68Ga and 188Re starch-based microparticles as theranostic tool for the hepatocellular carcinoma: Radiolabeling and preliminary in vivo rat studies

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Abstract

Purpose This work aims to develop, validate and optimize the radiolabeling of Starch-Based Microparticles (SBMP) by 188Re and 68Ga in the form of ready-to-use radiolabeling kits, the ultimate goal being to obtain a unique theranostic vector for the treatment of Hepatocellular Carcinoma. Methods Optimal labeling conditions and composition of freeze-dried kits were defined by monitoring the radiochemical purity while varying several parameters. In vitro stability studies were carried out, as well as an in vivo biodistribution as a preliminary approach with the intraarterial injection of 68Ga radiolabeled SBMP into the hepatic artery of DENA-induced rats followed by PET/CT imaging. Results Kits were optimized for 188Re and 68Ga with high and stable radiochemical purity (>95% and >98% respectively). The in vivo preliminary study was successful with more than 95% of activity found in the liver and mostly in the tumorous part. Conclusion SBMP are a promising theranostic agent for the Selective Internal Radiation Therapy of Hepatocellular carcinoma.

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Verger, E., Drion, P., Meffre, G., Bernard, C., Duwez, L., Lepareur, N., … Lacoeuille, F. (2016). 68Ga and 188Re starch-based microparticles as theranostic tool for the hepatocellular carcinoma: Radiolabeling and preliminary in vivo rat studies. PLoS ONE, 11(10). https://doi.org/10.1371/journal.pone.0164626

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