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

Apostolopoulou, Adamantia; Chiotellis, Aristeidis; Salvanou, Evangelia-Alexandra; Makrypidi, Konstantina; Tsoukalas, Charalambos; Kapiris, Fotis; Paravatou-Petsotas, Maria; Papadopoulos, Minas; Pirmettis, Ioannis; Koźmiński, Przemysław; Bouziotis, Penelope

doi:10.3390/nano11092406

Cited by 5 publications

(7 citation statements)

References 44 publications

(91 reference statements)

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“…It is of major importance that nanoparticles aiming to serve as theranostic agents have minimal interactions with blood components so as not to compromise their systemic administration. To this end, nanosystems such as iron oxide or gold nanoparticles must prove their biocompatibility before being intravenously injected into a living organism [ 61 , 62 ]. In our case, all samples exhibited minimal hemoglobin release from the RBCs, indicating negligible hemolysis according to the <10% acceptance limit for biopharmaceuticals [ 63 ].…”

Section: Resultsmentioning

confidence: 99%

Preliminary Evaluation of Iron Oxide Nanoparticles Radiolabeled with 68Ga and 177Lu as Potential Theranostic Agents

et al. 2022

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Theranostic radioisotope pairs such as Gallium-68 (68Ga) for Positron Emission Tomography (PET) and Lutetium-177 (177Lu) for radioisotopic therapy, in conjunction with nanoparticles (NPs), are an emerging field in the treatment of cancer. The present work aims to demonstrate the ability of condensed colloidal nanocrystal clusters (co-CNCs) comprised of iron oxide nanoparticles, coated with alginic acid (MA) and stabilized by a layer of polyethylene glycol (MAPEG) to be directly radiolabeled with 68Ga and its therapeutic analog 177Lu. 68Ga/177Lu- MA and MAPEG were investigated for their in vitro stability. The biocompatibility of the non-radiolabeled nanoparticles, as well as the cytotoxicity of MA, MAPEG, and [177Lu]Lu-MAPEG were assessed on 4T1 cells. Finally, the ex vivo biodistribution of the 68Ga-labeled NPs as well as [177Lu]Lu-MAPEG was investigated in normal mice. Radiolabeling with both radioisotopes took place via a simple and direct labelling method without further purification. Hemocompatibility was verified for both NPs, while MTT studies demonstrated the non-cytotoxic profile of the nanocarriers and the dose-dependent toxicity for [177Lu]Lu-MAPEG. The radiolabeled nanoparticles mainly accumulated in RES organs. Based on our preliminary results, we conclude that MAPEG could be further investigated as a theranostic agent for PET diagnosis and therapy of cancer.

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Section: Resultsmentioning

confidence: 99%

Preliminary Evaluation of Iron Oxide Nanoparticles Radiolabeled with 68Ga and 177Lu as Potential Theranostic Agents

et al. 2022

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“…Radioactive metals such as 99m Tc ( T 1/2 = 6 h, E y = 140 keV) and 188 Re ( T 1/2 = 17 h, E y = 2.12 MeV, penetration distance = 3.8 mm) are widely used in clinical practice for diagnostic and therapeutic purposes. , 99m Tc is a diagnostic γ emitter and can be detected by SPECT-CT, while 188 Re is a therapeutic β emitter and has great therapeutic potential for internal radiotherapy. According to previous works, − SnCl 2 is generally used as a reducing agent for the radiolabeling of NPs and is usually added to [ 99m Tc]TcO 4 – or [ 188 Re]ReO 4 – solutions. The radiolabeling protocol of the developed NPs was optimized for 188 Re.…”

Section: Resultsmentioning

confidence: 99%

Universal Chelator-Free Radiolabeling of Organic and Inorganic-Based Nanocarriers with Diagnostic and Therapeutic Isotopes for Internal Radiotherapy

