Abstract
PurposeThis 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.MethodsOptimal 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 intra-arterial injection of 68Ga radiolabeled SBMP into the hepatic artery of DENA-induced rats followed by PET/CT imaging.ResultsKits 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.ConclusionSBMP are a promising theranostic agent for the Selective Internal Radiation Therapy of Hepatocellular carcinoma.
Highlights
Hepatocellular Carcinoma (HCC), a liver cancer is the fifth most common cancer and the second leading cause of cancer death in men worldwide [1]
The in vivo preliminary study was successful with more than 95% of activity found in the liver and mostly in the tumorous part
188Re/68Ga Starch-Based Microparticles (SBMP) Labeling for HCC Theranostic patent WO2009013358
Summary
Hepatocellular Carcinoma (HCC), a liver cancer is the fifth most common cancer and the second leading cause of cancer death in men worldwide (seventh and sixth for women respectively) [1]. Scans post infusion of 99mTc-MAA allow firstly, the exclusion of patients with a high percentage of radioactivity being shunted into the lungs or spread into any other organ, such as the gastroduodenum and secondly, the determination of the predictive tumor dosimetry. Both steps (pre-therapeutic and therapy itself) are based on the assumption that the biodistribution of 90Y-microspheres and 99mTc-MAA will be identical. The MAA have a different size and morphology (aggregates with heterogeneous shapes with size comprised between 10–100μm [19]) in comparison with the 90Y-microspheres (spherical shape with size comprised between 20–40μm [20]) that can lead to a different biodistribution and an approximate tumor dosimetry [11,15,18,21,22]
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