Abstract
Background: The main obstacles of silymarin (SIL) application in liver diseases are its low bioavailability, elevated metabolism, rapid excretion in bile and urine, and inefficient intestinal resorption. The study aimed to synthesize and characterize silymarin-conjugated gold nanoparticles (SGNPs) formulation to improve SIL bioavailability and release for potentiating its antifibrotic action. Methods: Both SGNPs and gold nanoparticles (GNPs) were prepared and characterized using standard characterization techniques. The improved formulation was assessed for in vitro drug release study and in vivo study on rats using CCl4 induced hepatic fibrosis model. SIL, SGNPs, and GNPs were administered by oral gavage daily for 30 days. At the end of the study, rats underwent anesthesia and were sacrificed, serum samples were collected for biochemical analysis. Liver tissues were collected to measure the genes and microRNAs (miRNAs) expressions. Also, histopathological and immunohistochemistry (IHC) examinations of hepatic tissues supported these results. Results: The successful formation and conjugation of SGNPs were confirmed by measurements methods. The synthesized nanohybrid SGNPs showed significant antifibrotic therapeutic action against CCl4-induced hepatic damage in rats, and preserved normal body weight, liver weight, liver index values, retained normal hepatic functions, lowered inflammatory markers, declined lipid peroxidation, and activated the antioxidant pathway nuclear factor erythroid-2-related factor 2 (NRF2). The antifibrotic activities of SGNPs mediated through enhancing the hepatic expression of the protective miRNAs; miR-22, miR-29c, and miR-219a which results in suppressed expression of the main fibrosis mediators; TGFβR1, COL3A1, and TGFβR2, respectively. The histopathology and IHC analysis confirmed the anti-fibrotic effects of SGNPs. Conclusions: The successful synthesis of SGNPs with sizes ranging from 16 up to 20 nm and entrapment efficiency and loading capacity 96% and 38.69%, respectively. In vivo studies revealed that the obtained nano-formulation of SIL boosted its anti-fibrotic effects.
Highlights
Despite significant scientific advances in hepatology, the number of people suffering from liver diseases is increased in recent years, and the death rate remains high [1]
The results confirmed the successful synthesis of silymarin-conjugated gold nanoparticles (SGNPs) and were characterized using UV–visible spectrophotometry, Transmission Electron Microscopy (TEM), dynamic light scattering (DLS), and Fourier Transforms Infrared Spectroscopy (FT-IR)
This work was aimed to prepare and characterize silymarin-loaded gold nanoparticles formulated SGNPs were spherical with few inhomogeneity particles and distributed with formulations (SGNPs) to improve antifibrotic effects of in a ratofmodel of CCl sizes ranging from 16 upthe to 20 nm
Summary
Despite significant scientific advances in hepatology, the number of people suffering from liver diseases is increased in recent years, and the death rate remains high [1]. In 2017, an estimated 1.5 billion people globally have chronic liver disease (CLD), and the agestandardized incidence of CLD and cirrhosis is 20.7/100,000, a 13% rise since 2000 [2,3]. Nearly 2 million people die as a result of liver disease; 1 million as a result of cirrhosis complications, and 1 million as a result of viral hepatitis and hepatocellular carcinoma (HCC) [4]. The main obstacles of silymarin (SIL) application in liver diseases are its low bioavailability, elevated metabolism, rapid excretion in bile and urine, and inefficient intestinal resorption. The study aimed to synthesize and characterize silymarin-conjugated gold nanoparticles (SGNPs) formulation to improve SIL bioavailability and release for potentiating its antifibrotic action
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