Background: Iodine-131 labeled hypericin (I-Hyp) has been utilized as a necrosis-avid theragnostic tracer in a dual targeting pan-anticancer strategy called OncoCiDia. Widespread use of previously-tested solvent dimethyl sulfoxide (DMSO) is limited by safety concerns. To tackle this, the present study was designed to explore a clinically feasible excipient for the formulation of the hydrophobic I-Hyp for intravenous administration.
Method: Solubility of Hyp in serial solutions of already-approved hydroxypropyl-β-cyclodextrin (HP-β-CD) was evaluated by UVspectrophotometry and 50% HP-β-CD was chosen for further experiments. Two novel HP-β-CD-based formulations of I-Hyp were compared with previous DMSO-based formulation, with regards to necrosis-targetability and biodistribution, by magnetic resonance imaging, single-photon emission computed tomography (SPECT), gamma counting, autoradiography, fluorescence microscopy and histopathology.
Results: Hyp solubility was enhanced with increasing HP-β-CD concentrations. The radiochemical purity of I-Hyp was higher than 90% in all formulations. The necrosis-targetability of I-Hyp in the novel formulations was confirmed in vivo by SPECT and in vitro by autoradiography, fluorescence microscopy and histopathology. The plasma clearance of radioactivity was faster in the novel formulations.
Conclusion: The novel I-Hyp formulations with HP-β-CD could be a suitable pharmaceutical excipient for I-Hyp for intravenous administration.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ijpharm.2021.120393 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Multimodal Theranostic Nanoparticles for Necrosis Targeting, Fluorescence/SPECT Imaging, and Radiotherapy of Residual Tumors after Hepatocellular Carcinoma Ablation.
Mol Pharm
April 2024
Department of Interventional Radiology, The First Hospital of China Medical University, Shenyang 110001, China.
Thermal ablation has been commonly used as an effective treatment for hepatocellular carcinoma; however, peri-necrotic tumor residues after ablation play a significant role in tumor recurrence and poor prognosis. Therefore, developing agents that can effectively target and eliminate residual tumors is critically needed. Necrosis targeting strategies have potential implications for evaluating tumor necrosis areas and treating the surrounding residual tumors.
View Article and Find Full Text PDFRadioiodinated hypericin as a tracer for detection of acute myocardial infarction: SPECT-CT imaging in a swine model.
J Nucl Cardiol
December 2022
Department of Interventional Radiology, The First Hospital of China Medical University, Shenyang, China.
Purpose: Hypericin (Hyp) is a natural compound with a newly discovered necrosis-avidity, which can be exploited as a necrosis-avid tracer once labeled with radioactive iodine as has been tested in rodent models. This study was to evaluate the effect of radioiodinated Hyp (I-Hyp) for imaging detection of acute myocardial infarction (AMI) in conditions closer to clinical scenarios.
Methods: We established swine AMI models (n = 6) which were intravenously given I-Hyp and Tc-sestamibi and underwent SPECT-CT imaging with high- and low-energy collimators.
Preparation and validation of cyclodextrin-based excipients for radioiodinated hypericin applied in a targeted cancer radiotherapy.
Int J Pharm
April 2021
Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, China. Electronic address:
Background: Iodine-131 labeled hypericin (I-Hyp) has been utilized as a necrosis-avid theragnostic tracer in a dual targeting pan-anticancer strategy called OncoCiDia. Widespread use of previously-tested solvent dimethyl sulfoxide (DMSO) is limited by safety concerns. To tackle this, the present study was designed to explore a clinically feasible excipient for the formulation of the hydrophobic I-Hyp for intravenous administration.
View Article and Find Full Text PDFBiodistribution and tolerance of intravenous iodine-131-labelled hypericin in healthy dogs.
Vet Comp Oncol
September 2018
Small Animal Department, Faculty of Veterinary Medicine, Ghent University, Merelbeke, Belgium.
Hypericin (Hyp) is a necrosis-avid compound that can be efficiently labelled with radioiodine for both diagnostic and therapeutic purposes. Before I-Hyp can be considered as a clinically useful drug in a combination therapy for canine cancer patients, evaluation of its toxicity is necessary. The aim of this study was to investigate the biodistribution and tolerance of a single dose administration of I-Hyp.
View Article and Find Full Text PDFBiliary and duodenal drainage for reducing the radiotoxic risk of antineoplastic 131I-hypericin in rat models.
Exp Biol Med (Maywood)
December 2015
Lab of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, 210028 Nanjing, P.R. China Radiation Medical Institute, Shandong Academy of Medical Sciences, 250062 Jinan, P.R. China Department of Radiology, Campus Gasthuisberg, KU Leuven, 3000 Leuven, Belgium.
Article Synopsis
- The study investigates the use of (131)I-hypericin, a radiopharmaceutical, for treating solid tumors while identifying potential side effects due to its radioactivity after liver metabolism and bile excretion.
- Thirty-eight rats were injected with (131)I-Hyp, and different bile drainage methods were tested to measure their effectiveness in reducing intestinal radioactivity, with results showing significant reductions in 12 rats subjected to bile drainage.
- Findings suggest that effective bile drainage can prevent unwanted intestinal radioactivity, and this method might be translated into clinical practice for patients treated with (131)I-Hyp, using specialized drainage catheters.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!