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. 2015 Dec 14;60(3):1865-8.
doi: 10.1128/AAC.01609-15.

Novel Bone-Targeting Agent for Enhanced Delivery of Vancomycin to Bone

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Novel Bone-Targeting Agent for Enhanced Delivery of Vancomycin to Bone

Zaineb A F Albayati et al. Antimicrob Agents Chemother. .

Abstract

We examined the pharmacokinetic properties of vancomycin conjugated to a bone-targeting agent (BT) with high affinity for hydroxyapatite after systemic intravenous administration. The results confirm enhanced persistence of BT-vancomycin in plasma and enhanced accumulation in bone relative to vancomycin. This suggests that BT-vancomycin may be a potential carrier for the systemic targeted delivery of vancomycin in the treatment of bone infections, potentially reducing the reliance on surgical debridement to achieve the desired therapeutic outcome.

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Figures

FIG 1
FIG 1
Structures of vancomycin (left) and BT-vancomycin (right).
FIG 2
FIG 2
Plasma concentration-time profile of vancomycin (circles) and BT-vancomycin (squares) after i.v. administration of 50 mg/kg vancomycin or 63.85 mg/kg BT-vancomycin (molar equivalent to 50 mg/kg vancomycin). Results are the mean ± SEM (n = 5 rats). *, significantly higher than results for vancomycin, P < 0.05; **, significantly higher than results for vancomycin, P < 0.01; ***, significantly higher than results for vancomycin, P < 0.0001.
FIG 3
FIG 3
Concentration-time profile in bone of vancomycin (circles) and BT-vancomycin (squares) after i.v. administration of vancomycin (50 mg/kg) or BT-vancomycin (63.85 mg/kg). Results are the mean ± SEM (n = 5 rats per group). *, significantly higher than results for vancomycin, P < 0.05; **, significantly higher than results for vancomycin, P < 0.01; ***, significantly higher than results for vancomycin, P < 0.001.

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