Delivery of Sesamol Using Polyethylene-Glycol-Functionalized Selenium Nanoparticles in Human Liver Cells in Culture

Abstract

Anticancer nanoparticles were fabricated by linking the nanoparticles of two known anticancer agents, sesamol and selenium, using polyethylene glycol (PEG). The successful fabrication of the sesamol−PEG−selenium nanoparticles (PEG−SeNPs), which had a sesamol loading efficiency of 10.0 ± 0.5 wt %, was demonstrated using different spectroscopic techniques. The impact of the nanoparticles on model cancer cells (HepG2) was established using the cell activity test, morphological observation, and fluorescent staining, which all showed that nanoparticles effectively inhibited the HepG2 cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays showed that the concentration of the sample that inhibits 50% of the cells of PEG−SeNPs and sesamol−PEG−SeNPs on HepG2 cells was 413.8 and 68.7 μg/mL, respectively, which indicated the synergistic inhibition between sesamol and selenium nanoparticles. Furthermore, flow cytometry showed that sesamol−PEG−SeNPs exhibited higher apoptosis than either sesamol or PEG−SeNPs alone. Finally, western blot confirmed that the apoptostic ability of sesamol−PEG−SeNPs was associated with downregulation of Bcl-2 and procaspase-3, upregulation of Bax and PARP, and discharge of cytochrome c into the cytosol. Our findings suggest the novel sesamol nanoparticles may be efficient anticancer agents.

Selenium Nanoparticles for Biomedical Applications: From Development and Characterization to Therapeutics

“…PEG is an amphiphilic molecule soluble in both water and in several organic solvents, [ 134 ] and it has been widely explored as a stabilizer. [ 134,135 ] PEG is FDA approved for injectable, topical, rectal, and nasal formulations.…”

“…PEG is an amphiphilic molecule soluble in both water and in several organic solvents, [ 134 ] and it has been widely explored as a stabilizer. [ 134,135 ] PEG is FDA approved for injectable, topical, rectal, and nasal formulations. [ 40,112,136 ] Its popularity is mainly due to its favorable characteristics, such as overcoming several physicochemical instabilities, [ 134 ] high safety and stability at high temperatures, decreased nanoparticle clearance by the mononuclear phagocytic system, while preventing protein aggregation and enzymatic degradation, which increase NPs accumulation in the tumor site due to the enhanced permeability and retention (EPR) effect.…”

“…[ 134,135 ] PEG is FDA approved for injectable, topical, rectal, and nasal formulations. [ 40,112,136 ] Its popularity is mainly due to its favorable characteristics, such as overcoming several physicochemical instabilities, [ 134 ] high safety and stability at high temperatures, decreased nanoparticle clearance by the mononuclear phagocytic system, while preventing protein aggregation and enzymatic degradation, which increase NPs accumulation in the tumor site due to the enhanced permeability and retention (EPR) effect. In addition, PEG chains are used for NP functionalization by enabling the binding of specific targeting antibodies and other compounds identified by the cancer cells.…”

“…In addition, PEG chains are used for NP functionalization by enabling the binding of specific targeting antibodies and other compounds identified by the cancer cells. Accordingly, PEG–SeNPs presented potential for the treatment of hepatic [ 112,134 ] and lung cancer. [ 137 ] During the production of PEG‐stabilized SeNPs at high temperatures, its oxygen atom is sp3 hybridized and forms two carbon–oxygen covalent bonds and two lone‐pair electrons, which coordinate with the empty 4d orbitals of each Se atom.…”

“…[ 79 ] Overall, SeNPs are produced by reducing Se oxyanions into elemental Se, leading to solutions with color ranging from pink, orange, and red, [ 89,101,138 ] due to the excitations of the SeNPs surface plasmon resonance formed in the reaction mixture, [ 153 ] presenting a maximum absorption at 200–400 nm. [ 134 ] Therefore, SeNPs photoelectron spectroscopy pattern includes the distinctive Se 3d peak around 54–56 eV, as well as the Se 3p3, Se 3p1 and Sed3 peaks, [ 155,157 ] confirming the formation of its zero‐valent oxidation state, although usually accompanied by the peak correspondent to a residual Se(IV), around 56–60 eV. [ 26,123,157,158 ] Also, using X‐ray diffraction analysis, several studies identified a hexagonal ring lattice, [ 159–162 ] or a trigonal phase.…”