Preclinical Properties of N4-Hexadecyl- and N4- Octadecyl-1-β-D-Arabinofuranosylcytosine in Liposomal Preparations

作者: R. A. Schwendener , D. H. Horber , C. Ottiger , H. Schott

DOI: 10.3109/08982109509039906

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摘要: AbstractThe long chain N4-alkyl compounds N4-hexadecyl- and N4-octadecyl-1-β-D-arabinofuranosylcytosine (NHAC, NOAC) are new lipophilic derivatives of 1-β-D-arabinofuranosylcytosine (ara-C). They have the strongest antitumor activities in L1210 leukemia model among series substituents ranging from C6 to C22. Long circulating liposome formulations NHAC NOAC containing poly(ethylene)glycol modified lipids (PEG-liposomes) a better activity compared with plain liposomes. However, examination interactions both liposomal blood components revealed that drug is transferred liposomes at fast rates, regardless composition. mainly bound albumin, high low density lipoproteins HDL LDL erythrocytes. Thus, serve as pharmaceutical formulation permit solubilisation thei...

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