ArticlePharmaceutics2021
Enhanced Bioavailability and Efficacy of Silymarin Solid Dispersion in Rats with Acetaminophen-Induced Hepatotoxicity.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 33 citations in OpenAlex.
- Identification of Reactive Metabolites of Acetaminophen and Saxagliptin in Human Hepatocytes and Hepatic Organoids.Pharmaceutics · 2026Article
- Targeting metabolic dysfunction-associated steatotic liver disease with phytosomal silymarin and piperine: A natural alternative to fenofibrate in a rat model.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Silymarin and Silybin: Rejuvenating Traditional Remedies with Modern Delivery Strategies.Pharmaceutics · 2025Review
- Pharmaceutical technological trends containing flavonoids: a patent review.Future medicinal chemistry · 2025Review
- Silybin Cocrystals with Improved Solubility and Bioavailability.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Silymarin as a phytopharmaceutical agent: advances in mechanistic insights, formulation strategies, and pre-clinical applications.Frontiers in pharmacology · 2025Review
- Nanocrystal Formulation to Enhance Oral Absorption of Silybin: Preparation, In Vitro Evaluations, and Pharmacokinetic Evaluations in Rats and Healthy Human Subjects.Pharmaceutics · 2024Article
- A comparative study on the preparation and evaluation of solubilizing systems for silymarin.Drug delivery and translational research · 2024Article
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- Trained immunity in monocyte/macrophage: Novel mechanism of phytochemicals in the treatment of atherosclerotic cardiovascular disease.Frontiers in pharmacology · 2023Review
- Design and optimization of silymarin loaded in lyophilized fast melt tablets to attenuate lung toxicity inducedDrug delivery · 2022Article
- Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide.Pharmaceutics · 2021Article
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
We evaluated the bioavailability, liver distribution, and efficacy of silymarin-D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) solid dispersion (silymarin-SD) in rats with acetaminophen-induced hepatotoxicity (APAP) compared with silymarin alone. The solubility of silybin, the major and active component of silymarin, in the silymarin-SD group increased 23-fold compared with the silymarin group. The absorptive permeability of silybin increased by 4.6-fold and its efflux ratio decreased from 5.5 to 0.6 in the presence of TPGS. The results suggested that TPGS functioned as a solubilizing agent and permeation enhancer by inhibiting efflux pump. Thus, silybin concentrations in plasma and liver were increased in the silymarin-SD group and liver distribution increased 3.4-fold after repeated oral administration of silymarin-SD (20 mg/kg as silybin) for five consecutive days compared with that of silymarin alone (20 mg/kg as silybin). Based on higher liver silybin concentrations in the silymarin-SD group, the therapeutic effects of silymarin-SD in hepatotoxic rats were evaluated and compared with silymarin administration only. Elevated alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly decreased by silymarin-SD, silymarin, and TPGS treatments, but these decreases were much higher in silymarin-SD animals than in those treated with silymarin or TPGS. In conclusion, silymarin-SD (20 mg/kg as silybin, three times per day for 5 days) exhibited hepatoprotective properties toward hepatotoxic rats and these properties were superior to silymarin alone, which may be attributed to increased solubility, enhanced intestinal permeability, and increased liver distribution of the silymarin-SD formulation.
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