Yan Yining, Ding Lei, Liu Lin, Abualrejal Murad M A, Chen Hongda, Wang Zhenxin
Department of Radiology, China-Japan Union Hospital of Jilin University Xiantai Street Changchun 130033 P. R. China
State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences Changchun 130022 P. R. China
RSC Adv. 2020 Apr 6;10(23):13872-13878. doi: 10.1039/c9ra08974h. eCollection 2020 Apr 1.
Integration of high tumor-targeting capacity, controlling transport and low normal tissue retention into one engineered nanoparticle is a critical issue for future clinically translatable anti-cancer nanomedicines. Herein, hyaluronic acid functionalized 3.8 nm NaGdF nanodots (named NaGdF ND@HAs) have been prepared through conjugation of tryptone capped NaGdF nanodots (NaGdF ND@tryptone) with hyaluronic acid (HA, a naturally occurring glycosaminoglycan), which can recognize the overexpressed CD44 on cancer cell membranes. The as-prepared NaGdF ND@HAs have good paramagnetic properties (longitudinal relaxivity ( ) = 7.57 × 10 M S) and low cytotoxicity. The experimental results demonstrate that the NaGdF ND@HAs can not only efficiently accumulate in mouse-bearing MDA-MB-231 tumors ( 5.3% injection dosage (ID) g at 2 h post-injection), but also have an excellent renal clearance efficiency ( 75% injection dosage (ID) at 24 h post-injection). The as-prepared NaGdF ND@HAs have good paramagnetic properties with enhanced tumor-targeting capacity, which provides a useful strategy for the preparation of renal clearable magnetic resonance imaging (MRI) contrast agents for tumors.
将高肿瘤靶向能力、可控运输和低正常组织滞留性整合到一个工程化纳米颗粒中,是未来临床可转化抗癌纳米药物的关键问题。在此,通过将胰蛋白胨包覆的NaGdF纳米点(NaGdF ND@胰蛋白胨)与透明质酸(HA,一种天然存在的糖胺聚糖)共轭,制备了透明质酸功能化的3.8 nm NaGdF纳米点(命名为NaGdF ND@HAs),其可以识别癌细胞膜上过度表达的CD44。所制备的NaGdF ND@HAs具有良好的顺磁性质(纵向弛豫率( )= 7.57 × 10 M S)和低细胞毒性。实验结果表明,NaGdF ND@HAs不仅能在荷MDA-MB-231肿瘤小鼠中有效蓄积(注射后2小时为5.3%注射剂量(ID) g),而且具有优异的肾脏清除效率(注射后24小时为75%注射剂量(ID))。所制备的NaGdF ND@HAs具有良好的顺磁性质和增强的肿瘤靶向能力,为制备可肾脏清除的肿瘤磁共振成像(MRI)造影剂提供了一种有用的策略。