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THE COMPLEX POLYMER COMPOSITIONS BASED ON ANTIBIOTICS LINEZOLID, RIFABUTIN, PROTIONAMIDE

DOI: https://doi.org/10.29296/25877313-2018-05-05
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Issue: 
5
Year: 
2018

A.I. Murav′eva Laboratory Assistant Researcher, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow) E-mail: anna_muraveva_91@mail.ru V.V. Zavarzina Junior Research Scientist, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow) N.V. Gukasova Ph.D. (Biol.), Senior Research Scientist, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow) S.L. Kuznetsov Senior Research Scientist, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow) I.A. Tubasheva Ph.D. (Chem.), Leading Research Scientist, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow) E.A. Vorontsov Ph.D. (Chem.), Leading Research Scientist, Laboratory of Cell Biology and Molecular Medicine, Scientific Research Center «Kurchatov Institute» (Moscow)

One of the ways to increase the effectiveness of drugs is to create a transport system for their delivery to the target organ, by including the drug in the biodegradable polymer. The aim of the study was to obtain complex antimicrobial compositions include antibiotics linezolid, rifabutin, protionamide, as well as a copolymer of lactic and glycolic acids, D-mannitol and polyvinyl alcohol; to study the antimicrobial activity of the obtained polymer compositions of antibiotics against gram-positive, gram-negative bacteria and the nontuberculous strain-isolate Mycobacterium spp (R).The polymer compositions of antibiotics were prepared by the method of simple emulsions. The particle size distribution of the polymer composition samples was determined by the dynamic light scattering method in the aqueous suspension. The content of antibiotics was determined in the polymer compositions by high performance liquid chromatography (HPLC). The antibacterial activity of the samples was studied for control strains of microorganisms: Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 29213, Staphylococcus aureus ATCC 43300 (MRSA), Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Mycobacterium spp (R). The results and discussion: equal mass ratios of antibiotics and a fivefold excess of polymer were taken to obtain complex polymer compositions. The content of each antibiotic was 4.0−4.3% in the polymer compositions. The average hydrodynamic diameter of the particles was 314 nm (LR PLGA), 487 nm (LRP PLGA), 300 nm (L PLGA), 342 nm (R PLGA) and 371 nm (P PLGA). The complex polymer compositions in respect to the tested strains of bacteria had a similar or higher antibacterial activity than the individual antibiotic substances in respect to the tested strains of bacteria. The conclusion: the complex polymer compositions linezolid + rifabutin (LR-PLGA) and linezolid + rifabutin + protionamide (LRP-PLGA) complexes were obtained. Higher antibacterial activity was observed for the polymer composition LR-PLGA against E. faecalis and S. aureus strains as compared to individual substances, and for the polymer composition LRP-PLGA against the methicillin resistant strain S. aureus (MRSA).
Keywords: 
antibiotics
linezolid
rifabutin
protionamide
PLGA
polymer particles
antibacterial activity

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