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

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 chel...

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Bibliographic Details
Published in:Biopolymers 2015-11, Vol.104 (6), p.712-719
Main Authors: Goswami, Dibakar, Vitorino, Hector Aguilar, Machini, M. Teresa, Espósito, Breno P.
Format: Article
Language:English
Subjects:
Animals
Benzoates - chemistry
Biopolymers
Blood-brain barrier
Carrier Proteins - chemistry
Cell Line - chemistry
Cell Membrane Permeability
cell-penetrating peptides
Chromatography, High Pressure Liquid
Circular Dichroism
Conjugates
curcumin
Curcumin - administration & dosage
deferasirox
Drug Carriers
Drug delivery systems
Drugs
Hydrophobic and Hydrophilic Interactions
Iron
Micelles
Microscopy, Electron, Transmission
nanofibers
Nanostructure
neurodegeneration
penetratin
Rats
Spectrometry, Fluorescence
Spectrometry, Mass, Electrospray Ionization
Triazoles - chemistry
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Summary: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. © 2015 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 104: 712–719, 2015.
ISSN:0006-3525
1097-0282
DOI:10.1002/bip.22672