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Metronidazole loaded pectin microspheres for colon targeting
Ankur Vaidya1, Aviral Jain, Piush Khare
1Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar 470 003, Madhya Pradesh, India.
Journal of Pharmaceutical Sciences
|June 4, 2009
Summary
Colon-targeted delivery of metronidazole was achieved using Eudragit-coated pectin microspheres. These pH-sensitive microspheres demonstrated enzyme-biodegradable properties for effective drug release in the colon.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Colonic Drug Targeting
Background:
- Developing effective colon-targeted drug delivery systems is crucial for treating colonic diseases.
- Metronidazole is an antibiotic often requiring targeted delivery to the colon.
Purpose of the Study:
- To develop and evaluate a pH-sensitive and enzyme-biodegradable multiparticulate system for colon-specific delivery of metronidazole.
- To utilize pectin microspheres coated with Eudragit S-100 for enhanced colon targeting.
Main Methods:
- Pectin microspheres were prepared using an emulsion-dehydration technique.
- Microspheres were coated with Eudragit S-100 via an oil-in-oil solvent evaporation method.
- Surface morphology was characterized using Scanning Electron Microscopy (SEM).
Main Results:
- SEM confirmed a distinct Eudragit S-100 coating on pectin microspheres.
- In vitro studies showed no metronidazole release at gastric pH but sustained release at colonic pH.
- Drug release was significantly higher in the presence of rat caecal contents, indicating enzymatic degradation.
Conclusions:
- Eudragit-coated pectin microspheres are a promising system for colon-specific metronidazole delivery.
- The formulation exhibits pH-sensitivity and enzyme biodegradability, crucial for colonic targeting.
- In vivo studies supported the potential of this formulation for targeted drug release in the gastrointestinal tract.
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