Pharmaceutical development and technology

Design and evaluation of gamma-sterilized vancomycin hydrochloride-loaded poly(ɛ-caprolactone) microspheres for the treatment of biofilm-based medical device-related osteomyelitis.

PMID 26498171


There is a great necessity to find and use accomplished terminal sterilization technique for industrial manufacturing, research and development studies. Gamma (γ)-sterilization has been commonly employed for wide range of products as indicated by the pharmacopoeias. However, carefully examination should be performed prior to administration since γ-radiation can cause changes in drug and polymer excipients. No information is available in literature about γ-sterilization effects on vancomycin HCl-loaded poly (ɛ-caprolactone) (PCL) microspheres. Formulations were developed using a different preparation approach for the treatment of medical device-related osteomyelitis, and γ-sterilization effects on the physicochemical characterization of the formulations were examined. Water-in-oil-in-water (w/o/w) emulsion technique using polyvinyl alcohol (PVA) in inner and outer phase was applied to prepare formulations. Physicochemical properties of the formulations were investigated before and after γ-sterilization and the antibacterial activity against Staphylococcus aureus (S. aureus) and Staphylococcus epidermidis (S. epidermidis) were measured. The particle size of the nonsterilized formulations were between 58 and 134 μm. 60% or 20% of vancomycin HCl were released from 42.500 Mn or 70.000-90.000 Mn PCL microspheres, respectively, in 24 h. No difference was observed in the particle size, drug-loading efficiency, morphology, in vitro release and antimicrobial activity of the formulations after γ-sterilization (p > 0.05).