Treatment of l1210 murine leukemia with liposome‐incorporated N4‐hexadecyl‐1‐β‐D‐arabinofuranosyl cytosine
作者： R. A. Schwendener , H. Schott
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摘要: N4-alkyl-1-beta-D-arabinofuranosyl cytosines as lipophilic derivatives of the widely used anti-tumor drug 1-beta-D-arabinofuranosylcytosine (ara-C) were synthesized and incorporated into unilamellar liposomes. The resulting preparations yielded stable liposomes with diameters ranging between 40 70 nm. liposomal exhibited an increased effect against murine L1210 lymphoid leukemia at optimal molar concentrations which 16 times lower than those previously reported for free ara-C. N4-alkyl-ara-C alkyl chains containing 14-16 C-atoms highly effective whereas shorter showed no cytostatic effects. resistance to hydrolysis improved N4-hexadecyl-ara-C preparation compared other known N4-acyl-ara-C prodrugs, together possibility preparing large volumes sterile liposomes, hold out prospect more chemotherapy leukemias.
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