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Current Pharmaceutical Biotechnology

Editor-in-Chief

ISSN (Print): 1389-2010
ISSN (Online): 1873-4316

In vivo behavior and Safety of Lapatinib-Incorporated Lipid Nanoparticles

Author(s): Huile Gao, Chen Chen, Zhangjie Xi, Jun Chen, Qizhi Zhang, Shilei Cao and Xinguo Jiang

Volume 14 , Issue 12 , 2013

Page: [1062 - 1071] Pages: 10

DOI: 10.2174/1389201015666140113110746

Price: $65

Abstract

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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