A simple neridronate-based surface coating strategy for upconversion nanoparticles: highly colloidally stable¹²⁵I-radiolabeled NaYF₄:Yb³⁺/Er³⁺@PEG nanoparticles for multimodal<i>in vivo</i>tissue imaging

Abstract

In this report, monodisperse upconversion NaYF₄:Yb³⁺/Er³⁺ nanoparticles with superior optical properties were synthesized by the oleic acid-stabilized high-temperature co-precipitation of lanthanide chlorides in octadec-1-ene as a high-boiling organic solvent. To render the particles with biocompatibility and colloidal stability in bioanalytically relevant phosphate buffered saline (PBS), they were modified by using in-house synthesized poly(ethylene glycol)-neridronate (PEG-Ner), a bisphosponate. The NaYF₄:Yb³⁺/Er³⁺@PEG nanoparticles showed excellent long-term stability in PBS and/or albumin without any aggregation or morphology transformation. The in vitro cytotoxicity of the nanoparticles was evaluated using primary fibroblasts (HF) and a cell line derived from human cervical carcinoma (HeLa). The particles were subsequently modified by using Bolton-Hunter-hydroxybisphosphonate to enable radiolabeling with ¹²⁵I for single-photon emission computed tomography/computed tomography (SPECT/CT) bimodal imaging to monitor the biodistribution of the nanoparticles in non-tumor mice. The bimodal upconversion ¹²⁵I-radiolabeled NaYF₄:Yb³⁺/Er³⁺@PEG nanoparticles are prospective for near-infrared (NIR) photothermal/photodynamic and SPECT/CT cancer theranostics.