首页> 外文期刊>Journal of Applied Polymer Science >Gadolinium-conjugated FA-PEG-PAMAM-COOH nanoparticles as potential tumor-targeted circulation-prolonged macromolecular MRI contrast agents
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Gadolinium-conjugated FA-PEG-PAMAM-COOH nanoparticles as potential tumor-targeted circulation-prolonged macromolecular MRI contrast agents

机译:d缀合的FA-PEG-PAMAM-COOH纳米颗粒作为潜在的靶向肿瘤的循环延长的大分子MRI造影剂

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The aim of research is to develop potential tumor-targeted circulation-prolonged macromolecular magnetic resonance imaging (MRI) contrast agents without the use of low molecular gadolinium (Gd) ligands. The contrast agents were based on polymer-metal complex nanoparticles with controllable particle size to achieve the active and passive tumor-targeted potential. In particular, poly (amidoamine) (PAMAM) dendrimer with 32 carboxylic groups was modified with folate-conjugated poly (ethyleneglycol) amine (FA-PEG-NH _2, M_w: 2 k and 4 kDa). FA-PEG-PAMAM-Gd macromolecular MRI contrast agents were prepared by the complex reaction between the carboxylic groups in PAMAM and GdCl_3. The structure of FA-PEG-PAMAM-COOH was confirmed by nuclear magnetic resonance (~1H-NMR), Fourier transform infrared (FTIR) spectra, and electrospray ionization mass spectra (ESI-MS). The mass percentage content of Gd (III) in FA-PEG-PAMAM-Gd was measured by inductively coupled plasma-atomic emission spectrometer (ICP-AES). The sizes of these nanoparticles were about 70 nm measured by transmission electron microscopy, suggestion of their passive targeting potential to tumor tissue. In comparison with clinically available small molecular Gadopentetate dimeglumine, FA-PEG-PAMAM-Gd showed comparable cytotoxicity and higher relaxation rate, suggestion of their great potential as tumor-targeted nanosized macromolecular MRI contrast agents due to the overexpressed FA receptor in human tumor cell surfaces.
机译:研究的目的是在不使用低分子g(Gd)配体的情况下开发潜在的靶向肿瘤的循环延长的大分子磁共振成像(MRI)造影剂。造影剂基于具有可控制粒度的聚合物-金属复合纳米颗粒,以实现主动和被动靶向肿瘤的潜力。特别地,用叶酸偶联的聚(乙二醇)胺(FA-PEG-NH _2,M_w:2k和4kDa)修饰具有32个羧基的聚(酰胺基胺)(PAMAM)树状聚合物。 FA-PEG-PAMAM-Gd大分子MRI造影剂是通过PAMAM中的羧基与GdCl_3的复杂反应制备的。 FA-PEG-PAMAM-COOH的结构已通过核磁共振(〜1H-NMR),傅立叶变换红外(FTIR)光谱和电喷雾电离质谱(ESI-MS)确认。通过电感耦合等离子体原子发射光谱仪(ICP-AES)测量FA-PEG-PAMAM-Gd中Gd(III)的质量百分比含量。这些纳米颗粒的尺寸通过透射电子显微镜测量为约70nm,表明它们对肿瘤组织的被动靶向潜力。与临床可用的小分子ado戊二酸二聚丁二胺相比,FA-PEG-PAMAM-Gd显示出可比的细胞毒性和更高的弛豫率,表明它们在人肿瘤细胞表面中过表达的FA受体具有作为靶向肿瘤的纳米大分子MRI造影剂的巨大潜力。 。

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