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This study investigated the feasibility of utilizing iron-oxide nanoparticles as a platform for the delivery of functional proteins to brain tumors via magnetic targeting. β-galactosidase-loaded particles were administered to glioma-bearing rats through a non-occlusively catheterized carotid artery with (test group) or without (control) magnetic targeting. Non-invasive MRI monitoring confirmed delivery of targeted nanoparticles to the tumor. Tumor lesions of magnetically targeted rats exhibited 7-fold increase in β-galactosidase activity compared to non-targeted animals, demonstrating feasibility of our approach.