The maximum drug concentration of BBR-loaded in the liver was 20-fold higher than that in the blood.
Oral administration of BBR-loaded solid lipid nanoparticles inhibited body weight gain and reduced liver weight in db/db mice.
Serum alanine transaminase and liver triglyceride levels decreased following treatment with BBR-loaded solid lipid nanoparticles.
BBR-loaded solid lipid nanoparticles significantly reduced fat accumulation and lipid droplet sizes in the liver.
Key genes associated with fat production were downregulated, while a gene involved in fat breakdown was upregulated in treated livers.
Simplified
Berberine (BBR) shows very low plasma levels after oral administration due to its poor absorption by the gastrointestinal tract. We have previously demonstrated that BBR showed increased gastrointestinal absorption and enhanced antidiabetic effects in db/db mice after being entrapped into (SLNs). However, whether BBR-loaded SLNs (BBR-SLNs) also have beneficial effects on is not clear. We investigated the effects of BBR-SLNs on lipid metabolism in the liver using histological staining and reverse transcription polymerase chain reaction analysis. The results showed that oral administration of BBR-SLNs inhibited the increase of body weight and decreased liver weight in parallel with the reduction of serum alanine transaminase and liver triglyceride levels in db/db mice. The maximum drug concentration in the liver was 20-fold higher than that in the blood. BBR-SLNs reduced fat accumulation and lipid droplet sizes significantly in the liver, as indicated by hematoxylin and eosin and Oil Red O staining. The expression of lipogenic genes, including fatty acid synthase (FAS), stearoyl-CoA desaturase (SCD1), and sterol regulatory element-binding protein 1c (SREBP1c) were downregulated, while lipolytic gene carnitine palmitoyltransferase-1 (CPT1) was upregulated in BBR-SLN-treated livers. In summary, we have uncovered an unexpected effect of BBR-SLNs on hepatosteatosis treatment through the inhibition of lipogenesis and the induction of lipolysis in the liver of db/db mice.
Key numbers
20×
Liver Concentration Increase
BBR concentration in the liver compared to blood in BBR-SLN group.
100 mg/kg
Body Weight Gain Suppression
Dose of BBR- that significantly reduced body weight gain.
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