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 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.
Asai
T
T
Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan.
Shuto
S
S
Matsuda
A
A
Kakiuchi
T
T
Ohba
H
H
Tsukada
H
H
Oku
N
N
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D003561:Cytarabine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D008081:Liposomes; D008175:Lung Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy*; D008297:Male; D008546:Melanoma, Experimental / Q000000981:diagnostic imaging / Q000188:drug therapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D014055:Tomography, Emission-Computed
D000970:Antineoplastic Agents; D008081:Liposomes; D003561:Cytarabine; C070279:2'-cyano-2'-deoxyarabinofuranosylcytosine