Rh. Muller et al., CYTOTOXICITY OF MAGNETITE-LOADED POLYLACTIDE, POLYLACTIDE GLYCOLIDE PARTICLES AND SOLID LIPID NANOPARTICLES/, International journal of pharmaceutics, 138(1), 1996, pp. 85-94
Particles from polylactide (PLA), polylactide/glycolide (PLA/GA) and s
olid lipid nanoparticles (SLN) were produced and loaded with different
amounts of magnetite, The in vitro cytotoxicity was determined to ass
ess their toxicological acceptance as intravenous formulation for magn
etic resonance imaging and as potential carrier for drug targeting. Vi
ability determinations were performed in suspensions of human granuloc
ytes using the dimethylthiazolyl-diphenyltetrazolium (MTT) test. Parti
cle internalization by the granulocytes was followed using luminol enh
anced chemiluminescence (CL). The effective concentrations to reduce t
he viability to 50% (ED 50%) were 0.38% and 0.30% for high and low mol
ecular weight PLA, 0.15% for PLA/GA. The mechanism of toxicity is the
intracellular uptake, with the highest toxicity being observed for the
faster degrading polymers, low molecular weight PLA and PLA/GA. The s
olid lipid nanoparticles proved to be the least cytotoxic preparation
with an effective concentration (ED 50%) above 10%.