Facile preparation of radium-doped, functionalized nanoparticles as carriers for targeted alpha therapy

2019 ◽  
Vol 6 (6) ◽  
pp. 1341-1349 ◽  
Author(s):  
Falco Reissig ◽  
René Hübner ◽  
Jörg Steinbach ◽  
Hans-Jürgen Pietzsch ◽  
Constantin Mamat
Keyword(s):  
Functional Groups ◽  
Functionalized Nanoparticles ◽  
Targeted Alpha Therapy ◽  
Therapeutic Applications ◽  
Facile Preparation ◽  
Enhanced Properties ◽  
Co Precipitation ◽  
Alpha Therapy

A facile preparation of nanoparticles with enhanced properties obtained by co-precipitation containing radium-224 and functional groups to connect target (bio)molecules for therapeutic applications in oncology is described.

scholarly journals Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 906
Author(s):  
Romain Eychenne ◽  
Michel Chérel ◽  
Férid Haddad ◽  
François Guérard ◽  
Jean-François Gestin
Keyword(s):  
Production Process ◽  
Clinical Studies ◽  
Physical Characteristics ◽  
Preclinical Studies ◽  
Chemical Behavior ◽  
Targeted Alpha Therapy ◽  
Therapeutic Applications ◽  
Radium 223 ◽  
Chemical Design ◽  
Alpha Therapy

Among all existing radionuclides, only a few are of interest for therapeutic applications and more specifically for targeted alpha therapy (TAT). From this selection, actinium-225, astatine-211, bismuth-212, bismuth-213, lead-212, radium-223, terbium-149 and thorium-227 are considered as the most suitable. Despite common general features, they all have their own physical characteristics that make them singular and so promising for TAT. These radionuclides were largely studied over the last two decades, leading to a better knowledge of their production process and chemical behavior, allowing for an increasing number of biological evaluations. The aim of this review is to summarize the main properties of these eight chosen radionuclides. An overview from their availability to the resulting clinical studies, by way of chemical design and preclinical studies is discussed.

A224Ra-labeled polyoxopalladate as a putative radiopharmaceutical

2019 ◽  
Vol 55 (53) ◽  
pp. 7631-7634 ◽  
Author(s):  
Matthew Gott ◽  
Peng Yang ◽  
Ulrich Kortz ◽  
Holger Stephan ◽  
Hans-Jürgen Pietzsch ◽  
...  
Keyword(s):  
Protein Corona ◽  
Therapeutic Applications ◽  
The Core ◽  
Facile Preparation ◽  
Enhanced Properties

A facile preparation of polyoxopalladates with enhanced properties containing radium-224 in the core and a protein corona for further functionalization with targeting (bio)molecules for therapeutic applications in oncology is described.

Nanoconstructs in Targeted Alpha-Therapy

2015 ◽  
Vol 4 (2) ◽  
pp. 71-76 ◽  
Author(s):  
Jan Kozempel ◽  
Martin Vlk
Keyword(s):  
Targeted Alpha Therapy ◽  
Alpha Therapy

scholarly journals Manual on the proper use of sodium astatide ([211At]NaAt) injections in clinical trials for targeted alpha therapy (1st edition)

2021 ◽  
Author(s):  
Tadashi Watabe ◽  
Makoto Hosono ◽  
Seigo Kinuya ◽  
Takahiro Yamada ◽  
Sachiko Yanagida ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Japanese Society ◽  
Radiation Safety ◽  
Safety Management ◽  
Evaluation Methodology ◽  
Targeted Alpha Therapy ◽  
Safety Issues ◽  
Safety Standards ◽  
And Training ◽  
Alpha Therapy

AbstractWe present the guideline for use of [211At] sodium astatide (NaAt) for targeted alpha therapy in clinical trials on the basis of radiation safety issues in Japan. This guideline was prepared by a study supported by the Ministry of Health, Labour, and Welfare, and approved by the Japanese Society of Nuclear Medicine on 8th Feb, 2021. The study showed that patients receiving [211At]NaAt do not need to be admitted to a radiotherapy room and outpatient treatment is possible. The radiation exposure from the patient is within the safety standards of the ICRP and IAEA recommendations for the general public and caregivers. Precautions for patients and their families, safety management associated with the use of [211At]NaAt, education and training, and disposal of medical radioactive contaminants are also included in this guideline. Treatment using [211At]NaAt in Japan should be carried out according to this guideline. Although this guideline is applied in Japan, the issues for radiation protection and evaluation methodology shown here are considered internationally useful as well.

scholarly journals Evaluation of Actinium-225 radiolabeled cyclized alpha-melanocyte stimulating hormone (CycMSH) peptide for targeted alpha therapy

2021 ◽  
Vol 96-97 ◽  
pp. S101
Author(s):  
Victoria Brown ◽  
Cristina Rodríguez-Rodríguez ◽  
Chengcheng Zhang ◽  
Keiran Maskell ◽  
Francois Benard ◽  
...  
Keyword(s):  
Targeted Alpha Therapy ◽  
Melanocyte Stimulating Hormone ◽  
Alpha Therapy ◽  
Stimulating Hormone

scholarly journals Doping of Mg on ZnO Nanorods Demonstrated Improved Photocatalytic Degradation and Antimicrobial Potential with Molecular Docking Analysis

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Muhammad Ikram ◽  
Sidra Aslam ◽  
Ali Haider ◽  
Sadia Naz ◽  
Anwar Ul-Hamid ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Functional Groups ◽  
Zno Nanorods ◽  
Docking Studies ◽  
Trapping Efficiency ◽  
Wurtzite Phase ◽  
Binding Score ◽  
Doped Zno ◽  
Co Precipitation ◽  
Mg Doped

