[Enhanced activity of rifampicin loaded with polybutyl cyanoacrylate nanoparticles in relation to intracellularly localized bacteria].
Association of rifampicin with polybutylcyanoacrylate nanoparticles provided considerable enhancement of drug antibacterial activity. In vitro nanoparticle-loaded rifampicin was more active against Staphylococcus aureus and Mycobacterium avium, localized in isolated alveolar macrophages. Level of rifampicin in macrophages increased 2-3-fold after incubation with rifampicinloaded nanoparticles comparing to the free drug. High therapeutic efficacy of colloidal rifampicin was demonstrated in vivo. Use of nanoparticles provided 2-fold increase in rifampicin efficacy, comparing with the free drug at treatment of staphylococcus sepsis in mice. Single administration of nanoparticulate rifampicin in the dose 25 mg/kg resulted in 80% survival of mice with salmonellosis, while 50 mg/kg of free rifampicin could provide only 10% survival. It may be considered that high antibacterial efficacy of rifampicin bound to nanoparticles is due to its effective delivery to macrophages.
Moscow Research Institute of Medical Ecology, Moscow, Russia.
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Skidan
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Gel'perina
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Severin
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Guliaev
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000627:therapeutic use; D003102:Colloids / Q000008:administration & dosage; D004337:Drug Carriers; D004659:Enbucrilate / Q000737:chemistry; D006801:Humans; D007275:Injections, Intravenous; D016676:Macrophages, Alveolar / Q000382:microbiology*; D051379:Mice; D009162:Mycobacterium avium / Q000187:drug effects*; D011817:Rabbits; D012293:Rifampin / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D012480:Salmonella Infections / Q000097:blood / Q000188:drug therapy; D012486:Salmonella typhimurium; D018805:Sepsis / Q000097:blood / Q000188:drug therapy; D013203:Staphylococcal Infections / Q000097:blood / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D003102:Colloids; D004337:Drug Carriers; D004659:Enbucrilate; D012293:Rifampin