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Targeting liposomes to tumor endothelial cells for neutron capture therapy.

Koning GA, Fretz MM, Woroniecka U, Storm G, Krijger GC

Department of Radiochemistry, Interfaculty Reactor Institute, Delft University of Technology, Mekelweg 15, NL-2629JB Delft, The Netherlands. g.a.koning@iri.tudelft.nl

The aim of our work is to target (10)B to the tumor vasculature for neutron capture therapy (NCT). Alpha (v)-integrin specific RGD-peptides were coupled to liposomes that encapsulated dodecahydrododecaborate. These RGD-liposomes strongly associated with human umbilical vein endothelial cells (HUVEC) expressing this integrin and were internalized. Proliferating HUVEC proved sensitive to treatment with gamma-irradiation resulting in decreased cell viability and pronounced inhibition of DNA-synthesis with increasing dose. Irradiation of RGD-(10)B-liposome incubated HUVEC with neutrons strongly inhibited endothelial cell viability. These results suggest that efficient NCT can be achieved by targeting (10)B-liposomes to angiogenic endothelium in tumors.

Published 13 August 2004 in Appl Radiat Isot, 61(5): 963-7.
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