title: Bolaamphiphilic vesicles encapsulating iron oxide nanoparticles: new vehicles for magnetically targeted drug delivery.
abstract: Bolaamphiphiles - amphiphilic molecules consisting of two hydrophilic headgroups linked by a hydrophobic chain - form highly stable vesicles consisting of a monolayer membrane that can be used as vehicles to deliver drugs across biological membranes, particularly the blood-brain barrier (BBB). We prepared new vesicles comprising bolaamphiphiles (bolavesicles) that encapsulate iron oxide nanoparticles (IONPs) and investigated their suitability for targeted drug delivery. Bolavesicles displaying different headgroups were studied, and the effect of IONP encapsulation upon membrane interactions and cell uptake were examined. Experiments revealed more pronounced membrane interactions of the bolavesicles assembled with IONPs. Furthermore, enhanced internalization and stability of the IONP-bolavesicles were observed in b.End3 brain microvessel endothelial cells - an in vitro model of the blood-brain barrier. Our findings indicate that embedded IONPs modulate bolavesicles' physicochemical properties, endow higher vesicle stability, and enhance their membrane permeability and cellular uptake. IONP-bolavesicles thus constitute a promising drug delivery platform, potentially targeted to the desired location using external magnetic field.
authors.affiliation: Department of Chemistry and Ilse Katz Institute of Nanotechnology, Faculty of Natural Sciences, Ben-Gurion University of the Negev, Beer Sheva, Israel.
authors.forename: Liron
authors.initials: L
authors.lastname: Philosof-Mazor
authors.forename: George R
authors.initials: GR
authors.lastname: Dakwar
authors.forename: Mary
authors.initials: M
authors.lastname: Popov
authors.forename: Sofiya
authors.initials: S
authors.lastname: Kolusheva
authors.forename: Alexander
authors.initials: A
authors.lastname: Shames
authors.forename: Charles
authors.initials: C
authors.lastname: Linder
authors.forename: Sarina
authors.initials: S
authors.lastname: Greenberg
authors.forename: Eliahu
authors.initials: E
authors.lastname: Heldman
authors.forename: David
authors.initials: D
authors.lastname: Stepensky
authors.forename: Raz
authors.initials: R
authors.lastname: Jelinek
mesh_terms: D000818:Animals; D002460:Cell Line; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D004705:Endocytosis; D005663:Furans / Q000008:administration & dosage / Q000737:chemistry*; D008051:Lipid Bilayers / Q000378:metabolism; D060328:Magnetic Phenomena; D058185:Magnetite Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D051379:Mice; D011728:Pyridones / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D005663:Furans; D008051:Lipid Bilayers; D058185:Magnetite Nanoparticles; D011728:Pyridones; C543575:bolaamphiphile