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Title: Methotrexate-conjugated and hyperbranched polyglycerol-grafted Fe 3O4 magnetic nanoparticles for targeted anticancer effects
Authors: Li, M.
Neoh, K.-G. 
Wang, R.
Zong, B.-Y.
Tan, J.Y.
Kang, E.-T. 
Keywords: Active targeting
Hyperbranched polyglycerol
Iron oxide nanoparticles
Issue Date: 23-Jan-2013
Citation: Li, M., Neoh, K.-G., Wang, R., Zong, B.-Y., Tan, J.Y., Kang, E.-T. (2013-01-23). Methotrexate-conjugated and hyperbranched polyglycerol-grafted Fe 3O4 magnetic nanoparticles for targeted anticancer effects. European Journal of Pharmaceutical Sciences 48 (1-2) : 111-120. ScholarBank@NUS Repository.
Abstract: Superparamagnetic nanoparticles grafted with hyperbranched polyglycerol (HPG) and conjugated with methotrexate (MTX) (MNP-g-HPG-MTX) were synthesized via a sol-gel reaction followed by thiol-ene click chemistry and esterification reaction. The successful grafting of MTX and HPG onto the nanoparticles was confirmed by X-ray photoelectron spectroscopy (XPS), Fourier transform infrared (FT-IR) spectroscopy, and UV-visible spectroscopy. The HPG-graft layer confers the magnetic nanoparticles with good dispersibility and stability in aqueous medium and macrophage-evasive property while the MTX acts as a chemotherapeutic drug as well as a tumor targeting ligand. The dose-dependent targeting and anticancer effect of the MNP-g-HPG-MTX nanoparticles were evaluated, and the results showed that depending on the amount of conjugated MTX and the concentration of the incubated nanoparticles, the uptake of MNP-g-HPG-MTX nanoparticles by human head and neck cancer (KB) cells can be eight times or more higher than those by 3T3 fibroblasts and RAW macrophages. As a result, the MNP-g-HPG-MTX nanoparticles are capable of killing ∼50% of the KB cells while at the same time exhibiting low cytotoxicity towards 3T3 fibroblasts and RAW macrophages. Thus, such nanoparticles can potentially be used as active targeting anticancer agents. © 2012 Elsevier B.V. All rights reserved.
Source Title: European Journal of Pharmaceutical Sciences
ISSN: 09280987
DOI: 10.1016/j.ejps.2012.10.008
Appears in Collections:Staff Publications

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