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J Pharm Sci ; 109(2): 1130-1135, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31568775

RESUMO

A sustained-release carrier system for the drug cephalexin (CEF) using functionalized graphene oxide is reported. PEGylation of GO (GO-PEG) and successful loading of CEF into PEGylated graphene oxide (GO-PEG-CEF) nanoconjugate are confirmed by Fourier transform infrared spectroscopy, Raman spectroscopy, and thermogravimetric analysis. Encapsulation efficiency of 69% and a loading capacity of 19% are obtained with the optimized formulation of GO-PEG-CEF. In vitro CEF release profiles show an initial burst release followed by a more sustained release over a 96 h period with cumulative release of 80%. The half maximal inhibitory concentration (IC50) values have both dose- and time-dependent antibacterial activity for GO-PEG-CEF against both gram-positive and gram-negative bacteria while pure CEF showed only dose-dependent antibacterial activity. The minimum inhibitory concentration values of GO-PEG-CEF are 7.8 and 3.9 µg/mL against S. aureus and B. cereus, respectively, while it is 10 µg/mL with pure CEF against both gram-positive bacteria. This confirms the enhanced antibacterial activity of GO-PEG-CEF over pure CEF against gram-positive bacteria. These findings therefore show GO-PEG-CEF is promising as a sustained-release nanoantibiotic system for effective treatment against S. aureus and B. cereus infections.


Assuntos
Grafite , Nanocompostos , Antibacterianos/farmacologia , Cefalexina , Preparações de Ação Retardada , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Staphylococcus aureus
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