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Journal of Nanoparticle Research

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01.02.2018 | Research Paper

Glutathione-responsive core cross-linked micelles for controlled cabazitaxel delivery

verfasst von: Xiaoxiong Han, Feirong Gong, Jing Sun, Yueqi Li, XiaoFei Liu, Dan Chen, Jianwen Liu, Yaling Shen

Erschienen in: Journal of Nanoparticle Research | Ausgabe 2/2018

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Abstract

Stimulus-responsive polymeric micelles (PMs) have recently received attention due to the controlled delivery of drug or gene for application in cancer diagnosis and treatment. In this work, novel glutathione-responsive PMs were prepared to encapsulate hydrophobic antineoplastic drug, cabazitaxel (CTX), to improve its solubility and toxicity. These CTX-loaded micelles core cross-linked by disulfide bonds (DCL-CTX micelles) were prepared by a novel copolymer, lipoic acid grafted mPEG-PLA. These micelles had regular spherical shape, homogeneous diameter of 18.97 ± 0.23 nm, and a narrow size distribution. The DCL-CTX micelles showed high encapsulation efficiency of 98.65 ± 1.77%, and the aqueous solubility of CTX was improved by a factor of 1:1200. In vitro release investigation showed that DCL-CTX micelles were stable in the medium without glutathione (GSH), whereas the micelles had burst CTX release in the medium with 10 mM GSH. Cell uptake results implied that DCL-CTX micelles were internalized into MCF-7 cells through clathrin-mediated endocytosis and released cargo more effectively than Jevtana (commercially available CTX) owing to GSH-stimulated degradation. In MTT assay against MCF-7 cells, these micelles inhibited tumor cell proliferation more effectively than Jevtana due to their GSH-responsive CTX release. All results revealed the potency of GSH-responsive DCL-CTX micelles for stable delivery in blood circulation and for intracellular GSH-trigged release of CTX. Therefore, DCL-CTX micelles show potential as safe and effective CTX delivery carriers and as a cancer chemotherapy formulation.

Vorheriger Artikel Rapid synthesis of N, S co-doped carbon dots and their application for Fe3+ ion detection

Nächster Artikel An insight into the influence of crystallite size on the performances of microsized spherical Li(Ni0.5Co0.2Mn0.3)O2 cathode material composed of aggregated nanosized particles

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Titel: Glutathione-responsive core cross-linked micelles for controlled cabazitaxel delivery
verfasst von: Xiaoxiong Han
Feirong Gong
Jing Sun
Yueqi Li
XiaoFei Liu
Dan Chen
Jianwen Liu
Yaling Shen
Publikationsdatum: 01.02.2018
Verlag: Springer Netherlands
Erschienen in: Journal of Nanoparticle Research / Ausgabe 2/2018
Print ISSN: 1388-0764
Elektronische ISSN: 1572-896X
DOI: https://doi.org/10.1007/s11051-018-4128-3

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