Magnetoliposomes with high USPIO entrapping efficiency, stability and magnetic properties.

The DRV technique (followed by extrusion) was used for construction of hydrophilic-USPIO encapsulating liposomes. Magnetoliposomes (ML) were characterized for size, surface charge, entrapment, physical stability and magnetic properties (relaxivity). Results show that nanosized extruded-DRV MLs encapsulate higher amounts of USPIOs in comparison with sonicated vesicles. Fe (III) encapsulation efficiency (EE) is 12%, the highest reported to date for nanosized MLs. EE of MLs is influenced by ML membrane composition and polyethyleneglycol (PEG) coating. PEG-coating increases ML EE and stability; however, r(2)-to-r(1) ratios decrease (in comparison with non-PEGylated MLs). Most ML-types are efficient T2 contrast agents (because r(2)-to-r(1) ratios are higher than that of free USPIOs). Targeted MLs were formed by successfully immobilizing OX-26 monoclonal antibody on ML surface (biotin-streptavidin ligation), without significant loss of USPIOs. Targeted MLs retained their nanosize and integrity during storage for 1 month at 4 °C and up to 2 weeks at 37 °C.