Radiolabeling Strategies of Micron- And Submicron-Sized Core-Shell Carriers for in Vivo Studies

Mikhail V. Zyuzin, Dmitrii Antuganov, Yana V. Tarakanchikova, Timofey E. Karpov, Tatiana V. Mashel, Elena N. Gerasimova, Oleksii O. Peltek, Nominé Alexandre, Stéphanie Bruyere, Yulia A. Kondratenko, Albert R. Muslimov, Alexander S. Timin

Research output: Contribution to journalArticle

Abstract

Core-shell particles made of calcium carbonate and coated with biocompatible polymers using the Layer-by-Layer technique can be considered as a unique drug-delivery platform that enables us to load different therapeutic compounds, exhibits a high biocompatibility, and can integrate several stimuli-responsive mechanisms for drug release. However, before implementation for diagnostic or therapeutic purposes, such core-shell particles require a comprehensive in vivo evaluation in terms of physicochemical and pharmacokinetic properties. Positron emission tomography (PET) is an advanced imaging technique for the evaluation of in vivo biodistribution of drug carriers; nevertheless, an incorporation of positron emitters in these carriers is needed. Here, for the first time, we demonstrate the radiolabeling approaches of calcium carbonate core-shell particles with different sizes (CaCO3 micron-sized core-shell particles (MicCSPs) and CaCO3 submicron-sized core-shell particles (SubCSPs)) to precisely determine their in vivo biodistribution after intravenous administration in rats. For this, several methods of radiolabeling have been developed, where the positron emitter (68Ga) was incorporated into the particle's core (co-precipitation approach) or onto the surface of the shell (either layer coating or adsorption approaches). According to the obtained data, radiochemical bounding and stability of 68Ga strongly depend on the used radiolabeling approach, and the co-precipitation method has shown the best radiochemical stability in human serum (96-98.5% for both types of core-shell particles). Finally, we demonstrate the size-dependent effect of core-shell particles' distribution on the specific organ uptake, using a combination of imaging techniques, PET, and computerized tomography (CT), as well as radiometry of separate organs. Thus, our findings open up new perspectives of CaCO3-radiolabeled core-shell particles for their further implementation into clinical practice.

Original languageEnglish
Pages (from-to)31137-31147
Number of pages11
JournalACS Applied Materials and Interfaces
Volume12
Issue number28
DOIs
Publication statusPublished - 15 Jul 2020

Keywords

  • calcium carbonate
  • core-shell particles
  • in vivo biodistribution
  • Layer-by-Layer
  • nuclear imaging technique
  • PET
  • radiolabeling

ASJC Scopus subject areas

  • Materials Science(all)

Fingerprint Dive into the research topics of 'Radiolabeling Strategies of Micron- And Submicron-Sized Core-Shell Carriers for in Vivo Studies'. Together they form a unique fingerprint.

  • Cite this

    Zyuzin, M. V., Antuganov, D., Tarakanchikova, Y. V., Karpov, T. E., Mashel, T. V., Gerasimova, E. N., Peltek, O. O., Alexandre, N., Bruyere, S., Kondratenko, Y. A., Muslimov, A. R., & Timin, A. S. (2020). Radiolabeling Strategies of Micron- And Submicron-Sized Core-Shell Carriers for in Vivo Studies. ACS Applied Materials and Interfaces, 12(28), 31137-31147. https://doi.org/10.1021/acsami.0c06996