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Melanocortin 1 Receptor Targeted Imaging of Melanoma With Gold Nanocages and Positron Emission Tomography.
Molecular Imaging ( IF 2.8 ) Pub Date : 2018-06-07 , DOI: 10.1177/1536012118775827
Yongfeng Zhao 1, 2 , Bo Pang 3 , Lisa Detering 1 , Hannah Luehmann 1 , Miaoxin Yang 3 , Kvar Black 1 , Deborah Sultan 1 , Younan Xia 3 , Yongjian Liu 1
Affiliation  

PURPOSE Melanoma is a lethal skin cancer with unmet clinical needs for targeted imaging and therapy. Nanoscale materials conjugated with targeting components have shown great potential to improve tumor delivery efficiency while minimizing undesirable side effects in vivo. Herein, we proposed to develop targeted nanoparticles for melanoma theranostics. METHOD In this work, gold nanocages (AuNCs) were conjugated with α-melanocyte-stimulating hormone (α-MSH) peptide and radiolabeled with 64Cu for melanocortin 1 receptor-(MC1R) targeted positron emission tomography (PET) in a mouse B16/F10 melanoma model. RESULTS Their controlled synthesis and surface chemistry enabled well-defined structure and radiolabeling efficiency. In vivo pharmacokinetic evaluation demonstrated comparable organ distribution between the targeted and nontargeted AuNCs. However, micro-PET/computed tomography (CT) imaging demonstrated specific and improved tumor accumulation via MC1R-mediated delivery. By increasing the coverage density of α-MSH peptide on AuNCs, the tumor delivery efficiency was improved. CONCLUSION The controlled synthesis, sensitive PET imaging, and optimal tumor targeting suggested the potential of targeted AuNCs for melanoma theranostics.

中文翻译:

用金纳米笼和正电子发射断层扫描术对黑素瘤进行黑皮质素1受体靶向成像。

目的黑色素瘤是一种致死性皮肤癌,对靶向成像和治疗的临床需求尚未得到满足。与靶向成分缀合的纳米级材料已显示出巨大的潜力,可提高肿瘤的递送效率,同时将体内不良副作用降至最低。在本文中,我们建议开发用于黑色素瘤治疗学的靶向纳米颗粒。方法在这项工作中,金纳米笼(AuNCs)与α-黑素细胞刺激激素(α-MSH)肽缀合,并用64Cu放射性标记以对小鼠B16 / F10的黑素皮质素1受体(MC1R)靶向正电子发射断层扫描(PET)黑色素瘤模型。结果他们受控的合成和表面化学作用使结构明确,放射性标记效率高。体内药代动力学评估表明,靶向和非靶向AuNC之间的器官分布相当。然而,微型PET /计算机断层扫描(CT)成像通过MC1R介导的递送显示了特异性且改善的肿瘤蓄积。通过增加α-MSH肽在AuNCs上的覆盖密度,可以提高肿瘤的递送效率。结论受控的合成,灵敏的PET显像和最佳的肿瘤靶向表明靶向的AuNCs具有治疗黑色素瘤治疗的潜力。
更新日期:2019-11-01
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