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Enhanced In Vitro Antitumor Efficacy and Strong Anti‐Cell‐Migration Activity of a Hydroxycamptothecin‐Encapsulated Magnetic Nanovehicle
Authors:Dr. Guo‐Bin Ding  Dr. Hui‐Ying Liu  Yan‐Yun Lv  Xiao‐Feng Liu  Dr. Yi Guo  Prof. Dr. Chang‐Kai Sun  Prof. Dr. Li Xu
Affiliation:1. Key Laboratory for Molecular Enzymology and Engineering, The Ministry of Education, College of Life Science, Jilin University, Changchun 130012 (P.R. China), Fax: (+86)?431‐85155226;2. School of Stomatology, Dalian Medical University, Dalian 116044 (P. R. China);3. Liaoning Provincial Key Laboratory of Brain Diseases, Institute for Brain Disorders, Dalian Medical University, Dalian 116044 (P.R. China)
Abstract:A 10‐hydroxycamptothecin‐encapsulated magnetic nanovehicle (HEMN) was fabricated by coencapsulating Fe3O4 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 IC50 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.
Keywords:antitumor agents  cell migration  drug delivery  magnetic properties  nanovehicles
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