<p>Ellagic acid (EA) is a polyphenolic compound with potential anticancer properties. However, because of its low oral bioavailability and poor water solubility, its therapeutic applications have been restricted. Encapsulating EA on surface-modified nanocarrier systems and examining its anticancer effects was the main objective of this work. In this study, for the first time, EA was loaded onto bovine serum albumin nanoparticles (BSA NPs) using the desolation approach, and then, the surface of the NPs was coated with chitosan (EA-BSA-CS-NPs). Then, the EA loading efficiency and its release profile during 48&#xa0;h were evaluated by an absorption spectrophotometer. In addition, the cytotoxic and apoptotic effects of EA-BSA-CS-NPs were evaluated by MTT, flow cytometry, and fluorescent staining methods, respectively, on liver cancer (HepG2) and human umbilical vein endothelial (HUVEC) cell lines. The apoptotic effects of EA-BSA-CS-NPs were investigated using acridine orange/propidium iodide (AO/PI) staining. The synthesized NPs were spherical in shape, with an average diameter of 218.82&#xa0;nm, a polydispersity index of 0.29, as well as a surface charge of + 30.15&#xa0;mV. According to the drug release investigation, 71.45% of the EA was released in 48&#xa0;h, and the encapsulation efficiency was determined to be 91.35%. The NPs showed strong cytotoxicity in HepG2 cells, with an IC<sub>50</sub> value of 144&#xa0;ng/mL, and no cytotoxicity to normal cells. The results indicated that EA-BSA-CS-NPs induced G1-phase arrest and apoptosis in HepG2 cells. This work demonstrates the potential of EA-BSA-CS-NPs as an effective nanocarrier system to enhance the bioavailability and anticancer effects of ellagic acid for liver cancer treatment.</p>

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Synthesis and Characterization of Albumin Nanoparticles Loaded by Ellagic Acid and Chitosan and Investigation of Its Anticancer Activity Against Liver Cancer Cells

  • Amal J. Hashim,
  • Mohadese Alirezaei,
  • Mozhgan Soltani,
  • Ali Es-haghi,
  • Dariush Minai-Tehrani

摘要

Ellagic acid (EA) is a polyphenolic compound with potential anticancer properties. However, because of its low oral bioavailability and poor water solubility, its therapeutic applications have been restricted. Encapsulating EA on surface-modified nanocarrier systems and examining its anticancer effects was the main objective of this work. In this study, for the first time, EA was loaded onto bovine serum albumin nanoparticles (BSA NPs) using the desolation approach, and then, the surface of the NPs was coated with chitosan (EA-BSA-CS-NPs). Then, the EA loading efficiency and its release profile during 48 h were evaluated by an absorption spectrophotometer. In addition, the cytotoxic and apoptotic effects of EA-BSA-CS-NPs were evaluated by MTT, flow cytometry, and fluorescent staining methods, respectively, on liver cancer (HepG2) and human umbilical vein endothelial (HUVEC) cell lines. The apoptotic effects of EA-BSA-CS-NPs were investigated using acridine orange/propidium iodide (AO/PI) staining. The synthesized NPs were spherical in shape, with an average diameter of 218.82 nm, a polydispersity index of 0.29, as well as a surface charge of + 30.15 mV. According to the drug release investigation, 71.45% of the EA was released in 48 h, and the encapsulation efficiency was determined to be 91.35%. The NPs showed strong cytotoxicity in HepG2 cells, with an IC50 value of 144 ng/mL, and no cytotoxicity to normal cells. The results indicated that EA-BSA-CS-NPs induced G1-phase arrest and apoptosis in HepG2 cells. This work demonstrates the potential of EA-BSA-CS-NPs as an effective nanocarrier system to enhance the bioavailability and anticancer effects of ellagic acid for liver cancer treatment.