Abstract:

BACKGROUND: Based on its good water-solubility and histocompatibility, aldehyde sodium alginate (ASA) can be used as a modifier to improve surfactivity and stability of magnetic Fe3O4 nanoparticles. Folate acid (FA) can be used as a targeting molecule for carrier.
OBJECTIVE: To prepare cisplatin (CDDP)-loaded magnetic nanomedicine (CDDP-FA-ASA-MNPs) with abilities of folate receptor targeting and magnetic targeting.
METHODS: ASA was prepared from sodium alginate by sodium periodate oxidation. FA was activated by dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (NHS), and coupled with diaminopolyethylene glycol [PEG (NH2)2] to prepare FA-PEG. Fe3O4 nanoparticles were prepared using the chemical coprecipitation method. The carboxyl group in side chain of ASA was combined with hydroxyl group in Fe3O4 nanoparticles at 85 ℃. And then FA-PEG was connected with ASA by Schiff’s base. Finally, -Cl in CDDP was replaced by hydroxyl group in ASA based on principles of coordination complex, so FA and ASA modified CDDP-loaded magnetic nanoparticles (MNPs) were prepared.
RESULTS AND CONCLUSION: CDDP-FA-ASA-MNPs prepared by this method could distribute stably in aqueous solution. The mean diameter of Fe3O4 core was (8.116±0.24) nm, hydrodynamic diameter was (110.9±1.7) nm, Zeta potential was (-26.45± 1.26) mV, maximum saturation magnetization was 56.2 emu/g, CDDP encapsulation efficiency was (49.05±1.58)%, and drug loading property was (14.31±0.49)%. In vitro, CDDP-FA-ASA-MNPs were selectively uptaked by HNE-1 cells and Hep-2 cells which expressed folate receptors positively, but not uptaked by CNE-2 which expressed folate receptor negatively. CDDP-FA- ASA-MNPs prepared by this method have good water-solubility and stability. It can be uptaked by nasopharyngeal carcinoma cells and laryngeal carcinoma cells with folate receptors positively.