Phospholipid-nucleoside conjugates. 5. The interaction of selected 1-β-D-arabinofuranosylcytosine-5′-diphosphate-L-1,2-diacylglycerols with serum lipoproteins

Abstract The phospholipid-nucleoside conjugates 1-β- D -arabinofuranosylcytosine-5′-diphosphate- L -1,2-dipalmitin ( 1 ), -distearin ( 2 ), and -diolein ( 3 ) have been shown to interact rapidly with canine high density lipoprotein and with both high density and low density lipoproteins isolated from human serum. The extent of interaction with the high density lipoproteins appears to be dependent upon the characteristic gel-liquid crystalline phase transition of the conjugate's phospholipid. Since the phospholipid-nucleoside conjugates under study represent sustained release forms of the antileukemic agent 1-β- D -arabinofuranosylcytosine , the therapeutic efficacy of these conjugates should now be considered in light of these interactions.