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Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion

Naringenin (NRG) is a plant-derived flavonoid. Due to its antioxidant, anti-inflammatory, and analgesic activities it is beneficial to human health and is often used as a functional food ingredient; however, it has poor water solubility and low in vivo bioavailability. Therefore, the efficacy of NRG...

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Autores principales: Ishimoto, Kenji, Shimada, Yukiko, Ohno, Akane, Otani, Shuichi, Ago, Yukio, Maeda, Soya, Lin, Bangzhong, Nunomura, Kazuto, Hino, Nobumasa, Suzuki, Masayuki, Nakagawa, Shinsaku
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9093646/
https://www.ncbi.nlm.nih.gov/pubmed/35571922
http://dx.doi.org/10.3389/fnut.2022.850103
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author Ishimoto, Kenji
Shimada, Yukiko
Ohno, Akane
Otani, Shuichi
Ago, Yukio
Maeda, Soya
Lin, Bangzhong
Nunomura, Kazuto
Hino, Nobumasa
Suzuki, Masayuki
Nakagawa, Shinsaku
author_facet Ishimoto, Kenji
Shimada, Yukiko
Ohno, Akane
Otani, Shuichi
Ago, Yukio
Maeda, Soya
Lin, Bangzhong
Nunomura, Kazuto
Hino, Nobumasa
Suzuki, Masayuki
Nakagawa, Shinsaku
author_sort Ishimoto, Kenji
collection PubMed
description Naringenin (NRG) is a plant-derived flavonoid. Due to its antioxidant, anti-inflammatory, and analgesic activities it is beneficial to human health and is often used as a functional food ingredient; however, it has poor water solubility and low in vivo bioavailability. Therefore, the efficacy of NRG can be improved by enhancing its water solubility to increase gastrointestinal absorption. Conventional methods for the formulation of NRG are very complex and use toxic organic solvents, making them impractical for the production of functional foods. The objective of this study was to develop a safe and effective NRG-based functional food material. Previously, we established a technology to prepare amorphous solid dispersions (SDs) from functional food ingredients with poor water solubility and used hot-melt extrusion technology that is comparatively simple and does not involve the use of organic solvents. In this study, we prepared NRG SD and evaluated them both physicochemically and biochemically. NRG SD had superior water solubility and gastrointestinal absorption relative to native NRG and showed higher analgesic efficacy in rats than crystalline NRG. NRG SD was administered to mice in a mixed diet for 28 days, and organ weights and hematological/clinical biochemical parameters were assessed. NRG SD did not demonstrate severe adverse effects. The results suggest that NRG SD is a safe and highly efficacious formulation that can be used as a functional food material in the future.
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spelling pubmed-90936462022-05-12 Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion Ishimoto, Kenji Shimada, Yukiko Ohno, Akane Otani, Shuichi Ago, Yukio Maeda, Soya Lin, Bangzhong Nunomura, Kazuto Hino, Nobumasa Suzuki, Masayuki Nakagawa, Shinsaku Front Nutr Nutrition Naringenin (NRG) is a plant-derived flavonoid. Due to its antioxidant, anti-inflammatory, and analgesic activities it is beneficial to human health and is often used as a functional food ingredient; however, it has poor water solubility and low in vivo bioavailability. Therefore, the efficacy of NRG can be improved by enhancing its water solubility to increase gastrointestinal absorption. Conventional methods for the formulation of NRG are very complex and use toxic organic solvents, making them impractical for the production of functional foods. The objective of this study was to develop a safe and effective NRG-based functional food material. Previously, we established a technology to prepare amorphous solid dispersions (SDs) from functional food ingredients with poor water solubility and used hot-melt extrusion technology that is comparatively simple and does not involve the use of organic solvents. In this study, we prepared NRG SD and evaluated them both physicochemically and biochemically. NRG SD had superior water solubility and gastrointestinal absorption relative to native NRG and showed higher analgesic efficacy in rats than crystalline NRG. NRG SD was administered to mice in a mixed diet for 28 days, and organ weights and hematological/clinical biochemical parameters were assessed. NRG SD did not demonstrate severe adverse effects. The results suggest that NRG SD is a safe and highly efficacious formulation that can be used as a functional food material in the future. Frontiers Media S.A. 2022-04-27 /pmc/articles/PMC9093646/ /pubmed/35571922 http://dx.doi.org/10.3389/fnut.2022.850103 Text en Copyright © 2022 Ishimoto, Shimada, Ohno, Otani, Ago, Maeda, Lin, Nunomura, Hino, Suzuki and Nakagawa. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Nutrition
Ishimoto, Kenji
Shimada, Yukiko
Ohno, Akane
Otani, Shuichi
Ago, Yukio
Maeda, Soya
Lin, Bangzhong
Nunomura, Kazuto
Hino, Nobumasa
Suzuki, Masayuki
Nakagawa, Shinsaku
Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title_full Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title_fullStr Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title_full_unstemmed Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title_short Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
title_sort physicochemical and biochemical evaluation of amorphous solid dispersion of naringenin prepared using hot-melt extrusion
topic Nutrition
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9093646/
https://www.ncbi.nlm.nih.gov/pubmed/35571922
http://dx.doi.org/10.3389/fnut.2022.850103
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