ArticleEuropean journal of nuclear medicine and molecular imaging2013
Development of ⁶⁸Ga-labelled DTPA galactosyl human serum albumin for liver function imaging.
Article in European journal of nuclear medicine and molecular imaging, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed, 40 citations in OpenAlex.
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- Crystal structure of aqua-(2-{[2-({2-[bis-(carboxyl-ato-κActa crystallographica. Section E, Crystallographic communications · 2018Article
- [Molecular imaging and biology · 2017Article
- Investigations on the Ga(III) Complex of EOB-DTPA and Its 68Ga Radiolabeled Analogue.Journal of visualized experiments : JoVE · 2016Article
- Simultaneous SPECT imaging of multi-targets to assist in identifying hepatic lesions.Scientific reports · 2016Article
- 68Ga chelating bioorthogonal tetrazine polymers for the multistep labeling of cancer biomarkers.Chemical communications (Cambridge, England) · 2014Article
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7 authors at 2 institutions in 2 countries.
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Abstract
purposeThe hepatic asialoglycoprotein receptor is responsible for degradation of desialylated glycoproteins through receptor-mediated endocytosis. It has been shown that imaging of the receptor density using [(99m)Tc]diethylenetriamine pentaacetic acid (DTPA) galactosyl human serum albumin ([(99m)Tc]GSA) allows non-invasive determination of functional hepatocellular mass. Here we present the synthesis and evaluation of [(68)Ga]GSA for the potential use with positron emission tomography (PET).
methodsLabelling of GSA with (68)Ga was carried out using a fractionated elution protocol. For quality control thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and size exclusion chromatography (SEC) techniques were evaluated. Stability of [(68)Ga]GSA was studied in phosphate-buffered saline (PBS) and human serum. For in vivo evaluation [(68)Ga]GSA distribution in Lewis rats was compared with [(99m)Tc]GSA by using a dual isotope protocol. PET and planar imaging studies were performed using the same scaled molar dose of [(68)Ga]GSA and [(99m)Tc]GSA. Time-activity curves (TAC) for heart and liver were generated and corresponding parameters calculated (t50, t90).
results[(68)Ga]GSA can be produced with high radiochemical purity. The best TLC methods for determining potential free (68)Ga include 0.1 M sodium citrate as eluent. None of the TLC methods tested were able to determine potential colloids. This can be achieved by SEC. HPLC confirmed high radiochemical purity (>98%). Stability after 120 min incubation at 37 °C was high in PBS (>95% intact tracer) and low in human serum (∼27% intact tracer). Biodistribution studies simultaneously injecting both tracers showed comparable liver uptake, whereas activity concentration in blood was higher for [(68)Ga]GSA compared to [(99m)Tc]GSA. The [(99m)Tc]GSA TACs exhibited a small degree of hepatic metabolism compared to the [(68)Ga]GSA curves. The mean [(68)Ga]GSA t90 was higher than the mean t90 for [(99m)Tc]GSA. The mean [(68)Ga]GSA t50 was not significantly different from the mean t50 for [(99m)Tc]GSA.
conclusionThis study provides a promising new (68)Ga-labelled compound based on a commercially used kit for imaging the functional hepatocellular mass.
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