British Journal of Rheumatology 1995;34:241-245 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 /ig MTX per 250 fig lipid) was a potent inhibitor of both IL-1/? 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 ng lipid/well) of the same lipid composition and free MTX (up to 100 /xg/well) had no effect on either mediator