Chemical and Physical Characterisation of Macroaggregated Human Serum Albumin: Strength and Specificity of Bonds with 99mTc and 68Ga

Background: Macroaggregated human serum albumin (MAA) properties are widely used in nuclear medicine, labelled with 99mTc. The aim of this study is to improve the knowledge about the morphology, size, dimension and physical–chemical characteristics of MAA and their bond with 99mTc and 68Ga. Methods:...

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Published inMolecules (Basel, Switzerland) Vol. 27; no. 2; p. 404
Main Authors Canziani, Letizia, Marenco, Manuela, Cavenaghi, Giorgio, Manfrinato, Giulia, Taglietti, Angelo, Girella, Alessandro, Aprile, Carlo, Pepe, Giovanna, Lodola, Lorenzo
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 09.01.2022
MDPI
Subjects
99mTc
Albumin
Binding sites
Bonding strength
Chloride
Chromatography
Gallium isotopes
Human serum albumin
Isotherms
Isotopes
macroaggregated
Nuclear medicine
PET
Physical characteristics
Physical properties
Radioisotopes
radiopharmaceutical
Serum albumin
Sodium
Solvents
SPECT
Technetium isotopes
France
United States > US
Germany
Paris France
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Summary:Background: Macroaggregated human serum albumin (MAA) properties are widely used in nuclear medicine, labelled with 99mTc. The aim of this study is to improve the knowledge about the morphology, size, dimension and physical–chemical characteristics of MAA and their bond with 99mTc and 68Ga. Methods: Commercial kits of MAA (Pulmocis®) were used. Characterisation through experiments based on SEM, DLS and Stokes’ Law were carried out. In vitro experiments for Langmuir isotherms and pH studies on radiolabelling were performed and the stability of the radiometal complex was verified through competition reactions. Results: The study settles the MAA dimension within the range 43–51 μm. The Langmuir isotherm reveals for [99mTc]MAA: Bmax (46.32), h (2.36); for [68Ga]MAA: Bmax (44.54), h (0.893). Dual labelling reveals that MAA does not discriminate different radioisotopes. Experiments on pH placed the optimal pH for labelling with 99mTc at 6. Conclusion: Radiolabelling of MAA is possible with high efficiency. The nondiscriminatory MAA bonds make this drug suitable for radiolabelling with different radioisotopes or for dual labelling. This finding illustrates the need to continue investigating MAA chemical and physical characteristics to allow for secure labelling with different isotopes.
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ISSN:1420-3049
1420-3049
DOI:10.3390/molecules27020404