title: [Polymer Complexes of Ofloxacin and Their Antibacterial Activity].
abstract: To lower the toxicity and to prolong the action of the monofluoroquinolone ofloxacin, its water-soluble polymer complexes were developed. Cationic copolymers of N-vinylpyrrolidone (VP) with 2-aminoethylmethacrylate (2-AEM) and its hydrochloride (2-AEM-HCl), containing 10.9-28.3 mol. % -NH2 or -NH3Cl group with the molecular mass (MM) of 10500 to 89000 were synthesized as the complex-forming polymers. The cationic copolymers showed their own antimicrobial activity. The polymer complexes contained 18-36% of fluoroquinolone and had high antimicrobial activity against S. aureus and E. coli, that increased with an increase of the ofloxacin content in the complex and a decrease of its MM. The kinetic studies on the ofloxacin release from its polymer complex with MM of 60000, containing 36% of fluoroquinolone revealed prolongation of the medicinal substance release from the complex in the buffer solution at pH 2.0 and a temperature of 37 degrees C. The acute toxicity tests on mice with intraperitoneal administration of ofloxacin and copolymer VP containing 20.8 mol. % -NH3Cl group (MM of 51000) showed that ofloxacin was a nontoxic antimicrobial and the polymer carrier was a low toxic substance.
authors.forename: E P
authors.initials: EP
authors.lastname: Ananyeva
authors.forename: S S
authors.initials: SS
authors.lastname: Baranov
authors.forename: A V
authors.initials: AV
authors.lastname: Karavaeva
authors.forename: M S
authors.initials: MS
authors.lastname: Borisenko
authors.forename: M V
authors.initials: MV
authors.lastname: Solovskiy
authors.forename: N V
authors.initials: NV
authors.lastname: Zacharova
authors.forename: T A
authors.initials: TA
authors.lastname: Prazdnikova
authors.forename: E B
authors.initials: EB
authors.lastname: Tarabukina
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D065546:Drug Liberation; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D008689:Methacrylates / Q000737:chemistry; D051379:Mice; D008826:Microbial Sensitivity Tests; D015242:Ofloxacin / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D011760:Pyrrolidinones / Q000737:chemistry; D012995:Solubility
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008689:Methacrylates; D011760:Pyrrolidinones; C072703:2-aminoethylmethacrylate; C042670:N-vinyl-2-pyrrolidinone; D015242:Ofloxacin