AI Article Synopsis
- The study investigates how different formulations of radioiodinated hypericin affect its distribution in the body, ability to target necrosis, and effectiveness in killing tumor cells in a cancer treatment context.
- Researchers prepared two formulations using iodine-labeled hypericin and tested them on rats with vascular-disrupted tumors, analyzing their biodistribution and tumor response through various imaging and histological techniques.
- Findings revealed significant differences between the two formulations in terms of absorption in necrotic tissue and retention in organs like the lungs, spleen, and liver, highlighting the importance of formulation in the drug's therapeutic impact.
Article Abstract
Purpose: To study whether formulation influences biodistribution, necrosis avidity and tumoricidal effects of the radioiodinated hypericin, a necrosis avid agent for a dual-targeting anticancer radiotherapy.
Methods: Iodine-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.
Results: The 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).
Conclusions: The formulation of radioiodinated hypericin/hypericin appears crucial for its physical property, biodistribution, necrosis avidity and tumoricidal effects.
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| http://dx.doi.org/10.1007/s11095-013-1159-4 | DOI Listing |
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