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OPTICORE™, an innovative and accurate colonic targeting technology
Felipe Varum1, Ana Cristina Freire2, Roberto Bravo3
1Tillotts Pharma AG, Baslerstrasse 15, CH-4310 Rheinfelden, Switzerland; UCL School of Pharmacy, University College London, Brunswick Square, WC1N 1AX London, UK.
A new OPTICORE™ coating technology enhances colon drug delivery for inflammatory bowel disease (IBD) by combining pH and enzyme triggers. This improves treatment accuracy, especially for ulcerative colitis patients.
Area of Science:
- Gastroenterology
- Pharmaceutics
- Materials Science
Background:
- Inflammatory bowel disease (IBD) affects millions globally, with current treatments often relying on suboptimal colonic targeting.
- Existing colonic drug delivery systems primarily utilize the gastrointestinal pH gradient, which can be inconsistent.
Purpose of the Study:
- To introduce and evaluate the novel OPTICORE™ coating technology for enhanced colonic drug delivery.
- To investigate the mechanisms of accelerated drug release and improved targeting for IBD therapies.
Main Methods:
- Development of OPTICORE™ technology with a dual-trigger outer layer (pH and enzyme) and an inner release acceleration layer.
- Coating 5-aminosalicylic acid (5-ASA) tablets with various inner layer formulations, manipulating polymer type, buffer salt concentration, and neutralization pH.
- Analysis of drug release profiles influenced by buffer capacity, pH, ionic strength, and colonic bacterial enzymes.
Main Results:
- The inner layer's buffer capacity, influenced by polymer type and buffer salt concentration, significantly accelerates drug release.
- An interplay of buffer capacity, pH, and ionic strength is crucial for optimized release kinetics.
- Resistant starch in the outer layer enables enzyme-mediated drug release by colonic bacteria without compromising enteric properties.
Conclusions:
- OPTICORE™ technology offers a superior approach to colonic drug delivery compared to standard enteric coatings.
- The dual-trigger system ensures more precise drug delivery to the colon, benefiting patients with conditions like ulcerative colitis.
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