A. Kakee et al., STRUCTURE AND TUMOR NECROSIS FACTOR-INDUCING ACTIVITY OF DISPERSED PARTICLES OF A LIPID-A ANALOG, GLA-60, AND PHOSPHATIDYLCHOLINE MIXTURE, International journal of pharmaceutics, 111(1), 1994, pp. 15-24
A synthetic monosaccharide-analogue of lipid A, GLA-60, was co-dispers
ed with egg PC in aqueous solution. The size distribution and structur
e of the dispersed particles were investigated by the dynamic light sc
attering (DLS) and transmission electron microscopic (TEM) methods. Th
e particles were of liposomal structure with homogeneous size. The lea
kage of CF out of the liposomes in rat plasma was suppressed by augmen
ting GLA-60. Fluorescence anisotropy measurements showed that GLA-60 i
n lipid bilayers led to a rigid structure of the membranes. The activi
ty of tumor necrosis factor (TNF) induction in mice increased with the
content of GLA-60 in sonicated liposomes. The results showed that the
se liposomes were useful as GLA-60 formulations.