Synthesis of closo-Dodecaboryl Lipids and their Liposomal Formation for Boron Neutron Capture Therapy |
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Authors: | Hiroyuki Nakamura Jong-Dae Lee Manabu Ueno Yusuke Miyajima Hyun Seung Ban |
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Institution: | (1) Department of Chemistry, Faculty of Science, Gakushuin University, Tokyo 171-8588, Japan |
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Abstract: | High accumulation and selective delivery of boron into tumor tissues are the most important requirements to achieve efficient
neutron capture therapy of cancers. We focused on liposomal boron delivery system to achieve a large amount of boron delivery
to tumor. We succeeded in the synthesis of the double-tailed boron cluster lipids 4a–c and 5a–c, which has a B12H11S-moiety as a hydrophilic function, by S-alkylation of B12H11SH with bromoacetyl and chloroacetocarbamate derivatives of diacylglycerols. Size distribution of liposomes prepared from
the boron cluster lipid 4b, dimyristoylphosphatidylcholine, polyethyleneglycol-conjugated distearoylphosphatidylethanolamine, and cholesterol was determined
as 100 nm in diameter by an electrophoretic light scattering spectrophotometer. Calcein-encapsulation experiments revealed
that these boronated liposomes are stable at 37 °C in fetal bovine serum solution for 24 h. |
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Keywords: | closo-dodecaborate boron ion cluster lipid boron neutron capture therapy liposome mercaptoundecahydrododecaborate BSH |
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