VECTORIZED WATER-COMPATIBLE POLYMER MICELLAR PARTICLES FOR DELIVERY OF BIOLOGICALLY ACTIVE SUBSTANCES THROUGH BLOOD-BRAIN BARRIER Russian patent published in 2021 - IPC A61K9/08 A61K47/30 A61K47/64 C08F10/00 C08F12/00 C08F16/00 C08F20/00 C08F26/10 C08F28/04 B82Y5/00 

FIELD: medicine.

SUBSTANCE: group of inventions relates to the field of medicine, namely to a vectorized water-compatible polymer micellar carrier for the delivery of biologically active substances, which is a micelle consisting of amphiphilic polymers with an average molecular weight of 1 to 12 kDa, having in the hydrophilic part reactive groups capable of covalently binding the peptide vector, while amphiphilic polymers have the general formula

in which [- - - M - - -]_n is a hydrophilic part consisting of the same or several different irregularly ordered M monomers selected from the group:

,

where R1 independently represents H, C_1-4alkyl; R is the hydrophobic part of the overall structure , in which X is selected independently and represents H, OH, NH₂ or NH₃Cl, and the reactive group is an amine, carboxyl, amide or aldehyde group, and in the amphiphilic polymer at least 1 molar percent of monomers are monomers containing a reactive group; at the same time, the number of peptide vectors covalently bound to the micelle is at least one peptide molecule per micelle and the peptide vectors bound to one micelle are the same, as well as to a nanoscale form for the directed delivery of biologically active substances containing a vectorized water-compatible polymer micellar carrier, and to the use of a vectorized water-compatible polymer micellar carrier for the directed delivery of insoluble or poorly soluble biologically active substances in water, to the central nervous system. The group of inventions provides the development of biocompatible nanoscale carriers for the directed delivery of BAS based on polymer nanoparticles modified with peptide vectors, capable of penetrating the blood-brain barrier and delivering BAS to selected targets in the central nervous system, provides the directed delivery of vectorized water-compatible polymer micellar carriers to cells and tissues of the central nervous system; provides an increase in the stability of biologically active substances in the bloodstream, as well as their stabilization during storage; provides a long-term release of BAS in the body with the ability to control the distribution and release of BAS and provides an increase in the therapeutic effectiveness and bioavailability of BAS and drugs, or provides the manifestation of synergy of the peptide vector and the drug; makes the process of obtaining vectorized water-compatible polymer micellar carriers relatively simple and inexpensive, suitable for scaling, and the resulting particles are safe for use.

EFFECT: group of inventions provides development of biocompatible nanoscale carriers for the directed delivery of BAS based on polymer nanoparticles.

6 cl, 3 dwg, 2 tbl