Abstract

As one of the most critical types of cancer, hepatocellular carcinoma (HCC) affects many people worldwide. This study demonstrated the prospective use of atorvastatin, a drug that inhibits the mevalonate pathway, causing hypolipidemia, as a carrier to deliver the iodine-131 (131I) isotope to liver tissues for HCC radiotherapy. The atorvastatin radioiodination method was optimized for utilizing the 131I isotope. The radiochemical quality and the in vitro stability of the generated [131I]atorvastatin were investigated. In addition, the biodistribution experiments of [131I]atorvastatin were evaluated in both normal and HCC-induced rat models. [131I]atorvastatin was produced at a maximum radiochemical yield of 86.7 ± 0.49%. The [131I]atorvastatin solution purified via high-performance liquid chromatography showed good in vitro stability for 12 h after tagging. Biodistribution analyses revealed remarkable liver targeting capacity of [131I]atorvastatin and good localization of 131I in liver tissues. Overall, the encouraging biochemical profile and histopathological findings have been reported, and preliminary investigations on the possible use of [131I]atorvastatin as a radiotracer and its impact on HCC radiotherapy in rats show promise.

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