ORIGINAL RESEARCH

Contrast enhanced MRI of tumors using gadopentetic acid linked to cyclodextrin by an ester bond

Kulakov VN1, Lipengolts AA1,2, Grigorieva EYu2, Semeikin AV3, Abakumov MA3, Karakhanov EA4, Maximov AB4, Shimanovsky NL3
About authors

1 Burnasyan Federal Medical Biophysical Center of Federal Medical Biological Agency, Moscow, Russia

2 N. N. Blokhin Russian Cancer Research Center, Moscow, Russia

3 P. V. Sergeev Molecular Pharmacology and Radiobiology Department, Biomedical Faculty,
Pirogov Russian National Research Medical University, Moscow, Russia

4 Department of Petroleum Chemistry and Organic Catalysis, Faculty of Chemistry,
Lomonosov Moscow State University, Moscow, Russia

Correspondence should be addressed: Nikolay Shimanovsky
ul. Ostrovityanova, d. 1, Moscow, Russia, 117997; ur.umsr@namihs

About paper

Funding: this work was supported by Government Contract No. 11411.1008700.13.081 dated September 13, 2011 as part of the Federal Targeted Program for the Development of Pharmaceutical and Medical Industry of the Russian Federation until 2020.

Received: 2016-08-15 Accepted: 2016-08-25 Published online: 2017-01-05
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Contrast-enhanced magnetic resonance imaging has become a routine diagnostic procedure. One of the most common contrast agents used for MRI is gadopentetic acid (Gd-DTPA, marketed as Magnevist). In this work, we studied the relaxivity of Gd-DTPA covalently bonded to β-cyclodextrin and compared enhancement properties of this compound and Magnevist. Our work demonstrated high relaxivity of Gd-DTPA complex containing 80 % of Gd-DTPA-modified β-cyclodextrin mono-derivative, 10 % of Gd-DTPA-modified β-cyclodextrin di-derivative and 10 % of Gd-DTPA-modified β-cyclodextrin tri-derivative. Gd-DTPA residues were linked to β-cyclodextrin by an ester bond, in which a COOH group belongs to DTPA and OH is a β-cyclodextrin surface hydroxyl group. It was proved experimentally that the studied compound is not toxic in concentrations necessary for diagnostic procedures. Compared to Magnevist, it can provide similar enhancement when used in just half of the equivalent amount.

Keywords: fibroblasts, gadolinium, diethylenetriaminepentaacetic acid, β-cyclodextrin, tumor cells, relaxivity, tumor visualization

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