researchers develop an insulin pill

Diabetes is a disease caused by the dysfunction of the metabolic pathways of blood sugar regulation. Widely distributed in the world (mainly in the United States, where it affects 8% of the population), it is responsible for around 2% of mortality in Europe. The main treatment for diabetes is self-injection of insulin by the patient. However, the administration method can be overwhelming and put many people off. This is why researchers recently developed an alternative by developing an insulin pill. The first tests in rats have shown very satisfactory results.

Using layers of nanomaterials to package insulin, researchers developed a stable and efficient method of delivering the hormone orally to rats without subjecting it to destruction by stomach acids, solving a long-standing problem in pharmaceutical science. The system, described in a study published in the journal Chemical Science, could replace the traditional subcutaneous administration of insulin for diabetic patients.

This would eliminate the need for self-injection and make treatment more accessible. ” Imagine being able to take insulin with a pill instead of injecting it two or three times a day. The insulin has been placed in a system that protects it from the acidic environment of the stomach. Once in the body, the system can detect blood sugar levels and can release loaded insulin on demand. », Says Farah Benyettou, researcher at Trabolsi Research Group from New York University in Abu Dhabi.

Diabetes is the seventh leading cause of death in the world and its prevalence has quadrupled over the past 40 years. Patients with type 1 diabetes do not produce insulin at all, while those with type 2 diabetes do not produce enough, or their body does not respond to the insulin produced. Either way, in the absence of insulin, the body is no longer able to break down the sugar in the blood, which can be fatal. Insulin therapy is a life changing procedure.

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Self-injection of insulin: an off-putting method

And while about 30% of diabetic patients take insulin, many delay treatment because of fear of self-injection. Several studies have documented this effect. A review of the journal Diabetic Medicine found that about 30% of patients initially delay insulin therapy. Those who do do start often delay the start of treatment by two years or more. An insulin pill could solve this problem effectively.

« Our technology has the potential to enable oral insulin delivery in a safer, more efficient and more patient-friendly manner, alleviating the burden of treatment that is limited to intravenous or subcutaneous administration. », Explains lead author Ali Trabolsi. But an insulin pill is sort of a holy grail of diabetic pharmaceuticals. Insulin is delicate and is easily broken down by stomach acids, making it difficult to formulate it into a pill.

Work has been done to achieve oral insulin therapy. Some have even been approved by the Food and Drug Administration the United States. But a truly effective insulin pill has yet to hit the market. ” Despite clinical trials of several oral insulin formulations, sufficient commercial development has yet to be achieved », Says Trabolsi.

Protecting insulin while making it accessible: the solution of nanomaterials

The problem these systems have is the delivery mechanism or the way insulin gets into the blood. The system must protect insulin while allowing it to be delivered to where it is needed. It is this piece of the puzzle that Trabolsi and his team sought to solve. They did this by sandwiching insulin between layers of nanomaterials resistant to stomach acid, but sensitive to sugar.

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nanomaterial structure insulin microscope

A) Structure and synthesis of the nanomaterial TTA-DFP-nCOF. B) Image of the nanomaterial by transmission electron microscopy. C) Structural model of TTA-DFP-nCOF. D) Schematic representation of the encapsulation of insulin in TTA-DFP-nCOF. E) Microscopic image of the TTA-DFP-nCOF + insulin complex. G) Modeling of the TTA-DFP-nCOF + insulin complex. © Farah Benyettou et al. 2021

« Our work overcomes barriers to oral insulin delivery by using insulin-loaded nCOF nanoparticles, which confer protection of insulin in the stomach, as well as responsive glucose release. This technology responds quickly to a rise in blood sugar, but would stop quickly to avoid an insulin overdose, and ultimately will dramatically improve the well-being of diabetic patients worldwide. », Says Benyettou.

Nanomaterials are durable enough to withstand digestion and ensure that the treatment gets to the bloodstream. They are also able to contain and condition up to 65% of their own weight in insulin. And since the sugar itself triggers the release of insulin from the nanomaterials, the drug and the body form a feedback loop that prevents overdose, which can happen accidentally with injectable insulin.

Although the treatment shows great promise, the present study only describes its use in rats. The team will then work to refine the chemistry of their system by exploring and testing different types of nanoparticles. However, researchers are optimistic that in the future their treatment will change the way patients with diabetes approach their care.

Sources : Chemical Science

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