Silibinin-loaded cubosomes: a gateway to enhanced hepatoprotective activity

Abstract

Abstract Background The liver is a vital organ that detoxifies drugs and xenobiotics. However, breaking down toxins creates byproducts that can damage the liver. Silibinin possesses a proven hepatoprotective and antioxidant effect as it inhibits the free radicals produced from the metabolism of toxic substances, such as paracetamol and ethanol. Unfortunately, the poor bioavailability of silibinin hinders its use, which could be overcome by loading it into lipid nanocarriers, such as cubosomes. This study aims to formulate silibinin-loaded cubosomes and evaluate their hepatoprotective effect in vivo. Results A full factorial design was conducted to evaluate the percentage of poloxamer 407 and the sonication time. The prepared cubosomes were characterized by multiple characterization techniques. The in vitro release of silibinin from the chosen formulation was also evaluated. An induced acute paracetamol hepatotoxicity model in mice was utilized for in vivo evaluation. The particle size of the formulated cubosomes ranged from 123.2 to 210.9 nm, and the polydispersity index range was 0.226–0.560. The zeta potential of the formulations ranged between − 14.2 and − 25.6 mV. The chosen formulation displayed a controlled release pattern. The chosen formulation showed a significant hepatoprotective action by reducing the liver marker enzymes. The histopathological study also confirmed the hepatoprotective activity of the chosen cubosomes. The hepatoprotective effects of the chosen formulation can be attributed to positive impacts on oxidative stress, as demonstrated in oxidative stress markers. Conclusion The obtained results suggest that silibinin-loaded cubosomal formulation offers apotentially improved hepatoprotection effect against induced acute paracetamol hepatotoxicity. Graphical abstract