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Article

Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study

1
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China
2
Key Laboratory for Production Process Control and Quality Evaluation of Traditional Chinese Medicine, Beijing Municipal Science & Technology Commission, Beijing 102488, China
3
School of Life Sciences, Beijing University of Chinese Medicine, Beijing 102488, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2023, 15(1), 125; https://doi.org/10.3390/pharmaceutics15010125
Submission received: 1 November 2022 / Revised: 16 December 2022 / Accepted: 26 December 2022 / Published: 30 December 2022
(This article belongs to the Special Issue Design of Dosage Forms with Improved Biopharmaceutical Properties)

Abstract

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.
Keywords: surface-active drug; saponin; glycyrrhizic acid; biopharmaceutics; drug-loaded micelles surface-active drug; saponin; glycyrrhizic acid; biopharmaceutics; drug-loaded micelles
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MDPI and ACS Style

Dai, X.; Liao, Y.; Yang, C.; Zhang, Y.; Feng, M.; Tian, Y.; Qu, Q.; Sheng, M.; Li, Z.; Peng, X.; et al. Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study. Pharmaceutics 2023, 15, 125. https://doi.org/10.3390/pharmaceutics15010125

AMA Style

Dai X, Liao Y, Yang C, Zhang Y, Feng M, Tian Y, Qu Q, Sheng M, Li Z, Peng X, et al. Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study. Pharmaceutics. 2023; 15(1):125. https://doi.org/10.3390/pharmaceutics15010125

Chicago/Turabian Style

Dai, Xingxing, Yuyao Liao, Cuiting Yang, Yingying Zhang, Minfang Feng, Yuting Tian, Qingsong Qu, Mengke Sheng, Zhixun Li, Xinhui Peng, and et al. 2023. "Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study" Pharmaceutics 15, no. 1: 125. https://doi.org/10.3390/pharmaceutics15010125

APA Style

Dai, X., Liao, Y., Yang, C., Zhang, Y., Feng, M., Tian, Y., Qu, Q., Sheng, M., Li, Z., Peng, X., Cen, S., & Shi, X. (2023). Diammonium Glycyrrhizinate-Based Micelles for Improving the Hepatoprotective Effect of Baicalin: Characterization and Biopharmaceutical Study. Pharmaceutics, 15(1), 125. https://doi.org/10.3390/pharmaceutics15010125

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