Preparation of ciprofloxacin-encapsulated poly(DL-lactide-co-glycolide) microspheres and its antibacterial activity.
In this study, we created ciprofloxacin.HCl (CIP)-encapsulated poly(DL-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 properties 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 microm. 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.
Jeong
Young-Il
YI
Department of Polymer Science and Engineering, Sunchon, Jeonnam 540-742, Republic of Korea.
Na
Hee-Sam
HS
Nah
Jae-Woon
JW
Lee
Hyun-Chul
HC
D000465:Algorithms; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D002850:Chromatography, Gel; D002939:Ciprofloxacin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D005079:Excipients; D005260:Female; D019344:Lactic Acid; D051379:Mice; D008807:Mice, Inbred BALB C; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012480:Salmonella Infections / Q000188:drug therapy / Q000382:microbiology; D012486:Salmonella typhimurium / Q000187:drug effects
D000900:Anti-Bacterial Agents; D005079:Excipients; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002939:Ciprofloxacin