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

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. © 2015 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 104: 712–719, 2015.