Aggregation‐Induced Emission Gold Clustoluminogens for Enhanced Low‐Dose X‐ray‐Induced Photodynamic Therapy

Abstract

The use of gold nanoparticles as radiosensitizers is an effective way to boost the killing efficacy of radiotherapy while drastically limiting the received dose and reducing the possible damage to normal tissues. Herein, we designed aggregation‐induced emission gold clustoluminogens (AIE‐Au) to achieve efficient low‐dose X‐ray‐induced photodynamic therapy (X‐PDT) with negligible side effects. The aggregates of glutathione‐protected gold clusters (GCs) assembled through a cationic polymer enhanced the X‐ray‐excited luminescence by 5.2‐fold. Under low‐dose X‐ray irradiation, AIE‐Au strongly absorbed X‐rays and efficiently generated hydroxyl radicals, which enhanced the radiotherapy effect. Additionally, X‐ray‐induced luminescence excited the conjugated photosensitizers, resulting in a PDT effect. The in vitro and in vivo experiments demonstrated that AIE‐Au effectively triggered the generation of reactive oxygen species with an order‐of‐magnitude reduction in the X‐ray dose, enabling highly effective cancer treatment.

Molecular Engineering of Aptamer Self-Assemblies Increases in Vivo Stability and Targeted Recognition

“…34 GNCs possess good water solubility, biocompatibility, and fluorescence properties, as well as molecular-like properties. 33,36 In addition, they can be excreted from the body in various ways with only negligible toxicity. 33,35 In this study, we report a covalent modification-free strategy to construct stable aptamer assemblies using GNCs (Scheme 1).…”

“…Recently, gold nanomaterials have attracted much attention because of adjustable size and easy surface functional modification. − Gold nanoclusters (GNCs), in particular, are a type of gold NPs synthesized with a particle size of about 2 nm . GNCs possess good water solubility, biocompatibility, and fluorescence properties, as well as molecular-like properties. , In addition, they can be excreted from the body in various ways with only negligible toxicity. , …”

Size-Controllable Nanosystem with Double Responsive for Deep Photodynamic Therapy

“…In order to address the issue of light penetration, many near-infrared (NIR) light excitation strategies [ 11 , 12 , 13 ] for deep-tissue PDT have been proposed, especially upconversion luminescence [ 14 , 15 ]. Different from traditional energy down-conversion based fluorescence luminescence [ 16 ], upconversion luminescence is a process capable of converting two or more low-energy photons that have been absorbed into the emission of photons with a relatively high energy [ 17 ], which dramatically reduces the autofluorescence background and improves tissue penetration as well as diminishes phototoxicity [ 18 ].…”

Endowing AIE with Extraordinary Potential: A New Au(I)‐Containing AIEgen for Bimodal Bioimaging‐Guided Multimodal Synergistic Cancer Therapy

“…In this regard, it has been well documented that gold‐based compounds or nanoparticles not only can serve as high‐efficiency emitters, photodynamic therapy, drug delivery, Raman and photothermal imaging in vitro, but also can be applied in CT imaging in vivo and radiotherapy due to the excellent X‐ray attenuation ability of gold with a high atomic number. [ 21–27 ] Inspired by these inherent superiority and the versatile functions of gold, we envisioned that whether gold could be introduced into AIEgen to accomplish the construction of desired small‐molecule AIEgens mentioned above. If this approach works, the CT imaging based on gold in such a distinctive system can substantially make up for the deficiency of AIEgen in FL imaging.…”