In vitro characterization of calcium phosphate biomaterial loaded with linezolid for osseous bone defect implantation.
Osteomyelitis is a severe bone infection frequently caused by Staphylococcus aureus, which shows significant resistance to methicillin. One therapeutic treatment would be to insert a bone substitute loaded to an antibiotic, which would enable the bone to be filled while the illness is being treated. Linezolid is an oxazolidinone antibiotic with a large spectrum of action. It is effective against most Gram-positive bacteria and displays a specific mode of action. The aim of this work was to study the association of linezolid with a calcium phosphate-deficient apatite matrix. Granules containing 10% and 50% linezolid were prepared by wet granulation and characterized. Porosity analyses performed by mercury porosimetry and scanning electron microscopy revealed that grain porosity with 50% linezolid was higher than that of the grains containing 10% linezolid. NMR analyses showed no change in structure of linezolid when linked to calcium-deficient apatite. These results were confirmed by studying the antibacterial activity of linezolid, which remained proportional to the quantity of loaded linezolid, proving that the antibiotic released was active. The in vitro release time varied from 9 days for granules containing 10% linezolid to 26 days for granules containing 50% linezolid.
Gautier
Hélène
H
INSERM, U 791, Laboratoire d'Ingénierie Ostéo-Articulaire et Dentaire, LIOAD, Faculté de Chirurgie Dentaire, 1 Place A. Ricordeau, Nantes, F-44042, France. helene.gautier@univ-nantes.fr
Plumecocq
Adrien
A
Amador
Gilles
G
Weiss
Pierre
P
Merle
Christian
C
Bouler
Jean-Michel
JM
D000081:Acetamides / Q000008:administration & dosage* / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001031:Apatites / Q000737:chemistry; D001672:Biocompatible Materials / Q000737:chemistry*; D002130:Calcium Phosphates / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D000069349:Linezolid; D010019:Osteomyelitis / Q000188:drug therapy; D023303:Oxazolidinones / Q000008:administration & dosage* / Q000494:pharmacology
D000081:Acetamides; D000890:Anti-Infective Agents; D001031:Apatites; D001672:Biocompatible Materials; D002130:Calcium Phosphates; D004337:Drug Carriers; D023303:Oxazolidinones; C020243:calcium phosphate; D000069349:Linezolid