Synthesis and Biodistribution of <sup>99m</sup>Tc-Labeled PLGA Nanoparticles by Microfluidic Technique

Michela Varani; Giuseppe Campagna; Valeria Bentivoglio; Matteo Serafinelli; Maria Luisa Martini; Filippo Galli; Alberto Signore

doi:10.3390/pharmaceutics13111769

Pharmaceutics (Oct 2021)

Synthesis and Biodistribution of <sup>99m</sup>Tc-Labeled PLGA Nanoparticles by Microfluidic Technique

Michela Varani,
Giuseppe Campagna,
Valeria Bentivoglio,
Matteo Serafinelli,
Maria Luisa Martini,
Filippo Galli,
Alberto Signore

Affiliations

Michela Varani: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Giuseppe Campagna: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Valeria Bentivoglio: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Matteo Serafinelli: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Maria Luisa Martini: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Filippo Galli: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy
Alberto Signore: Nuclear Medicine Unit, Department of Medical-Surgical Sciences and of Translational Medicine, Faculty of Medicine and Psychology, “Sapienza” University of Rome, 00161 Rome, Italy

DOI: https://doi.org/10.3390/pharmaceutics13111769
Journal volume & issue: Vol. 13, no. 11
p. 1769

Abstract

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The aim of present study was to develop radiolabeled NPs to overcome the limitations of fluorescence with theranostic potential. Synthesis of PLGA-NPs loaded with technetium-99m was based on a Dean-Vortex-Bifurcation Mixer (DVBM) using an innovative microfluidic technique with high batch-to-batch reproducibility and tailored-made size of NPs. Eighteen different formulations were tested and characterized for particle size, zeta potential, polydispersity index, labeling efficiency, and in vitro stability. Overall, physical characterization by dynamic light scattering (DLS) showed an increase in particle size after radiolabeling probably due to the incorporation of the isotope into the PLGA-NPs shell. NPs of 60 nm (obtained by 5:1 PVA:PLGA ratio and 15 mL/min TFR with 99mTc included in PVA) had high labeling efficiency (94.20 ± 5.83%) and >80% stability after 24 h and showed optimal biodistribution in BALB/c mice. In conclusion, we confirmed the possibility of radiolabeling NPs with 99mTc using the microfluidics and provide best formulation for tumor targeting studies.

Published in Pharmaceutics

ISSN: 1999-4923 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Medicine: Pharmacy and materia medica
Website: http://www.mdpi.com/journal/pharmaceutics/

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