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- W68354317 abstract "We previously demonstrated that osteoadsorptive BP conjugates of fluoroquinolones (E41, ciprofloxacin-BP), carried on CP particles (μ-sized Skelite™), packed into a traumatized bony defect, showed value in the treatment of rat tibial osteomyelitis (British J Surg, 2004;91:1192–1196). A Gatifloxacin-BP conjugate (GB) was contrasted to E41 for activity against methicillin-susceptible Staphylococcus aureus, and other pathogens. Minimum inhibitory concentration (MIC) and Mininum Bactericidal Concentrations (MBC) were determined. In vitro binding studies, holding levels of E41 and GB constant (2 μg/ml), while increasing levels of CP (nm-sized NanOss™), were determined by measurement of fluoroquinolone-BP associated fluorescence. GB showed greater MIC and MBC activity against several Gram-positive and Gram-negative pathogens, e.g., an 8-fold difference with S. aureus (Table). Binding appeared to be saturable. Maximal binding was: E41, 89.7 % ± 4.74, vs. GB, 76.8 % ± 2.35 (p≤0.05). The dissociation constant was: E41, 1.35 × 10−8 mM (NanOss™), vs GB, 1.83 × 10−8 mM (p≤0.05). Versus E41, GB has (i) improved activity against bone-pathogenic S. aureus, and other bacteria, and (ii) shows a similar binding affinity to NanOss™, used as a CP vehicle for topical drug delivery." @default.
- W68354317 created "2016-06-24" @default.
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- W68354317 date "2008-03-01" @default.
- W68354317 modified "2023-10-16" @default.
- W68354317 title "Two fluoroquinolone‐bisphosphonate (BP) derivatives show similar binding affinity to calcium phosphate (CP) particles, but have different antibacterial activity" @default.
- W68354317 doi "https://doi.org/10.1096/fasebj.22.1_supplement.1136.23" @default.
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