Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers
Phytosterols (PS) offer significant health benefits in human diet, but its poor solubility limits its effectiveness and application. This study explored enhancing PS solubility by testing thirteen food-grade coformers, three preparation methods and proportions screening to obtain the optimal formula...
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| Format: | Article |
| Language: | English |
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Elsevier
2025-01-01
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| Series: | Current Research in Food Science |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2665927125000152 |
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| author | Yuxin Li Yingting Luo Xuening Song Yuzhuo Wang Simiao Liu Fazheng Ren Lingyan Kong Hao Zhang |
| author_facet | Yuxin Li Yingting Luo Xuening Song Yuzhuo Wang Simiao Liu Fazheng Ren Lingyan Kong Hao Zhang |
| author_sort | Yuxin Li |
| collection | DOAJ |
| description | Phytosterols (PS) offer significant health benefits in human diet, but its poor solubility limits its effectiveness and application. This study explored enhancing PS solubility by testing thirteen food-grade coformers, three preparation methods and proportions screening to obtain the optimal formulation. Nicotinamide (Nic) was identified as the most effective coformer. A 20:1 (w/w) PS-Nic co-amorphous (CM) mixture, prepared via freeze-drying, achieved a solubility of 1536.4 μg/mL, significantly higher than pure PS. X-ray diffraction and differential scanning calorimetry confirmed the amorphous state of the mixture. Fourier-transform infrared, Raman, and 1H NMR spectroscopies, along with molecular dynamics simulations, revealed strong intermolecular interactions between PS and Nic. The PS-Nic CM demonstrated up to 60% in vitro dissolution and release within 2 h and maintained stable after storage at 4 °C for 6 months and under accelerated conditions equivalent to 10 months at room temperature. In sum, the crystal structure of PS was altered, and formed a co-amorphous system by using Nic as the optimal ligand via lyophilization to increase solubility. These findings suggest that the PS-Nic CM system has potential applications in functional foods, offering a feasible strategy to enhance the bioavailability of PS. |
| format | Article |
| id | doaj-art-693387c0c16b4a4b832508b71632be54 |
| institution | Kabale University |
| issn | 2665-9271 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Current Research in Food Science |
| spelling | doaj-art-693387c0c16b4a4b832508b71632be542025-01-24T04:45:41ZengElsevierCurrent Research in Food Science2665-92712025-01-0110100984Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformersYuxin Li0Yingting Luo1Xuening Song2Yuzhuo Wang3Simiao Liu4Fazheng Ren5Lingyan Kong6Hao Zhang7College of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, China; Beijing Laboratory of Food Quality and Safety, Department of Nutrition and Health, China Agricultural University, Beijing, 100091, China; Food Laboratory of Zhongyuan, Luohe, 462300, Henan, ChinaDepartment of Human Nutrition, Hospitality and Sport Management, The University of Alabama, Tuscaloosa, 35487, Alabama, USACollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, China; Beijing Laboratory of Food Quality and Safety, Department of Nutrition and Health, China Agricultural University, Beijing, 100091, China; Food Laboratory of Zhongyuan, Luohe, 462300, Henan, China; Corresponding author. College of Food Science and Nutritional Engineering, China Agricultural University, Beijing, 100083, China.Phytosterols (PS) offer significant health benefits in human diet, but its poor solubility limits its effectiveness and application. This study explored enhancing PS solubility by testing thirteen food-grade coformers, three preparation methods and proportions screening to obtain the optimal formulation. Nicotinamide (Nic) was identified as the most effective coformer. A 20:1 (w/w) PS-Nic co-amorphous (CM) mixture, prepared via freeze-drying, achieved a solubility of 1536.4 μg/mL, significantly higher than pure PS. X-ray diffraction and differential scanning calorimetry confirmed the amorphous state of the mixture. Fourier-transform infrared, Raman, and 1H NMR spectroscopies, along with molecular dynamics simulations, revealed strong intermolecular interactions between PS and Nic. The PS-Nic CM demonstrated up to 60% in vitro dissolution and release within 2 h and maintained stable after storage at 4 °C for 6 months and under accelerated conditions equivalent to 10 months at room temperature. In sum, the crystal structure of PS was altered, and formed a co-amorphous system by using Nic as the optimal ligand via lyophilization to increase solubility. These findings suggest that the PS-Nic CM system has potential applications in functional foods, offering a feasible strategy to enhance the bioavailability of PS.http://www.sciencedirect.com/science/article/pii/S2665927125000152PhytosterolCo-amorphousSolubilityNicotinamideLyophilization |
| spellingShingle | Yuxin Li Yingting Luo Xuening Song Yuzhuo Wang Simiao Liu Fazheng Ren Lingyan Kong Hao Zhang Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers Current Research in Food Science Phytosterol Co-amorphous Solubility Nicotinamide Lyophilization |
| title | Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers |
| title_full | Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers |
| title_fullStr | Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers |
| title_full_unstemmed | Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers |
| title_short | Enhancing water solubility of phytosterols through Co-amorphization with food-grade coformers |
| title_sort | enhancing water solubility of phytosterols through co amorphization with food grade coformers |
| topic | Phytosterol Co-amorphous Solubility Nicotinamide Lyophilization |
| url | http://www.sciencedirect.com/science/article/pii/S2665927125000152 |
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