Preparation, characterization and in vitro antimicrobial activity of liposomal ceftazidime and cefepime against Pseudomonas aeruginosa strains
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Data
2012-09
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Resumo
Pseudomonas aeruginosa is an opportunistic microorganism with the ability to respond to a wide variety of
environmental changes, exhibiting a high intrinsic resistance to a number of antimicrobial agents. This low
susceptibility to antimicrobial substances is primarily due to the low permeability of its outer membrane,
efflux mechanisms and the synthesis of enzymes that promote the degradation of these drugs.
Cephalosporins, particularty ceftazidime and cefepime are effective against P. aeruginosa, however, its
increasing resistance has limited the usage of these antibiotics. Encapsulating antimicrobial drugs into
unilamellar liposomes is an approach that has been investigated in order to overcome microorganism
resistance. In this study, antimicrobial activity of liposomal ceftazidime and cefepime against P. aeruginosa
ATCC 27853 and P. aeruginosa SPM-1 was compared to that of the free drugs. Liposomal characterization
included diameter, encapsulation efficiency and stability. Minimum Inhibitory Concentration (MIC) was
determined for free and liposomal forms of both drugs. Minimum Bactericidal Concentration (MBC) was
determined at concentrations 1, 2 and 4 times MIC. Average diameter of liposomes was 131.88 nm and
encapsulation efficiency for cefepime and ceftazidime were 2.29% end 5.77%, respectively. Improved
stability was obtained when liposome formulations were prepared with a 50% molar ratio for cholesterol in
relation to the phospholipid. MIC for liposomal antibiotics for both drugs were 50% lower than that of the
free drug, demonstrating that liposomal drug delivery systems may contribute to increase the antibacterial
activity of these drugs.
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Pseudomonas aeruginosa, Cephalosporins, Liposomes
Citação
TORRES, Ieda Maria Sapateiro et al. Preparation, characterization and in vitro antimicrobial activity of liposomal ceftazidime and cefepime against Pseudomonas aeruginosa strains. Brazilian Journal of Microbiology, São Paulo, v. 43, n. 3, p. 984-992, July/Sept. 2012.