title: 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 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.
authors.affiliation: Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, Av. Lineu Prestes 748, 05508-000, São Paulo, Brazil.|Bio-Organic Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085, India.
authors.forename: Dibakar
authors.initials: D
authors.lastname: Goswami
authors.affiliation: Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, Av. Lineu Prestes 748, 05508-000, São Paulo, Brazil.
authors.forename: Hector Aguilar
authors.initials: HA
authors.lastname: Vitorino
authors.affiliation: Departamento de Bioquímica, Instituto de Química, Universidade de São Paulo, Av. Lineu Prestes 748, 05508-000, São Paulo, Brazil.
authors.forename: M Teresa
authors.initials: MT
authors.lastname: Machini
authors.affiliation: Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, Av. Lineu Prestes 748, 05508-000, São Paulo, Brazil.
authors.forename: Breno P
authors.initials: BP
authors.lastname: Espósito
mesh_terms: D000818:Animals; D001565:Benzoates / Q000737:chemistry*; D002352:Carrier Proteins / Q000737:chemistry*; D002460:Cell Line / Q000737:chemistry*; D002463:Cell Membrane Permeability; D057846:Cell-Penetrating Peptides; D002851:Chromatography, High Pressure Liquid; D002942:Circular Dichroism; D003474:Curcumin / Q000008:administration & dosage; D000077588:Deferasirox; D004337:Drug Carriers; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D051381:Rats; D013050:Spectrometry, Fluorescence; D021241:Spectrometry, Mass, Electrospray Ionization; D014230:Triazoles / Q000737:chemistry*
chemical_list: D001565:Benzoates; D002352:Carrier Proteins; D057846:Cell-Penetrating Peptides; D004337:Drug Carriers; D008823:Micelles; D014230:Triazoles; C414409:penetratin; D003474:Curcumin; D000077588:Deferasirox
keywords: cell-penetrating peptides; curcumin; deferasirox; iron; nanofibers; neurodegeneration; penetratin