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

2'-C-cyano-2'-deoxy-1-beta -D-arabino-pentofuranosylcytosine (CNDAC) is a p otent anti-cancer agent, and we previously observed that liposomal formulat ion of 5'-O-dipalmitoylphosphatidyl derivative of CNDAC (DPP-CNDAC) is desi rable for targeting. For targeting to pulmonary cancer, we investigated the in vivo behavior of liposomes containing DPP-CNDAC by a non-invasive metho d using positron emission tomography. Liposomes composed of DPP-CNDAC and c holesterol (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 f ormulation or soluble CNDAC. These results suggest that DPP-CNDAC/CH liposo mes are useful for metastatic pulmonary cancer. (C) 2001 Elsevier Science I reland Ltd. All rights reserved.