Targeting and anti-tumor efficacy of liposomal 5'-O-dipalmitoylphosphatidyl 2'-C-cyano-2'-deoxy-1-beta-D-arabino-pentofuranosylcytosine in mice lung bearing B16BL6 melanoma

Cancer Lett. 2001 Jan 10;162(1):49-56. doi: 10.1016/s0304-3835(00)00633-9.

Abstract

2'-C-cyano-2'-deoxy-1-beta-D-arabino-pentofuranosylcytosine (CNDAC) is a potent anti-cancer agent, and we previously observed that liposomal formulation of 5'-O-dipalmitoylphosphatidyl derivative of CNDAC (DPP-CNDAC) is desirable for targeting. For targeting to pulmonary cancer, we investigated the in vivo behavior of liposomes containing DPP-CNDAC by a non-invasive method using positron emission tomography. Liposomes composed of DPP-CNDAC and cholesterol (DPP-CNDAC/CH liposomes) were markedly accumulated in mice lung bearing B16BL6 melanoma. In metastatic pulmonary cancer model, DPP-CNDAC/CH liposomes significantly reduced the lung colonization in a dose-dependent manner. The activity was significantly superior to conventional liposomal formulation or soluble CNDAC. These results suggest that DPP-CNDAC/CH liposomes are useful for metastatic pulmonary cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Cytarabine / administration & dosage
  • Cytarabine / analogs & derivatives*
  • Liposomes
  • Lung Neoplasms / diagnostic imaging
  • Lung Neoplasms / drug therapy*
  • Male
  • Melanoma, Experimental / diagnostic imaging
  • Melanoma, Experimental / drug therapy*
  • Mice
  • Mice, Inbred C57BL
  • Tomography, Emission-Computed

Substances

  • Antineoplastic Agents
  • Liposomes
  • Cytarabine
  • 2'-cyano-2'-deoxyarabinofuranosylcytosine