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Thiomers: promising platform for macromolecular drug delivery
Flavia Laffleur1, Andreas Bernkop-Schnürch
1Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry & Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
Future Medicinal Chemistry
|November 30, 2012
Summary
Thiolated polymers, or thiomers, enhance macromolecule drug delivery by improving mucoadhesion and enzyme inhibition. A new generation, preactivated thiomers, offers superior oxidation resistance for better therapeutic applications.
Area of Science:
- Polymer Chemistry
- Drug Delivery Systems
- Biotechnology
Background:
- Macromolecules show therapeutic potential for cancer and cardiovascular diseases.
- Current delivery strategies for macromolecules are inefficient, unsafe, and lack specificity.
- Thiolated polymers (thiomers) offer improved mucoadhesion and enzyme inhibition compared to unmodified polymers.
Purpose of the Study:
- To review recent findings on polymeric excipients for macromolecule drug delivery.
- To discuss the synthesis and distinctive features of thiomers and preactivated thiomers.
- To highlight solutions for thiomer limitations in drug delivery.
Main Methods:
- Synthesis of thiomers by immobilizing sulfhydryl-bearing ligands on polymer backbones.
- Development of preactivated thiomers as mixed disulfides.
- Evaluation of thiomer properties including mucoadhesion and enzyme inhibition.
Main Results:
- Thiomers demonstrate enhanced mucoadhesion and enzyme/efflux pump inhibition.
- Preactivated thiomers exhibit improved oxidation resistance compared to conventional thiomers.
- Preactivated thiomers offer enhanced features for macromolecule delivery.
Conclusions:
- Thiomers represent a promising strategy for overcoming challenges in macromolecule drug delivery.
- Preactivated thiomers address the oxidation susceptibility of conventional thiomers.
- Advanced polymeric excipients like preactivated thiomers are crucial for efficient and safe macromolecule therapeutics.
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