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KMID : 1148920190530030189
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Nuclear Medicine and Molecular Imaging
2019 Volume.53 No. 3 p.189 ~ p.198
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Development of a Novel Imaging Agent for Determining Albumin Uptake in Solid Tumors
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Daum S.
Magnusson J. P.
Pes L.
Fernandez J. Garcia
Chercheja S.
Medda F.
Nollmann F. I.
Koester S. D.
Galan P. Perez
Warnecke A.
Ajaj K. Abu
Kratz Felix
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Abstract
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Purpose: The purpose of this study was to investigate the albumin-binding compound 111In-C4-DTPA as an imaging agent for the detection of endogenous albumin accumulation in tumors.
Methods: 111In-C4-DTPA was injected in healthy nude mice for pharmacokinetic and biodistribution studies (10 min, 1, 6, 24, and 48 h, n?=?4) and subsequently in tumor-bearing mice for single-photon emission computed tomography/X-ray-computed tomography (SPECT/CT) imaging studies. Four different human tumor xenograft models (LXFL529, OVXF899, MAXFTN401, and CXF2081) were implanted subcutaneously unilaterally or bilaterally (n?=?4?8). After intravenous administration of 111In-C4-DTPA, SPECT/CT images were collected over 72 h at 4?6 time points. Additionally, gamma counting was performed for the blood, plasma, lungs, heart, liver, spleen, kidneys, muscle, and tumors at 72 h post-injection.
Results: 111In-C4-DTPA bound rapidly to circulating albumin upon injection, and the radiolabeled albumin conjugate thus formed was stable in murine and human serum. SPECT/CT images demonstrated a time-dependent uptake with a maximum of 2.7?3.8% ID/cm3 in the tumors at approximately 24 h post-injection and mean tumor/muscle ratios in the range of 3.2?6.2 between 24 and 72 h post-injection. The kidneys and bladder were the predominant elimination organs. Gamma counting at 72 h post-injection showed 1.3?2.5% ID/g in the tumors and mean tumor/muscle ratios in the range of 4.9?9.4.
Conclusion: 111In-C4-DTPA bound rapidly to circulating albumin upon injection and showed time-dependent uptake in the tumors demonstrating a potential for clinical application as a companion imaging diagnostic for albumin-binding anticancer drugs.
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KEYWORD
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Albumin, Drug carrier, Imaging agent, SPECT/CT imaging, Tumor accumulation, 111In
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