Cytotoxicity of solid lipid nanoparticles as a function of the lipid matrix and the surfactant.
OBJECTIVE
Assessment of the in vitro cytotoxicity of solid lipid nanoparticles (SLNs) as a function of lipid matrix (Dynasan 114, Compritol ATO 888), and stabilizing surfactant (poloxamers, Tween 80, soya lecithin, and sodium dodecyl sulphate). Comparison with other colloidal carriers should determine their potential use in the clinic.


METHODS
SLNs were produced by high pressure homogenisation. Cytotoxicity was assessed by measuring the viability of HL60 cells and human granulocytes after incubation with SLNs. Particle internalisation was quantified by chemiluminescence measurements.


RESULTS
The nature of the lipid had no effect on viability; distinct differences were found for the surfactants. 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 characteristics by retinoic acid treatment-yielded results identical to freshly isolated human granulocytes. In general, the SLNs showed a lower cytotoxicity compared to polyalkylcyanoacrylate and polylactic/glycolic acid (PLA/ GA) nanoparticles.


CONCLUSIONS
Because the results are identical when using human granulocytes, differentiated HL60 cells can be used as an easily accessible in vitro test system for i.v. injectable SLN formulations. The SLNs appear suitable as a drug carrier system for potential intravenous use due to their very low cytotoxicity in vitro.
Müller
R H
RH
Department of Pharmaceutics, Biopharmaceutics & Biotechnology, Free University of Berlin.
Rühl
D
D
Runge
S
S
Schulze-Forster
K
K
Mehnert
W
W
D002470:Cell Survival / Q000187:drug effects*; D004337:Drug Carriers; D018922:HL-60 Cells; D006801:Humans; D008055:Lipids / Q000737:chemistry / Q000633:toxicity*; D010316:Particle Size; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology*
D004337:Drug Carriers; D008055:Lipids; D013501:Surface-Active Agents