Renal Clearable Peptide Functionalized NaGdF4 Nanodots for High-Efficiency Tracking Orthotopic Colorectal Tumor in Mouse

Renal Clearable Peptide Functionalized NaGdF4 Nanodots for High-Efficiency Tracking Orthotopic Colorectal Tumor in Mouse
复制标题

肾可清除肽功能化 NaGdF4 纳米点用于高效追踪小鼠原位结直肠肿瘤

DOI:
10.1021/acs.molpharmaceut.7b00361
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发表时间:
2017-09-01
影响因子:
4.9
通讯作者:
Wang, Zhenxin
Wang, Zhenxin
中科院分区:
医学2区
文献类型:
--
作者:
Chen, Hongda;Li, Xiaodong;Wang, Zhenxin

文献摘要

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将生物成像探针有效递送至选定的癌组织对于生物学研究和临床研究具有广泛的意义。在此,通过在疏水性NaGdF4纳米点(直径4.2 nm)与混合磷酸化肽配体(包括肿瘤靶向磷酸肽和细胞穿透磷酸肽)之间形成Gd-膦酸配位键,制备了肽功能化的NaGdF4纳米点(称为p肽-NaGdF4纳米点),用于肿瘤的高效磁共振成像(MRI)。肿瘤靶向pPeptide-NaGdF4纳米点具有顺磁性,具有超小的流体动力学直径(HD,约7.3 nm),大大提高了肿瘤的MRI造影能力,并有利于肾脏清除。具体而言,通过跟踪小鼠体内小型药物诱导的原位结直肠肿瘤(体积约 195 mm(3)),成功评估了 pPeptide-NaGdF4 纳米点作为体内 MRI 高效造影剂的能力。
The effective delivery of bioimaging probes to a selected cancerous tissue has extensive significance for biological studies and clinical investigations. Herein, the peptide functionalized NaGdF4 nanodots (termed as, pPeptide-NaGdF4 nanodots) have been prepared for highly efficient magnetic resonance imaging (MRI) of tumor by formation of Gd-phosphonate coordinate bonds among hydrophobic NaGdF4 nanodots (4.2 nm in diameter) with mixed phosphorylated peptide ligands including a tumor targeting phosphopeptide and a cell penetrating phosphopeptide. The tumor targeting pPeptide-NaGdF4 nanodots have paramagnetic property with ultrasmall hydrodynamic diameter (HD, c.a., 7.3 nm) which greatly improves their MRI contrast ability of tumor and facilitates renal clearance. In detail, the capability of the pPeptide-NaGdF4 nanodots as high efficient contrast agent for in vivo MRI is evaluated successfully through tracking small drug induced orthotopic colorectal tumor (c.a., 195 mm(3) in volume) in mouse.