Synthesis and biodistribution of novel magnetic-poly(HEMA-APH) nanopolymer radiolabeled with iodine-131 and investigation its fate in vivo for cancer therapy
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2013
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Abstract
Herein, we investigated the biological uptake, distribution, and radiopharmaceutical potential of a novel molecule based on 2-hydroxyethyl methacrylate (HEMA) and anilinephtalein (APH) in the metabolism of Albino Wistar rats. In order to achieve this, we synthesized APH using organic synthesis methods and copolymerized APH with HEMA using a common polymerization method, surfactant-free emulsion polymerization. In the presence of Fe3O 4 particles, we obtained a new generation magnetic-nano-scale polymer, magnetic-poly(HEMA-APH). This new molecule was chemically identified and approved by several characterization methods using Fourier transform infrared spectroscopy, scanning electron microscope, energy dispersive X-ray spectroscopy, electron spin resonance, atomic force microscope, and Zeta particle-size analysis. To evaluate the biological activity in live metabolism and anti-cancer potential of mag-poly(HEMA-APH), molecule was radioiodinated by a widely used labeling technique, iodogen method, with a gamma diffuser radionuclide, 131I. Thin-layer radiochromatography experiments demonstrated that 131I binded to nanopolymer with the labeling yield of 90 %. Lipophilicity and stability experiments were conducted to determine the condition of cold and labeled mag-poly(HEMA-APH) in rat blood and lipid medium. Results demonstrated that radioiodinated molecule stayed as an intact complex in rat metabolism for 24 h and experimental lipophilicity was determined as 0.12 ± 0.02. In vivo results obtained by imaging and biological distribution experiments indicated that mag-poly(HEMA-APH) labeled with 131I [131I-mag-poly(HEMA-APH)] highly incorporated into tissues of the uterus, the ovarian, the prostate, and the lungs in rat metabolism. Based on these results, it may be evaluated that novel mag-poly(HEMA-APH) molecule labeled with 131I is a compound which has a significant potential for being used as an anti-cancer agent. Certain results can only be obtained whether this molecule is applied to adenocarcinoma cell models and tumor-bearing animals. © 2013 Springer Science+Business Media Dordrecht.
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Aniline , Atomic force microscopy , Bioactivity , Chromatography , Diseases , Drug delivery , Emulsification , Emulsion polymerization , Energy dispersive spectroscopy , Fourier transform infrared spectroscopy , Iodine , Iron oxides , Magnetic moments , Magnetite , Medical nanotechnology , Metabolism , Molecules , Nanomagnetics , Particle size , Particle size analysis , Rats , Scanning electron microscopy , magnetic poly 2 hydroxyethyl methacrylate anilinephtalein i 131 , radiopharmaceutical agent , unclassified drug , Anilinephtalein , Cancer therapeutics , Iodine-131 , Nano polymers , Poly(HEMA) , animal experiment , antineoplastic activity , article , biological activity , cancer chemotherapy , drug distribution , drug metabolism , drug synthesis , drug uptake , electron microscope , electron spin resonance , female , in vivo study , infrared spectroscopy , isotope labeling , lipophilicity , male , nonhuman , particle size , priority journal , radiochromatography , rat , zeta potential , Electron spin resonance spectroscopy