Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 9, Pages 3059-3065Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.03.050
Keywords
Boron neutron capture therapy (BNCT); Boron delivery system (BDS); Boronated liposomes; closo-Dodecaborate lipids
Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan
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closo-Dodecaborate lipid liposomes were developed as new vehicles for boron delivery system (BDS) of neutron capture therapy. The current approach is unique because the liposome shell itself possesses cytocidal potential in combination with neutron irradiation. The liposomes composed of closo-dodecaborate lipids DSBL and DPBL displayed high cytotoxicity with thermal neutron irradiation. The closo-dodecaborate lipid liposomes were taken up into the cytoplasm by endocytosis without degradation of the liposomes. Boron concentration of 22.7 ppm in tumor was achieved by injection with DSBL-25% PEG liposomes at 20 mg B/kg. Promising BNCT effects were observed in the mice injected with DSBL-25% PEG liposomes: the tumor growth was significantly suppressed after thermal neutron irradiation (1.8 x 10(12) neutrons/cm(2)). (c) 2010 Elsevier Ltd. All rights reserved.
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