26 June 2018

Insulin in tablets

Biotechnologists from the USA have created the first insulin pills

RIA News

Doctors from California and Boston have created insulin pills that can survive the "journey" through the stomach and deliver the right amount of hormone to the diabetic's body. Their description was published in the journal PNAS (Banerjee et al., Ionic liquids for oral insulin delivery).

"If you just take and drink insulin, then its molecules will have to overcome a huge mass of obstacles before they can enter the bloodstream. We have created a kind of "Swiss knife", which has all the necessary tools built into it to protect insulin from the threats it encounters on its way," said Samir Mitragotri from Harvard (in a press release Delivering insulin in a pill – VM).

According to WHO statistics, there are about 340 million people suffering from diabetes in the world today. Most of them are forced to take two or even 5-6 injections of insulin a day in order to stabilize blood sugar levels. Insulin is a rather dangerous hormone and its overdose as a result of switching to a new brand of the drug can cause severe damage to health or even death as a result of hypolycemia – a sharp decrease in the proportion of sugar in the blood.

In recent years, scientists have been actively trying to create a safe analogue of insulin with a similar chemical formula, or such systems of hormone injection into the body that would protect it from overdose. For example, in early 2013, American biochemists created a special micro-dropper-a "jellyfish" that can be inserted under the skin, where it will slowly release insulin for several days. 

Doctors and patients themselves, as Mitragotri notes, have long dreamed that insulin could be taken in the same way as aspirin or any other pills. Until now, this was impossible, since gastric juice and enzymes digesting protein food decomposed its molecules even before they were absorbed by the intestinal walls.

Scientists from Harvard and the University of California at Santa Barbara solved this problem with the help of two things – a shell resistant to the action of gastric acid, and a special substance that chemists call "ionic liquid".

By this word, scientists understand a mixture of certain salts, which does not contain a single molecule of water, but at the same time behaves like a liquid, due to the extremely low melting point. Scientists have suggested that they can be used as a kind of "liquid armor" for insulin, protecting it from enzymes during movement through the intestine.

The secret of its work, as Mitragotri explains, is that it behaves differently in an environment with different pH levels - in an "acidic" stomach, it remains stable and prevents its juice from penetrating inside, and in an "alkaline" intestine, the ionic liquid gradually disintegrates and releases hormone molecules.

In addition, the ionic liquid, as shown by experiments on mice, helps insulin molecules penetrate the barrier between the intestinal walls and blood flow, and stabilizes hormone molecules, allowing tablets based on it to act for about 12 hours and be stored for about two months in a first aid kit, even at room temperature.

As Mitragotri and his colleagues hope, their pills will pass all phases of clinical trials and animal experiments in the shortest possible time, and will appear in pharmacies in the next few years. Great hopes for this are given by the fact that two components of the ionic liquid – vitamin B4 and geranium acid – are already used as food additives, which will simplify the testing of these tablets for toxicity.

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