Improved hepatoprotective activity of silymarin via encapsulation in the novel vesicular nanosystem bilosomes

Abstract

The main objective of the present work was to formulate, characterize, and evaluate silymarin (SM)-loaded bilosomes, compared to conventional liposomes, aiming at increasing the hepatoprotective activity of the drug. SM-loaded bilosomes were prepared by thin film hydration technique employing soybean phosphatidyl choline (SPC) and different bile salts. After being subjected to different methods of characterization, SM-loaded bilosomes were investigated for their hepatoprotective activity, in CCl₄ hepatointoxicated rat model. The developed SM dispersions exhibited an entrapment efficiency ranging from 21.80 ± 2.01 to 84.54 ± 2.51% and a particle size diameter in the nanometric dimensions (413 ± 96.9 to 686.9 ± 62.38 nm), with a negative zeta potential values (<–45 mV). In vitro release study revealed a lower cumulative amount of drug released from the developed formulae, compared to free drug. Ex vivo intestinal uptake study, performed using confocal laser scanning calorimetry, revealed the superiority of bilosomal uptake compared to that of liposomes. In vivo studies revealed an enhanced hepatoprotective effect of SM-loaded bilosomes/liposomes compared to free drug. These results were in good correlation with histopathological examination. These findings support the potential use of bilosomes for improving the hepatoprotective activity of SM via oral administration.

Graphical Abstract

Keywords:

• Silymarin
• bilosomes
• liposomes
• bile salts
• liver
• hepatoprotection
• histopathology

Acknowledgements

The authors would like to express their deep appreciation to Prof Dr. Manal A. Badawi, Department of Pathology, National Research Centre, for her great help in the histopathological studies.

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.