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. 2023 Jul-Aug:122-123:108363.
doi: 10.1016/j.nucmedbio.2023.108363. Epub 2023 Jun 22.

Biokinetics, radiopharmacokinetics and estimation of the absorbed dose in healthy organs due to Technetium-99m transported in the core and on the surface of reconstituted high-density lipoprotein nanoparticles

Diana L Pérez-Velasco  1 , Enrique Morales-Avila  2 , Blanca Ocampo-García  3 , Eugenio Torres-García  4 , Germán Izquierdo  5 , Nallely Jiménez-Mancilla  3 , Rigoberto Oros-Pantoja  6 , Luis E Díaz-Sánchez  5 , Liliana Aranda-Lara  7 , Keila Isaac-Olivé  8
Affiliations

Biokinetics, radiopharmacokinetics and estimation of the absorbed dose in healthy organs due to Technetium-99m transported in the core and on the surface of reconstituted high-density lipoprotein nanoparticles

Diana L Pérez-Velasco et al. Nucl Med Biol. 2023 Jul-Aug.

Abstract

The development of rHDL-radionuclide theragnostic systems requires evaluation of the absorbed doses that would be produced in healthy tissues and organs at risk. Technetium-99m is the most widely used radionuclide for diagnostic imaging, therefore, the design of theragnostic reconstituted high density-lipoprotein (rHDL) nanosystems labeled with Technetium-99m offers multiple possibilities.

Objective: To determine the biokinetics, radiopharmacokinetics and estimate the absorbed doses induced in healthy organs by Technetium-99m transported in the core and on the surface of rHDL.

Methods: Biokinetic and radiopharmacokinetic models of rHDL/[99mTc]Tc-HYNIC-DA (Technetium-99m in the core) and [99mTc]Tc-HYNIC-rHDL (Technetium-99m on the surface) were calculated from their ex vivo biodistribution in healthy mice. Absorbed doses were estimated by the MIRD formalism using OLINDA/EXM and LMFIT softwares.

Results: rHDL/[99mTc]Tc-HYNIC-DA and [99mTc]Tc-HYNIC-rHDL show instantaneous absorption in kidney, lung, heart and pancreas, with slower absorption in spleen. rHDL/[99mTc]Tc-HYNIC-DA is absorbed more slowly in the intestine, while [99mTc]Tc-HYNIC-rHDL is absorbed more slowly in the liver. The main target organ for rHDL/[99mTc]Tc-HYNIC-DA, which is hydrophobic in nature, is the liver, whereas the kidney is for the more hydrophilic [99mTc]Tc-HYNIC-rHDL. Assuming that 925 MBq (25 mCi) of Technetium-99m, carried in the core or on the surface of rHDL, are administered, the maximum tolerated doses for the organs of greatest accumulation are not exceeded.

Conclusion: Theragnostic systems based on 99mTc-labeled rHDL are safe from the dosimetric point of view. The dose estimates obtained can be used to adjust the 99mTc-activity to be administered in future clinical trials.

Keywords: (99m)Tc-radiolabeled nanoparticles; Absorbed dose; Reconstituted high-density lipoprotein (rHDL); Theragnostic nanosystems.

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Conflict of interest statement

Declaration of competing interest The authors declare no conflicts of interest.

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    Pérez-Medina C, Fisher EA, Fayad ZA, Mulder WJM, Teunissen AJP. Pérez-Medina C, et al. Eur J Nucl Med Mol Imaging. 2025 Apr 28:10.1007/s00259-025-07281-4. doi: 10.1007/s00259-025-07281-4. Online ahead of print. Eur J Nucl Med Mol Imaging. 2025. PMID: 40293448 Free PMC article. Review.

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