ИСТИНА

Methods of synthesis of amphiphilic derivatives of a number of water-soluble polymers, in particular, poly-N-vinylpyrrolidone, have been worked out. In experiments on cells and experimental animals, the harmlessness of the polymers obtained was shown. The synthesized amphiphilic polymers are capable of spontaneous aggregation in aqueous solutions with the formation of nanoscale micelle-like aggregates and are suitable for modifying liposomal membranes. The influence of the structure of amphiphilic polymers on the tendency to aggregation has been established. Such systems can be used as carriers of poorly soluble and water-insoluble medicinal substances. It was shown, what aggregates of amphiphilic polymers of N-vinylpyrrolidone proved to be suitable for use as carriers and modifiers of various proteins and peptides (blood factor IX, angiostatin, Bowman- Birk soybean proteinase inhibitor (BBI)). In these cases, immobilization with the use of polymeric aggregates increases the resistance of proteins to denaturing effects, and thereof their total biological activity. Methods have been developed for the introduction into the synthesized amphiphilic polymers of various functional groups. For example, introduction of additional side aminoacid groups in the polymeric part of amphiphilic systems allows the use of aggregates as carriers of nucleic acids and their subsequent application for transfection in genetic engineering. Using fluorescent labels and probes, it was shown that the immobilized substance introduced into larger size aggregates penetrates into the living cell due to endocytosis, localizing in the cytoplasm inside the endosome. On the other hand, when immobilized active agent is introduced in smaller-sized aggregates, it evenly spreads both in the cytoplasm of the cell and in its nucleus. When studying the transport of aggregates of amphiphilic polymers of Nvinylpyrrolidone in the body (rats), it was established that a fluorescent probe immobilized in aggregates of amphiphilic polymers, when injected into the tail of experimental animals, quickly reaches the vessels of the eye.