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Colon-specific drug delivery: Influence of solution reticulation properties upon pectin beads performance
O Chambin1, G Dupuis, D Champion
1Pharmaceutical Powder Technology Group, IMSAPS Team, EA 581, School of Pharmacy, 7 Boulevard Jeanne d'Arc, University of Burgundy, 21 079 Dijon Cedex, France. odile.chambin@u-bourgogne.fr
International Journal of Pharmaceutics
|June 23, 2006
Summary
Zinc pectinate beads effectively deliver drugs to the colon. This formulation prevents upper gastrointestinal release, with pectinolytic enzymes enabling specific drug release in the colon.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Colon drug delivery systems are crucial for treating colonic diseases and improving therapeutic efficacy.
- Pectin-based hydrogels offer potential for controlled drug release due to their biocompatibility and biodegradability.
Purpose of the Study:
- To develop and characterize zinc pectinate beads for targeted colon drug delivery.
- To investigate the influence of formulation parameters on bead properties and drug release kinetics.
- To evaluate the potential of these beads for oral administration and specific drug release in the colon.
Main Methods:
- Ionotropic gelation method was employed to produce pectinate gel beads.
- Ketoprofen was used as a model drug for entrapment.
- Formulation parameters, including cross-linking agent concentration and pH, were varied.
- Bead properties (e.g., gel network strength) and drug release profiles were assessed at different pH values and in the presence of pectinolytic enzymes.
Main Results:
- Zinc pectinate beads formed a strong gel network at pH 1.6 with 10% counter-ions, attributed to "egg-box" dimer formation and hydrogen bonding.
- The compact gel network structure minimized drug release in the upper gastrointestinal tract (pH 1.2 and 7.4).
- Specific ketoprofen release was observed in the colon, mediated by pectinolytic enzymes.
- Drug release rates were found to be modifiable by adjusting counter-ion concentration during reticulation.
Conclusions:
- Pectinate beads are a promising carrier system for targeted oral drug delivery to the colon.
- The formulation parameters significantly influence bead properties and drug release profiles.
- This approach offers an efficient strategy for localized drug action within the colon.
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