Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China; Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, Stanford, CA, USA.
Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, Stanford, CA, USA; Department of Pharmaceutics, School of Pharmacy, Nanjing Medical University, Nanjing, China.
Nanomedicine. 2020 Oct;29:102248. doi: 10.1016/j.nano.2020.102248. Epub 2020 Jun 20.
Melanin is a group of natural pigments found in living organism. It can be used for positron emission tomography (PET) imaging due to its inherent chelating ability to radioactive cupric ion. This study was to prepare Cu-labeled PEGylated melanin nanoparticles (Cu-PEG-MNPs), and to further take advantage of the enhanced permeability and retention (EPR) effect of radiolabeled nanoparticles to realize the integration of tumor diagnosis and treatment. We successfully synthesized PEG-MNPs. Saline and serum stability experiments demonstrated good stability. PET/CT showed high tumor aggregation. Moreover, Cu-PEG-MNPs resulted in a therapeutic effect on the A431 tumor-bearing mice in the treatment group. The pathological results further confirmed that the therapeutic doses of Cu-PEG-MNPs cause pathological changes of tumor tissues while showing minimal toxicity to normal tissues. Our data successfully demonstrate the good imaging performance of Cu-PEG-MNPs on A431 tumors and further proved its therapeutic effect, highlighting a great potential in targeted radionuclide therapy.
黑色素是存在于生物体中的一类天然色素。由于其对放射性铜离子的固有螯合能力，它可用于正电子发射断层扫描（PET）成像。本研究旨在制备 Cu 标记的聚乙二醇化黑色素纳米颗粒（Cu-PEG-MNPs），并进一步利用放射性标记纳米颗粒的增强渗透和保留（EPR）效应，实现肿瘤诊断和治疗的一体化。我们成功合成了 PEG-MNPs。盐水和血清稳定性实验表明其具有良好的稳定性。PET/CT 显示出高肿瘤聚集性。此外，在治疗组中，Cu-PEG-MNPs 对 A431 荷瘤小鼠产生了治疗效果。病理结果进一步证实，治疗剂量的 Cu-PEG-MNPs 导致肿瘤组织的病理性变化，同时对正常组织的毒性最小。我们的数据成功地证明了 Cu-PEG-MNPs 对 A431 肿瘤的良好成像性能，并进一步证实了其治疗效果，突出了其在靶向放射性核素治疗中的巨大潜力。
