Therapeutic effect of reticuloendothelial system (RES)-avoiding liposomes containing a phospholipid analogue of 5-fluorouracil, dipalmitoylphosphatidylfluorouridine, in Meth A sarcoma-bearing mice.

Abstract

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.

• Authors: K Doi, N Oku, T Toyota, S Shuto, A Sakai, H Itoh, S Okada
• Journal: Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 17 Issue 10 Pg. 1414-6 (Oct 1994) ISSN: 0918-6158 [Print] Japan
• PMID: 7874068 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Drug Carriers
• Glucuronates
• Glycerophospholipids
• Lipid Bilayers
• Liposomes
• Phosphatidic Acids
• Phosphatidylglycerols
• Phospholipids
• 1,2-dipalmitoylphosphatidylfluorouridine
• 1-O-palmitylglucuronic acid
• 1,2-Dipalmitoylphosphatidylcholine
• Methylcholanthrene
• Fluorouracil
• 1,2-dipalmitoylphosphatidylglycerol
• Uridine

Topics

• 1,2-Dipalmitoylphosphatidylcholine (metabolism, pharmacology, therapeutic use)
• Animals
• Antineoplastic Agents (administration & dosage, pharmacology, therapeutic use)
• Cell Division (drug effects)
• Drug Carriers
• Drug Delivery Systems
• Fluorouracil (analogs & derivatives, therapeutic use)
• Glucuronates (metabolism, pharmacology)
• Glycerophospholipids
• Injections, Intravenous
• Lipid Bilayers (metabolism)
• Liposomes
• Methylcholanthrene
• Mice
• Mice, Inbred BALB C
• Mononuclear Phagocyte System (drug effects, metabolism)
• Phosphatidic Acids (administration & dosage, pharmacology, therapeutic use)
• Phosphatidylglycerols (metabolism, pharmacology, therapeutic use)
• Phospholipids (therapeutic use)
• Sarcoma, Experimental (chemically induced, drug therapy)
• Uridine (administration & dosage, analogs & derivatives, pharmacology, therapeutic use)