Vancomycin biodegradable poly(lactide-co-glycolide) microparticles for bone implantation. Influence of the formulation parameters on the size, morphology, drug loading and in vitro release.
The present study investigates vancomycin microencapsulation in biodegradable PLAGA microparticles. To optimize encapsulation efficiency by the double emulsion (w/o/w) solvent evaporation/extraction process, two parameters were studied: surfactant (Span 80) rate and external aqueous phase saturation. In vitro dissolution studies, laser granulometry and scanning electron microscopy were performed to characterize the microparticles. The best results were obtained by stabilizing the first emulsion with 0.5% Span 80 and saturating the external phase with sodium chloride. Such parameters allowed a 95% drug encapsulation efficiency. This process yielded round microparticles with a mean diameter of approximately 170 microm and presenting a smooth surface without any pores. Moreover, this formulation induces a sustained drug release at a constant rate over a period of 10 days. Such materials could be associated with biphasic calcium phosphate granules to form an antibiotic-loaded injectable bone substitute offering a long-term activity in situ.
Billon
A
A
Laboratoire de Pharmacie Galénique, Faculté de Pharmacie de Nantes, Nantes, France. aurelie.billon@sante.univ-nantes.fr
Chabaud
L
L
Gouyette
A
A
Bouler
J-M
JM
Merle
C
C
D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D001673:Biodegradation, Environmental; D016025:Bone Transplantation; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D006801:Humans; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008863:Microspheres; D010316:Particle Size; D011098:Polyglactin 910; D012965:Sodium Chloride; D013499:Surface Properties; D014640:Vancomycin
D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D011098:Polyglactin 910; D012965:Sodium Chloride; D014640:Vancomycin