Enhanced antitumor effect of novel dual-targeted paclitaxel liposomes

Nanotechnology. 2010 Oct 15;21(41):415103. doi: 10.1088/0957-4484/21/41/415103. Epub 2010 Sep 17.

Abstract

A novel dual-targeted peptide containing an alpha V integrins specific ligand and a neuropilin-1 specific motif was developed which showed an increased specific targeting affinity to tumors. Active dual-targeted liposomes were then produced with this peptide and exhibited greater binding activity than single-targeted liposomes in vitro. Paclitaxel entrapped in this formulation greatly increased the uptake of paclitaxel in the targeting cells and significantly suppressed the growth of HUVEC and A549 cells compared with general paclitaxel injections (Taxol) and single-targeted paclitaxel liposomes. The treatment of tumor xenograft models with dual-targeted paclitaxel liposomes also resulted in better tumor growth inhibition than any other treatment groups. Therefore, the dual-targeted paclitaxel liposomes prepared in the present study might be a more promising drug for cancer treatment. Furthermore, the dual-targeting approach may produce synergistic effects that can be applied in the development of new targeted drug delivery systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Delivery Systems*
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Female
  • Fluorescein-5-isothiocyanate / metabolism
  • Fluorescence
  • Humans
  • Liposomes / metabolism*
  • Mice
  • Mice, Inbred BALB C
  • Molecular Sequence Data
  • Paclitaxel / pharmacology*
  • Peptides / chemistry
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Liposomes
  • Peptides
  • Fluorescein-5-isothiocyanate
  • Paclitaxel