Chapter 11
Radiolabeling Method: Core/Surface
Labeling, Chemical and Physical
Labeling
Dong Soo Lee, Minseok Suh and Yun-Sang Lee
Abstract Radiolabeled nanomaterials can be used for diagnosis, therapy and
theranostics of certain diseases. The core concept of radionanomedicine relies on
efficient and reliable radiolabeling methods, to bind appropriate isotope with
well-functionalized nanoparticles (NPs), and the use of tracer amounts of radiolabeled NPs. In this chapter, we focused on the three issues of producing radiolabeled
NPs: choosing appropriate radionuclides for labeling, construction of
well-functionalized NPs with surface modification and different labeling methods of
NPs with radionuclides. Firstly, choosing ideal isotope starts from understanding
the characteristics of each isotopes, such as half-life, decay energy and availability,
and understanding of purpose of the study. Secondly, to increase the specific
delivery of NPs to the target tissues while decreasing the nonspecific binding to
normal tissues well functionalized NPs are necessary, which can be achieved by
surface modification. Especially, micelle encapsulation method is an efficient
method for producing multifunctional NPs. Finally, ideal labeling method should be
adopted, which should not only be quick, easy, and highly efficient but also should
not change the biological properties of target molecules. Both intrinsic and extrinsic
radiolabeling methods should be chosen in the base of thorough understanding of
pros and cons of each labeling methods. In conclusion, the development of the
methods to enable surface labeling with ligands and chelators should be solved first.
The development of the imaging methods to track the in vivo administered
D. S. Lee (&) Á M. Suh Á Y.-S. Lee
Department of Nuclear Medicine, Seoul National University College
of Medicine, Seoul 03080, Republic of Korea
e-mail: dsl@snu.ac.kr
M. Suh
e-mail: mandu0902@hotmail.com
Y.-S. Lee
e-mail: wonza43@snu.ac.kr
D. S. Lee Á M. Suh Á Y.-S. Lee
Department of Molecular Medicine and Biopharmaceutical Sciences,
Graduate School of Convergence Science and Technology,
Seoul National University, Seoul 03080, Republic of Korea
© Springer International Publishing AG, part of Springer Nature 2018
D. S. Lee (ed.), Radionanomedicine, Biological and Medical Physics,
Biomedical Engineering, https://doi.org/10.1007/978-3-319-67720-0_11
209
Radiolabeling Method: Core/Surface
Labeling, Chemical and Physical
Labeling
Dong Soo Lee, Minseok Suh and Yun-Sang Lee
Abstract Radiolabeled nanomaterials can be used for diagnosis, therapy and
theranostics of certain diseases. The core concept of radionanomedicine relies on
efficient and reliable radiolabeling methods, to bind appropriate isotope with
well-functionalized nanoparticles (NPs), and the use of tracer amounts of radiolabeled NPs. In this chapter, we focused on the three issues of producing radiolabeled
NPs: choosing appropriate radionuclides for labeling, construction of
well-functionalized NPs with surface modification and different labeling methods of
NPs with radionuclides. Firstly, choosing ideal isotope starts from understanding
the characteristics of each isotopes, such as half-life, decay energy and availability,
and understanding of purpose of the study. Secondly, to increase the specific
delivery of NPs to the target tissues while decreasing the nonspecific binding to
normal tissues well functionalized NPs are necessary, which can be achieved by
surface modification. Especially, micelle encapsulation method is an efficient
method for producing multifunctional NPs. Finally, ideal labeling method should be
adopted, which should not only be quick, easy, and highly efficient but also should
not change the biological properties of target molecules. Both intrinsic and extrinsic
radiolabeling methods should be chosen in the base of thorough understanding of
pros and cons of each labeling methods. In conclusion, the development of the
methods to enable surface labeling with ligands and chelators should be solved first.
The development of the imaging methods to track the in vivo administered
D. S. Lee (&) Á M. Suh Á Y.-S. Lee
Department of Nuclear Medicine, Seoul National University College
of Medicine, Seoul 03080, Republic of Korea
e-mail: dsl@snu.ac.kr
M. Suh
e-mail: mandu0902@hotmail.com
Y.-S. Lee
e-mail: wonza43@snu.ac.kr
D. S. Lee Á M. Suh Á Y.-S. Lee
Department of Molecular Medicine and Biopharmaceutical Sciences,
Graduate School of Convergence Science and Technology,
Seoul National University, Seoul 03080, Republic of Korea
© Springer International Publishing AG, part of Springer Nature 2018
D. S. Lee (ed.), Radionanomedicine, Biological and Medical Physics,
Biomedical Engineering, https://doi.org/10.1007/978-3-319-67720-0_11
209