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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
Dual-responsive core-crosslinked polyphosphoester-based nanoparticles for pH/redox-triggered anticancer drug delivery
Yue Sun1, Xueqiong Du, Jinlin He
1College of Chemistry, Chemical Engineering and Materials Science, State and Local Joint Engineering Laboratory for Novel Functional Polymeric Materials, Jiangsu Key Laboratory of Advanced Functional Polymer Design and Application, Suzhou Key Laboratory of Macromolecular Design and Precision Synthesis, Soochow University, Suzhou 215123, P. R. China. phni@suda.edu.cn.
This study developed novel dual-responsive nanoparticles for cancer therapy, enhancing drug delivery and reducing side effects. These intelligent nanoparticles effectively release drugs inside cancer cells, improving treatment outcomes.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Polymer Chemistry
Background:
- Intelligent nanoparticles enhance drug bioavailability and reduce side effects in anticancer therapeutics.
- Developing stimuli-responsive drug delivery systems is crucial for targeted cancer therapy.
Purpose of the Study:
- To design and synthesize novel biodegradable polyphosphoester-based functional copolymer prodrug nanoparticles (NPs).
- To create pH/redox dual-responsive core-crosslinked nanoparticles (DOX/CCL NPs) for controlled intracellular drug release.
Main Methods:
- Synthesized a biodegradable polymeric prodrug PTX-PBYP-b-PEEP using paclitaxel (PTX) as an initiator.
- Utilized thiol-ene click chemistry to introduce carboxyl groups for drug encapsulation and crosslinking.
- Formed dual-responsive nanoparticles via amidation with cystamine, creating disulfide linkages.
Main Results:
- Achieved high doxorubicin (DOX) loading content (14.6%) and efficiency (73.1%) in the NPs.
- Demonstrated pH (5.0) and redox (10 mM GSH) dual-responsive drug release due to disulfide bond cleavage and electrostatic interactions.
- Observed efficient internalization by HeLa cells and significant inhibition of cellular proliferation.
Conclusions:
- The developed DOX/CCL NPs show promise as an intelligent drug delivery system for cancer therapy.
- The pH/redox dual-responsive nature enables controlled intracellular drug release, enhancing therapeutic efficacy.
- This strategy offers a viable approach for advanced anticancer therapeutics with reduced side effects.

