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基于羧甲基壳聚糖与柔红霉素共价接枝共轭物的pH响应性纳米颗粒用于抗癌药物递送

pH-Responsive Nanoparticles Based on Covalently Grafted Conjugates of Carboxymethyl Chitosan and Daunorubicin for the Delivery of Anti-Cancer Drugs.

作者信息

Cao Jun, Zheng Haoran, Hu Rui, Liao Jianhong, Fei Zengming, Wei Xuan, Xiong Xiong, Zhang Fanglin, Zheng Hua, Li Dan

出版信息

J Biomed Nanotechnol. 2017 Dec 1;13(12):1647-1659. doi: 10.1166/jbn.2017.2462.

DOI:10.1166/jbn.2017.2462
PMID:29490753
Abstract

The drug controlled release responding to tumour microenvironment is a hotspot for cancer therapy research. Herein, pH-sensitive shell-core nanoparticles (NPs) were devised and fabricated for tumour treatment. The detailed characterisations of their structures demonstrated the successful formation of the precursors and NPs. More importantly, the NPs show excellent features, i.e., negative surface potential, narrow size distribution, and suitable dimension for cell penetration. And they have superior stability in pH 7.4 buffer (i.e., blood environment). In addition, owing to the existence of the pH-labile imine bond, a controlled release of drugs from NPs was achieved in drug release test. Confocal laser scanning microscopy (CLSM) and flow cytometry proved the internalization of NPs into HeLa cells and their further translocation into cell nuclei. The cytotoxicity results also revealed a remarkable cytotoxicity of the NPs to HeLa cells. Thus, this type of NP may be potentially useful for the efficient drug delivery.

摘要

响应肿瘤微环境的药物控释是癌症治疗研究的热点。在此,设计并制备了用于肿瘤治疗的pH敏感核壳纳米颗粒(NPs)。对其结构的详细表征证明了前体和纳米颗粒的成功形成。更重要的是,纳米颗粒具有优异的特性,即表面负电位、窄尺寸分布和适合细胞穿透的尺寸。并且它们在pH 7.4缓冲液(即血液环境)中具有优异的稳定性。此外,由于存在对pH敏感的亚胺键,在药物释放试验中实现了药物从纳米颗粒中的控释。共聚焦激光扫描显微镜(CLSM)和流式细胞术证明了纳米颗粒被HeLa细胞内化并进一步转运到细胞核中。细胞毒性结果还显示纳米颗粒对HeLa细胞具有显著的细胞毒性。因此,这种类型的纳米颗粒可能对高效药物递送具有潜在的用途。

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