Large unilamellar liposomes with low uptake into the reticuloendothelial system.
Particulate drug carriers, including liposomes, are rapidly removed from blood by cells of the reticuloendothelial system (RES) with resulting adverse effects on this important host defense system. In order to overcome this and other major disadvantages of liposomes, we have altered liposome composition in an effort to achieve prolonged circulation half-lives. Gangliosides and sphingomyelin act synergistically to dramatically diminish the rate and extent of uptake of liposomes by macrophages in vivo. The significantly extended circulation times achieved by these modified large unilamellar liposomes overcome an important barrier to the targeting of particulate drug carriers to specific tissues in vivo.
Allen
T M
TM
Department of Pharmacology, University of Alberta, Edmonton, Canada.
Chonn
A
A
D002784:Cholesterol; D003692:Delayed-Action Preparations; D004705:Endocytosis; D005732:Gangliosides / Q000378:metabolism*; D008081:Liposomes / Q000493:pharmacokinetics*; D012157:Mononuclear Phagocyte System / Q000502:physiology*; D010713:Phosphatidylcholines; D013109:Sphingomyelins / Q000378:metabolism; D014018:Tissue Distribution
D003692:Delayed-Action Preparations; D005732:Gangliosides; D008081:Liposomes; D010713:Phosphatidylcholines; D013109:Sphingomyelins; D002784:Cholesterol