Abstract

Objective: The objective of this research was to synthesize and prepare radiopharmaceuticals containing neutron-activated Ho 166. The in vitro stability of Ho-166-radiopharmaceuticals was tested, and the interaction of the radiopharmaceuticals with hepatoma cells was investigated. Materials and Methods: In order to generate Ho 166, the non-radioactive Ho-165-acetylacetonate (Ho-165-AcAc) was prepared and irradiated in the Tsing Hua Open-Pool Reactor. Multiple channel analyzer was used for analysis of the radioactivity and the purity of the Ho-166-AcAc. Lipiodol was used as a carrier of Ho-166-AcAc. The stability of Ho-166-AcAc-lipiodol in serum was tested. The interaction of Ho-l65-AcAc lipiodol with human hepatoma cells (HepG2 cells) was investigated. Result: In this study, the prepared Ho-l65-AcAc samples were irradiated in the nuclear reactor for up to 10 hr and yielded 16-l8mCi/SOmg of specific activity. In addition, in vitro analysis of the stability of Ho-166-AcAc-lipiodol in plasma revealed a 98% retention of Ho-166 in the Ho-l66-AcAc-lipiodol after 120 hr. In vitro treatment of HepG2 cells for 24 hr with Ho-165-AcAc-lipiodol resulted in a retention of 1.3µg of Ho-165-AcAc in 106 cells. Thus, from the specific activity of Ho-166-AcAc-lipiodol the potential radioactivity of Ho-166 in HepG2 cells can be evaluated. Conclusion: Ho I 66-AcAc-lipiodol contained sufficient high energy J3 emitter and has a high stability in serum. in vitro cell culture analysis showed that large amount of I-lo-165-AcAc-lipiodol can be uptake by hepatoma cells. Results of this in vitro study provided important basic information for future development and in vitro tests. The Ho-I 66-AcAc-lipiodol has potential for future hepatoma therapy.

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