Self‐Assemble Polymeric Nanoparticle with GSH Exhaustion for SPECT Imaging–Guided Enhanced Radioisotope Therapy

Exploiting biocompatible nanomaterials for cancer theranostics has attracted great attention in recent years. Herein, a multifunctional self‐assembled nanoparticle based on a biocompatible polymer that contains 3‐(4‐hydroxyphenyl) propionic acid N‐hydroxysuccinimide ester (HOPA) for radiolabeling an...

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Bibliographic Details
Published in:Particle & particle systems characterization 2019-06, Vol.36 (6), p.n/a
Main Authors: Tao, Yugui, Ren, Pengfei, Yi, Xuan, Zhou, Hailin, Xiong, Saisai, Ge, Fei, Chen, Lei, Yang, Kai
Format: Article
Language:English
Subjects:
Anticancer properties
Biocompatibility
Cancer
Chemotherapy
Exhausting
Exhaustion
Glutathione
glutathione exhaustion
Imaging
Nanomaterials
Nanoparticles
polymeric nanoparticles
Propionic acid
radioisotope therapy
Radioisotopes
Radiolabelling
single‐photon emission computed tomography imaging
Toxicity
Tumors
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Summary:Exploiting biocompatible nanomaterials for cancer theranostics has attracted great attention in recent years. Herein, a multifunctional self‐assembled nanoparticle based on a biocompatible polymer that contains 3‐(4‐hydroxyphenyl) propionic acid N‐hydroxysuccinimide ester (HOPA) for radiolabeling and piperlongumine (PL) for exhausting endogenous glutathione (GSH) (HOPA‐C18PMH‐PEG/PL) is successfully synthesized. With radionuclide 125I labeling, SPECT imaging shows high tumor uptake of HOPA‐C18PMH‐PEG/PL after intravenous injection. The in vitro and in vivo combined radioisotope therapy (RIT) and chemotherapy using 131I‐labeled HOPA‐C18PMH‐PEG/PL is then carried out, achieving synergistic antitumor effect. This is because the reactive oxygen species (ROS) level in the tumor sites of mice treated with 131I‐labeled HOPA‐C18PMH‐PEG/PL is increased after the exhaustion of GSH by PL. Additionally, such a strategy (exhausting GSH and increasing ROS) induces no obvious toxicity to normal tissue. Therefore, as‐made polymeric nanoparticles exhibit multifunctional properties for SPECT imaging–guided combined RIT and chemotherapy in one system. This finding will further promote polymeric nanoparticle–based RIT of cancer and is expected to be used for future clinical transformation. Self‐assembled polymeric nanoparticles (HOPA‐C18PMH‐PEG/PL) with GSH exhaustion and radionuclides labeling are developed for SPECT imaging–guided combined therapy. In vitro and in vivo combined radioisotope therapy and chemotherapy using 131I‐HOPA‐C18PMH‐PEG/PL significantly inhibit tumor growth after intravenous injection.
ISSN:0934-0866
1521-4117
DOI:10.1002/ppsc.201900018