Radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent
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Radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent H. A. El-Sabagh1 • M. I. Aydia2 • A. M. Amin1 • K. M. El-Azony2
Received: 14 April 2020 / Revised: 11 August 2020 / Accepted: 20 August 2020 China Science Publishing & Media Ltd. (Science Press), Shanghai Institute of Applied Physics, the Chinese Academy of Sciences, Chinese Nuclear Society and Springer Nature Singapore Pte Ltd. 2020
Abstract Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta particles. Lacosamide (LCM) is a newly approved antiepileptic medication for focal drug-resistant epilepsy. Rhenium-188 was separated with high elution yield and high purity using the new 188W/188Re generator based on the ZrSiW gel matrix. 188Re-LCM was prepared with high radiochemical yield and high purity. Biodistribution of 188Re-LCM in normal Swiss albino mice was investigated to determine its utility as a potential brain therapy agent. The 188W/188Re generator was used to obtain 188Re based on the ZrSi188W gel matrix, and the chemical, radiochemical, and radionuclidic purity of the obtained 188Re was determined using inductively coupled plasma optical emission spectrometry (ICP-AES), a paper chromatography technique, and high-purity germanium (HPGe) detection, respectively, to assess its validity for LCM labeling. Various factors, such as the pH, reaction time, and LCM quantity, were therefore studied in order to improve the yield and purity of 188Re-LCM, as determined by various chromatographic techniques such as electrophoresis, thin layer chromatography (TLC), and highpressure liquid chromatography (HPLC). 188Re was obtained with a high elution yield (75 ± 3%) and a low 188 W breakthrough (0.001 ± 0.0001%). The maximum & K. M. El-Azony [email protected] 1
Labeled Compound Department, Radioisotopes Production Division, Hot Laboratory Center, Atomic Energy Authority, P.O. Box 13759 Cairo, Egypt
2
Radioactive Isotopes and Generators Department, Radioisotopes Production Division, Hot Laboratory Center, Atomic Energy Authority, P.O. Box 13759 Cairo, Egypt
radiochemical yield of 188Re-LCM (87.5 ± 1.8%) was obtained using 50 ll LCM (4 mM), 250 ll stannous chloride (4.4 mM) at pH 4, 100 ll 188Re (37 MBq), within 30 min, at room temperature (25 ± 3 C), as determined by TLC, electrophoresis, and HPLC techniques. Biodistribution analysis showed that 188Re-LCM was primarily localized in the brain (5.1%) with a long residence time (240 min). Keywords Lacosamide Radiolabeling
188
Re
188
W/188Re generator
1 Introduction One of the most common radioisotopes is 188Re (T1/2 = 16.9 h). It is appropriate for both radiotherapy and radiodiagnosis as it emits beta particles (Emax= 2.12 MeV) and gamma rays (Ec = 155 keV, Ic = 15%). In several studies, two radionuclides have been combined for theranostic applications, such as in the case of DOTA-rituximab labeled with 111In and 90Y, where these isotopes ar
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