Radiopharmaceutical Drugs Discovery and Evaluation

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (30 September 2019) | Viewed by 4259

Special Issue Editors


E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs, “Sapienza” University of Rome, 00185 Roma, Italy
Interests: drug discovery; epigenetics; medicinal chemistry; chemical biology; radiopharmaceuticals
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Institute of Nuclear Medicine, Università Cattolica del Sacro Cuore, Rome, Italy
Interests: nuclear medicine; radiomics; personalized medicine; radionuclide imaging; rradionuclide therapy; radiopharmaceuticals; radiation protection

Special Issue Information

Dear Colleagues,

this Special Issue is related to recent advances in the field of research and development of radiopharmaceuticals.

Nuclear medicine plays a major role in the early detection, early therapy assessment and treatment follow-up of malignancies, cardiological and neurobiological disorders, infections, kidney and liver abnormalities. This is made possible by the application of radiopharmaceuticals for non-invasive imaging and/or treatment purposes. A tremendous amount of innovation is related to the use of a multiplicity of radionuclides, new or optimized multimodality imaging devices, and a plethora of recently marketed radiopharmaceuticals in all medical domains, particularly, in oncology, cardiology and neurology.

With this Special Issue we aim to highlight recent efforts in the radiopharmaceuticals’ development field with a special focus on innovative medicinal/pharmaceutical chemistry, chemical biology, pharmacological, and clinical approaches for identifying novel, highly potent, selective and safe radiopharmaceuticals. We expect new insights into the diagnostic and/or therapeutic potential of old and new radiopharmaceuticals, with special emphasis on their design and optimization, on the pharmacological evaluation, and the identification of new drug candidates, targets, and new potential applications in different medical settings.

Since the design, development and pharmacological validation of radiopharmaceuticals is a rather interdisciplinary process covering various disciplines of health and natural sciences, we are going to especially welcome original research articles, short communications as well as a limited number of review articles focused on innovative interdisciplinary approaches in the field of radiopharmaceutical drug development and evaluation. For planned papers, a title and a short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Dr. Dante Rotili
Prof. Alessandro Giordano
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Nuclear medicine
  • Radiochemistry
  • Radiolabeling approaches
  • Multimodality imaging probes
  • Medicinal Chemistry
  • Target validation
  • Radiotracer metabolism
  • Tumor imaging
  • Tumor radio-guided surgery
  • Radiopharmaceuticals

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

17 pages, 3583 KiB  
Article
Preparation and In Vitro Evaluation of Neutron-Activated, Theranostic Samarium-153-Labeled Microspheres for Transarterial Radioembolization of Hepatocellular Carcinoma and Liver Metastasis
by Yin How Wong, Hun Yee Tan, Azahari Kasbollah, Basri Johan Jeet Abdullah and Chai Hong Yeong
Pharmaceutics 2019, 11(11), 596; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11110596 - 12 Nov 2019
Cited by 9 | Viewed by 3539
Abstract
Introduction: Transarterial radioembolization (TARE) has been proven as an effective treatment for unresectable liver tumor. In this study, neutron activated, 153Sm-labeled microspheres were developed as an alternative to 90Y-labeled microspheres for hepatic radioembolization. 153Sm has a theranostic advantage as it [...] Read more.
Introduction: Transarterial radioembolization (TARE) has been proven as an effective treatment for unresectable liver tumor. In this study, neutron activated, 153Sm-labeled microspheres were developed as an alternative to 90Y-labeled microspheres for hepatic radioembolization. 153Sm has a theranostic advantage as it emits both therapeutic beta and diagnostic gamma radiations simultaneously, in comparison to the pure beta emitter, 90Y. Methods: Negatively charged acrylic microspheres were labeled with 152Sm ions through electrostatic interactions. In another formulation, the Sm-labeled microsphere was treated with sodium carbonate solution to form the insoluble 152Sm carbonate (152SmC) salt within the porous structures of the microspheres. Both formulations were neutron-activated in a research reactor. Physicochemical characterization, gamma spectrometry, and radiolabel stability tests were carried out to study the performance and stability of the microspheres. Results: The Sm- and SmC-labeled microspheres remained spherical and smooth, with a mean size of 35 µm before and after neutron activation. Fourier transform infrared (FTIR) spectroscopy indicated that the functional groups of the microspheres remained unaffected after neutron activation. The 153Sm- and 153SmC-labeled microspheres achieved activity of 2.53 ± 0.08 and 2.40 ± 0.13 GBq·g−1, respectively, immediate after 6 h neutron activation in the neutron flux of 2.0 × 1012 n·cm−2·s−1. Energy-dispersive X-ray (EDX) and gamma spectrometry showed that no elemental and radioactive impurities were present in the microspheres after neutron activation. The retention efficiency of 153Sm in the 153SmC-labeled microspheres was excellent (~99% in distilled water and saline; ~97% in human blood plasma), which was higher than the 153Sm-labeled microspheres (~95% and ~85%, respectively). Conclusion: 153SmC-labeled microspheres have demonstrated excellent properties for potential application as theranostic agents for hepatic radioembolization. Full article
(This article belongs to the Special Issue Radiopharmaceutical Drugs Discovery and Evaluation)
Show Figures

Graphical abstract

Back to TopTop