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Block ionomer complexes containing cationic antibiotics to kill intracellular Brucella melitensis in vitro
Author(s) -
Pothayee N.,
Jain N.,
Vadala T. P.,
Johnson L. M.,
MejiaAriza R.,
Sriranganathan N.,
Davis R. M.,
Riffle J. S.
Publication year - 2012
Publication title -
polymers for advanced technologies
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.61
H-Index - 90
eISSN - 1099-1581
pISSN - 1042-7147
DOI - 10.1002/pat.2070
Subject(s) - ethylene oxide , acrylate , materials science , cationic polymerization , antibiotics , propylene oxide , microbiology and biotechnology , copolymer , polymer chemistry , chemistry , organic chemistry , biology , polymer
Brucellosis, caused by Brucella spp., is the most common zoonotic disease worldwide. It is difficult to eradicate because the pathogen resides partially within phagocytic host cells and the polar antibiotics that are recommended for treatment do not enter cells efficiently. Core‐shell block ionomer complexes (BICs) carrying antibiotics in their cores were designed to transport these drugs into cells. Polyether–polyacrylate copolymers were condensed with cationic aminoglycoside antibiotics to form BICs with diameters of 170–340 nm in water. An anionic poly(acrylate‐ b ‐ethylene oxide‐ b ‐propylene oxide‐ b ‐ethylene oxide‐ b ‐acrylate) copolymer blended with a poly(ethylene oxide‐ b ‐acrylate) diblock was condensed with gentamicin to afford complexes containing up to 42 wt% of the antibiotic. The poly(propylene oxide) contributed hydrophobic interactions that enhanced stability of the complexes in aqueous media, whereas the hydrophilic blocks provided a steric brush to keep the structures dispersed. In vitro efficacy of the BICs to reduce intracellular Brucella was studied in murine macrophage‐like cells. Significant bacterial reductions of 2.78 and 2.85 logs were obtained relative to only 0.75 logs for the free drug. This suggests that the BICs are efficient transporters of polar antibiotics into phagocytic cells. Copyright © 2011 John Wiley & Sons, Ltd.