N. Scholer et al., Surfactant, but not the size of solid lipid nanoparticles (SLN) influencesviability and cytokine production of macrophages, INT J PHARM, 221(1-2), 2001, pp. 57-67
After intravenous (i.v.) injection, solid lipid nanoparticles (SLN) interac
t with mononuclear cells. Murine peritoneal macrophages were incubated with
SLN formulations consisting of Dynasan 114 coated with different surfactan
ts. The present study was performed to examine the impact of surfactants, w
hich are important surface defining components of SLN, on viability and cyt
okine production by macrophages. Cytotoxicity, as assessed by the 3-(4,5-di
methylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) test, was strong
ly influenced by the surfactant used being marked with cetylpyridinium chlo
ride- (CPC-) coated SLN at a concentration of 0.001%, and further increased
at SLN concentrations of 0.01 and 0.1%. All other SLN formulations - conta
ining Poloxamine 908 (P908), Poloxamer 407 (P407), Poloxamer 188 (P188), So
lutol HS15 (HS15), Tween 80 (T80), Lipoid S75 (S75), sodium cholate (SC), o
r sodium dodecylsulfate (SDS) - when used at the same concentrations reduce
d cell viability only slightly. None of the SLN formulations tested induced
cytokine production but a concentration-dependent decrease of IL-6 product
ion was observed, which appeared to be associated with cytotoxic effects. I
L-12 and TNF-alpha were detected neither in supernatants of macrophages tre
ated with SLN at any concentration nor in those of untreated cells. In cont
rast to the type of surfactant, the size of SLN was found neither to affect
cytotoxicity, of SLN nor to result in induction or digression of cytokine
production by macrophages. In conclusion, testing the effects of surfactant
s on SLN on activity of macrophages is a prerequisite prior to in vivo use
of SLN, (C) 2001 Elsevier Science B.V. All rights reserved.