PEG-chitosan-coated iron oxide nanoparticles with high saturated magnetization as carriers of 10-hydroxycamptothecin: Preparation, characterization and cytotoxicity studies

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2013-02, Vol.102, p.37-44
• Main Authors: Qu, Jian-Bo, Shao, Hui-Hui, Jing, Guang-Lun, Huang, Fang
• Format: Article
• Language: English
• Subjects: 10-Hydroxycamptothecin; Anticancer; Camptothecin - analogs & derivatives; Camptothecin - chemistry; Cell Survival - drug effects; Chitosan - chemistry; Drug Carriers - adverse effects; Drug Carriers - chemistry; Ferric Compounds - chemistry; Hep G2 Cells; Humans; Magnetic composite nanoparticles; Nanoparticles - adverse effects; Nanoparticles - chemistry; Nonspecific adsorption; Polyethylene Glycols - chemistry; Reverse ultrasonic emulsification; Superparamagnetic
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2012.08.004

[Display omitted] ► A nano-sized carrier with a high saturated magnetization was prepared by a novel reverse ultrasonic emulsification method. ► The unspecific adsorption of protein on PEG-CS-Fe3O4 decreased significantly after coupling PEG. ► Water-insoluble HCPT was loaded onto PEG-CS-Fe3O4 by a subtle precipitation method. ► The HCPT-loaded PEG-CS-Fe3O4 exhibited a high cytotoxicity against HepG2 cells. A magnetic nano-sized carrier for 10-hydroxycamptothecin (HCPT) was prepared by using Fe3O4 nanoparticles as cores and chitosan (CS) as a polymeric shell by a novel reverse ultrasonic emulsification method. Poly(ethylene glycol) (PEG) chains were then coupled onto the magnetic particles (CS-Fe3O4) to improve their biocompatibility (PEG-CS-Fe3O4). HCPT was loaded onto PEG-CS-Fe3O4 by a subtle precipitation method. Under optimum conditions, the CS-Fe3O4 was close to spherical in shape with an average size of 174nm and a high saturated magnetization. After coupling PEG chains, the unspecific adsorption of bovine serum albumin (BSA) on PEG-CS-Fe3O4 decreased significantly. The drug loading content and loading efficiency were 9.8–11.8% and 49–59% for magnetic composite nanoparticles, respectively. HCPT-loaded magnetic composite nanoparticles showed sustained release profiles up to 48h, and the cumulative release amount of HCPT from nanoparticles at 45°C increased significantly compared to that at 37°C. Cytotoxicity assay suggests that CS-Fe3O4 does not exhibit noteworthy cytotoxicity against HepG2 cells, but the antitumor activities of HCPT-loaded magnetic composite nanoparticles against HepG2 cells increased significantly in comparison with that of pristine HCPT powder. These results reveal the promising potential of PEG-CS-Fe3O4 as a stable magnetic targeting drug carrier in cancer therapy.