Preparation of Ciprofloxacin-Encapsulated Poly(DL-Lactide-co-glycolide) Microspheres and Its Antibacterial Activity

• Published in: Journal of pharmaceutical sciences Vol. 98; no. 10; pp. 3659 - 3665
• Main Authors: Jeong, Young-Il, Na, Hee-Sam, Nah, Jae-Woon, Lee, Hyun-Chul
• Format: Journal Article
• Language: English
• Published: Hoboken Elsevier Inc 01.10.2009; Wiley Subscription Services, Inc., A Wiley Company; Wiley; American Pharmaceutical Association
• Subjects: Algorithms; Animals; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antibacterial activity; Biological and medical sciences; Blood; Chemistry, Pharmaceutical; Chromatography, Gel; Ciprofloxacin - administration & dosage; Ciprofloxacin - chemistry; Ciprofloxacin - pharmacology; ciprofloxacin·HCl; Controlled release; Drug delivery; Drugs; Evaporation; Excipients; Female; General pharmacology; infection model; Lactic Acid; Medical sciences; Mice; Mice, Inbred BALB C; microencapsulation; Microorganisms; microsphere; Microspheres; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; poly(DL-lactide-co-glycolide); Polyglycolic Acid; polylactide-co-glycolide; Salmonella Infections - drug therapy; Salmonella Infections - microbiology; Salmonella typhimurium - drug effects; Scanning electron microscopy; Solvents; sustained-release; microsphere; infection model; poly(DL-lactide-co-glycolide); ciprofloxacin·HCl; sustained-release; Encapsulation; Glycolic acid copolymer; Lactone copolymer; Microsphere; Pharmaceutical technology; Controlled release form; Lactic acid copolymer; Infection; Fluoroquinolone derivatives; Preparation; Dosage form; Microparticle; Copolymer; Antibacterial agent; Ciprofloxacin; Quinolone derivatives
• ISSN: 0022-3549; 1520-6017; 1520-6017
• DOI: 10.1002/jps.21680

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 µm. 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. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:3659–3665, 2009