title: PEG-chitosan-coated iron oxide nanoparticles with high saturated magnetization as carriers of 10-hydroxycamptothecin: preparation, characterization and cytotoxicity studies.
abstract: A magnetic nano-sized carrier for 10-hydroxycamptothecin (HCPT) was prepared by using Fe(3)O(4) 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-Fe(3)O(4)) to improve their biocompatibility (PEG-CS-Fe(3)O(4)). HCPT was loaded onto PEG-CS-Fe(3)O(4) by a subtle precipitation method. Under optimum conditions, the CS-Fe(3)O(4) was close to spherical in shape with an average size of 174 nm and a high saturated magnetization. After coupling PEG chains, the unspecific adsorption of bovine serum albumin (BSA) on PEG-CS-Fe(3)O(4) 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 48 h, 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-Fe(3)O(4) 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-Fe(3)O(4) as a stable magnetic targeting drug carrier in cancer therapy.
authors.affiliation: Center for Bioengineering and Biotechnology, China University of Petroleum (East China), QingDao 266580, PR China. jbqu@upc.edu.cn
authors.forename: Jian-Bo
authors.initials: JB
authors.lastname: Qu
authors.forename: Hui-Hui
authors.initials: HH
authors.lastname: Shao
authors.forename: Guang-Lun
authors.initials: GL
authors.lastname: Jing
authors.forename: Fang
authors.initials: F
authors.lastname: Huang
mesh_terms: D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000009:adverse effects / Q000737:chemistry*; D005290:Ferric Compounds / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D053758:Nanoparticles / Q000009:adverse effects / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D005290:Ferric Compounds; C000499:ferric oxide; D011092:Polyethylene Glycols; D048271:Chitosan; C028098:10-hydroxycamptothecin; D002166:Camptothecin