Preparation of salvianolic acid B, tanshinone Ⅱ_A, and glycyrrhetinic acid lipid emulsion and its protective effect against acute liver injury induced by acetaminophen.
10.19540/j.cnki.cjcmm.20220705.302
- Author:
Xiu-Rong ZHANG
1
;
Tao LIN
1
;
Xiu-Li WANG
1
;
Xiao-Jie WANG
2
;
Heng GU
3
Author Information
1. School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.
2. College of Bioengineering,Beijing Polytechnic Beijing 100176, China.
3. TCM Pharmacy, Kunming Municipal Hospital of Traditional Chinese Medicine Kunming 650011, China.
- Publication Type:Journal Article
- Keywords:
acetaminophen;
acute liver injury;
emulsion;
glycyrrhetinic acid;
salvianolic acid B;
tanshinone Ⅱ_A
- MeSH:
Abietanes/therapeutic use*;
Acetaminophen/therapeutic use*;
Alanine Transaminase/metabolism*;
Animals;
Antipyretics/therapeutic use*;
Aspartate Aminotransferases/metabolism*;
Benzofurans/therapeutic use*;
Chemical and Drug Induced Liver Injury/prevention & control*;
Depsides/therapeutic use*;
Emulsions;
Glycyrrhetinic Acid/therapeutic use*;
Liver/drug effects*;
Malondialdehyde;
Mice
- From:
China Journal of Chinese Materia Medica
2022;47(17):4634-4642
- CountryChina
- Language:Chinese
-
Abstract:
Salvianolic acid B(Sal B), tanshinone Ⅱ_A(TSN Ⅱ_A), and glycyrrhetinic acid(GA) lipid emulsion(GTS-LE) was prepared by the high-speed dispersion method combined with ultrasonic emulsification.The preparation process of the emulsion was optimized by single-factor method and D-optimal method with appearance, centrifugal stability, and particle size of the emulsion as evalua-tion indexes, followed by verification.In vitro release of Sal B, TSN Ⅱ_A, and GA in GTS-LE was performed by reverse dialysis.In vivo pharmacokinetic evaluation was carried out in mice.The acute liver injury model was induced by acetaminophen.The effect of oral GTS-LE on the acute liver injury was investigated by serum liver function indexes and pathological changes in liver tissues of mice.The results showed that under the optimal preparation process, the average particle size of GTS-LE was(145.4±9.25) nm and the Zeta potential was(-33.6±1.45) mV.The drug-loading efficiencies of Sal B, TSN Ⅱ_A, and GA in GTS-LE were above 95%, and the drug release in vitro conformed to the Higuchi equation.The pharmacokinetic results showed that the C_(max) of Sal B, TSN Ⅱ_A, and GA in GTS-LE was 3.128, 2.7, and 2.85 times that of the GTS-S group, and AUC_(0-t) of Sal B, TSN Ⅱ_A, and GA in GTS-LE was 3.09, 2.23, and 1.9 times that of the GTS-S group.After intragastric administration of GTS-LE, the activities of alanine aminotransferase and aspartate aminotransferase were significantly inhibited, the content of malondialdehyde was reduced, and the structure of hepatocytes recovered to normal.In conclusion, GTS-LE can delay the release of Sal B and promote the release of TSN Ⅱ_A and GA.The encapsulation of three drug components in the emulsion can improve the oral bioavailability to varying degrees and can effectively prevent the acute liver injury caused by acetaminophen.
