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|標題:||Synthesis and in vitro evaluation of the phenylboric acid derivative entrapped lipiodol in boron neutron capture therapy for hepatoma||作者:||Chou, F.I.
|關鍵字:||hepatoma;neutron capture therapy;PBAD-lipiodol;alpha track;hepatocellular-carcinoma;arterial chemoembolization;sodium;borocaptate;enhanced survival;liver-tumors;boronophenylalanine;melanoma;delivery;cancer;chemistry||Project:||Anticancer Research||期刊/報告no：:||Anticancer Research, Volume 23, Issue 5A, Page(s) 3955-3963.||摘要:||
Background: Hepatoma, a common cancer in Taiwan. responds poorly to conventional therapies. Boron neutron capture therapy (BNCT) may provide a promising approach for hepatoma therapy. In this study, a pharmaceutical composition, phenylboric acid derivative entrapped lipiodol (PBAD-lipiodol), was synthesized and characterized. In vitro study was used for evaluation of PRAD-lipiodol for the BNCT of hepatoma. Materials and Methods: a Track observation was used to identify the boron compound in the TLC plate and to evidence the uniform distribution of boron in the PBAD-lipiodol. Inductively coupled plasma-atomic emission spectroscopy and neutron activation analysis were used to determine the concentrations of boron and lipiodol, respectively. Human hepatoma HepG2 cells were used for in vitro experiments. A Nomarski optical microscope was used to investigate the uptake of PBAD-lipiodol globules in individual hepatoma cells. Results: PBAD-lipiodol was stable in human serum. The boron source, PBAD, was uniformly distributed in PBAD-lipiodol. Many of the PBAD-lipiodol globules were internalized and retained in HepG2 cells, and the boron concentration of HepG2 cells reached 269 ppm after 72 hours of PBAD-lipiodol treatment. Conclusion: In vitro studies revealed that PBAD-lipiodol could deliver a therapeutically effective amount of PBAD as a boron source for the BNCT of hepatoma. PBAD-lipiodol is a potential new boron drug for the BNCT of hepatoma.
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