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Updated: May 1, 2026

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 17, 2013
Trends in drug delivery through tissue barriers containing tight junctions
Christian Tscheik1, Ingolf E Blasig1, Lars Winkler1
1Leibniz Institut für Molekulare Pharmakologie; Berlin-Buch, Germany.
Targeting tight junctions (TJs) with novel methods can enhance drug delivery by improving permeation through tissue barriers. Specific modulation of TJ proteins offers a promising strategy over unspecific enhancers like sodium caprate.
Area of Science:
- Pharmacology
- Biophysics
- Cell Biology
Background:
- Drug uptake is limited by tissue barrier permeation.
- Tight junctions (TJs) regulate barrier permeability, controlling paracellular diffusion.
- Transient TJ modulation is a key strategy for enhancing drug delivery.
Purpose of the Study:
- To review current progress in TJ modulation for drug delivery.
- To discuss novel approaches for specific TJ protein targeting.
- To evaluate the impact of these strategies on TJ barrier function.
Main Methods:
- Review of studies on surfactant-like absorption enhancers (e.g., sodium caprate).
- Exploration of novel approaches targeting TJ-associated proteins and claudins.
- Discussion of synthetic peptidomimetics and RNA interference techniques for TJ protein downregulation.
Main Results:
- Sodium caprate modulates TJs unspecifically, limiting its therapeutic potential.
- Specific modulation of TJ proteins (claudins) offers a more targeted approach.
- Synthetic peptidomimetics and RNAi show promise in downregulating TJ protein expression.
Conclusions:
- Specific TJ modulation is a potent strategy to overcome drug delivery limitations.
- Targeting TJ proteins and claudins represents a novel and effective approach.
- Further research into these targeted methods is crucial for advancing drug delivery systems.
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