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Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications
Lycopene is a carotenoid with potential use in the treatment of chronic illnesses. Here, different formulations of lycopene were studied: lycopene-rich extract from red guava (LEG), purified lycopene from red guava (LPG) and a self-emulsifying drug delivery system loaded with LPG (nanoLPG). The effe...
Autores principales: | , , , , , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10301544/ https://www.ncbi.nlm.nih.gov/pubmed/37375852 http://dx.doi.org/10.3390/ph16060905 |
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author | Alves, Maíra Bernardes Vasconcelos, Andreanne Gomes Silva de Carvalho, Amandda Évelin Slompo, Robson Camilotti Sá, Bruno Silva Gonçalves, Maria Júlia Lima Lima Moura, Liz Nayara Ribeiro da Costa Brito, Ana Karolinne da Silva França, José Vinícius de Sousa Martins, Maria do Carmo de Carvalho e Rizzo, Márcia dos Santos Soares, Susana Bastos, Verónica Saldanha de Araujo, Felipe Mogharbel, Bassam Felipe de Carvalho, Katherine Athayde Teixeira Oliveira, Helena Plácido, Alexandra Arcanjo, Daniel Dias Rufino Barbosa, Eder Alves Leite, José Roberto de Souza de Almeida |
author_facet | Alves, Maíra Bernardes Vasconcelos, Andreanne Gomes Silva de Carvalho, Amandda Évelin Slompo, Robson Camilotti Sá, Bruno Silva Gonçalves, Maria Júlia Lima Lima Moura, Liz Nayara Ribeiro da Costa Brito, Ana Karolinne da Silva França, José Vinícius de Sousa Martins, Maria do Carmo de Carvalho e Rizzo, Márcia dos Santos Soares, Susana Bastos, Verónica Saldanha de Araujo, Felipe Mogharbel, Bassam Felipe de Carvalho, Katherine Athayde Teixeira Oliveira, Helena Plácido, Alexandra Arcanjo, Daniel Dias Rufino Barbosa, Eder Alves Leite, José Roberto de Souza de Almeida |
author_sort | Alves, Maíra Bernardes |
collection | PubMed |
description | Lycopene is a carotenoid with potential use in the treatment of chronic illnesses. Here, different formulations of lycopene were studied: lycopene-rich extract from red guava (LEG), purified lycopene from red guava (LPG) and a self-emulsifying drug delivery system loaded with LPG (nanoLPG). The effects of administering orally various doses of LEG to hypercholesterolemic hamsters were evaluated regarding the liver function of the animals. The cytotoxicity of LPG in Vero cells was analyzed by a crystal violet assay and by fluorescence microscopy. In addition, nanoLPG was employed in stability tests. LPG and nanoLPG were tested for their cytotoxic effect on human keratinocytes and antioxidant capacity on cells in an endothelial dysfunction model in an isolated rat aorta. Finally, the effect of different nanoLPG concentrations on the expression of immune-related genes (IL-10, TNF-α, COX-2 and IFN-γ) from peripheral blood mononuclear cells (PBMC) using real-time PCR was also analyzed. Results suggest that LEG, despite not being able to improve blood markers indicative of liver function in hypercholesterolemic hamsters, reduced hepatic degenerative changes. Additionally, LPG did not show cytotoxicity in Vero cells. In relation to nanoLPG, the effects produced by heat stress evaluated by Dynamics Light Scattering (DLS) and visually were loss of color, texture change and phase separation after 15 days without interfering with the droplet size, so the formulation proved to be efficient in stabilizing the encapsulated lycopene. Although LPG and nanoLPG showed moderate toxicity to keratinocytes, which may be related to cell lineage characteristics, both revealed potent antioxidant activity. LPG and nanoLPG showed vasoprotective effects in aortic preparations. The gene expression assay indicates that, although no significant differences were observed in the expression of IL-10 and TNF-α, the PBMCs treated with nanoLPG showed a reduction in transcriptional levels of IFN-γ and an increased expression of COX-2. Thus, the work adds evidence to the safety of the use of lycopene by humans and shows that tested formulations, mainly nanoLPG due to its stability, stand out as promising and biosafe products for the treatment of diseases that have oxidative stress and inflammation in their etiopathology. |
format | Online Article Text |
