Asialoglycoprotein receptor-targeted superparamagnetic iron oxide nanoparticles.

摘要: Superparamagnetic iron oxide (SPIO) nanoparticles are primarily used as contrast agents in magnetic resonance imaging. SPIO have also been derivatized to add targeting and drug-carrier functionality drug delivery devices. The preparation characterization of amino-functionalized (ASPIO) lactose-derivatized galactose-terminal-ASPIO now reported. target for is the cell-surface asialoglycoprotein receptor (ASGPR) expressed by hepatocytes. Two batches ASPIO with average particle sizes 61 [42]nm 127 [125]nm [full-width half maximum; FWHM] were prepared. small increased from nm 278 [309]nm upon lactosylation (Gal-ASPIO-278) 302 [280] N-acetylation (NAcASPIO-302); larger afforded galactosyl-terminal 337 [372]nm N-acetylated 326 [308]nm. LD50 Gal-ASPIO-278 was 1500 microg/mL HepG2 cells; associated cells vitro, whereas NAcSPIO-302, prepared same batch, did not. NAcASPIO-302 not bound ASPGR non-expressing 143B cells. association reduced free galactose, supporting model ASGPR-mediated binding. These data underline potential application Gal-ASPIO a targeted ligand ASPGR-expressing vivo.