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Enhancing the antitumor effect of methotrexate in intro and in vivo by a novel targeted single-walled carbon nanohorn-based drug delivery system

机译:新型靶向单壁碳纳米药物递送系统,增强甲氨蝶呤和体内甲氨蝶呤的抗肿瘤作用

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The present research reports a smart multifunctional oxidized single-wall carbon nanohorns (oxSWNHs) drug delivery system (DDS) which could enhance the anti-tumor effect of methotrexate (MTX). In this DDS (MTX@oxSWNHs–PEG–Tf), oxSWNHs loaded MTX was wrapped with DSPE–PEG–NH _(2) to prolong blood circulation half-life and target tumors with the help of covalent grafting of transferrin (Tf). The obtained DDS was characterized by scanning electron microscopy, UV-vis spectrophotometry, size distribution analysis and Z -potential measurement. Cell uptake studies on MAD-MB-231 and HepG2 cell lines confirmed that the MTX@oxSWNHs–PEG–Tf exerted higher antitumor activity compared with free drug or non-targeted counterpart. The in vivo antitumor efficacy of MTX@oxSWNHs–PEG–Tf was much stronger than that of the free drug group by comparing the change of tumor volume and weight. Toxicity studies showed little perceivable cardiotoxicity, hepatotoxicity and pulmonary toxicity of MTX@oxSWNHs–PEG–Tf, indicating that this new tumor-targeting DDS significantly enhanced the anti-tumor effect of MTX and decreased its side effects.
机译:本研究报告了一种智能多功能氧化单壁碳纳米(OXSWNHS)药物递送系统(DDS),其可以增强甲氨蝶呤(MTX)的抗肿瘤作用。在该DDS(MTX @ Oxswnhs-PEG-TF)中,伴随着DSPE-PEG-NH _(2)包裹的OXSWNHS MTX以促进转铁蛋白(TF)的共价接枝延长血液循环半衰期和靶肿瘤。通过扫描电子显微镜,UV-Vis分光光度法,尺寸分布分析和Z-Zential测量来表征获得的DDS。对MAD-MB-231和HepG2细胞系的细胞吸收研究证实,与游离药物或非靶向对应相比,MTX @ Oxswnhs-PEG-TF施加了更高的抗肿瘤活性。通过比较肿瘤体积和重量的变化,MTX @ Oxswnhs-PEG-TF的体内抗肿瘤功效比游离药物的效果强。毒性研究表明,MTX @ Oxswnhs-PEG-TF的肝毒性和肺毒性很小,表明这种新的肿瘤靶向DDS显着提高了MTX的抗肿瘤作用并降低了其副作用。

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