Utility of liposomes coated with polysaccharide bearing 1-amino-lactose as targeting chemotherapy for AH66 hepatoma cells.
The cell recognition element is very important for drug delivery systems. We synthesized cholesteryl pullulan (CHP) bearing 1-aminolactose (1-AL) and introduced a saccharide, cholesteryl pullulan bearing 1-aminolactose (1-AL/CHP), to an outer layer of the conventional liposome as a cell recognition element. Lectin recognized the beta-galactose by aggregation of 1-AL/CHP coated liposome (1-AL/CHP liposome). The uptake of this liposome to AH66 rat hepatoma cells was greater than in liposomes without 1-aminolactose in vitro. Furthermore, 1-AL/CHP liposomal adriamycin showed a stronger antitumor effect in comparison with other types of liposomal adriamycin in vitro. When in vivo tumor-targeting efficacy was investigated in AH66 tumor transplanted mice using 3H-liposome, the tumor/serum radioactivity ratio in mice injected with 1-AL/CHP liposome was higher than that of mice injected with other liposomes. These observations suggest that 1-AL is effective as a cell recognition element. As a result, 1-AL/CHP liposome is considered to be a good carrier of anticancer drugs for the active targeting of tumor cells.
Yamamoto
M
M
Department of Surgery II, Nagasaki University School of Medicine, Nagasaki 852-8501, Japan.
Ichinose
K
K
Ishii
N
N
Khoji
T
T
Akiyoshi
K
K
Moriguchi
N
N
Sunamoto
J
J
Kanematsu
T
T
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D004317:Doxorubicin / Q000008:administration & dosage; D016503:Drug Delivery Systems; D005936:Glucans / Q000008:administration & dosage*; D008081:Liposomes; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D051381:Rats; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D005936:Glucans; D008081:Liposomes; D004317:Doxorubicin; C009109:pullulan