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<p>Researchers recognize hepatocellular carcinoma (HCC) as a highly lethal form of cancer with a poor prognosis. This study focuses on the effectiveness of treatment on a global scale. It describes the development of a novel silymarin drug nanocomplex based on galactosylated chitosan nanoparticles as a potential nanoplatform for imaging or treating HCC in rats. Silymarin/chitosan nanoparticles (galactosylated/SILCsNPs) were synthesized, characterized, and radiolabeled with iodine-131 (<sup>131</sup>I) to trace their distribution in vivo. The synthesized galactosylated/SILCsNPs were analyzed using DLS, TEM, SEM, XRD, and FTIR to obtain a comprehensive characterization profile of their particulate properties. Additionally, in vitro assays, such as drug release studies, were performed for both free silymarin and galactosylated/SILCsNPs. Galactosylated/SILCsNPs exhibited enhanced cytotoxicity against HepG2 cells and improved selectivity compared to free silymarin, while maintaining higher cell viability in normal L02 cells, indicating their potential as a targeted therapeutic delivery system for liver cancer. For in vivo studies, normal male Wistar rats were induced to develop HCC using diethylnitrosamine (DEN), carbon tetrachloride (CCl₄), and thioacetamide (TAA). Results showed a hydrodynamic average size of 180.1&#xa0;nm and a zeta potential of + 55.6&#xa0;mV, with a spherical morphology. Galactosylated/SILCsNPs were radioiodinated with <sup>131</sup>I, achieving a radiochemical yield (RCY) of 93.6%. Liver histopathology confirmed the successful induction of HCC. A biodistribution study in HCC-induced rats showed the highest uptake in the liver. Overall, the galactosylated/SILCsNP nanocomplex exhibits superior characteristics as a theranostic agent for HCC.</p>

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Silymarin Functionalized Chitosan Nanoparticles as a Promising Theranostic Nanoplatform for Hepatocellular Carcinoma: Preparation, Characterization and In Vivo Biodistribution Assessment

  • 期刊论文

  • 发表日期：

    2025年5月19日

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  • Mohamed S. Nasr,
  • Zienab E. Eldin,
  • Hend Fayez,
  • Mai Raslan,
  • A. S. A. El-Bayoumy,
  • Sohair Abdallah,
  • Ahmed A. G. El-Shahawy

摘要

Researchers recognize hepatocellular carcinoma (HCC) as a highly lethal form of cancer with a poor prognosis. This study focuses on the effectiveness of treatment on a global scale. It describes the development of a novel silymarin drug nanocomplex based on galactosylated chitosan nanoparticles as a potential nanoplatform for imaging or treating HCC in rats. Silymarin/chitosan nanoparticles (galactosylated/SILCsNPs) were synthesized, characterized, and radiolabeled with iodine-131 (131I) to trace their distribution in vivo. The synthesized galactosylated/SILCsNPs were analyzed using DLS, TEM, SEM, XRD, and FTIR to obtain a comprehensive characterization profile of their particulate properties. Additionally, in vitro assays, such as drug release studies, were performed for both free silymarin and galactosylated/SILCsNPs. Galactosylated/SILCsNPs exhibited enhanced cytotoxicity against HepG2 cells and improved selectivity compared to free silymarin, while maintaining higher cell viability in normal L02 cells, indicating their potential as a targeted therapeutic delivery system for liver cancer. For in vivo studies, normal male Wistar rats were induced to develop HCC using diethylnitrosamine (DEN), carbon tetrachloride (CCl₄), and thioacetamide (TAA). Results showed a hydrodynamic average size of 180.1 nm and a zeta potential of + 55.6 mV, with a spherical morphology. Galactosylated/SILCsNPs were radioiodinated with 131I, achieving a radiochemical yield (RCY) of 93.6%. Liver histopathology confirmed the successful induction of HCC. A biodistribution study in HCC-induced rats showed the highest uptake in the liver. Overall, the galactosylated/SILCsNP nanocomplex exhibits superior characteristics as a theranostic agent for HCC.