ArticlePharmaceutical research2014
Radioiodinated hypericin: its biodistribution, necrosis avidity and therapeutic efficacy are influenced by formulation.
Article in Pharmaceutical research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 21 citations in OpenAlex.
- Role of Radioiodine in Cancer Therapy: A Review of the Design and Challenges in Selecting Radioligands from Natural Sources.Drug design, development and therapy · 2025Review
- Future Prospective of Radiopharmaceuticals from Natural Compounds Using Iodine Radioisotopes as Theranostic Agents.Molecules (Basel, Switzerland) · 2022Review
- Biodegradable Hypericin-Containing Nanoparticles for Necrosis Targeting and Fluorescence Imaging.Molecular pharmaceutics · 2020Article
- Predicting Clinical Efficacy of Vascular Disrupting Agents in Rodent Models of Primary and Secondary Liver Cancers: An Overview with Imaging-Histopathology Correlation.Diagnostics (Basel, Switzerland) · 2020Review
- Updated developments on molecular imaging and therapeutic strategies directed against necrosis.Acta pharmaceutica Sinica. B · 2019Article
- Avenues to molecular imaging of dying cells: Focus on cancer.Medicinal research reviews · 2018Review
- Pre-clinical Evaluation of a Cyanine-Based SPECT Probe for Multimodal Tumor Necrosis Imaging.Molecular imaging and biology · 2016Article
- Effects of Glycosylation on Biodistribution and Imaging Quality of Necrotic Myocardium of Iodine-131-Labeled Sennidins.Molecular imaging and biology · 2016Article
- Illuminating necrosis: From mechanistic exploration to preclinical application using fluorescence molecular imaging with indocyanine green.Scientific reports · 2016Article
- Radiopharmaceutical study on Iodine-131-labelled hypericin in a canine model of hepatic RFA-induced coagulative necrosis.La Radiologia medica · 2015Article
- An overview of translational (radio)pharmaceutical research related to certain oncological and non-oncological applications.World journal of methodology · 2013Review
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo study whether formulation influences biodistribution, necrosis avidity and tumoricidal effects of the radioiodinated hypericin, a necrosis avid agent for a dual-targeting anticancer radiotherapy.
methodsIodine-123- and 131-labeled hypericin ((123)I-Hyp and (131)I-Hyp) were prepared with Iodogen as oxidant, and formulated in dimethyl sulfoxide (DMSO)/PEG400 (polyethylene glycol 400)/water (25/60/15, v/v/v) or DMSO/saline (20:80, v/v). The formulations with excessive Hyp were optically characterized. Biodistribution, necrosis avidity and tumoricidal effects were studied in rats (n = 42) without and with reperfused liver infarction and implanted rhabdomyosarcomas (R1). To induce tumor necrosis, R1-rats were pre-treated with a vascular disrupting agent. Magnetic resonance imaging, tissue-gamma counting, autoradiography and histology were used.
resultsThe two formulations differed significantly in fluorescence and precipitation. (123)I-Hyp/Hyp in DMSO/PEG400/water exhibited high uptake in necrosis but lower concentration in the lung, spleen and liver (p < 0.01). Tumor volumes of 0.9 ± 0.3 cm(3) with high radioactivity (3.1 ± 0.3% ID/g) were detected 6 days post-treatment. By contrast, (131)I-Hyp/Hypin DMSO/saline showed low uptake in necrosis but high retention in the spleen and liver (p < 0.01). Tumor volumes reached 2.6 ± 0.7 cm(3) with low tracer accumulation (0.1 ± 0.04%ID/g).
conclusionsThe formulation of radioiodinated hypericin/hypericin appears crucial for its physical property, biodistribution, necrosis avidity and tumoricidal effects.
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