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Modular design of redox-responsive stabilizers for nanocrystals
Kathrin Fuhrmann1, Anna Połomska, Carmen Aeberli
1Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology Zurich (ETH Zürich), Wolfgang-Pauli-Straße 10, 8093 Zurich, Switzerland.
ACS Nano
|August 24, 2013
Summary
Researchers developed new polymer stabilizers for drug nanocrystals (NCs). These stabilizers prevent aggregation and can be triggered by oxidation, offering control over NC size and drug release for improved therapeutic applications.
Area of Science:
- Materials Science
- Nanotechnology
- Polymer Chemistry
Background:
- Poor aqueous solubility limits intravenous administration of potent drugs.
- Drug nanocrystals (NCs) are a strategy to improve solubility but require stabilization.
- Stabilizers need high affinity for NCs and a trigger mechanism for controlled release.
Purpose of the Study:
- To develop a systematic strategy for optimizing polymeric stabilizers for drug NCs.
- To create redox-responsive stabilizers with tunable affinity and triggered release.
- To investigate the influence of oxidation on NC size and dissolution.
Main Methods:
- Preparation of a library of 10 redox-responsive polymer stabilizers via postpolymerization modification.
- Utilizing the thiol-yne reaction for polymer synthesis.
- Characterization of paclitaxel NCs stabilized by the developed polymers.
Main Results:
- Demonstrated a modular approach to optimize stabilizer affinity for drug NCs.
- Showcased redox-responsive polymers that stabilize paclitaxel NCs.
- Observed oxidation-induced changes in NC size and dissolution influenced by reactive oxygen species (ROS).
Conclusions:
- Developed versatile, triggered-sheddable stabilizing coatings for nanoparticles.
- The strategy allows for identification of optimal responsiveness for specific applications.
- Provides general tools for nanoparticle stabilization and controlled drug delivery.
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