Intracellular peptide delivery using amphiphilic lipid-based formulations

Biotechnol Bioeng. 2011 Oct;108(10):2477-87. doi: 10.1002/bit.23182. Epub 2011 Apr 25.

Abstract

Peptides, highly diverse by their nature, are important biochemical and pharmaceutical tools: ligands for cellular receptors, transcription factors, immunosuppressants, vaccines, etc. As the majority of their targets are intracellular, peptides need to cross the plasma membrane and gain access to the cytoplasm. However, due to their physicochemical properties, most peptides need to be entrapped by a molecular vehicle to be able to reach the cytosol compartment. In this study, we present new biological tools to enhance intracellular peptides delivery. Based on electrostatic interactions, two complementary types of amphiphilic molecules have been designed as delivery vehicles. A diverse set of fluorescently labeled peptides have successfully been delivered. This opens the avenue for the use of peptides combined to delivery vehicles as therapeutic aids.

Keywords: amphiphilic lipids; cell uptake; intracellular peptide delivery; live cells.

MeSH terms

  • Drug Delivery Systems / methods*
  • HeLa Cells
  • Humans
  • Lipids / chemistry*
  • Peptides / chemistry*

Substances

  • Lipids
  • Peptides