The methods of synthesis of biologically active nanostructured systems based on functional and natural polymers are reviewed. The formation of nanosystems in the process of interaction between synthetic water-soluble polyelectrolytes and amphiphilic ionic surfactants is discussed. The influence of structure and stability of these systems on their biological activity is considered. The complexation between DNA and polycations with the formation of compacted DNA molecules, and the transport of resulting complexes into the cells are discussed. The data on nanostructuring of hemoglobin using polyfunctional crosslinkers and the data on the use of the obtained nanoparticles as oxygen-transporting blood substitutes are summarized. Using nanodisperse silver stabilized with poly(vinylpyrrolidone) as an example it was demonstrated, that transferring silver into nanodisperse state results in widening its bioactivity. © 2017, Springer Science+Business Media, LLC, part of Springer Nature.