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Biological Efficacy of Boronated Low-Density Lipoprotein for Boron Neutron Capture Therapy as Measured in Cell Culture¹

Medical Department, Brookhaven National Laboratory, Upton, New York 11973 [B. H. L., E. A. P., R. G. F.]; School of Pharmacy, Department of Pharmaceutical Chemistry, University of California, San Francisco, California 94143-0446 [S. B. K., D. W. P.]; and Department of Radiation Oncology, University Hospital at Stony Brook, Stony Brook, New York 11794 [B. H. L.]

Low-density lipoproteins (LDLs) are known to be internalized by the cell through receptor-mediated mechanisms. There is evidence that LDLs may be taken up avidly by tumor cells to provide cholesterol for the synthesis of cell membranes. Thus, the possibility exists that LDLs may provide an ideal vehicle for the transport of boron to tumor cells for boron neutron capture therapy. A boronated analogue of LDL has recently been synthesized for possible application in boron neutron capture therapy. The analogue was tested in cell culture for uptake and biological efficacy in the thermal neutron beam at the Brookhaven Medical Research Reactor. It was found that boron concentrations 10 times higher than that required in tumors for boron neutron capture therapy were easily obtained and that the amount of uptake was consistent with a receptor-mediated binding mechanism. The measured intracellular concentration of 240 µg ¹⁰B/g cells is significantly higher than that obtained with any other boron compound previously evaluated for possible clinical application.

¹ Research was carried out at Brookhaven National Laboratory under the auspices of the U.S. Department of Energy, under Contract DE-ACO2-76CH00016, and was supported by National Institutes of Health Grant CA41487 at University of California, San Francisco.

² To whom requests for reprints should be addressed, at Medical Department, Brookhaven National Laboratory, Associated Universities, Inc., Upton, Long Island, NY 11973.

Received 1/ 4/91. Accepted 6/25/91.