Ultrasmall Gold Nanoparticles Radiolabeled with Iodine-125 as Potential New Radiopharmaceutical

Area of Science:

• Radiochemistry
• Nanomedicine
• Nuclear Medicine

Background:

• Auger emitters offer potent cancer cell killing due to high linear energy transfer and clustered DNA damage.
• Theranostic applications are possible due to co-emitted gamma or positron radiation.
• Limited development of Auger emitter radiopharmaceuticals stems from the short range of Auger electrons, necessitating precise cellular delivery.

Purpose of the Study:

• To develop a novel radiopharmaceutical using an Auger emitter and ultrasmall gold nanoparticles.
• To investigate the nuclear accumulation and therapeutic efficacy of the developed radiopharmaceutical.
• To assess the potential of ultrasmall nanoparticles for targeted radionuclide therapy.

Main Methods:

• Combination of the Auger emitter 125I with ultrasmall gold nanoparticles.
• Evaluation of nanoparticle accumulation in cell nuclei.
• Assessment of tumor-killing efficiency in 2D and 3D cell models.

Main Results:

• The 125I-labeled gold nanoparticles demonstrated accumulation within the cell nucleus.
• High tumor-killing efficiency was observed in both 2D and 3D tumor cell models.
• Ultrasmall nanoparticles showed passive accumulation in the cell nucleus.

Conclusions:

• Ultrasmall nanoparticles accumulating in the cell nucleus show potential for targeted radionuclide therapy.
• The developed 125I-labeled gold nanoparticles exhibit significant tumor-killing capabilities.
• Conjugation of tumor-targeting moieties could further enhance therapeutic efficiency.