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Hypericin (Hy) compound presents a high photoactivity in photodynamic therapy (PDT), photodiagnosis and theranostics applications. The maintenance of this compound in monomeric form could undermine the potential benefits of its photophysical and photodynamic activity. In this study, we demonstrated that the Hy formulated in a system based on the use of the F127 copolymer and the 1,2-dipalmitoyl-sn-3-glycerol-phosphatidylcholine (DPPC) as micelles, liposomal vesicles and Copolymer-Lipid coated systems, have improved its photophysical properties for many clinical modalities. Based on the results of the triplet state lifetime values (τt), the singlet oxygen quantum yield (ΦΔ1O2), the fluorescence lifetime (τF) and the fluorescence quantum yield (ΦF), all Hy formulations had its photophysical properties described in different models of drug delivery systems (DDS). In addition, the transient spectra profile of those formulations was unaffected by the Hy incorporation process, except for the liposomal system, which demonstrated to be the less stable one by flash photolysis technique. The cytotoxic effects of those formulations were also investigated for CaCo-2 and HaCat cells line. The cytotoxic concentrations for 50% (CC50) were 0.56, 1.05, 1.33 and 4.80 µmol L-1 for Copolymer-Lipid/Hy, DPPC/Hy, F127/Hy and ethanol/Hy for CaCo-2 cells, respectively, and 0.69, 2.02, 1.45 and 1.16 µmol L-1 for Copolymer-Lipid/Hy, DPPC/Hy, F127/Hy and ethanol/Hy for HaCat cells, respectively. The F127 copolymer had a significant role in many photophysical parameters determined for Copolymer-Lipid/Hy coated system. Although all those formulations had shown satisfactory results, Copolymer-Lipid/Hy proved to be superior in many aspects, being the most promising formulation for PDT, photodiagnosis and theranostics applications. Copyright © 2020 Elsevier B.V. All rights reserved.


Flávia Amanda Pedroso de Morais, Renato Sonchini Gonçalves, Katieli Souza Campanholi, Bruna Martins de França, Otávio Augusto Capeloto, Danielle Lazarin-Bidoia, Rodolfo Bento Balbinot, Celso Vataru Nakamura, Luis Carlos Malacarne, Wilker Caetano, Noboru Hioka. Photophysical characterization of Hypericin-loaded in micellar, liposomal and copolymer-lipid nanostructures based F127 and DPPC liposomes. Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy. 2021 Mar 05;248:119173

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PMID: 33316657

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