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Tablet formulation with dual control concept for efficient colonic drug delivery.
Viviane Doggwiler1, Michael Lanz2, Valeria Paredes2
1School of Life Sciences, University of Applied Sciences Northwestern Switzerland, Hofackerstrasse 30, 4132 Muttenz, Switzerland; Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.
International Journal of Pharmaceutics
|December 18, 2022
Summary
This study developed a dual-control tablet for targeted colon drug delivery using a pH-sensitive coating and a xyloglucan matrix. The formulation demonstrated controlled release in the colon, triggered by microbiome enzymes.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Gastrointestinal Pharmacology
Background:
- Targeted colon drug delivery is crucial for treating colonic diseases.
- Conventional formulations often fail to reach the colon intact or release drugs prematurely.
- Developing advanced drug delivery systems with dual control mechanisms is essential for enhanced efficacy.
Purpose of the Study:
- To engineer a tablet formulation for precise drug release in the colon.
- To implement a dual control system combining a pH-sensitive coating and a xyloglucan matrix.
- To investigate microbiome-triggered drug release in the colonic environment.
Main Methods:
- Development of a tablet with Eudragit® FS 30 D pH-sensitive coating and a xyloglucan matrix.
- In vitro dissolution testing simulating gastrointestinal transit with a four-stage protocol.
- Incorporation of microbial xyloglucanase to mimic colonic microbiome activity.
- Monitoring of matrix erosion via reducing sugar equivalents and drug release kinetics.
Main Results:
- Achieved limited drug release in gastric and small intestinal stages, with predominant release in the colon.
- Xyloglucan matrix formed a gummy layer, controlling release post-coating dissolution.
- Matrix degradation and drug release were enzyme-dependent, leading to erosion-controlled release.
- Drug release was completed within colonic transit time at physiological enzyme concentrations.
- Dual control system showed similar release rates for caffeine and 5-ASA in the presence of xyloglucanase.
Conclusions:
- The developed dual-control tablet formulation successfully achieves targeted colonic drug release.
- The combination of pH-sensitive coating and xyloglucan matrix offers effective control over drug release kinetics.
- Microbiome-triggered degradation of the xyloglucan matrix is a viable strategy for colon-specific drug delivery.
- The formulation's performance is consistent across different drug solubilities, indicating broad applicability.
Keywords:
5-aminosalicylic acidColonic deliveryColonic microbiomeDissolution testingErosion-controlledXyloglucanMore Related Videos
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