Rh. Muller et al., CYTOTOXICITY OF SOLID LIPID NANOPARTICLES AS A FUNCTION OF THE LIPID MATRIX AND THE SURFACTANT, Pharmaceutical research, 14(4), 1997, pp. 458-462
Purpose. Assessment of the in vitro cytotoxicity of solid lipid nanopa
rticles (SLNs) as a function of lipid matrix (Dynasan 114, Compritol A
TO 888), and stabilizing surfactant (poloxamers, Tween 80, soya lecith
in, and sodium dodecyl sulphate). Comparison with other colloidal carr
iers should determine their potential use in the clinic. Methods, SLNs
were produced by high pressure homogenisation. Cytotoxicity was asses
sed by measuring the viability of HL60 cells and human granulocytes af
ter incubation with SLNs. Particle internalisation was quantified by c
hemiluminescence measurements. Results. The nature of the lipid had no
effect on viability; distinct differences were found for the surfacta
nts. Binding to the SLN surface reduced markedly the cytotoxic effect
of the surfactants, e.g., up to a factor of 65 for poloxamer 184. The
permanent HL60 cell line-differentiated from cells with granulocyte ch
aracteristics by retinoic acid treatment-yielded results identical to
freshly isolated human granulocytes. In general, the SLNs showed a low
er cytotoxicity compared to polyalkylcyanoacrylate and polylactic/glyc
olic acid (PLA/GA) nanoparticles. Conclusions. Because the results are
identical when using human granulocytes, differentiated HL60 cells ca
n be used as an easily accessible in vitro test system for i.v. inject
able SLN formulations. The SLNs appear suitable as a drug carrier syst
em for potential intravenous use due to their very low cytotoxicity in
vitro.