AbstractVarious concentrations of Mg-doped ZnO nanorods (NRs) were prepared using co-precipitation technique. The objective of this study was to improve the photocatalytic properties of ZnO. The effect of Mg doping on the structure, phase constitution, functional groups presence, optical properties, elemental composition, surface morphology and microstructure of ZnO was evaluated with XRD, FTIR, UV–Vis spectrophotometer, EDS, and HR-TEM, respectively. Optical absorption spectra obtained from the prepared samples showed evidence of blueshift upon doping. XRD results revealed hexagonal wurtzite phase of nanocomposite with a gradual decrease in crystallite size with Mg addition. PL spectroscopy showed trapping efficiency and migration of charge carriers with electron–hole recombination behavior, while HR-TEM estimated interlayer d-spacing. The presence of chemical bonding, vibration modes and functional groups at the interface of ZnO was revealed by FTIR and Raman spectra. In this study, photocatalytic, sonocatalytic and sonophotocatalytic performance of prepared NRs was systematically investigated by degrading a mixture of methylene blue and ciprofloxacin (MBCF). Experimental results suggested that improved degradation performance was shown by Mg-doped ZnO NRs. We believe that the product synthesized in this study will prove to be a beneficial and promising photocatalyst for wastewater treatment. Conclusively, Mg-doped ZnO exhibited substantial (p < 0.05) efficacy against gram-negative (G-ve) as compared to gram-positive (G+ve) bacteria. In silico molecular docking studies of Mg-doped ZnO NRs against DHFR (binding score: − 7.518 kcal/mol), DHPS (binding score: − 6.973 kcal/mol) and FabH (− 6.548 kcal/mol) of E. coli predicted inhibition of given enzymes as possible mechanism behind their bactericidal activity.

scholarly journals Extended single-dose toxicity study of [211At]NaAt in mice for the first-in-human clinical trial of targeted alpha therapy for differentiated thyroid cancer

2021 ◽  
Author(s):  
Tadashi Watabe ◽  
Kazuko Kaneda-Nakashima ◽  
Kazuhiro Ooe ◽  
Yuwei Liu ◽  
Kenta Kurimoto ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Body Weight ◽  
Thyroid Cancer ◽  
Single Dose ◽  
General Condition ◽  
Blood Test ◽  
Differentiated Thyroid Cancer ◽  
Targeted Alpha Therapy ◽  
Evaluation Point ◽  
Alpha Therapy

Abstract Objective Astatine (211At) is a promising alpha emitter as an alternative to iodine (131I). We are preparing the first-in-human (FIH) clinical trial of targeted alpha therapy for differentiated thyroid cancer in consultation with Pharmaceuticals and Medical Devices Agency. Here, we performed an extended single-dose toxicity examination under a reliability standard, as a preclinical safety assessment of [211At]NaAt to determine the FIH dose. Methods [211At]NaAt solution was injected into normal 6-week-old mice (male (n = 50) and female (n = 50), body weight: male 33.2 ± 1.7 g, female 27.3 ± 1.5 g), which were then divided into four groups: 5 MBq/kg (n = 20), 20 MBq/kg (n = 20), 50 MBq/kg (n = 30), saline control (n = 30). The mice were followed up for 5 days (primary evaluation point for acute toxicity: n = 80) or 14 days (n = 20: evaluation point for recovery) to monitor general condition and body weight change. At the end of the observation period, necropsy, blood test, organ weight measurement, and histopathological examination were performed. For body weight, blood test, and organ weight, statistical analyses were performed to compare data between the control and injected groups. Results No abnormal findings were observed in the general condition of mice. In the 50 MBq/kg group, males (days 3 and 5) showed a significant decrease in body weight compared with the control. However, necropsy did not differ significantly beyond the range of spontaneous lesions. In the blood test, males (50 MBq/kg) and females (50 MBq/kg) showed a decrease in white blood cell and platelet counts on day 5, and recovery on day 14. In the testis, a considerable weight decrease was observed on day 14 (50 MBq/kg), and multinucleated giant cells were observed in all mice, indicating a significant change related to the administration of [211At]NaAt. Conclusions In the extended single-dose toxicity study of [211At]NaAt, administration of high doses resulted in weight loss, transient bone marrow suppression, and pathological changes in the testis, which require consideration in the FIH clinical trial.

scholarly journals Gold nanoparticle bioconjugates labelled with 211At for targeted alpha therapy

RSC Advances ◽  
2017 ◽  
Vol 7 (65) ◽  
pp. 41024-41032 ◽  
Author(s):  
L. Dziawer ◽  
P. Koźmiński ◽  
S. Męczyńska-Wielgosz ◽  
M. Pruszyński ◽  
M. Łyczko ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Gold Nanoparticle ◽  
Radionuclide Therapy ◽  
Targeted Alpha Therapy ◽  
Alpha Therapy

Gold nanoparticles labeled with 211At are very effective in radionuclide therapy.

scholarly journals Facile Preparation of Nanofibrillar Networks of “Ureido‐Chitin” Containing Ureido and Amine as Chelating Functional Groups

2018 ◽  
Vol 24 (72) ◽  
pp. 19332-19340 ◽  
Author(s):  
Kathirvel Ganesan ◽  
Markus Heyer ◽  
Lorenz Ratke ◽  
Barbara Milow
Keyword(s):  
Functional Groups ◽  
Facile Preparation
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