MEDICINAL PRODUCT FOR PHOTODYNAMIC THERAPY AND FLUORESCENT DIAGNOSTICS AND A METHOD OF ITS PRODUCTION Russian patent published in 2023 - IPC A61K47/00 A61K49/04 A61K33/26 A61K33/242 B82B3/00 B82Y5/00 B82Y30/00 B82Y40/00 

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to a preparation for photodynamic therapy and fluorescence diagnostics, comprising magnetite-gold dimer nanoparticles and a FRET-pair of chromophores, such as a photosensitizer (PS) of the bacteriopheophorbide series, which is 131-(4-aminobutylcarbomoyl) bacteriochlorin methyl ester and fluorophore (FPh) cyanine series, which is a Cy5 derivative containing a disulfide bond, obtained by mixing the NHS-ester of Cy5 with cystamine dihydrochloride, where the PS is immobilized on the surface of magnetite nanoparticles 8–11 nm in size stabilized by 3,4-dihydroxyphenylacetic acid (DOPAC) and polyethylene glycol (PEG), FF is immobilized on the surface of gold nanoparticles with a size of 3–5 nm, and the size of magnetite-gold nanoparticles is 12–15 nm and the nanoparticles are dumbbell-shaped, and also relates to a method of obtaining a medicinal product for photodynamic therapy and fluorescence diagnostics, including the synthesis of dimer magnetite-gold nanoparticles, where the size of the nanoparticles is 12–15 nm and the nanoparticles are dumbbell-shaped, by the joint thermal decomposition of Fe(CO)₅ and HAuCl₄ in an organic solvent in an inert gas atmosphere in the presence of 1,2-hexadecanediol and an organic acid with in situ formed nanoparticles Au, stabilization of the surface of magnetite nanoparticles, immobilization with a FRET-pair of chromophores, characterized by the following: during the synthesis of nanoparticles, a mixture of 1,2-hexadecanediol, oleic acid, oleylamine, and 1-octadecene was stirred in an intense flow of argon at a temperature of 120°C for 20 minutes, followed by a decrease in the flow of argon, by connecting a reflux condenser to the system, 0.9 ml of iron pentacarbonyl was added, after 3 minutes a mixture consisting of 40 mg of HAuCl₄ *(H₂O)3_, was _introduced into _the solution 0.5 ml of oleylamine and 5 ml of 1-octadecene, previously kept in an argon atmosphere for 7 minutes until a straw-yellow color of the solution appears, then the mixture was heated at a rate of 25°C per minute to a boiling point of 300–310°C, and kept at this temperature for 45 minutes, after which the resulting solution was cooled to room temperature and subjected to oxidation in air for an hour; the surface of magnetite nanoparticles was modified with a photosensitizing agent (PS) of the bacteriophorbide series, which is 131-(4-aminobutylcarbomoyl)bacteriochlorin methyl ester, by chemical conjugation with the magnetite surface stabilized by DOPAC and PEG with purification by centrifugation and HPLC; the surface of gold nanoparticles was modified with a fluorophore (FPh) of the cyanine series, based on a tenfold excess of the fluorophore relative to the number of nanoparticles, due to covalent bonding with the surface of gold with purification by centrifugation, HPLC, and dialysis, where the fluorophore (FPh) of the cyanine series is a derivative of Cy5 containing a disulfide bond obtained by mixing the NHS-ether Cy5 with cystamine dihydrochloride.

EFFECT: group of inventions provides effective combination of two chromophores with leveling of undesirable effects (energy transfer) on the surface of magnetite-gold nanoparticles to create successful new-generation agents (with the possibility of joint use) in cancer theranostics.

3 cl, 5 dwg, 3 ex