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载铜(II)双硫仑黑色素纳米点的癌症诊疗一体化。

Copper(II)-disulfiram loaded melanin-dots for cancer theranostics.

机构信息

Institute of Molecular Medicine, College of Life and Health Sciences, Northeastern University, Shenyang, China.

Institute of Molecular Medicine, College of Life and Health Sciences, Northeastern University, Shenyang, China.

出版信息

Nanomedicine. 2021 Feb;32:102340. doi: 10.1016/j.nano.2020.102340. Epub 2020 Nov 21.

DOI:10.1016/j.nano.2020.102340
PMID:33227540
Abstract

Copper(II) diethyldithiocarbamate complex (CuET), the metabolite of disulfiram complexed with copper, is the component responsible for cancer treatment efficacy of disulfiram. But the hydrophobic property of CuET limits its use in vivo, and an appropriate drug delivery system needs to be developed. Ultrasmall melanin nanoparticle (M-Dot) with excellent biosafety and biocompatibility properties has been synthesized in our previous studies. Herein we prepared CuET loaded with M-Dots through hydrophobic interaction, which could enhance the water solubility significantly. After the administration of M-Dots-CuET in mice tumor models, the nanoparticles showed good tumor accumulation as evidenced by the enhanced photoacoustic signal in tumor regions. M-Dots-CuET also displayed excellent tumor inhibition capability, and the tumor growth inhibition value (TGI) was 45.1%. When combined with photothermal therapy, the TGI reached up to 78.6%. In summary, M-Dots-CuET provide a new potential strategy for cancer theranostics.

摘要

铜(II)乙二硫代氨基甲酸盐络合物(CuET)是与铜络合的戒酒硫的代谢物,是戒酒硫治疗癌症疗效的组成部分。但 CuET 的疏水性限制了其在体内的应用,需要开发一种合适的药物输送系统。在我们之前的研究中,已经合成了具有优异生物安全性和生物相容性的超小黑素纳米颗粒(M-Dot)。在此,我们通过疏水相互作用制备了负载 M-Dot 的 CuET,这可以显著提高其水溶性。在小鼠肿瘤模型中给予 M-Dots-CuET 后,通过肿瘤区域增强的光声信号证明了纳米颗粒具有良好的肿瘤积累。M-Dots-CuET 还表现出优异的肿瘤抑制能力,肿瘤生长抑制率(TGI)为 45.1%。当与光热疗法结合时,TGI 高达 78.6%。总之,M-Dots-CuET 为癌症治疗提供了一种新的潜在策略。

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