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Article

The Release of a Highly Cytotoxic Paullone Bearing a TEMPO Free Radical from the HSA Hydrogel: An EPR Spectroscopic Characterization

1
Faculty of Physical Chemistry, University of Belgrade, Studentski trg 12-16, 11158 Belgrade, Serbia
2
Institute of Inorganic Chemistry, University of Vienna, Währinger Strasse 42, A-1090 Vienna, Austria
3
MTA-SZTE Lendület Functional Metal Complexes Research Group, Department of Inorganic and Analytical Chemistry, University of Szeged, Dóm tér 7, H-6720 Szeged, Hungary
4
Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Albert Szent-Györgyi Medical School, University of Szeged, Semmelweis u. 6, H-6725 Szeged, Hungary
*
Author to whom correspondence should be addressed.
Academic Editors: Tiziana Esposito and Giulia Auriemma
Pharmaceutics 2022, 14(6), 1174; https://doi.org/10.3390/pharmaceutics14061174
Received: 3 May 2022 / Revised: 25 May 2022 / Accepted: 27 May 2022 / Published: 30 May 2022
(This article belongs to the Special Issue Hydrogels in Drug Delivery: Progress and Challenges)
This study shows the potential of a thermally induced human serum albumin (HSA) hydrogel to serve as a drug depot for sustained release of a highly cytotoxic modified paullone ligand bearing a TEMPO free radical (HL). The binding of HL to HSA was studied by electron paramagnetic resonance (EPR) spectroscopy and imaging. The EPR protocol was also implemented for the study of matrix degradation, and ligand diffusion rate, in two additional spin-labeled hydrogels, containing 5-doxylstearate and 3-carbamoyl-proxyl. The results showed that the hydrogel is an efficient HL reservoir as it retained 60% of the ligand during 11 days of dialysis in physiological saline. Furthermore, upon incubation with Colo 205 human colon adenocarcinoma cells for 3 days, the HL/HSA hydrogel did not exhibit cytotoxic activity, demonstrating that it is also an efficient ligand depot in the presence of living cells. It was observed that the percentage of HL release is independent of its initial concentration in the hydrogel, suggesting that HSA possesses a specific binding site for the ligand, most likely Sudlow site 2, as predicted by molecular docking. The intrinsic property of albumin to bind and transport various substances, including hydrophobic drugs, may be fine-tuned by appropriate physical/chemical hydrogel preparation procedures, providing optimal drug delivery. View Full-Text
Keywords: cytotoxic ligand; drug release; EPR spectroscopy and imaging; HSA hydrogel; paullones; spin labeling cytotoxic ligand; drug release; EPR spectroscopy and imaging; HSA hydrogel; paullones; spin labeling
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MDPI and ACS Style

Vesković, A.; Nakarada, Đ.; Vasiljević, O.; Dobrov, A.; Spengler, G.; Enyedy, É.A.; Arion, V.B.; Popović Bijelić, A. The Release of a Highly Cytotoxic Paullone Bearing a TEMPO Free Radical from the HSA Hydrogel: An EPR Spectroscopic Characterization. Pharmaceutics 2022, 14, 1174. https://doi.org/10.3390/pharmaceutics14061174

AMA Style

Vesković A, Nakarada Đ, Vasiljević O, Dobrov A, Spengler G, Enyedy ÉA, Arion VB, Popović Bijelić A. The Release of a Highly Cytotoxic Paullone Bearing a TEMPO Free Radical from the HSA Hydrogel: An EPR Spectroscopic Characterization. Pharmaceutics. 2022; 14(6):1174. https://doi.org/10.3390/pharmaceutics14061174

Chicago/Turabian Style

Vesković, Ana, Đura Nakarada, Olga Vasiljević, Anatolie Dobrov, Gabriella Spengler, Éva A. Enyedy, Vladimir B. Arion, and Ana Popović Bijelić. 2022. "The Release of a Highly Cytotoxic Paullone Bearing a TEMPO Free Radical from the HSA Hydrogel: An EPR Spectroscopic Characterization" Pharmaceutics 14, no. 6: 1174. https://doi.org/10.3390/pharmaceutics14061174

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