<abstract xmlns="http://www.w3.org/1999/xhtml">To design a potent agent for positron emission tomography/magnetic resonance imaging (PET/MRI) imaging and targeted magnetic hyperthermia-radioisotope cancer therapy radiolabeled surface modified superparamagnetic iron oxide nanoparticles (SPIONs) were used as nanocarriers. Folic acid was conjugated for increasing selective cellular binding and internalization through receptor-mediated endocytosis. SPIONs were synthesized by the thermal decomposition of tris (acetylacetonato) iron (III) to achieve narrow and uniform nanoparticles. To increase the biocompatibility of SPIONs, they were coated with (3-aminopropyl) triethoxysilane (APTES), and then conjugated with synthesized folic acid-polyethylene glycol (FA-PEG) through amine group of (3-aminopropyl) triethoxysilane. Finally, the particles were labeled with 64Cu (<italic>t</italic>1/2 = 12.7 h) using 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid mono (<italic>N-</italic>hydroxy succinimide ester) DOTA-NHS chelator. After the characterization of SPIONs, their cellular internalization was evaluated in folate receptor (FR) overexpressing KB (established from a HeLa cell contamination) and mouse fibroblast cell (MFB) lines. Eventually, active and passive targeting effects of complex were assessed in KB tumor-bearing Balb/C mice through biodistribution studies. Synthesized bare SPIONs had low toxicity effect on healthy cells, but surface modification increased their biocompatibility. Moreover, KB cells viability was reduced when using folate conjugated SPIONs due to FR-mediated endocytosis, while having little effect on healthy cells (MFB). Moreover, this radiotracer had tolerable <italic>in vivo</italic> characteristics and tumor uptake. In the receptor blocked case, tumor uptake was decreased, indicating FR-specific uptake in tumor tissue while enhanced permeability and retention effect was major mechanism for tumor uptake.</abstract>

To design a potent agent for positron emission tomography/magnetic resonance imaging (PET/MRI) imaging and targeted magnetic hyperthermia-radioisotope cancer therapy radiolabeled surface modified superparamagnetic iron oxide nanoparticles (SPIONs) were used as nanocarriers. Folic acid was conjugated for increasing selective cellular binding and internalization through receptor-mediated endocytosis. SPIONs were synthesized by the thermal decomposition of tris (acetylacetonato) iron (III) to achieve narrow and uniform nanoparticles. To increase the biocompatibility of SPIONs, they were coated with (3-aminopropyl) triethoxysilane (APTES), and then conjugated with synthesized folic acid-polyethylene glycol (FA-PEG) through amine group of (3-aminopropyl) triethoxysilane. Finally, the particles were labeled with 64Cu (t1/2 = 12.7 h) using 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid mono (N-hydroxy succinimide ester) DOTA-NHS chelator. After the characterization of SPIONs, their cellular internalization was evaluated in folate receptor (FR) overexpressing KB (established from a HeLa cell contamination) and mouse fibroblast cell (MFB) lines. Eventually, active and passive targeting effects of complex were assessed in KB tumor-bearing Balb/C mice through biodistribution studies. Synthesized bare SPIONs had low toxicity effect on healthy cells, but surface modification increased their biocompatibility. Moreover, KB cells viability was reduced when using folate conjugated SPIONs due to FR-mediated endocytosis, while having little effect on healthy cells (MFB). Moreover, this radiotracer had tolerable in vivo characteristics and tumor uptake. In the receptor blocked case, tumor uptake was decreased, indicating FR-specific uptake in tumor tissue while enhanced permeability and retention effect was major mechanism for tumor uptake.

Synthesis and evaluation of radiolabeled, folic acid-PEG conjugated, amino silane coated magnetic nanoparticles in tumor bearing Balb/C mice

Department of Engineering, Garmsar Branch, Islamic Azad University, Garmsar, Iran, Tel.: +9891 0942 2335, Fax: 026 3446 4053

Department of Energy Engineering and Physics, Amirkabir University of Technology, Tehran, Iran

Young Researchers and Elite Club, South Tehran Branch, Islamic Azad University, Tehran, Iran

Biomedical Engineering Department, Science and Research Branch, Islamic Azad University, Tehran, Iran

Nuclear Medicine Research Group, Alborz Research Center, Karaj, Iran

Nuclear Engineering Department, East Tehran Branch, Islamic Azad University, Tehran, Iran

Nukleonika

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

To design a potent agent for positron emission tomography/magnetic resonance imaging (PET/MRI) imaging and targeted magnetic hyperthermia-radioisotope cancer...

Synthesis and evaluation of radiolabeled, folic acid-PEG conjugated, amino silane coated magnetic nanoparticles in tumor bearing Balb/C mice

Published Online: Aug 06, 2015

Page range: 497 - 502

Received: Dec 23, 2014

Accepted: Jun 01, 2015

DOI: https://doi.org/10.1515/nuka-2015-0066

Keywords
superparamagnetic iron oxide nanoparticles (SPIONs), (3-aminopropyl) triethoxysilane (APTES), poly ethylene glycol (PEG), folic acid, KB cells, copper-64

© Javad Razjouyan et al.

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Synthesis and evaluation of radiolabeled, folic acid-PEG conjugated, amino silane coated magnetic nanoparticles in tumor bearing Balb/C mice

Published Online: Aug 06, 2015

Page range: 497 - 502

Received: Dec 23, 2014

Accepted: Jun 01, 2015

DOI: https://doi.org/10.1515/nuka-2015-0066

Keywordssuperparamagnetic iron oxide nanoparticles (SPIONs), (3-aminopropyl) triethoxysilane (APTES), poly ethylene glycol (PEG), folic acid, KB cells, copper-64

© Javad Razjouyan et al.

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
superparamagnetic iron oxide nanoparticles (SPIONs), (3-aminopropyl) triethoxysilane (APTES), poly ethylene glycol (PEG), folic acid, KB cells, copper-64