Self-assembled penetratin-deferasirox micelles as potential carriers for hydrophobic drug delivery

Biopolymers. 2015 Nov;104(6):712-9. doi: 10.1002/bip.22672.

Abstract

There has been a growing interest in the use of micelles with nanofiber geometry as nanocarriers for hydrophobic drugs. Here we show that the conjugate of penetratin, a cell-penetrating peptide (CPP) with blood-brain barrier (BBB) permeability, and deferasirox (DFX), a hydrophobic iron chelator, self-assembles to form micelles at a very low concentration (∼15 mg/L). The critical micelle concentration (CMC) was determined, and the micelles were used for solubilizing curcumin, a hydrophobic anti-neurodegenerative drug, for successful delivery across RBE4 cells, a BBB model. Transmission Electron Microscope images of the curcumin-loaded micelles confirmed the formation of nanofibers. These results indicate the potential of CPP-drug conjugates for use as nanocarriers.

Keywords: cell-penetrating peptides; curcumin; deferasirox; iron; nanofibers; neurodegeneration; penetratin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoates / chemistry*
  • Carrier Proteins / chemistry*
  • Cell Line / chemistry*
  • Cell Membrane Permeability
  • Cell-Penetrating Peptides
  • Chromatography, High Pressure Liquid
  • Circular Dichroism
  • Curcumin / administration & dosage
  • Deferasirox
  • Drug Carriers*
  • Hydrophobic and Hydrophilic Interactions
  • Micelles*
  • Microscopy, Electron, Transmission
  • Rats
  • Spectrometry, Fluorescence
  • Spectrometry, Mass, Electrospray Ionization
  • Triazoles / chemistry*

Substances

  • Benzoates
  • Carrier Proteins
  • Cell-Penetrating Peptides
  • Drug Carriers
  • Micelles
  • Triazoles
  • penetratin
  • Curcumin
  • Deferasirox