Optimization of Drug Anchor for Ortho-Carborane in Reconstitution of Low Density Lipoproteins for Neutron Capture Therapy
Low density lipoproteins (LDL) have considerable potential as carriers for site-specific drug delivery.1 The core of native LDL is composed mainly of cholesteryl esters of long chain unsaturated fatty acids, which can be removed and replaced with other hydrophobic compounds. These core compounds can be regarded as specific combinations of structural units that not only provide efficient packing in the core environment, but also enhance passage through the phospholipid coat into the core. For example, it has been demonstrated that esters of unsaturated fatty acids are incorporated into heptane-extracted LDL far more effectively than esters of the corresponding saturated fatty acids.2 The aim of the present study, which is an extension of the pioneering work of Kahl et a1,3–7 is to find which combination of these structural elements forms the best drug anchor for delivery of o-carborane to a tumour in reconstituted LDL.
KeywordsCholesteryl Ester Boron Compound Cholesteryl Oleate Chain Unsaturated Fatty Acid Idaho National Engineer Laboratory
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