Abstract
Silymarin, a known extract, is used in the treatment of liver diseases with various origins, but its current administration form cannot target the liver because of its poor oral bioavailability. A new type of oral silymarin proliposome aimed at improving silymarin’s poor bioavailability and hepatoprotective effects, is introduced in this work. Silymarin-loaded liquid proliposome were prepared using a simple dissolving process. The morphology, particle size, zeta potential, and entrapment efficiency of the silymarin liposomes were analysed. The everted gut sac transport model was used to measure the intestinal transport of liposomes. The liposomal hepatoprotective activity was evaluated in three types of experimental hepatitis animal models. After staining with haematoxylin and eosin, the livers were microscopically examined to analyse any pathological changes. The prepared silymarin proliposome formed silymarin liposomes with a multilayer liposome structure and improved intestinal transport. In an injured liver, the silymarin liposomes produced a stronger hepatoprotective effect through a significant decrease in both the aminotransferase and MDA levels and a significant increase in the SOD and GSH-PX levels compared to orally administered silymarin tablets. This effect was also confirmed histopathologically. In a word, incorporation of silymarin into a liposomal carrier system increased intestinal absorption and showed better hepatoprotective effects compared to silymarin tablets.
Highlights
Silymarin is the main active flavonoid extract in the dried fruits of S. marianum and has been widely used in the treatment of various liver diseases
Silymarin Proliposome and Its Hepatoprotective Effects protect the liver against injury, its ability to reduce glutathione oxidation to enhance its own levels in the liver, and its ability to stabilize the cell membrane of the liver and increase hepatocyte protein synthesis
The entrapment efficiency is not significantly high, our study proves that silymarin can be incorporated into liposomes, as expected, and that its effects can be seen in the following transport and hepatoprotective-activity studies
Summary
Silymarin is the main active flavonoid extract in the dried fruits of S. marianum and has been widely used in the treatment of various liver diseases. The absorption of silymarin by the gastrointestinal tract is only between 20–50% due to its poor water solubility and partial degradation by gastric fluid, both of which limit its application[3]. To overcome these problems and improve silymarin’s bioavailability, many approaches have been investigated, including incorporating it into solid dispersion systems[4]; forming polyhydroxyphenyl chromanone salts, soluble derivatives and complexes with phospholipids[5]; encapsulating it into liposomes[6,7]; and solubilising it in self-microemulsifying drug-delivery systems[8,9]and nanoparticles[10,11]
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