Metronidazole loaded pectin microspheres for colon targeting

• Published in: Journal of pharmaceutical sciences 2009-11, Vol.98 (11), p.4229-4236
• Main Authors: vaidya, Ankur, Jain, Aviral, Khare, Piush, Agrawal, Ram K., Jain, Sanjay K.
• Format: Article
• Language: English
• Subjects: amoebiasis; Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiprotozoal Agents - administration & dosage; Antiprotozoal Agents - chemistry; Antiprotozoal Agents - pharmacokinetics; Biological and medical sciences; Cecum - metabolism; Cecum - microbiology; Coated Materials, Biocompatible - chemistry; Colon - metabolism; colon delivery; Drug Carriers - chemistry; Drug Delivery Systems - methods; Excipients - chemistry; Gastrointestinal Contents - chemistry; General pharmacology; Hydrogen-Ion Concentration; Medical sciences; metronidazole; Metronidazole - administration & dosage; Metronidazole - chemistry; Metronidazole - pharmacokinetics; Microscopy, Electron, Scanning; Microspheres; Miscellaneous. Antibiotics with multiple activities; Particle Size; pectin; Pectins - chemistry; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Rats
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.21742

A multiparticulate system having pH-sensitive property and specific enzyme biodegradability for colon-targeted delivery of metronidazole was developed. Pectin microspheres were prepared using emulsion-dehydration technique. These microspheres were coated with Eudragit® S-100 using oil-in-oil solvent evaporation method. The SEM was used to characterize the surface of these microspheres and a distinct coating over microspheres could be seen. The in vitro drug release studies exhibited no drug release at gastric pH, however continuous release of drug was observed from the formulation at colonic pH. Further, the release of drug from formulation was found to be higher in the presence of rat caecal contents, indicating the effect of colonic enzymes on the pectin microspheres. The in vivo studies were also performed by assessing the drug concentration in various parts of the GIT at different time intervals which exhibited the potentiality of formulation for colon targeting. Hence, it can be concluded that Eudragit coated pectin microspheres can be used for the colon specific delivery of drug. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4229–4236, 2009