[68Ga]NOTA-Galactosyl Human Serum Albumin: a Tracer for Liver Function Imaging with Improved Stability

Biodistribution Human serum albumin Metabolic stability PET Imaging
DOI: 10.1007/s11307-017-1046-1 Publication Date: 2017-02-13T13:23:08Z
ABSTRACT
Non-invasive techniques allowing quantitative determination of the functional liver mass are great interest for patient management in a variety clinical settings. Recently, we presented [68Ga]DTPA-GSA to target hepatic asialoglycoprotein receptor this purpose. Here, introduce [68Ga]NOTA-GSA improve metabolic stability radiopharmaceutical and compare imaging properties with [68Ga]DTPA-GSA. Labeling compounds was carried out at room temperature using 1.9 M sodium acetate as buffer. For quality control, thin-layer, high-performance liquid, size exclusion chromatographies were used. Metabolic studied rat human serums. vivo evaluation, Fischer rats scanned by positron emission tomography magnetic resonance subsequently sacrificed biodistribution studies. Time activity curves (TACs) heart generated corresponding parameters (T50, T90, LHL15, HH15) calculated. can be produced high radiochemical yield purity (>95 %) within 15 min. Stability studies revealed almost no metabolite formation over 2-h observation period. Analysis TACs showed comparable results most investigated parameters. The only significant difference found T90 value, where slower uptake comparison 68Ga-DTPA-GSA (123 ± 10 vs. 89 3 s, p < 0.01). increase organs lower background activity. However, LHL15 HH15 indicates that increased did not further diagnostic value. Thus, used equivalent function tomography.
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