Key-properties outlook of a levofloxacin-loaded acrylic bone cement with improved antibiotic delivery

[Display omitted] •Novel lactose-modified acrylic bone cement with improved antibiotic (levofloxacin) release.•7-week release of levofloxacin with antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis and Escherichia coli.•Improved inhibition of Staphylococcus aureus biofi...

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Veröffentlicht in:International journal of pharmaceutics 2015-05, Vol.485 (1-2), p.317-328
Hauptverfasser: Matos, Ana C., Ribeiro, Isabel A.C., Guedes, Rita C., Pinto, Rosana, Vaz, Mário A., Gonçalves, Lídia M., Almeida, António J., Bettencourt, Ana F.
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Sprache:eng
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Zusammenfassung:[Display omitted] •Novel lactose-modified acrylic bone cement with improved antibiotic (levofloxacin) release.•7-week release of levofloxacin with antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis and Escherichia coli.•Improved inhibition of Staphylococcus aureus biofilm development by the lactose-modified bone cement matrix, when compared to the commercial acrylic bone cement matrix.•Maintenance of both mechanical integrity and biocompatibility of the modified acrylic bone cement.•Favorable covalent and non-covalent interactions between levofloxacin and the bone cement are evidenced by density functional calculations. Antibiotic-loaded acrylic bone cements (ALABCs) are widely used to decrease the occurrence of bone infections in cemented arthroplasties and actually being considered as a more cost-effective procedure when compared to cementless implants. However, ALABCs have a major drawback, which is the incomplete release of the antibiotics and, as a result, pathogens that commonly are responsible for those infections are becoming resistant. Consequently, it is of most relevance to find new antibacterial agents to load into BC with an effective mechanism against those microorganisms. This research work intended to load levofloxacin, a fluoroquinolone with anti-staphylococcal activity and adequate penetration into osteoarticular tissues, on lactose-modified commercial bone cement (BC). This modified BC matrix exhibited increased levofloxacin release and delayed Staphylococcus aureus biofilm formation. Further insights on material-drug interaction during BC setting were investigated by density functional theory calculations. The obtained results suggested that favorable covalent and non-covalent interactions could be established between levofloxacin and the BC. Moreover, BC mechanical and biocompatibility properties were maintained. These features justify the potential of levofloxacin-loaded modified-BC as a valuable approach for local antibiotic delivery in bone infections management.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2015.03.035