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Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy.

Yang Liu1, Zhengyuan Zhou2, Yutian Feng2

  • 1Department of Biomedical Engineering, Duke University, Durham, NC, 27708, USA.

International Journal of Nanomedicine
|November 5, 2021
PubMed
Summary

Gold nanostars (GNS) were developed for targeted alpha-particle therapy (TAT). This innovative 211At nanoplatform demonstrates high radiolabeling efficiency and excellent in vivo stability for potential cancer treatment.

Keywords:
211AtGNSTATastatine-211cancer therapygold nanostarstargeted alpha-particle therapy

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Area of Science:

  • Nanotechnology
  • Radiochemistry
  • Oncology

Background:

  • Targeted alpha-particle therapy (TAT) offers a promising approach for cancer treatment due to the high cytotoxicity of alpha emitters.
  • Developing stable radiolabeled nanoplatforms is crucial for effective TAT delivery and minimizing off-target effects.

Purpose of the Study:

  • To create an innovative 211At nanoplatform with high radiolabeling efficiency and reduced in vivo de-radonization.
  • To assess the potential of this platform for future targeted alpha-particle therapy (TAT) in cancer treatment.

Main Methods:

  • Gold nanostars (GNS) were utilized as the nanoplatform for 211At radiolabeling.
  • Radiolabeling efficiency was optimized under various conditions.
  • In vivo stability was evaluated by measuring thyroid and stomach uptake post-administration.
  • Preliminary therapeutic efficacy was assessed in a U87MG human glioma xenograft murine model.

Main Results:

  • Near 100% radiolabeling efficiency of GNS with 211At was achieved rapidly (1 minute).
  • In vitro stability in serum exceeded 99% 211At retention on GNS after 24 hours.
  • In vivo studies showed minimal thyroid and stomach uptake, indicating excellent stability.
  • Intratumoral administration of 211At-labeled GNS significantly reduced tumor growth in a murine model.

Conclusions:

  • The 211At radiolabeling strategy using GNS is simple, efficient, and exhibits minimal in vivo dissociation.
  • This GNS-based platform is a promising candidate for developing TAT agents.
  • Further preclinical evaluation is warranted for potential clinical translation.