et al. 2022

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Biomedical application of various nanoparticles (NPs) for bioimaging and therapeutic purposes attracts huge interest. In particular, NPs can be used as nanocarriers of radionuclides for radiotherapy of malignant neoplasms. However, most approaches for NP radiolabeling are complicated, and their transfer into clinical practice is difficult due to their multistep process, limited reproducibility, and lack of an automated radiolabeling procedure. Here, we develop a universal method suitable for radiolabeling of various NPs (either organic or inorganic) for internal radiotherapy of B16-F10 melanoma tumors. The obtained NPs (polylactide, silica, gold, and iron oxide) were labeled with diagnostic ( 99m Tc) and therapeutic ( 188 Re) radionuclides with a high radiolabeling efficiency (∼94− 98%) and radiochemical stability (>95%). After their intratumoral administration, these various 188 Re-labeled NPs mostly remained in the tumor, inhibiting the tumor growth rate compared to the untreated tumors. The absence of any significant leakage of the radiolabeled NPs in healthy tissues (the liver, heart, kidneys, lungs, and spleen) was confirmed by single-photon emission computed tomography (SPECT) and direct radiometry analysis. Histological analysis revealed no abnormal changes in healthy organs after the therapy (e.g., no acute pathologic findings were detected in the liver and kidneys). As a result, the treatment of mice with 188 Relabeled NPs led to a prolonged survival compared to the control group. Thus, our study provides general guidance for the use of different types of radiolabeled NPs in radionuclide therapy.

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“…Τhe synthesis and characterization of the AuNPs and the thiol ligand (Figure 1) have been previously described [23]. Both samples were prepared according to the same procedure, during which 500, 500 × 10 −1 , 500 × 10 −2 and 500 × 10 −3 µg of AuNPs were each mixed with 0.29 mg of the ligand previously dissolved in DMSO and allowed to stay overnight on a magnetic stirrer.…”

Section: Functionalization Of Gold Nanoparticles With a Thiol Trident...mentioning

confidence: 99%

“…Cytotoxicity studies were performed following a previously reported procedure using the 4T1 cancer cell line [23]. Cell viability of bare AuNPs and ligand-functionalized AuNPs was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay.…”

Section: Cell Viability By Mtt Assaymentioning

confidence: 99%

“…The radiolabeling procedure was simple and straightforward. The labeling precursor [ 99m Tc][Tc(H 2 O) 3 (CO) 3 ] + was prepared as described in the literature [23]. After functionalization of AuNPs with the ligand, all samples of AuNPs were incubated with 100 µL of 99m Tc-tricarbonyl core-[ 99m Tc][Tc(H 2 O) 3 (CO) 3 ] + (30-80 MBq) at 70 • C for 2 h. Radiochemical yield and purity were determined by HPLC.…”

Section: Radiolabeling With [ 99m Tc][tc(h 2 O) 3 (Co) 3 ] +mentioning

confidence: 99%

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How Does the Concentration of Technetium-99m Radiolabeled Gold Nanoparticles Affect Their In Vivo Biodistribution?

Apostolopoulou,

Salvanou,

Chiotellis

et al. 2024

Applied Sciences

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Gold nanoparticles (AuNPs) radiolabeled with therapeutic and diagnostic radioisotopes have been broadly studied as a promising platform for early diagnosis and treatment of many diseases including cancer. Our main goal for this study was the comparison of the biodistribution profiles of four different concentrations of gold nanoconjugates radiolabeled with Technetium-99m (99mTc). More specifically, AuNPs with an average diameter of 2 nm were functionalized with a tridentate thiol ligand. Four different concentrations were radiolabeled with 99mTc-tricarbonyls with high radiolabeling yields (>85%) and were further purified, leading to radiochemical purity of >95%. In vitro stability of the radiolabeled nanoconstructs was examined in cysteine and histidine solutions as well as in human serum, exhibiting robust radiolabeling up to 24 h post-preparation. Moreover, in vitro cytotoxicity studies were carried out in 4T1 murine mammary cancer cells. In vivo tracking of the radiolabeled nanoconjugates at both concentrations was examined in normal mice in order to examine the effect of AuNPs’ concentration on their in vivo kinetics. Our work demonstrates that varying concentrations of radiolabeled AuNPs lead to notably different biodistribution profiles.

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

Cited by 5 publications

References 44 publications

Preliminary Evaluation of Iron Oxide Nanoparticles Radiolabeled with 68Ga and 177Lu as Potential Theranostic Agents

Preliminary Evaluation of Iron Oxide Nanoparticles Radiolabeled with 68Ga and 177Lu as Potential Theranostic Agents

Universal Chelator-Free Radiolabeling of Organic and Inorganic-Based Nanocarriers with Diagnostic and Therapeutic Isotopes for Internal Radiotherapy

How Does the Concentration of Technetium-99m Radiolabeled Gold Nanoparticles Affect Their In Vivo Biodistribution?

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