ADMET and DMPK (Nov 2021)

Synthesis of silymarin−selenium nanoparticle conjugate and examination of its biological activity in vitro

  • Sergey Staroverov,
  • Sergey Kozlov,
  • Alexander Fomin,
  • Konstantin Gabalov,
  • Vitaliy Khanadeev,
  • Dmitry Soldatov,
  • Ivan Domnitsky,
  • Lev Dykman,
  • Sergey V. Akchurin,
  • Olga Guliy

DOI
https://doi.org/10.5599/admet.1023

Abstract

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Silymarin (Sil) was conjugated to selenium nanoparticles (SeNPs) to increase Sil bioavailability. The conjugates were monodisperse; the average diameter of the native SeNPs was ~ 20-50 ± 1.5 nm, whereas that of the conjugates was 30-50 ± 0.5 nm. The use of SeNPs to increase the bioavailability of Syl was examined with the MH-22a, EPNT-5, HeLa, Hep-2, and SPEV-2 cell lines. The EPNT-5 (glioblastoma) cells were the most sensitive to the conjugates compared to the conjugate-free control. The conjugates increased the activity of cellular dehydrogenases and promoted the penetration of Sil into the intracellular space. Possibly, SeNPs play the main part in Sil penetration of cells and Sil penetration is not associated with phagocytosis. Thus, SeNPs are promising for use as a Sil carrier and as protective antigens.