate this number is likely to increase to 643 million by 2030. Despite diligent efforts, no oral insulin has yet made its way to the market.

Presently, scientists from UiT The Arctic University of Norway, in collaboration with researchers from the University of Sydney, have successfully formulated an oral insulin. The effectiveness of this innovation has already been validated in animal models, and plans are underway to initiate human clinical trials by 2025.

According to Peter McCourt, a co-author of the study, “This method of administering insulin is more precise, delivering the insulin rapidly to the specific areas of the body that require it the most. In contrast, when insulin is administered with a syringe, it is distributed throughout the body, potentially leading to unwanted side effects.”

Individuals with diabetes often rely on injectable insulin or continuous insulin infusions through pumps to maintain precise blood glucose control and mitigate the risk of long-term complications such as cardiovascular disease, kidney disorders, neurological issues, and eye diseases. However, monitoring for acute events like hyperglycemia (high blood glucose) and hypoglycemia (low blood glucose) is crucial, as both pose significant health risks.

Previously, researchers had discovered the potential to deliver medication to the liver using nanocarriers, as the liver is the primary site where insulin acts in healthy individuals. However, the challenge was ensuring the delivery system’s survival through the stomach’s high acidity and the action of digestive enzymes, which can render medications ineffective.

To address this, the researchers developed a pH- and enzyme-sensitive coating using a chitosan and glucose copolymer applied to insulin bound to silver sulfide (Ag2S) quantum dots. This coating protects insulin from breakdown by stomach acid and digestive enzymes, allowing it to reach the liver intact. In the liver, the coating is broken down by enzymes activated only when blood glucose is high, releasing insulin. This prompts glucose storage in the liver, muscles, and fat for use as an energy source, reducing blood glucose levels.

Nicholas Hunt, the lead and co-corresponding author of the study, explained, “When blood sugar is high, there is a rapid release of insulin, and even more importantly, when blood sugar is low, no insulin is released.”

The researchers conducted tests on nematodes (C. elegans), mice, and rats before moving on to baboons, who were administered the oral insulin incorporated into sugar-free chocolate to enhance palatability. The oral insulin was well-received by the baboons, and treatment resulted in a 10% to 13% reduction in blood glucose levels without causing hypoglycemia. The effects were observed between 15 and 30 minutes after administration.

The success of these experiments opens up promising possibilities for the development of an oral insulin option, offering a more convenient and effective way to manage blood glucose levels in individuals with diabetes.

Apart from being more convenient and patient-friendly, with no need for injections, increased discretion, and no requirement for refrigeration, the researchers highlight that their drug’s mode of action closely emulates the natural functioning of insulin in healthy individuals.

Nicholas Hunt explained, “When you inject insulin under the skin with a syringe, a larger portion of it goes to the muscles and adipose tissues than would occur if it were released from the pancreas. This can lead to the accumulation of fats and, potentially, hypoglycemia, which poses risks for people with diabetes.”

The next step for the researchers is to conduct trials on humans. Nicholas Hunt stated, “Trials on humans will commence in 2025, led by the spin-out company Endo Axiom Pty Ltd. The clinical trials will follow a three-phase process. In phase I, we will assess the safety of the oral insulin and closely examine the incidence of hypoglycemia in both healthy individuals and those with type 1 diabetes. Our team is eagerly anticipating the possibility of replicating the absence of hypoglycemia observed in baboons in human subjects, as this would represent a significant advancement. These experiments adhere to stringent quality standards and necessitate collaboration with physicians to ensure the safety of the test subjects. Following a successful phase I, confirming its safety for humans, phase 2 trials will explore how it can replace injections for diabetic patients.”

The researchers are optimistic that their oral insulin could be available for use within the next two to three years, marking a substantial leap forward in diabetes management.