Abstract

Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl choline & cholesterol so as to increase its oral bioavailability and liver targeted enhanced hepatoprotection.
 Methodology: Thin film hydration technique was used for the development of liposomes by using phosphatidyl choline, cholesterol and drug. Liposomes were evaluated for vesicle size, zeta potential, PDI, encapsulation efficiency, surface morphology and in vitro drug release study. Further the optimized formulation was evaluated for APAP-induced alterations in liver and kidney function tests in rats and histopathological studies.
 Results: The results were promising with a sustained drug release of 80% within 20hrs, optimized vesicle size of 276nm and 89% encapsulation efficiency. The animal studies demonstrated superior hepatoprotective effect compared to silybin solution.
 Conclusion: The silybin liposomes showed better in-vitro release & in-vivo hepatoprotection along with better animal activity & improvement in histopathological changes as compared to silybin.

Highlights

  • 2.1 Pre-formulation StudiesSilymarin (SM) is an herb obtained from Silybum marianum possessing hepatoprotective activity for the treatment of liver disorders

  • Ratsspecific tumor necrosis factor-α (TNF-α), Interleukin (IL)-1β, and IL-6 enzyme-linked immunosorbent assay (ELISA) Kit were obtained from Bethyl Laboratories Inc. (Montgomery, TX, USA)

  • The solubility of Silybin in different solvents like Water, Ethanol, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer were mentioned in table 1

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Summary

Introduction

Silymarin (SM) is an herb obtained from Silybum marianum possessing hepatoprotective activity for the treatment of liver disorders. This herb consists of a mixture of Silybin, Isosilybin, Silydianin, and Silychristin. Silybin is a known hepatoprotectant but due to its low serum, tissue levels, low solubility & absorption lead to its poor oral bioavailability [3,4]. Many research studies have been performed, such as solid dispersions, porous silica nanoparticles, lipid complexes, etc so as to improve the solubility & bioavailability of Silybin [5,6,7,8,9,10], but none of the methods were useful to achieve a sustainable bioavailability

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