Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study
Saponins are an important class of surface-active substances. When formulated as an active ingredient or co-used with other drugs, the effect of their surface activity on efficacy or safety must be considered. In this paper, diammonium glycyrrhizinate (DG), a clinical hepatoprotective drug that has...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/1/125 |
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| author | Xingxing Dai Yuyao Liao Cuiting Yang Yingying Zhang Minfang Feng Yuting Tian Qingsong Qu Mengke Sheng Zhixun Li Xinhui Peng Shuai Cen Xinyuan Shi |
| author_facet | Xingxing Dai Yuyao Liao Cuiting Yang Yingying Zhang Minfang Feng Yuting Tian Qingsong Qu Mengke Sheng Zhixun Li Xinhui Peng Shuai Cen Xinyuan Shi |
| author_sort | Xingxing Dai |
| collection | DOAJ |
| description | Saponins are an important class of surface-active substances. When formulated as an active ingredient or co-used with other drugs, the effect of their surface activity on efficacy or safety must be considered. In this paper, diammonium glycyrrhizinate (DG), a clinical hepatoprotective drug that has long been used as a biosurfactant, was taken as the research object to study its combined hepatoprotective effect with baicalin (BAI). Animal experiments proved that the preparation of DG and BAI integrated into micelles (BAI-DG Ms) had a better protective effect on acute liver injury caused by carbon tetrachloride than the direct combined use of the two. From the perspective of biopharmaceutics, the synergistic mechanism of BAI-DG Ms was further explored. The results showed that after forming BAI-DG Ms with DG, the solubility of BAI increased by 4.75 to 6.25 times, and the cumulative percentage release in the gastrointestinal tract also increased by 2.42 times. In addition, the negatively charged BAI-DG Ms were more likely to penetrate the mucus layer and be absorbed by endocytosis. These findings provide support for the rational application of glycyrrhizin, and other saponins. |
| first_indexed | 2024-03-09T11:27:37Z |
| format | Article |
| id | doaj.art-78421f8d25274015a682a3212101ae32 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T11:27:37Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-78421f8d25274015a682a3212101ae322023-11-30T23:58:02ZengMDPI AGPharmaceutics1999-49232022-12-0115112510.3390/pharmaceutics15010125Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical StudyXingxing Dai0Yuyao Liao1Cuiting Yang2Yingying Zhang3Minfang Feng4Yuting Tian5Qingsong Qu6Mengke Sheng7Zhixun Li8Xinhui Peng9Shuai Cen10Xinyuan Shi11School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Life Sciences, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Life Sciences, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, ChinaSaponins are an important class of surface-active substances. When formulated as an active ingredient or co-used with other drugs, the effect of their surface activity on efficacy or safety must be considered. In this paper, diammonium glycyrrhizinate (DG), a clinical hepatoprotective drug that has long been used as a biosurfactant, was taken as the research object to study its combined hepatoprotective effect with baicalin (BAI). Animal experiments proved that the preparation of DG and BAI integrated into micelles (BAI-DG Ms) had a better protective effect on acute liver injury caused by carbon tetrachloride than the direct combined use of the two. From the perspective of biopharmaceutics, the synergistic mechanism of BAI-DG Ms was further explored. The results showed that after forming BAI-DG Ms with DG, the solubility of BAI increased by 4.75 to 6.25 times, and the cumulative percentage release in the gastrointestinal tract also increased by 2.42 times. In addition, the negatively charged BAI-DG Ms were more likely to penetrate the mucus layer and be absorbed by endocytosis. These findings provide support for the rational application of glycyrrhizin, and other saponins.https://www.mdpi.com/1999-4923/15/1/125surface-active drugsaponinglycyrrhizic acidbiopharmaceuticsdrug-loaded micelles |
| spellingShingle | Xingxing Dai Yuyao Liao Cuiting Yang Yingying Zhang Minfang Feng Yuting Tian Qingsong Qu Mengke Sheng Zhixun Li Xinhui Peng Shuai Cen Xinyuan Shi Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study Pharmaceutics surface-active drug saponin glycyrrhizic acid biopharmaceutics drug-loaded micelles |
| title | Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study |
| title_full | Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study |
| title_fullStr | Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study |
| title_full_unstemmed | Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study |
| title_short | Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study |
| title_sort | diammonium glycyrrhizinate based micelles for improving the hepatoprotective effect of baicalin characterization and biopharmaceutical study |
| topic | surface-active drug saponin glycyrrhizic acid biopharmaceutics drug-loaded micelles |
| url | https://www.mdpi.com/1999-4923/15/1/125 |
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