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Issue 10, 2019
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Cysteine-based redox-responsive nanoparticles for small-molecule agent delivery

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As a significant part of molecular-targeted therapies, small-molecule agents (SMAs) have been increasingly used for cancer treatment. Nevertheless, most SMAs are currently administered orally due to their poor solubility, resulting in a low bioavailability and unavoidable side effects. Herein, we proposed a promising SMA delivery strategy using a biocompatible and redox-responsive nanoparticle (NP) delivery system to improve their bioavailability, alleviate side effects and enhance therapeutic performance. To demonstrate the feasibility of this strategy, a type of cysteine-based hydrophobic polymer was employed to construct a redox-sensitive nanoplatform for the delivery of various hydrophobic oral SMAs. These SMA-loaded nanoparticles (SMA-NPs) all have a small particle size and good drug-loading capacity. Particularly, lapatinib-loaded nanoparticles (LAP-NPs) with a minimal particle size (79.71 nm) and an optimal drug-loading capacity (12.5%) were utilized as a model to systemically explore the in vitro and in vivo anticancer potential of SMA-NPs. As expected, the LAP-NPs exhibited rapid redox-responsive drug release, enhanced in vitro cytotoxicity and cell apoptosis, and demonstrated notable anti-metastasis ability and desirable intracellular localization. Additionally, the in vivo results demonstrated the preferential accumulation of LAP-NPs in tumor tissues and the significant suppression of tumor growth. Therefore, the generated SMA-NP delivery system shows great SMA delivery potential for advanced molecular-targeted therapies.

Graphical abstract: Cysteine-based redox-responsive nanoparticles for small-molecule agent delivery

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Publication details

The article was received on 11 Jun 2019, accepted on 24 Jul 2019 and first published on 25 Jul 2019

Article type: Paper
DOI: 10.1039/C9BM00907H
Biomater. Sci., 2019,7, 4218-4229

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    Cysteine-based redox-responsive nanoparticles for small-molecule agent delivery

    L. Wang, X. You, Q. Lou, S. He, J. Zhang, C. Dai, M. Zhao, M. Zhao, H. Hu and J. Wu, Biomater. Sci., 2019, 7, 4218
    DOI: 10.1039/C9BM00907H

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