[Tissue distribution of TPGS modified artesunate liposome and its metabolites in rats]

Zhongguo Zhong Yao Za Zhi. 2018 Jan;43(2):325-331. doi: 10.19540/j.cnki.cjcmm.20171023.006.
[Article in Chinese]

Abstract

Artesunate, which is a widely used anti-malaria medicine, can be made into liposome to overcome its poor bioactivity. Its tissue distribution in rats may change with different dosage forms, which therefore shall be studied after ARS-TPGS-Lipo was injected. Based on this experiment, ARS-TPGS-Lipo and ARS-Lipo were prepared by thin-film hydration method. LC-MS/MS method was used to simultaneously determine ARS and DHA in rat tissues at different time points. The results showed that this method was suitable for the content analysis of ARS and DHA in biological samples. The distribution of ARS and DHA in ARS-TPGS-Lipo, ARS-Lipo and ARS groups were quite different. The content of ARS-TPGS-Lipo in liver was the highest, with significant differences.ARS and DHA contents in ARS group eliminated rapidly. ARS and DHA contents in ARS-Lipo group were higher in liver and spleen, while those in ARS-TPGS-Lipo group significantly increased only in liver (P<0.05).

Keywords: LC-MS/MS; TPGS modified artesunate liposome; tissue distribution.

MeSH terms

  • Animals
  • Artesunate / pharmacokinetics*
  • Chromatography, Liquid
  • Liposomes*
  • Rats
  • Tandem Mass Spectrometry
  • Tissue Distribution
  • Vitamin E*

Substances

  • Liposomes
  • Vitamin E
  • Artesunate
  • tocophersolan