id | pubmed-10301544 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-103015442023-06-29 Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications Alves, Maíra Bernardes Vasconcelos, Andreanne Gomes Silva de Carvalho, Amandda Évelin Slompo, Robson Camilotti Sá, Bruno Silva Gonçalves, Maria Júlia Lima Lima Moura, Liz Nayara Ribeiro da Costa Brito, Ana Karolinne da Silva França, José Vinícius de Sousa Martins, Maria do Carmo de Carvalho e Rizzo, Márcia dos Santos Soares, Susana Bastos, Verónica Saldanha de Araujo, Felipe Mogharbel, Bassam Felipe de Carvalho, Katherine Athayde Teixeira Oliveira, Helena Plácido, Alexandra Arcanjo, Daniel Dias Rufino Barbosa, Eder Alves Leite, José Roberto de Souza de Almeida Pharmaceuticals (Basel) Article Lycopene is a carotenoid with potential use in the treatment of chronic illnesses. Here, different formulations of lycopene were studied: lycopene-rich extract from red guava (LEG), purified lycopene from red guava (LPG) and a self-emulsifying drug delivery system loaded with LPG (nanoLPG). The effects of administering orally various doses of LEG to hypercholesterolemic hamsters were evaluated regarding the liver function of the animals. The cytotoxicity of LPG in Vero cells was analyzed by a crystal violet assay and by fluorescence microscopy. In addition, nanoLPG was employed in stability tests. LPG and nanoLPG were tested for their cytotoxic effect on human keratinocytes and antioxidant capacity on cells in an endothelial dysfunction model in an isolated rat aorta. Finally, the effect of different nanoLPG concentrations on the expression of immune-related genes (IL-10, TNF-α, COX-2 and IFN-γ) from peripheral blood mononuclear cells (PBMC) using real-time PCR was also analyzed. Results suggest that LEG, despite not being able to improve blood markers indicative of liver function in hypercholesterolemic hamsters, reduced hepatic degenerative changes. Additionally, LPG did not show cytotoxicity in Vero cells. In relation to nanoLPG, the effects produced by heat stress evaluated by Dynamics Light Scattering (DLS) and visually were loss of color, texture change and phase separation after 15 days without interfering with the droplet size, so the formulation proved to be efficient in stabilizing the encapsulated lycopene. Although LPG and nanoLPG showed moderate toxicity to keratinocytes, which may be related to cell lineage characteristics, both revealed potent antioxidant activity. LPG and nanoLPG showed vasoprotective effects in aortic preparations. The gene expression assay indicates that, although no significant differences were observed in the expression of IL-10 and TNF-α, the PBMCs treated with nanoLPG showed a reduction in transcriptional levels of IFN-γ and an increased expression of COX-2. Thus, the work adds evidence to the safety of the use of lycopene by humans and shows that tested formulations, mainly nanoLPG due to its stability, stand out as promising and biosafe products for the treatment of diseases that have oxidative stress and inflammation in their etiopathology. MDPI 2023-06-20 /pmc/articles/PMC10301544/ /pubmed/37375852 http://dx.doi.org/10.3390/ph16060905 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Alves, Maíra Bernardes Vasconcelos, Andreanne Gomes Silva de Carvalho, Amandda Évelin Slompo, Robson Camilotti Sá, Bruno Silva Gonçalves, Maria Júlia Lima Lima Moura, Liz Nayara Ribeiro da Costa Brito, Ana Karolinne da Silva França, José Vinícius de Sousa Martins, Maria do Carmo de Carvalho e Rizzo, Márcia dos Santos Soares, Susana Bastos, Verónica Saldanha de Araujo, Felipe Mogharbel, Bassam Felipe de Carvalho, Katherine Athayde Teixeira Oliveira, Helena Plácido, Alexandra Arcanjo, Daniel Dias Rufino Barbosa, Eder Alves Leite, José Roberto de Souza de Almeida Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title | Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title_full | Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title_fullStr | Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title_full_unstemmed | Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title_short | Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications |
title_sort | lycopene from red guava (psidium guajava l.): from hepatoprotective effect to its use as promising self-emulsifying drug delivery system for anti-inflammatory and antioxidant applications |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10301544/ https://www.ncbi.nlm.nih.gov/pubmed/37375852 http://dx.doi.org/10.3390/ph16060905 |
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