Pharmacokinetics, Tissue Distribution and Excretion of AgS Quantum Dots in Mice and Rats: the Effects of Injection Dose, Particle Size and Surface Charge.

PURPOSE

We systematically investigated the effects of injection dose, particle size and surface charge on the pharmacokinetics, tissue distribution and excretion of AgS quantum dots (Qds) in rats and mice.

METHODS

Three different doses of AgS Qds with similar size and composition were administrated to rats and mice. The effect of size and surface charge was investigated with the injection of three sizes (5, 15 and 25 nm) of AgS Qds possessing similar surface charge, as well as 5 nm Qds with a positive surface charge.

RESULTS

Results indicated that pharmacokinetics and biodistribution of AgS Qds were strongly dose, particle size and surface charge dependent. By increasing the dose from 0.5 to 4.0 mg/kg, mean residence time (MRT) and apparent volume of distribution at steady state (V) were increased while clearance (CL) was decreased. Qds with a negative surface charge had significantly larger MRT and V values than positively charged particles, but their CL was about 50% lower than that of positively charged ones. By increasing Qds size from 5 to 25 nm, CL was increased while MRT and AUC were decreased.

CONCLUSIONS

This study establishes comprehensive principles for the rational design and tailoring of AgS Qds for biomedical applications. Graphical Abstract The effects of injection dose, particle size and surface charge on pharmacokinetics and tissue distribution of AgS Qds after intravenous injection into rats and mice were investigated.