Cellular Effects of Cyclodextrins: Studies on HeLa Cells

Molecules. 2022 Feb 28;27(5):1589. doi: 10.3390/molecules27051589.


Cyclodextrins are high molecular weight, hydrophilic, cyclic, non-reducing oligosaccharides, applied as excipients for the improvement of the solubility and permeability of insoluble active pharmaceutical ingredients. On the other hand, beta-cyclodextrins are used as cholesterol sequestering agents in life sciences. Recently, we demonstrated the cellular internalization and intracellular effects of cyclodextrins on Caco-2 cells. In this study, we aimed to further investigate the endocytosis of (2-hydroxylpropyl)-beta-(HPBCD) and random methylated-beta-cyclodextrin (RAMEB) to test their cytotoxicity, NF-kappa B pathway induction, autophagy, and lysosome formation on HeLa cells. These derivatives were able to enter the cells; however, major differences were revealed in the inhibition of their endocytosis compared to Caco-2 cells. NF-kappa B p65 translocation was not detected in the cell nuclei after HPBCD or RAMEB pre-treatment and cyclodextrin treatment did not enhance the formation of autophagosomes. These cyclodextrin derivates were partially localized in lysosomes after internalization.

Keywords: HPBCD; HeLa; NF-κB; RAMEB; autophagy; endocytosis; lysosomes.

MeSH terms

  • Caco-2 Cells
  • Cyclodextrins* / pharmacology
  • Excipients
  • HeLa Cells
  • Humans
  • Solubility


  • Cyclodextrins
  • Excipients