Construction of Tax-PC/SDC/PVP-K30 micelles and their protective effect on alcoholic liver injury
10.16438/j.0513-4870.2024-0758
- VernacularTitle:花旗松素-磷脂/胆盐/聚维酮-K30胶束的构建及对酒精性肝损伤的保护作用
- Author:
Shi-yu ZHANG
1
;
Jing-meng SUN
2
;
Dong-dong LI
1
;
Xin ZHANG
1
;
Jia-hui ZHANG
1
;
Wei-yu ZHANG
1
Author Information
1. College of Pharmacy, Changchun University of Chinese Medicine, Changchun 130117, China
2. Department of Clinical Pharmacy, Hospital No. 1, Jilin University, Changchun 130061, China
- Publication Type:Research Article
- Keywords:
taxifolin;
micelle;
preparation process;
alcoholic liver injury;
characterization
- From:
Acta Pharmaceutica Sinica
2025;60(2):488-497
- CountryChina
- Language:Chinese
-
Abstract:
Taxifolin (Tax) has been proved to be a medicinal edible substance with protective effects against alcoholic liver injury, however, its poor hydrophilicity and permeability have hindered the clinical application of Tax. In this study, we prepared taxifolin-phosphatidylcholine/sodium deoxycholate/PVP-K30 micells (Tax-MLs). Box-Behnken test was used to obtain the optimal preparation process, and Tax-MLs were characterised by transmission electron microscopy and fourier transform infrared spectroscopy. Physicochemical parameters such as proximate micelle concentration, equilibrium solubility and oil-water partition coefficient were determined, and the release pattern of Tax-MLs was investigated by in vitro digestion simulation. Alcoholic liver injury model to explore the in vivo efficacy of Tax-MLs. The results showed that the average particle size, polydispersity index (PDI) and zeta potential of Tax-MLs were 36.90 ± 4.57 nm, 0.194 ± 0.01 and -32.6 ± 0.35 mV, respectively, and the uniform size and distribution of Tax-MLs were observed by transmission electron microscopy. The formation of Tax-MLs was proved by differential scanning calorimetry and fourier transform infrared spectroscopy. In terms of physicochemical properties, the solubility of Tax-MLs in water increased by 92.02 times compared with Tax, and its oil-water partition coefficient in water increased from 0.43 to 1.14, which proved that Tax-MLs could improve its solubility and permeability. The in vivo pharmacodynamic results showed that compared with the Tax group, Tax-MLs low, medium and high dose groups showed a significant reduction in liver indices and serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) (P < 0.05), and enhanced the activities of superoxide dismutase (SOD) and glutathione (GSH), and lowered the levels of malondialdehyde (MDA) more significantly in the hepatic tissues. Tax-MLs effectively improved drug solubility and permeability, and enhanced the protective effect against alcoholic liver injury. Animal experiments were conducted with approval from the Animal Ethics Committee of Changchun University of Traditional Chinese Medicine (approval number: 2023601).
