title: Enhanced in vitro antitumor efficacy and strong anti-cell-migration activity of a hydroxycamptothecin-encapsulated magnetic nanovehicle.
abstract: A 10-hydroxycamptothecin-encapsulated magnetic nanovehicle (HEMN) was fabricated by coencapsulating Fe(3)O(4) nanoparticles and 10-hydroxycamptothecin (HCPT) into a micelle core self-assembled from the amphiphilic copolymer methoxy-poly(ethylene glycol)-poly(d,l-lactide-co-glycolide) through a facile dialysis method. A satisfactory drug-loading content of (9.03 ± 0.67) % and a relatively high encapsulation efficiency of (53.52 ± 6.46) % were achieved. In vitro drug release was performed by membrane dialysis and a pH-dependent release behavior was observed. In comparison with free HCPT dissolved in dimethylsulfoxide, HEMNs showed a greatly improved in vitro antitumor efficacy against three different human cancer cell lines-HeLa, A549, and HepG2-and lower IC(50) values were measured. The mechanism of cell death was investigated, and it was clearly demonstrated that the apoptosis process was triggered. An in vitro wound-healing assay and a transwell assay indicated that HEMNs exerted much stronger activity in inhibiting HeLa cell migration. The cellular uptake of HEMNs in a desired area can be significantly enhanced by an external magnetic field. These results demonstrate HCPT-encapsulated magnetic nanovehicles might have important potential in clinical applications for inhibiting tumor metastasis and for targeted drug delivery.
authors.affiliation: Key Laboratory for Molecular Enzymology and Engineering, The Ministry of Education, College of Life Science, Jilin University, Changchun, PR China.
authors.forename: Guo-Bin
authors.initials: GB
authors.lastname: Ding
authors.forename: Hui-Ying
authors.initials: HY
authors.lastname: Liu
authors.forename: Yan-Yun
authors.initials: YY
authors.lastname: Lv
authors.forename: Xiao-Feng
authors.initials: XF
authors.lastname: Liu
authors.forename: Yi
authors.initials: Y
authors.lastname: Guo
authors.forename: Chang-Kai
authors.initials: CK
authors.lastname: Sun
authors.forename: Li
authors.initials: L
authors.lastname: Xu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D052203:Ferrosoferric Oxide / Q000737:chemistry; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D060526:Magnetic Fields; D058185:Magnetite Nanoparticles / Q000737:chemistry*; D008823:Micelles
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D058185:Magnetite Nanoparticles; D008823:Micelles; C028098:10-hydroxycamptothecin; D052203:Ferrosoferric Oxide; D002166:Camptothecin