Folic acid-modified diatrizoic acid-linked dendrimer-entrapped gold nanoparticles as nanoprobes for targeted CT imaging of human cervical cancer

Objective(s): The development of multifunctional nanoprobes for specific targeting and imaging of tumors presents a great challenge. Herein, we report the synthesis and characterization of folic acid (FA) gold nanoparticles (AuNPs) through diatrozic acid (DTA) linking for in vitro and in vivo targeted imaging of HeLa cells by computed tomography (CT). Materials and Methods: In this study, G5 dendrimers were used as templates to synthesize AuNPs within the dendrimer interiors. The cytotoxicity and hemocompatibility of the particles were evaluated by morphological observation of cells after hematoxylin and eosin staining, cell viability assay, flow cytometric analysis of cell cycle and apoptosis, and hemolytic assay. The cellular uptake of the particles was confirmed through inductively coupled plasma atomic emission spectroscopy determination of silver and transmission electron microscopy. Finally, in vitro and in vivo targeted CT imaging performances were evaluated using HeLa cells and a xenografted HeLa tumor model, respectively. Results: We showed that Au DENPs-FA-DTA did not significantly affect cell morphology, viability, or the cell cycle and apoptosis, thereby indicating their good biocompatibility and stability in the given concentration range. Micro-CT images showed that HeLa cells could be detected by X-ray after incubation with Au DENPs-FA-DTA in vitro and that the xenograft tumor model could be imaged after intravenous and intratumoral administration of the particles. The FAmodified AuNPs enabled targeted CT imaging of HeLa cells overexpressing FA receptors in vitro and the corresponding xenografted tumor model in vivo. Conclusion: Our results demonstrated that the designed AuNPs show great potential as probes for targeted CT imaging of human cervical cancer.