Therapeutic effect of reticuloendothelial system (RES)-avoiding liposomes containing a phospholipid analogue of 5-fluorouracil, dipalmitoylphosphatidylfluorouridine, in Meth A sarcoma-bearing mice.
Reticuloendothelial system (RES)-avoiding liposomes are known to accumulate in tumor tissues due to passive targeting. Dipalmitoylphosphatidylfluorouridine (DPPF), a potent antitumor agent readily incorporated into the lipid bilayer, was embedded in RES-avoiding liposomes modified with a uronic acid derivative, palmityl-D-glucuronide (PGlcUA). The therapeutic effect of DPPF in PGlcUA-liposomes was examined in tumor-bearing mice. Free or liposomal DPPF was injected intravenously into BALB/c mice bearing subcutaneously implanted Meth A sarcomas. The RES-avoiding liposomal formulation using PGlcUA was effective in reducing tumors, and prolonging survival time compared with free DPPF and also DPPF in conventional liposomes. Therefore, PGlcUA-liposomes might be of practical use as drug carriers for anticancer agents, especially their derivatives for embedding in liposomal membranes.
Doi
K
K
Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Oku
N
N
Toyota
T
T
Shuto
S
S
Sakai
A
A
Itoh
H
H
Okada
S
S
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use; D002455:Cell Division / Q000187:drug effects; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000031:analogs & derivatives / Q000627:therapeutic use; D005965:Glucuronates / Q000378:metabolism / Q000494:pharmacology; D020404:Glycerophospholipids; D007275:Injections, Intravenous; D008051:Lipid Bilayers / Q000378:metabolism; D008081:Liposomes; D008748:Methylcholanthrene; D051379:Mice; D008807:Mice, Inbred BALB C; D012157:Mononuclear Phagocyte System / Q000187:drug effects / Q000378:metabolism; D010712:Phosphatidic Acids / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use; D010715:Phosphatidylglycerols / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D010743:Phospholipids / Q000627:therapeutic use; D012513:Sarcoma, Experimental / Q000139:chemically induced / Q000188:drug therapy*; D014529:Uridine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use
D000970:Antineoplastic Agents; D004337:Drug Carriers; D005965:Glucuronates; D020404:Glycerophospholipids; D008051:Lipid Bilayers; D008081:Liposomes; D010712:Phosphatidic Acids; D010715:Phosphatidylglycerols; D010743:Phospholipids; C082139:1,2-dipalmitoylphosphatidylfluorouridine; C065782:1-O-palmitylglucuronic acid; D015060:1,2-Dipalmitoylphosphatidylcholine; D008748:Methylcholanthrene; D005472:Fluorouracil; C030345:1,2-dipalmitoylphosphatidylglycerol; D014529:Uridine