OBJECTIVE: To prepare vancomycin-loaded chitosan sustained-release microspheres and to study its drug release and antibacterial effects in vitro. METHODS: The emulsion cross-linking was used to prepare vancomycin-loaded chitosan sustained-release microspheres, and the particle size and morphology of microspheres were observed. The contents of vancomycin in microspheres was determined by UV spectrophotometry, and drug-loading amount of entrapment efficiency were calculated. Drug release of prepared microspheres and vancomycin hydrochloride within 24 h were compared by release trial in vitro, and then its accumulative release rate (Q) within 7 d was investigated. The effects of prepared microspheres on the diameter of inhibition zone to Staphylococcus aureus after treated for 20 d were observed through in vitro antibacterial test. RESULTS: The microspheres were spherical and complete round without obvious bump and pore. The average particle size of the microspheres was (165.6±19.7) μm; average drug-loading amount was (32.6±3.2)%; average encapsulation efficiency was (53.8±6.3)%; Q7 d was 82.7%. Q2 h of prepared microspheres and vancomycin hydrochloride were 18.6% and 91.3%. The diameter of inhibition zone was higher than 3 cm after treated for 1 d, and then decreased gradually as time. CONCLUSIONS: Vancomycin-loaded chitosan sustained-release microspheres can be prepared successfully, and show obvious in vitro sustained-release effect and antibacterial effects.
关键词
万古霉素壳聚糖微球体外释药体外抑菌
Keywords
VancomycinchitosanMicrosphereRelease in vitroAntibacterial effect in vitro