Synthesis and In Vitro Evaluation of Gold Nanoparticles Functionalized with Thiol Ligands for Robust Radiolabeling with 99mTc

Radiolabeled gold nanoparticles (AuNPs) have been widely used for cancer diagnosis and therapy over recent decades. In this study, we focused on the development and in vitro evaluation of four new Au nanoconjugates radiolabeled with technetium-99m (99mTc) via thiol-bearing ligands attached to the NP...

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Published in:Nanomaterials (Basel, Switzerland) Switzerland), 2021-09, Vol.11 (9), p.2406
Main Authors: Apostolopoulou, Adamantia, Chiotellis, Aristeidis, Salvanou, Evangelia-Alexandra, Makrypidi, Konstantina, Tsoukalas, Charalampos, Kapiris, Fotis, Paravatou-Petsotas, Maria, Papadopoulos, Minas, Pirmettis, Ioannis C., Koźmiński, Przemysław, Bouziotis, Penelope
Format: Article
Language:English
Subjects:
99mTc-carbonyls
Biocompatibility
Cancer
Carbonyl compounds
Carbonyls
Cytotoxicity
Evaluation
Experiments
Gold
gold nanoparticles
hemolysis assay
Histidine
Iodine
Labeling
Ligands
Light scattering
Lipophilicity
Morphology
MTT
Nanoparticles
NMR
Nuclear magnetic resonance
Peptides
Photon correlation spectroscopy
Polyethylene glycol
Prostate cancer
Radiation therapy
Radiochemistry
radiolabeling
Radiolabelling
Solvents
Technetium
Technetium isotopes
Toxicity
Transmission electron microscopy
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cited_by cdi_FETCH-LOGICAL-c3006-6ac439a7515ae0e737a2a87720eeee9c03d11a279cf585b6869bbf9ec18380c83
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container_title Nanomaterials (Basel, Switzerland)
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creator Apostolopoulou, Adamantia
Chiotellis, Aristeidis
Salvanou, Evangelia-Alexandra
Makrypidi, Konstantina
Tsoukalas, Charalampos
Kapiris, Fotis
Paravatou-Petsotas, Maria
Papadopoulos, Minas
Pirmettis, Ioannis C.
Koźmiński, Przemysław
Bouziotis, Penelope
description Radiolabeled gold nanoparticles (AuNPs) have been widely used for cancer diagnosis and therapy over recent decades. In this study, we focused on the development and in vitro evaluation of four new Au nanoconjugates radiolabeled with technetium-99m (99mTc) via thiol-bearing ligands attached to the NP surface. More specifically, AuNPs of two different sizes (2 nm and 20 nm, referred to as Au(2) and Au(20), respectively) were functionalized with two bifunctional thiol ligands (referred to as L1H and L2H). The shape, size, and morphology of both bare and ligand-bearing AuNPs were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS) techniques. In vitro cytotoxicity was assessed in 4T1 murine mammary cancer cells. The AuNPs were successfully radiolabeled with 99mTc-carbonyls at high radiochemical purity (>95%) and showed excellent in vitro stability in competition studies with cysteine and histidine. Moreover, lipophilicity studies were performed in order to determine the lipophilicity of the radiolabeled conjugates, while a hemolysis assay was performed to investigate the biocompatibility of the bare and functionalized AuNPs. We have shown that the functionalized AuNPs developed in this study lead to stable radiolabeled nanoconstructs with the potential to be applied in multimodality imaging or for in vivo tracking of drug-carrying AuNPs.
doi_str_mv 10.3390/nano11092406
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subjects 99mTc-carbonyls
Biocompatibility
Cancer
Carbonyl compounds
Carbonyls
Cytotoxicity
Evaluation
Experiments
Gold
gold nanoparticles
hemolysis assay
Histidine
Iodine
Labeling
Ligands
Light scattering
Lipophilicity
Morphology
MTT
Nanoparticles
NMR
Nuclear magnetic resonance
Peptides
Photon correlation spectroscopy
Polyethylene glycol
Prostate cancer
Radiation therapy
Radiochemistry
radiolabeling
Radiolabelling
Solvents
Technetium
Technetium isotopes
Toxicity
Transmission electron microscopy
title Synthesis and In Vitro Evaluation of Gold Nanoparticles Functionalized with Thiol Ligands for Robust Radiolabeling with 99mTc
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