The Exciting Opportunities That Radiopharmaceuticals Have to Offer: Nuclear Medicine Imaging, Therapy and Drug Delivery Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (30 November 2025) | Viewed by 186

Special Issue Editors


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Guest Editor
Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
Interests: PET imaging; radiochemistry; molecular imaging probes; neuroimaging; radiopharmaceutical development

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Guest Editor
1. Nuclear Engineering Institute, Brazilian Nuclear Energy Commission, Rio de Janeiro 21941-906, Brazil
2. Laboratory of Nanoradiopharmacy, Rio de Janeiro State University, Rio de Janeiro 23070-200, Brazil
Interests: radiopharmacy; radiopharmaceuticals; nano-radiopharmaceuticals; nanotechnology; nanoparticles and theranostics
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Special Issue Information

Dear Colleagues,

Radiopharmaceuticals play a transformative role in nuclear medicine by enabling both precise imaging and targeted treatment at the molecular level. With the growing need for non-invasive diagnostic tools and effective site-specific therapies, this field offers unprecedented opportunities across oncology, neurology, cardiology, and more. Recent innovations in radiochemistry, molecular probe design, and drug delivery platforms have significantly enhanced the specificity, bioavailability, and therapeutic index of these agents. Advances in targeted radionuclide therapy (TRT), including alpha- and beta-emitting isotopes, have opened up new therapeutic pathways for combatting cancer and inflammatory diseases. At the same time, engineering drug delivery systems—such as nanocarriers and ligand-conjugated scaffolds—has improved the in vivo stability, biodistribution, and cell/tissue penetration of radiopharmaceuticals.

This Special Issue aims to gather original research and reviews on cutting-edge developments in the design, synthesis, and application of radiopharmaceuticals for both diagnostic and therapeutic purposes. Topics of interest include novel imaging probes, PET/SPECT tracers, theranostic agents, and innovative drug delivery approaches for crossing biological barriers. Contributions highlighting the translational and clinical potential of radiopharmaceuticals are particularly welcome. We hope this collection will provide new insights into how radiopharmaceuticals are reshaping modern medicine.

Dr. Yanli Wang
Dr. Ralph Santos-Oliveira
Guest Editors

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Keywords

  • PET imaging
  • theranostics
  • molecular imaging probes
  • radionuclide therapy
  • neuroimaging
  • radiochemistry

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Published Papers (1 paper)

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Research

15 pages, 2701 KB  
Article
A Novel 68Ga-Labeled Integrin α4β7-Targeted Radiopharmaceutical for PET/CT Imaging of DSS-Induced Murine Colitis
by Guangjie Yang, Haiqiong Zhang and Li Huo
Pharmaceutics 2025, 17(12), 1591; https://doi.org/10.3390/pharmaceutics17121591 - 10 Dec 2025
Abstract
Background: Inflammatory bowel diseases (IBD) rely on invasive methods for detecting intestinal inflammation, with the needs for non-invasive molecular imaging tools being unmet. Integrin α4β7 is a key target in IBD pathogenesis due to its role in the recruitment of T cells. [...] Read more.
Background: Inflammatory bowel diseases (IBD) rely on invasive methods for detecting intestinal inflammation, with the needs for non-invasive molecular imaging tools being unmet. Integrin α4β7 is a key target in IBD pathogenesis due to its role in the recruitment of T cells. This study aimed to develop a novel 68Ga-labeled integrin α4β7-targeted radiopharmaceutical (68Ga-A2) and evaluate its feasibility for non-invasive PET/CT imaging of IBD inflammation in a dextran sulfate sodium (DSS)-induced murine colitis model. Methods: 68Ga-A2 was synthesized via radiolabeling DOTA-A2 with 68Ga. In vitro properties (radiochemical purity, stability, binding specificity, and affinity) of 68Ga-A2 were validated. The DSS-induced colitis model was established and confirmed in C57BL/6J mice, followed by in vivo PET/CT imaging, ex vivo biodistribution studies, and histological (HE and IHC) analyses to evaluate the targeting efficacy of 68Ga-A2. Results: 68Ga-A2 was prepared efficiently (20 min) with a radiochemical purity of >95% and demonstrated good in vitro stability. It exhibited specific binding to integrin α4β7 with a Kd of 68.48 ± 6.55 nM. While whole-body PET/CT showed no visible inflammatory focus uptake, ex vivo imaging and biodistribution of colon tissue revealed significantly higher uptake in DSS-treated mice compared to that in healthy/blocking groups, which was consistent with histological evidence of inflammation. Conclusions: 68Ga-A2 demonstrated specific targeting of IBD inflammatory foci in vitro and ex vivo. Despite whole-body imaging limitations, further optimization of its structure may enable it to become a promising non-invasive PET agent for IBD. These findings support future clinical investigations to validate its utility in IBD diagnosis and monitoring. Full article
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