Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications

<b>Background/Objectives:</b> Leishmaniasis, caused by protozoa of the genus <i>Leishmania</i>, is a major global health issue due to the limitations of current treatments, which include low efficacy, high costs, and severe side effects. This study aimed to develop a more eff...

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Main Authors: Monica Araujo das Neves, Caroline Martins de Jesus, Jhones Luiz de Oliveira, Samuel dos Santos Soares Buna, Lucilene Amorim Silva, Leonardo Fernandes Fraceto, Cláudia Quintino da Rocha
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/16/12/1603
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author Monica Araujo das Neves
Caroline Martins de Jesus
Jhones Luiz de Oliveira
Samuel dos Santos Soares Buna
Lucilene Amorim Silva
Leonardo Fernandes Fraceto
Cláudia Quintino da Rocha
author_facet Monica Araujo das Neves
Caroline Martins de Jesus
Jhones Luiz de Oliveira
Samuel dos Santos Soares Buna
Lucilene Amorim Silva
Leonardo Fernandes Fraceto
Cláudia Quintino da Rocha
author_sort Monica Araujo das Neves
collection DOAJ
description <b>Background/Objectives:</b> Leishmaniasis, caused by protozoa of the genus <i>Leishmania</i>, is a major global health issue due to the limitations of current treatments, which include low efficacy, high costs, and severe side effects. This study aimed to develop a more effective and less toxic therapy by utilizing zein nanoparticles (ZNPs) in combination with a nonpolar fraction (DCMF) from <i>Fridericia platyphylla</i> (Syn. <i>Arrabidaea brachypoda</i>), a plant rich in dimeric flavonoids called brachydins. <b>Methods:</b> Zein nanoparticles were used as carriers to encapsulate DCMF. The system was characterized by measuring particle diameter, polydispersity index, zeta potential, and encapsulation efficiency. Analytical techniques such as FTIR, DSC, and AFM were employed to confirm the encapsulation and stability of DCMF. Antileishmanial activity was assessed against <i>Leishmania amazonensis</i> promastigotes and amastigotes, while cytotoxicity was tested on RAW264.7 macrophages. <b>Results:</b> The ZNP-DCMF system exhibited favorable properties, including a particle diameter of 141 nm, a polydispersity index below 0.2, and a zeta potential of 11.3 mV. DCMF was encapsulated with an efficiency of 94.6% and remained stable for 49 days. In antileishmanial assays, ZNP-DCMF inhibited the viability of promastigotes with an IC50 of 36.33 μg/mL and amastigotes with an IC50 of 0.72 μg/mL, demonstrating higher selectivity (SI = 694.44) compared to DCMF alone (SI = 43.11). ZNP-DCMF was non-cytotoxic to RAW264.7 macrophages, with a CC50 > 500 μg/mL. <b>Conclusions:</b> Combining <i>F. platyphylla</i> DCMF with zein nanoparticles as a carrier presents a promising approach for leishmaniasis treatment, offering improved efficacy, reduced toxicity, and protection of bioactive compounds from degradation.
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spelling doaj-art-8fa1ed0908e64f23bb0e1f77de8fd0192024-12-27T14:46:39ZengMDPI AGPharmaceutics1999-49232024-12-011612160310.3390/pharmaceutics16121603Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial ApplicationsMonica Araujo das Neves0Caroline Martins de Jesus1Jhones Luiz de Oliveira2Samuel dos Santos Soares Buna3Lucilene Amorim Silva4Leonardo Fernandes Fraceto5Cláudia Quintino da Rocha6PostGraduate Program in Chemistry, Center for Exact Sciences and Technology (CCET), UFMA-Federal University of Maranhão, São Luís 65080-805, BrazilPostGraduate Program in Health Sciences, Center for Biological and Health Sciences (CCBS), UFMA-Federal University of Maranhão, São Luís 65080-805, BrazilDepartment of Environmental Engineering, Institute of Science and Technology of Sorocaba, São Paulo State University (UNESP), Sorocaba 18087-180, BrazilPostGraduate Program in Chemistry, Center for Exact Sciences and Technology (CCET), UFMA-Federal University of Maranhão, São Luís 65080-805, BrazilPostGraduate Program in Health Sciences, Center for Biological and Health Sciences (CCBS), UFMA-Federal University of Maranhão, São Luís 65080-805, BrazilDepartment of Environmental Engineering, Institute of Science and Technology of Sorocaba, São Paulo State University (UNESP), Sorocaba 18087-180, BrazilPostGraduate Program in Chemistry, Center for Exact Sciences and Technology (CCET), UFMA-Federal University of Maranhão, São Luís 65080-805, Brazil<b>Background/Objectives:</b> Leishmaniasis, caused by protozoa of the genus <i>Leishmania</i>, is a major global health issue due to the limitations of current treatments, which include low efficacy, high costs, and severe side effects. This study aimed to develop a more effective and less toxic therapy by utilizing zein nanoparticles (ZNPs) in combination with a nonpolar fraction (DCMF) from <i>Fridericia platyphylla</i> (Syn. <i>Arrabidaea brachypoda</i>), a plant rich in dimeric flavonoids called brachydins. <b>Methods:</b> Zein nanoparticles were used as carriers to encapsulate DCMF. The system was characterized by measuring particle diameter, polydispersity index, zeta potential, and encapsulation efficiency. Analytical techniques such as FTIR, DSC, and AFM were employed to confirm the encapsulation and stability of DCMF. Antileishmanial activity was assessed against <i>Leishmania amazonensis</i> promastigotes and amastigotes, while cytotoxicity was tested on RAW264.7 macrophages. <b>Results:</b> The ZNP-DCMF system exhibited favorable properties, including a particle diameter of 141 nm, a polydispersity index below 0.2, and a zeta potential of 11.3 mV. DCMF was encapsulated with an efficiency of 94.6% and remained stable for 49 days. In antileishmanial assays, ZNP-DCMF inhibited the viability of promastigotes with an IC50 of 36.33 μg/mL and amastigotes with an IC50 of 0.72 μg/mL, demonstrating higher selectivity (SI = 694.44) compared to DCMF alone (SI = 43.11). ZNP-DCMF was non-cytotoxic to RAW264.7 macrophages, with a CC50 > 500 μg/mL. <b>Conclusions:</b> Combining <i>F. platyphylla</i> DCMF with zein nanoparticles as a carrier presents a promising approach for leishmaniasis treatment, offering improved efficacy, reduced toxicity, and protection of bioactive compounds from degradation.https://www.mdpi.com/1999-4923/16/12/1603neglected diseasesbrachydinspolymeric nanoparticlezeinleishmaniasis
spellingShingle Monica Araujo das Neves
Caroline Martins de Jesus
Jhones Luiz de Oliveira
Samuel dos Santos Soares Buna
Lucilene Amorim Silva
Leonardo Fernandes Fraceto
Cláudia Quintino da Rocha
Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
Pharmaceutics
neglected diseases
brachydins
polymeric nanoparticle
zein
leishmaniasis
title Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
title_full Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
title_fullStr Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
title_full_unstemmed Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
title_short Zein Nanoparticles-Loaded Flavonoids-Rich Fraction from <i>Fridericia platyphylla</i>: Potential Antileishmanial Applications
title_sort zein nanoparticles loaded flavonoids rich fraction from i fridericia platyphylla i potential antileishmanial applications
topic neglected diseases
brachydins
polymeric nanoparticle
zein
leishmaniasis
url https://www.mdpi.com/1999-4923/16/12/1603
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