期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 98, 期 10, 页码 3659-3665出版社
WILEY
DOI: 10.1002/jps.21680
关键词
ciprofloxacin center dot HCl; sustained-release; poly(DL-lactide-co-glycolide); microsphere; infection model
资金
- Ministry of Knowledge Economy (MKE) [RTI05-01-01]
In this study, we created ciprofloxacin center dot HCl (CIP)-encapsulated poly(D-lactide-co-glycolide) (PLGA) microspheres by the solvent evaporation method. Their antibacterial activity was evaluated with pathogenic microorganisms in vitro and in vivo. Since the half-life of CIP in the blood stream is short, sustained-release proper-ties of microspheres may provide enhanced antibacterial activity. CIP-encapsulated microspheres of PLGA were prepared by the O/O method. CIP-encapsulated PLGA microspheres showed spherical shapes under a scanning electron microscope (SEM), and their particle sizes ranged from 10 to 50 mu m. In an in vitro drug release study, CIP was continuously released over 3 weeks from the microspheres, and a burst effect was observed for the first 3 days. In the in vitro antibacterial activity test, CIP-microspheres showed lower antibacterial activity compared to free CIP because of their sustained-release properties, while empty microspheres did not affect the growth of microorganisms. In the in vivo antibacterial activity test, the number of microorganisms following treatment with CIP-encapsulated microspheres was significantly lower than after treatment with free CIP at 5 days postinjection. These results suggest that encapsulated CIP keeps its antibacterial activity after microencapsulation. (C) 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm. Sci 98:3659-3665, 2009
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