Radiochemical Studies Laboratory, Institute of Nuclear & Radiological Sciences & Technology, Energy & Safety (INRASTES), National Centre for Scientific Research (NCSR) "Demokritos", Athens 15341, Greece; Laboratory of Medicinal Chemistry, Section of Pharmaceutical Chemistry, Department of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis - Zografou, Athens 15771, Greece.
Radiochemical Studies Laboratory, Institute of Nuclear & Radiological Sciences & Technology, Energy & Safety (INRASTES), National Centre for Scientific Research (NCSR) "Demokritos", Athens 15341, Greece; Laboratory of Inorganic Chemistry, Section of Ιnorganic Chemistry - Inorganic Chemical Technology - Environmental Chemistry, Department of Chemistry, National and Kapodistrian University of Athens Panepistimiopolis - Zografou, Athens 15771, Greece.
Int J Pharm. 2022 Aug 25;624:122008. doi: 10.1016/j.ijpharm.2022.122008. Epub 2022 Jul 9.
Prostate cancer (PCa) is the most common malignancy worldwide in men. This is a proof-of-concept study describing the development of Ga-magnetic iron oxide nanoparticles (mNP) targeting prostate specific membrane antigen (PSMA) and gastrin releasing peptide (GRPR) receptors as potential tools for diagnosis of PCa with PET/MRI. Two pharmacophores targeting PSMA, 1, and GRPR, 2, were coupled to mNPs carrying -SH (mNP-S1/2) or -NH (mNP-N1/2) groups. The mNP-S1/2 and mNP-N1/2 were characterized for their size, zeta potential, structure, and efficiency of functionalization using dynamic light scattering (DLS), FT-IR and RP-HPLC. A direct Ga-labelling procedure was followed, where Ga-mNP-N1/2 proved superior to Ga-mNP-S1/2 regarding radiolabelling efficiency, and thus were further evaluated in vitro. Toxicity studies in PCa cells (LNCaP, PC-3) showed low toxicity, and minimal hemolysis of red blood cells. In vitro assays in cells expressing PSMA (LNCaP), and GRPR (PC-3), showed specific time-dependent binding (40 min to plateau), high avidity (PC-3: K = 28.27 nM, LNCaP: K = 11.49 nM) and high internalization rates for Ga-mNP-N1/2 in both cell lines.
前列腺癌 (PCa) 是全球男性最常见的恶性肿瘤。这是一项概念验证研究，描述了针对前列腺特异性膜抗原 (PSMA) 和胃泌素释放肽 (GRPR) 受体的 Ga-磁性氧化铁纳米颗粒 (mNP) 的开发，作为用于 PET/MRI 诊断 PCa 的潜在工具。两种针对 PSMA 的药效团 1 和 GRPR 的药效团 2 被偶联到带有 -SH (mNP-S1/2) 或 -NH (mNP-N1/2) 基团的 mNP 上。使用动态光散射 (DLS)、FT-IR 和 RP-HPLC 对 mNP-S1/2 和 mNP-N1/2 的大小、zeta 电位、结构和功能化效率进行了表征。随后进行了直接 Ga 标记程序，其中 Ga-mNP-N1/2 在放射性标记效率方面优于 Ga-mNP-S1/2，因此进一步进行了体外评估。在表达 PSMA (LNCaP) 和 GRPR (PC-3) 的 PCa 细胞中进行的毒性研究显示出低毒性和最小的红细胞溶血。在表达 PSMA (LNCaP) 和 GRPR (PC-3) 的细胞中的体外测定显示出特异性的时间依赖性结合 (40 分钟达到平台期)、高亲和力 (PC-3: K = 28.27 nM，LNCaP: K = 11.49 nM) 和 Ga-mNP-N1/2 在两种细胞系中的高内化率。
Eur J Nucl Med Mol Imaging. 2016-5
Int J Nanomedicine. 2024
Insights Imaging. 2024-2-27
Pharmaceuticals (Basel). 2023-2-17
Zotero 插件