Construction of ultrasmall gold nanoparticles based contrast agent via Host-Guest interaction for Tumor-targeted magnetic resonance imaging

• Published in: Materials & design 2022-05, Vol.217, p.110620, Article 110620
• Main Authors: Zhang, Yiwei, Li, Xinxin, Chen, Xing, Zhang, Yingfan, Deng, Yun, Yu, Yanhua, Wang, Bing, Xue, Yanan, Huang, Yulun, Liu, Min
• Format: Article
• Language: English
• Subjects: Contrast agent; Host–guest interaction; Magnetic resonance imaging; Tumor targeting; Ultrasmall gold nanoparticle
• ISSN: 0264-1275; 1873-4197
• DOI: 10.1016/j.matdes.2022.110620

[Display omitted] •To achieve the goal of precision diagnosis, ultrasmall AuNPs based contrast agent were fabricated through host–guest interaction for tumor-targeted magnetic resonance imaging.•β-cyclodextrin-modified ultrasmall gold nanoparticle (AuNP@CD) was prepared as a functional core, and then reacted with AD-PEG2000-PLL(Gd-DTPA) through host–guest interaction followed by conjugation of tumor targeting ligand.•AuNP@CD-AD-PEG2000-PLL(DTPA-Gd)-FA nanocomposite could effectively permeate through tumor and accumulate in the tumor region, thus acquiring MR images with high resolution. In order to overcome the shortcomings of small-molecule contrast agents (CAs) in clinic, gadolinium-based CAs have attracted increasingly interesting in tumor diagnosis. Herein, β-cyclodextrin-modified ultrasmall gold nanoparticle (AuNP@CD) was prepared as a functional core, which provided a large number of binding sites through host–guest interaction. Afterward, AD-PEG2000-PLL(Gd-DTPA) was anchored on the surface of AuNP@CD followed by the conjugation of folic acid through bioorthogonal chemistry, which endowed the AuNP with the capability to targeting tumor cells. Compared to Magnevist (Gd-DTPA, r1 = 4.25 mM−1 s−1) used in clinic, the AuNP nanocomposite exhibited higher longitudinal relaxivity (r1 = 19.47 mM−1 s−1), and presented excellent biocompatibility. Furthermore, in vivo studies indicated that AuNP@CD-AD-PEG2000-PLL (DTPA-Gd) nanocomposite could effectively permeate through tumor and accumulate in the tumor region, thus acquiring MR images with high resolution. These results suggest that this AuNP nanocomposite could be a potential candidate as MRI CA for tumor-targeted diagnosis.