Scientists around the world have long been struggling with the problem of how to minimize the dosage of drugs. In the same direction, experts from the Swiss university, located in the city of Basel, also work. They are trying to create a Swiss medicine of a new generation. These studies are designed to optimize the doses of many drugs, especially potent, such as antibiotics or cytotoxins, thereby reducing the burden on the body when they are used.
Nanoreactor and prodrugs
One of these methods is the use of prodrugs that will be converted to conventional drugs by enzymes located in a specific place in the body, for example, in the center of inflammation, the tissues of a cancerous tumor or around the implant. In order to become a similar "catalyst", the enzyme should be protected from environmental degradation, but at the same time, "protection" should not be very resistant to easily "let go" the molecules and ions of active substances at the site of application.
This will make it possible not only to significantly reduce the dosage, but also significantly reduce the side effects when taking medications, since it will be active only if it is really necessary.
To solve this difficult task, a chemical nanoreactor was developed by scientists of the University located in the city of Basel. It protects the molecules of drugs and transports them to the organs and tissues of the body and consists of pencilinase, which is required for the "production" of an antibiotic in the human body.
Small molecules of the substrate penetrate the membrane located around the enzyme deep into the "reactor", as if falling into a trap, and the resulting active substance easily leaves the shell and begins to affect the affected organ and tissues. The efficiency of the novelty was tested on the example of cephalexin.
This antibiotic was formed directly in the human body by the action of penicillinase from the "delivered" prodrug and methyl ester. Cephalexin, obtained inside the human body, does not differ in its properties from the finished one, produced by standard industrial technology.
"Barrels" with molecules
Another area, which studies scientists from Switzerland, developing new pharmacological technologies - the application of cucurbituril. These are molecular containers that look like an empty pumpkin with a "cover" of oxygen atoms of highly carbonyl groups. Such caps are also called portals. What makes these "containers" so attractive and how can they help humanity?
- Inside cucurbitur can be placed ions of a trace element or even two, as well as the molecules of the desired drug, to deliver them to the affected organs or tissues. There, the fragile "portal lid" will open, releasing the drug substance to the outside. A large number of substances have already been identified that can be transported in this way. These studies on the problem of reversible inclusion of molecules in "containers" have a great future;
- Thus, it is possible to deliver to those parts of the body where they are needed: amino acids, peptides, oligonucleotides, cytostatics, antigens, antibiotics. Only in organs and tissues after the opening of the portal the medicine will start to act;
- This will significantly reduce the dose of drugs taken by patients and reduce the number of "pobochek" and contraindications.
Every year nanotechnology is increasingly used in various industries and pharmaceutical chemistry is no exception.