Integrin αvβ3-Targeted [ 64 Cu]CuS Nanoparticles for PET/CT Imaging and Photothermal Ablation Therapy

Lili Cui, Chiyi Xiong, Min Zhou, Sixiang Shi, Diana S.L. Chow, Chun Li

Research output: Journal article publicationJournal articleAcademic researchpeer-review

27 Citations (Scopus)


Copper sulfide (CuS) nanoparticles have been considered one of the most clinical relevant nanosystems because of their straightforward chemistry, small particle size, low toxicity, and intrinsic theranostic characteristics. In our previous studies, radioactive [ 64 Cu]CuS nanoparticles were successfully developed to be used as efficient radiotracers for positron emission tomography and for photothermal ablation therapy of cancer cells using near-infrared laser irradiation. However, the major challenge of CuS nanoparticles as a theranostic platform is the lack of a means for effective targeted delivery to the tumor site. To overcome this challenge, we designed and synthesized angiogenesis-targeting [ 64 Cu]CuS nanoparticles, which are coupled with cyclic RGDfK peptide [c(RGDfK)] through polyethylene glycol (PEG) linkers using click chemistry. In assessing their tumor-targeting efficacy, we found that the tumor uptakes of [ 64 Cu]CuS-PEG-c(RGDfK) nanoparticles at 24 h after intravenous injection were significantly greater (8.6% ± 1.4% injected dose/gram of tissue) than those of nontargeted [ 64 Cu]CuS-PEG nanoparticles (4.3% ± 1.2% injected dose/gram of tissue, p < 0.05). Irradiation of tumors in mice administered [ 64 Cu]CuS-PEG-c(RGDfK) nanoparticles induced 98.7% necrotic areas. In contrast, irradiation of tumors in mice administered nontargeted CuS-PEG nanoparticles induced 59% necrotic areas (p < 0.05). The angiogenesis-targeting [ 64 Cu]CuS nanoparticles may serve as a promising platform for image-guided ablation therapy with high efficacy and minimal side effects in future clinical translation of this novel class of multifunctional nanomaterials.

Original languageEnglish
Pages (from-to)4062-4071
Number of pages10
JournalBioconjugate Chemistry
Issue number12
Early online date15 Nov 2018
Publication statusPublished - 19 Dec 2018
Externally publishedYes

ASJC Scopus subject areas

  • Biotechnology
  • Bioengineering
  • Biomedical Engineering
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry


Dive into the research topics of 'Integrin αvβ3-Targeted [ 64 Cu]CuS Nanoparticles for PET/CT Imaging and Photothermal Ablation Therapy'. Together they form a unique fingerprint.

Cite this