Background: Theranostic oncology combines therapy and diagnosis and is a new field
of medicine that specifically targets the disease by using targeted molecules to destroy the cancerous
cells without damaging the surrounding healthy tissues.
Objective: We aimed to develop a tool that exploits enzymatic TQ release from glucuronide (G)
for the imaging and treatment of lung cancer. We added magnetic nanoparticles (MNP) to enable
magnetic hyperthermia and MRI, as well as 131I to enable SPECT imaging and radionuclide therapy.
Methods: A glucuronide derivative of thymoquinone (TQG) was enzymatically synthesized and
conjugated with the synthesized MNP and then radioiodinated with 131I. New Zealand white rabbits
were used in SPECT and MRI studies, while tumor modeling studies were performed on 6–7-
week-old nude mice utilized with bioluminescence imaging.
Results: Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR)
spectra confirmed the expected structures of TQG. The dimensions of nanoparticles were below 10
nm and they had rather polyhedral shapes. Nanoparticles were radioiodinated with 131I with over
95% yield. In imaging studies, in xenograft models, tumor volume was significantly reduced in
TQGMNP-treated mice but not in non-treated mice. Among mice treated intravenously with
TQGMNP, xenograft tumor models disappeared after 10 and 15 days, respectively.
Conclusion: Our findings suggest that TQGMNP in solid, semi-solid and liquid formulations can
be developed using different radiolabeling nuclides for applications in multimodality imaging
(SPECT and MRI). By altering the characteristics of radionuclides, TQGMNP may ultimately be
used not only for diagnosis but also for the treatment of various cancers as an in vitro diagnostic kit
for the diagnosis of beta glucuronidase-rich cancers.