Treat and not cripple

The dose of drugs can be reduced tenfold

Alexey Khadaev, Rossiyskaya Gazeta

Even the best drugs have serious side effects. It is no accident that the world's leading laboratories are trying to create a "golden bullet". She should not shoot a "cannon at sparrows", destroying healthy cells, but only hitting sick ones. To "cast" such a bullet, scientists come up with very sophisticated and expensive methods. Until they all came out of the walls of the laboratories.

The method developed by Siberian scientists is much simpler and cheaper. And although it does not target diseased cells, it is nevertheless quite effective. In any case, it allows you to reduce the dose of the drug tenfold. How was this achieved?

Pharmacologists themselves admit that most of the medicine contained in the tablet is wasted. There are several reasons. For example, many medications are absorbed only partially in the intestine. Especially poorly absorbed substances insoluble in water, such as vitamins A, D, E. In addition, to get into the cell, the drug must overcome a protective barrier – the cell membrane. Therefore, the patient has the only way out: to achieve a significant effect from the drug, it is necessary to take large doses. As a result, there are numerous side effects.

It would seem that there is a way out: you need to replace a poorly soluble tablet with an injection. But not every one of us is able to give himself an injection, in addition, the injection procedure itself is unsafe.

– The decision was prompted by nature itself, – says Tatiana Tolstikova, Doctor of Biological Sciences from the Novosibirsk Institute of Organic Chemistry SB RAS. – The fact is that each of us contains a huge amount of substances that are practically insoluble in water, for example, hormones, and yet they constantly travel through the body. There are special carrier proteins for everyone in it. They have a cavity inside where the hormone is packed and then delivered to the right place, where its "unloading" takes place. Moreover, the carrier is able to find a common language with the cell membrane, and it passes the "load" inside the cell.

Siberian scientists decided to do the same with a drug molecule. But where to get such a carrier? Sorting through various substances, the scientists settled on licorice, which has long been known to doctors. More precisely, glycyrrhizic acid isolated from its root. It has a number of interesting properties. For example, four of its molecules form a structure inside which there is an empty space. It is here that you can place the medicine. Chemists call host-guest compounds clathrates. The "guest" molecule enters the "host" cavity, stays there for a while, and when the complex is destroyed, it is released.

But this is in theory, but how to create such a clathrate? And how to put the medicine inside the capsule? To solve the problem, chemists attracted scientists from the Institute of Solid State Chemistry and Mechanochemistry SB RAS, who developed a unique technology for the synthesis of clathrates. But it is not enough to deliver the medicine to the cell, it must penetrate inside, breaking the membrane barrier. And here a third partner entered into cooperation – the Institute of Chemical Kinetics and Gorenje SB RAS (IHKG).

"Our research has shown that by interacting with cell membranes, clathrates increase their porosity," said Nikolai Polyakov, a leading researcher at the IHCG SB RAS. – Moreover, at the moment of such contact, the clathrate itself is destroyed, the drug is released and hits the target. Animal tests have shown that by this method, the dose of anti-inflammatory and anti-cancer drugs can be reduced tenfold.

The substance obtained from licorice root can also help in the creation of effective drugs to improve vision. Most of them contain lutein, which protects the retina from ailments. But lutein from tablets is poorly absorbed in the body. But if it is hidden in a capsule, the solubility of the drug increases thousands of times. Siberian scientists conducted these studies together with colleagues from the University of Utah (USA).

Portal "Eternal youth" http://vechnayamolodost.ru  18.05.2016