The effect of liposomally conjugated methotrexate upon mediator release from human peripheral blood monocytes.
The ability of methotrexate (MTX) and a liposomal preparation containing a lipophilic conjugate of methotrexate (MTX-LIPO) to modulate pro-inflammatory mediator release from lipopolysaccharide-stimulated human peripheral blood monocytes was investigated. At non-toxic concentrations MTX-LIPO (10 micrograms MTX per 250 micrograms lipid) was a potent inhibitor of both IL-1 beta and TNF release resulting in 70.07 +/- 2.3% and 59.19 +/- 2.36% (mean +/- S.E.M.) inhibition, respectively, whereas empty liposomes (E-LIPO; 250 micrograms lipid/well) of the same lipid composition and free MTX (up to 100 micrograms/well) had no effect on either mediator.
Williams
A S
AS
Rheumatology Research Laboratory, University of Wales College of Medicine, Heath Park, Cardiff.
Punn
Y L
YL
Amos
N
N
Cooper
A M
AM
Williams
B D
BD
D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers; D006801:Humans; D007375:Interleukin-1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D007963:Leukocytes, Mononuclear / Q000187:drug effects* / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D008081:Liposomes; D008727:Methotrexate / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism*
D004337:Drug Carriers; D007375:Interleukin-1; D008070:Lipopolysaccharides; D008081:Liposomes; D014409:Tumor Necrosis Factor-alpha; D008727:Methotrexate