单肿瘤靶向和多肿瘤靶向配体包被的超小氧化钆纳米颗粒：增强肿瘤成像和血液循环

Mono and Multiple Tumor-Targeting Ligand-Coated Ultrasmall Gadolinium Oxide Nanoparticles: Enhanced Tumor Imaging and Blood Circulation.

作者信息

Ho Son Long, Yue Huan, Lee Sangyeol, Tegafaw Tirusew, Ahmad Mohammad Yaseen, Liu Shuwen, Saidi Abdullah Khamis Ali Al, Zhao Dejun, Liu Ying, Nam Sung-Wook, Chae Kwon Seok, Chang Yongmin, Lee Gang Ho

机构信息

Department of Chemistry, College of Natural Sciences, Kyungpook National University, Taegu 41566, Korea.

Department of Medical & Biological Engineering, Kyungpook National University, Taegu 41944, Korea.

出版信息

Pharmaceutics. 2022 Jul 12;14(7):1458. doi: 10.3390/pharmaceutics14071458.

Hydrophilic and biocompatible PAA-coated ultrasmall GdO nanoparticles (d = 1.7 nm) were synthesized and conjugated with tumor-targeting ligands, i.e., cyclic arginylglycylaspartic acid (cRGD) and/or folic acid (FA). FA-PAA-GdO and cRGD/FA-PAA-GdO nanoparticles were successfully applied in U87MG tumor-bearing mice for tumor imaging using T magnetic resonance imaging (MRI). cRGD/FA-PAA-GdO nanoparticles with multiple tumor-targeting ligands exhibited higher contrasts at the tumor site than FA-PAA-GdO nanoparticles with mono tumor-targeting ligands. In addition, the cRGD/FA-PAA-GdO nanoparticles exhibited higher contrasts in all organs, especially the aorta, compared with those of the FA-PAA-GdO nanoparticles, because of the blood cell hitchhiking effect of cRGD in the cRGD/FA-PAA-GdO nanoparticles, which prolonged their circulation in the blood.

合成了具有亲水性和生物相容性的聚丙烯酸（PAA）包覆的超小氧化钆纳米颗粒（直径 = 1.7 纳米），并将其与肿瘤靶向配体，即环精氨酰甘氨酰天冬氨酸（cRGD）和/或叶酸（FA）偶联。FA-PAA-GdO 和 cRGD/FA-PAA-GdO 纳米颗粒成功应用于荷 U87MG 肿瘤小鼠，用于采用 T 磁共振成像（MRI）进行肿瘤成像。具有多种肿瘤靶向配体的 cRGD/FA-PAA-GdO 纳米颗粒在肿瘤部位比具有单一肿瘤靶向配体的 FA-PAA-GdO 纳米颗粒表现出更高的对比度。此外，与 FA-PAA-GdO 纳米颗粒相比，cRGD/FA-PAA-GdO 纳米颗粒在所有器官中，尤其是主动脉中，表现出更高的对比度，这是因为 cRGD/FA-PAA-GdO 纳米颗粒中的 cRGD 具有血细胞搭便车效应，延长了它们在血液中的循环时间。