Purpose: Hepatocellular carcinoma (HCC) is a most common liver malignancy. The objective of this study was to prepare silybin nanoparticles (NPs) and optimize the prepared nanoparticles using central composite rotatable design-response surface methodology.
Methods: HCC was induced in rats by supplementing 100 mg/L of diethylnitrosamine (DENA) in drinking water for 8 weeks. Saline, silybin 30 mg/kg body weight and nanoformulation of silybin equivalent to silybin dose were administered orally to 3 groups of 6 animals each. Anticancer activity was evaluated by counting the liver nodules, and H & E staining analysis of tissue sections.
Results: The results showed that silybin NPs under optimized conditions gave rise to the entrapment efficiency (EE) of 88%, drug loading (DL) of 15%, mean diameter of 216 nm of the NPs prepared and zeta potential value of -15 mV. In rats treated with silybin NPs, the number of neoplastic nodules was significantly lower, the animals did not exhibit decrease in mean body weight, the number of liver nodules was reduced by >93% with significantly high localization in the liver.
Conclusion: Orally administered silybin NPs showed improved efficacy and safety compared to silybin for the treatment of HCC in rats.