Effect of Cholesterol Content on Antitumor Activity and Toxicity of Liposome-encapsulated 1-β-D-Arabinofuranosylcytosine in Vivo

Ram Ganapathi, Awtar Krishan, C. Gordon Zubrod, Isidore Wodinsky, Lawrence J. Lesko

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Abstract

1-β-D-Arabinofuranosylcytosine (ara-C) was encapsulated in anionic multilamellar liposomes prepared with different lecithin:cholesterol (L:C) ratios. The chemotherapeutic activity of encapsulated ara-C was compared with comparable doses of ara-C in 0.85% saline solution (single- and multiple-dose schedules) in mice bearing L1210 (i.p.) leukemia. Maximum survival was obtained in animals given injections of ara-C (40 mg/kg) encapsulated in liposomes with a L:C ratio of 1:1. The effect of L:C ratio on survival was not pronounced in multiple-dose schedules. Multiple doses (every 4.5 hr for 3 separate injections) of 40 mg/kg with L:C ratios of 1:1 and 1:0.5 were toxic, resulting in 83 and 50% mortality, respectively, of mice by Day 7. This study shows that drug efflux and in vivo antitumor activity and toxicity of encapsulated ara-C is influenced by the cholesterol content of the liposomal lipid bilayer.

Original languageEnglish (US)
Pages (from-to)630-633
Number of pages4
JournalCancer Research
Volume40
Issue number3
StatePublished - Mar 1 1980

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ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Ganapathi, R., Krishan, A., Zubrod, C. G., Wodinsky, I., & Lesko, L. J. (1980). Effect of Cholesterol Content on Antitumor Activity and Toxicity of Liposome-encapsulated 1-β-D-Arabinofuranosylcytosine in Vivo. Cancer Research, 40(3), 630-633.