07 August 2015

Scientists presented a review of liposomes

Fundamentals for the medicines of the Future


An international group of scientists, including Vladimir Chupin, Head of the Department of Biophysics at FOPF, and Vladimir Torchilin, one of the leading pharmacology specialists in the world (Northeastern University, USA), presented an overview of liposomes, microscopic capsules that are actively used to create new drugs around the world, on the pages of Chemical Review magazine. The researchers systematized the main achievements in this field and pointed out the most promising areas for its further development. 

Liposomes (figure: Dennis Barten / Wikimedia) are microscopic spheres whose walls are arranged in the same way as a cell membrane. They were first obtained back in the 1960s, in the 1970s, scientists proposed using liposomes to deliver drugs, and now drugs in liposomes are used to treat a number of diseases from influenza to various types of malignant neoplasms.

Thousands of different publications are devoted to liposomes, they are actively studied in many laboratories around the world, and a new article (Bhushan S. Pattni, Vladimir V. Chupin, and Vladimir P. Torchilin, New Developments in Liposomal Drug Delivery) contains a detailed list of the main achievements in this field. In it: 
  • modern methods of obtaining liposomes are indicated, the strengths and weaknesses of various technologies are listed;the main types of liposomes with different wall structures and different additional molecules for selective interaction with cells are shown;
  • different methods of drug delivery inside liposomes are considered.
  • Artificial microspheres can either circulate in the body for a long time and slowly secrete the drug, or release the drug immediately after a collision with certain cells.Liposomes can carry out targeted delivery of substances to where they are needed.
The concept of "targeted delivery" accompanies almost any story about the prospects for the development of pharmacology, and this is not accidental – with cancer chemotherapy, for example, only targeted delivery can reduce the severity of side effects from sufficiently toxic drugs. But in addition to targeted delivery, liposomes have several other interesting applications – for example, a new dosage form for diclofenac, a widely used nonsteroidal anti-inflammatory agent, is being developed with their help.The same drug can be produced in different forms.

The medicine that should be given to a small child is more likely to be made in the form of syrup than a tablet, but for topical use ointments, creams and gels are used. All these are different dosage forms.

If diclofenac is "packed" inside liposomes and a substance is added that increases the permeability of the skin, then an ointment with such microcapsules will be more effective against local inflammatory reactions. Liposomes can also help an anesthetic such as lidocaine, also facilitating its delivery directly to the nerve endings. Along with experimental cancer drugs, liposomes can improve drugs that have long been known to non-specialists.

Nonsteroidal anti-inflammatory drugs, or NSAIDs, are the basis of most commonly used over-the-counter pain medications. These include aspirin, ibuprofen, paracetamol and the already mentioned diclofenac, sold, in particular, under the brand name "Voltaren". All these drugs work by suppressing biochemical reactions leading to the development of inflammation, but they do not remove the cause and therefore do not cancel the need to visit a doctor.

In addition to drug delivery, the authors of the new review briefly described the use of liposomes for other purposes. With their help, special tags can be delivered to cells for both diagnostic and research tests, and a liposomal gel (many microscopic beads) with special signaling molecules can be used for chemical analysis of various substances.

In Russia and UkraineThe main author of the new review, Vladimir Petrovich Torchilin, is one of the founders of the liposomal direction in the USSR, winner of the Lenin Prize in 1982, author of more than four hundred scientific publications (the Hirsch index is over 70) and a recognized expert in this field.

At the end of the 1970s, Soviet researchers began to conduct practical work in the field of creating liposomal preparations, and after a while the production of medicines was organized in Kharkov, on the basis of the Biolek enterprise.

Now the antitumor drug lipodox (cytostatic – that is, the substance suppressing cell division – doxorubicin in liposomes), eye drops lipoflavone (anti-inflammatory agent) and a dozen other potential drugs are being mass-produced, from biological and laboratory to clinical. Currently, the production of liposomal drugs is organized already in the Moscow region ("Technology of medicines", Vitaly Shvets took an active part in this, who developed together with Vladimir Torchilin a program for the development of liposomal direction).

One of the first practical applications of liposomal drugs related not to treatment, but to the diagnosis of diseases: diagnostic tests for syphilis were created on the basis of liposomes. As Vladimir Chupin explained to the MIPT press service, such tests turned out to be more accurate than traditional ones.

In Phys TechThe MIPT press service had a conversation with Vladimir Viktorovich Chupin, Doctor of Chemical Sciences and Head of the Department of Biophysics of the FOPF, Faculty of General and Applied Physics: "I previously worked at the Institute of Bioorganic Chemistry of the Russian Academy of Sciences, and before that I graduated from the Moscow Institute of Fine Chemical Technology and postgraduate studies in the Netherlands.

I came to MIPT because my good colleagues work here, well-equipped laboratories and the Department of Biophysics are based here. We have received several large grants from the Ministry of Education and Science, programs 5-100; graduates come to us both from abroad and directly from MIPT, including the Faculty of General and Applied Physics."

The scientist said that recently two new rooms equipped with the necessary equipment for working with liposomes and other nanosystems were opened in the applied mathematics building (KPM, where not only "mathematical" faculties have been located for a long time – new "protein" laboratories are located there). Inside the new laboratories there is a special cold room, the temperature in which can be lowered up to plus 6 degrees Celsius, regardless of the other rooms. In the 2010s, the institute, which has made a name for itself on physical research and training of physicists, is actively developing the field of living systems sciences, life sciences, and both "biological" faculties like FBMF or FMHF and the traditionally "purely physical" FOPF are involved in this process. According to Vladimir Chupin, this is not an accident or a tribute to fashion, but a natural development: "Previously, a strong department of physics and nanostructure technology was formed at the FOPF, so it was logical to deal with nanoscale liposomes and other biological nanoobjects there and make another department, the Department of Biophysics."

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07.08.2015
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