Title:Radiolabeling of Zonisamide for a Diagnostic Perspective
Volume: 17
Issue: 1
Author(s): Emine Dervis, Kadriye Busra Karatay, Kubra Durkan*Ayfer Yurt Kilcar
Affiliation:
- Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Izmir, Turkey
Keywords:
Zonisamide (ZNS), antiepileptic drugs, epilepsy, technetium-99m (99mTc), neuroimaging, in vitro.
Abstract: Objective: Epilepsy is one of the oldest and the most common chronic neurological
diseases. Antiepileptic drugs (AEDs) are the backbone of epilepsy treatment. However, epileptogenesis
has not been fully elucidated. One of the critical reasons for this is the lack of reliable
biomarkers. Neuroimaging suggests a non-invasive examination and investigation tool that can
detect critical pathophysiological changes involved in epileptogenesis and monitor disease progression.
In the current study, the radiolabeling potential of Zonisamide (ZNS) (the secondgeneration
AED) with Technetium-99m (99mTc) is examined to neuroimage the epileptogenic
processes by contributing to the development of potential radiotracers.
Methods: ZNS was labeled with 99mTc and the radiochemical yield of [99mTc]Tc-ZNS was determined
with TLRC (Thin Layer Liquid Radio Chromatography and HPLRC (High Performance
Liquid Radio Chromatography) radiochromatographic methods. In vitro behavior of
[99mTc]Tc-ZNS was determined with time-dependent uptake of [99mTc]Tc-ZNS on the SHSY5Y
human neuroblastoma cells.
Results: The radiochemical yield of [99mTc]Tc-ZNS was determined as 98.03 ± 1.24% (n = 6)
according to radiochromatographic studies results. [99mTc]Tc-ZNS demonstrated 5.38 and 6.18
times higher uptake values than the control group on the human neuroblastoma SH-SY5Y cell
line at 120 and 240 minutes, respectively.
Conclusion: This study showed that the current radiolabeled antiepileptic drug has a diagnostic
potential to be used in imaging neurological processes.