In vivo behavior and Safety of Lapatinib-Incorporated Lipid Nanoparticles
To improve the solubility, bioavailability and anti-tumor effect of lapatinib, lapatinib-incorporated lipid
nanoparticles (LTNPs) were prepared and characterized. The particle size of LTNPs was 88.6 nm with a zeta potential of
20 mV. Laptinib was loaded into LTNPs with a non-crystal structure as determined by FT-IR. In vitro, LTNPs could be
effectively uptaken into C6 glioma cells at a concentration-dependent manner. In vivo, LTNPs showed a relative higher
AUC, which was 5.27- and 3.21-fold as that of Tykerb and lapatinib suspension (LTS) group. LTNPs also showed highest
glioma concentration, which may benefit from the enhanced permeability and retention effect and active targeting ability.
In toxicity studies, LTNPs displayed a half lethal dose over 250 mg/kg. Repeated administering 30 mg/kg of LTNPs could
led to toxicity to hematology which might owe to the bovine serum albumin, a foreign protein to mice. However, there
was no organic change observed through HE staining. In conclusion, LTNPs could target to glioma with high concentration
and low side effect.
Keywords: Lapatinib, pharmacokinetic, tissue distribution, toxicity.
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