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Radiolabeled Nanoparticles: Molecular Design, Targeting, Therapy, and Imaging

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Nanochemistry".

Deadline for manuscript submissions: 31 August 2026 | Viewed by 213

Special Issue Editors


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Guest Editor
Division of Astatine-Based Drug Development and Translational Research, Interdisciplinary Research Center for Radiation Sciences, Institute for Radiation Sciences, The University of Osaka, Suita, Osaka 565-0871, Japan
Interests: organic synthesis; organic and inorganic nanoparticles; RI-labeling; cancer targeting; nuclear medicine

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Guest Editor
Discovering Molecular Probes Research Unit, Innovative Integrated Bio-Research Core, Institute for Frontier Science Initiative, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan
Interests: theranostics; radiolabeling; radiopharmaceuticals; molecular imaging; cancer; radionuclide therapy; radiosynthesis
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Special Issue Information

Dear Colleague,

Recently, DDS has attracted attention because it maximizes drug efficacy and minimizes side effects by selectively delivering drugs to diseased areas. Focusing on cancer theranostics, Kratochwil et. al. reported that [225Ac]PSMA-617 showed strong therapeutic effects against metastatic prostate cancer. Watabe et al. disclosed high accumulation and detection of [18F]FAPI-74 to primary and metastatic lesions.

Nanoparticles are also widely used for transporting radionuclides into tumors, e.g., 177Lu-, 225Ac- or 211At-labeled gold nanoparticles for Therapeutics, as well as 99mTc-, 111ln- or 64Cu-labeled liposomes for imaging probes. Additionally, nanoparticles are an excellent tool for drug immobilization; thus, they can be directly administered to the lesion-affected part.

In this Special Issue, we invite researchers who submit innovative research articles related to the synthesis of radiolabeled nanoparticles and its evaluation. The evaluation of nanoparticles includes in vitro and in vivo experiments, such as cytotoxicity, biodistribution, therapeutic effect and imaging tests. The choice of target disease is not limited, but we would appreciate it if there was novelty in the structure and shape of the nanoparticles, as well as be interested in reports on comparisons of biological functions based on their differences. 

Dr. Yuichiro Kadonaga
Prof. Dr. Kazuma Ogawa
Guest Editors

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Keywords

  • synthesis of radiolabeled nanoparticles
  • biological evaluation of radiolabeled nanoparticles
  • theranostics
  • drug delivery
  • surface modification of nanoparticles
  • structural analysis
  • nuclear medicine
  • organic chemistry
  • inorganic chemistry

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Published Papers (1 paper)

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Research

18 pages, 1670 KB  
Article
Preparation and Evaluation of Radiolabeled Porphyrin-Functionalized Lipid Nanodroplets for Cancer Theranostics
by Nur Izni Binti Ramzi, Kisa Tamamura, Masayuki Munekane, Kenji Mishiro, Takeshi Fuchigami, Xiaojun Hu, Renata Jastrząb, Seigo Kinuya, Kazuaki Ninomiya and Kazuma Ogawa
Molecules 2026, 31(7), 1114; https://doi.org/10.3390/molecules31071114 (registering DOI) - 27 Mar 2026
Abstract
[111In]In-diethylenetriaminepentaacetic acid-5,10,15,20-tetraphenylporphyrin ([111In]In-DTPA-TPP) nanodroplets were developed for cancer theranostics, featuring ultrasound-sensitive properties. The designed nanodroplets that encapsulate the low-boiling-point liquid perfluorocarbon and IR-780 iodide, a near-infrared fluorescent dye, with surface conjugation of 111In-labeled porphyrin derivative, were synthesized and [...] Read more.
[111In]In-diethylenetriaminepentaacetic acid-5,10,15,20-tetraphenylporphyrin ([111In]In-DTPA-TPP) nanodroplets were developed for cancer theranostics, featuring ultrasound-sensitive properties. The designed nanodroplets that encapsulate the low-boiling-point liquid perfluorocarbon and IR-780 iodide, a near-infrared fluorescent dye, with surface conjugation of 111In-labeled porphyrin derivative, were synthesized and evaluated by in vitro and in vivo experiments. The cellular uptake of [111In]In-DTPA-TPP nanodroplets was significantly higher than that of control nanodroplets without TPP. Biodistribution experiments revealed greater tumor accumulation in mice injected with [111In]In-DTPA-TPP nanodroplets than in those injected with control nanodroplets lacking TPP. Additionally, the accumulation of [111In]In-DTPA-TPP nanodroplets in the tumor was visualized by single-photon emission computed tomography. Sonodynamic therapeutic experiments revealed that DTPA-TPP nanodroplets at 10 µmol total lipids/kg weight with a single ultrasound irradiation onto the tumor area significantly inhibited tumor growth. These results indicate that [111In]In-DTPA-TPP nanodroplets would be promising cancer theranostic agents. Full article
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