Bolaamphiphilic vesicles encapsulating iron oxide nanoparticles: New vehicles for magnetically targeted drug delivery

• Published in: International journal of pharmaceutics Vol. 450; no. 1-2; pp. 241 - 249
• Main Authors: Philosof-Mazor, Liron, Dakwar, George R., Popov, Mary, Kolusheva, Sofiya, Shames, Alexander, Linder, Charles, Greenberg, Sarina, Heldman, Eliahu, Stepensky, David, Jelinek, Raz
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 25.06.2013
• Subjects: Animals; Bolaamphiphiles; Cell Line; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Endocytosis; Furans - administration & dosage; Furans - chemistry; Iron oxide nanoparticles; Lipid Bilayers - metabolism; Magnetic nanoparticles; Magnetic Phenomena; Magnetite Nanoparticles - administration & dosage; Magnetite Nanoparticles - chemistry; Mice; Nano-drug delivery systems; Pyridones - administration & dosage; Pyridones - chemistry; Targeted drug delivery; Targeted drug delivery; Nano-drug delivery systems; Iron oxide nanoparticles; Bolaamphiphiles; Magnetic nanoparticles
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2013.04.017

Cells incubated with IONPs-containing bolavesicles (GLH-20). The background has been colored (green). Rapid migration of the cells (dark blue) toward the externally placed magnet was recorded. 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.