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 CCl 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.

Formulation and evaluation of pH-sensitive rutin nanospheres against colon carcinoma using HCT-116 cell line

“…These results are attributed to the free acrylic acid groups of Eudragit S100, as an anionic polymer [12] . The magnitude of zeta potential indicates the potential stability of colloidal system [38] . Usually, the possibility of particle aggregation is much lower for charged particles with zeta potential >|20| [39] , thus all the investigated nanospheres formulations showed a good physical stability.…”

Therapeutic Effect of Dunaliella salina Microalgae on Thioacetamide- (TAA-) Induced Hepatic Liver Fibrosis in Rats: Role of TGF-β and MMP9

“…Silymarin used to treat chronic liver disease in hepatofibrotic experimental animals and clinical studies [38]. However, silymarin absorption and its first-pass metabolism limited its treatment effect against severe liver damage [39], so alternative therapeutic agents from natural origin are needed as antihepatofibrotic agents. D. salina, a natural source of β-carotene, has a reversal role in TAAinduced liver fibrosis in rat.…”

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

“…In a recent work, silymarin poly( d , l -lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) have been developed to improve the therapeutic efficacy of silymarin towards prostate cancer by single emulsion solvent evaporation technique [ 16 ]. Conventional liposomes, mainly composed of phospholipids and cholesterol, are susceptible to disintegration due to the effects of the gastric acid, pancreatic lipase, and intestinal bile salts; thus, more recently, stable hybrid liposomes-encapsulated silymarin [ 26 ] and novel vesicular nanosystem bilosomes loading silymarin have been produced and compared to conventional liposomes, aiming at increasing the hepatoprotective activity of the drug [ 27 ].…”