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 bioavailability. Therefore, the efficacy of NRG can be...

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Published inFrontiers in nutrition (Lausanne) Vol. 9; p. 850103
Main Authors Ishimoto, Kenji, Shimada, Yukiko, Ohno, Akane, Otani, Shuichi, Ago, Yukio, Maeda, Soya, Lin, Bangzhong, Nunomura, Kazuto, Hino, Nobumasa, Suzuki, Masayuki, Nakagawa, Shinsaku
Format Journal Article
LanguageEnglish
Published Switzerland Frontiers Media S.A 27.04.2022
Subjects
amorphous solid dispersion
analgesia
functional food
gastrointestinal absorption
hot-melt extrusion
naringenin
Nutrition
naringenin
poor water solubility
toxicity
gastrointestinal absorption
analgesia
functional food
hot-melt extrusion
amorphous solid dispersion
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Abstract 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 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.
AbstractList 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.
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.
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 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.
Author Ishimoto, Kenji
Ago, Yukio
Hino, Nobumasa
Shimada, Yukiko
Ohno, Akane
Maeda, Soya
Nunomura, Kazuto
Otani, Shuichi
Lin, Bangzhong
Nakagawa, Shinsaku
Suzuki, Masayuki
AuthorAffiliation 3 Global Center for Medical Engineering and Informatics, Osaka University , Osaka , Japan
5 Mitsui Norin Co., Ltd., R&D Group , Shizuoka , Japan
6 Department of Cellular and Molecular Pharmacology, Graduate School of Biomedical and Health Sciences, Hiroshima University , Hiroshima , Japan
1 Laboratory of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University , Osaka , Japan
2 Laboratory of Innovative Food Science, Graduate School of Pharmaceutical Sciences, Osaka University , Osaka , Japan
4 Center for Supporting Drug Discovery and Life Science Research, Graduate School of Pharmaceutical Sciences, Osaka University , Osaka , Japan
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Copyright Copyright © 2022 Ishimoto, Shimada, Ohno, Otani, Ago, Maeda, Lin, Nunomura, Hino, Suzuki and Nakagawa.
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Keywords naringenin
poor water solubility
toxicity
gastrointestinal absorption
analgesia
functional food
hot-melt extrusion
amorphous solid dispersion
Language English
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Reviewed by: Vineet Kumar, Lovely Professional University, India; Marcilio Cunha Filho, University of Brasília, Brazil; Roshan Tiwari, Amneal Pharmaceuticals, United States
This article was submitted to Food Chemistry, a section of the journal Frontiers in Nutrition
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Snippet Naringenin (NRG) is a plant-derived flavonoid. Due to its antioxidant, anti-inflammatory, and analgesic activities it is beneficial to human health and is...
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SubjectTerms amorphous solid dispersion
analgesia
functional food
gastrointestinal absorption
hot-melt extrusion
naringenin
Nutrition
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Title Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion
URI https://www.ncbi.nlm.nih.gov/pubmed/35571922
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