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Chou, F.I. et al.

Chou, Chung, Shieh, Huang, Chung, Liu, Yang, Chi, Lin, Lui, Kai,

Synthesis and in vitro evaluation of the phenylboric acid derivative entrapped lipiodol in boron neutron capture therapy for hepatoma.

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 PBAD-lipiodol for the BNCT of hepatoma. MATERIALS AND METHODS: alpha 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.[1]

References

Synthesis and in vitro evaluation of the phenylboric acid derivative entrapped lipiodol in boron neutron capture therapy for hepatoma. Chou, F.I., Chung, H.P., Shieh, M.S., Huang, C.W., Chung, R.J., Liu, H.M., Yang, J.Y., Chi, C.W., Lin, Y.C., Lui, W.Y., Kai, J.J. Anticancer Res. (2003) [Pubmed]

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