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Radioiodinated Portable Albumin Binder as a Versatile Agent for in vivo Imaging with Single-Photon Emission Computed Tomography
摘要： In this study, radioiodinated 4-(p-iodophenyl)butyric acid ([131I]IBA) was synthesized and evaluated as a portable albumin-binder for potential applications in SPECT imaging of blood pool, tumor and lymph node with significantly improved pharmacokinetic properties. The [131I]IBA was prepared under the catalyst of Cu2O/1,10-phenanthroline. After that, the albumin-binding capability of [131I]IBA was tested in vitro, ex vivo and in vivo, respectively. [131I]IBA was obtained with very high radiolabeling yield (> 99%) and good radiochemical purity (> 98%) within 10 min. It binds to albumin effectively with high affinity (IC50= 46.5 μM) and has good stability. The results of biodistribution indicated that the [131I]IBA was mainly accumulated in blood with good retention (10.51±2.58%ID/g at 30 min p.i. and 4.63±0.17%ID/g at 4 h p.i.). In the SPECT imaging of mice models with [131I]IBA, blood pool, lymph node and tumors could be imaged clearly with high target-to-background ratio. Overall, the radioiodinated albumin binder of [131I]IBA with long blood half-life and excellent stability could be used to decorate diversified albumin-binding radioligands and developed as a versatile theranostic agent.
关键词： SPECT,in vivo imaging,radioiodination,albumin binder,animal models
更新于2025-09-23 15:23:52
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New 55Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging
摘要： Overexpression of folate receptors (FRs) on di?erent tumor types (e.g., ovarian, lung) make FRs attractive in vivo targets for directed diagnostic/therapeutic agents. Currently, no diagnostic agent suitable for positron emission tomography (PET) has been adopted for clinical FR imaging. In this work, two 55Co-labeled albumin-binding folate derivatives-[55Co]Co-cm10 and [55Co]Co-rf42-with characteristics suitable for PET imaging have been developed and evaluated. High radiochemical yields (≥95%) and in vitro stabilities (≥93%) were achieved for both compounds, and cell assays demonstrated FR-mediated uptake. Both 55Co-labeled folate conjugates demonstrated high tumor uptake of 17% injected activity per gram of tissue (IA/g) at 4 h in biodistribution studies performed in KB tumor-bearing mice. Renal uptake was similar to other albumin-binding folate derivatives, and liver uptake was lower than that of previously reported [64Cu]Cu-rf42. Small animal PET/CT images con?rmed the biodistribution results and showed the clear delineation of FR-expressing tumors.
关键词： folate receptors,cobalt-55,PET imaging,albumin binder,ovarian cancer,folic acid
更新于2025-09-12 10:27:22