Evaluation of the cytotoxicity of α-cyclodextrin derivatives on the caco-2 cell line and human erythrocytes

Eszter Róka, Zoltán Ujhelyi, Mária Deli, Alexandra Bocsik, Éva Fenyvesi, Lajos Szente, Ferenc Fenyvesi, Miklós Vecsernyés, Judit Váradi, Pálma Fehér, Rudolf Gesztelyi, Caroline Félix, Florent Perret, Ildikó Katalin Bácskay

Research output: Contribution to journalArticle

22 Citations (Scopus)


Cyclodextrins, even the 6-membered α-cyclodextrin, are approved in the various pharmacopoeias as pharmaceutical excipients for solubilizing and stabilizing drugs as well as for controlling drug release. Recently α-cyclodextrin has also been marketed as health food with beneficial effects on blood lipid profiles. However, the concentration of α-cyclodextrin used may be very high in these cases, and its toxic attributes have to be seriously considered. The objective of this study was to investigate the cytotoxicity of various, differently substituted α-cyclodextrin derivatives and determine relationship between the structures and cytotoxicity. Three different methods were used, viability tests (MTT assay and Real Time Cell Electronic Sensing on Caco-2 cells) as well as hemolysis test on human red blood cells. The effect of α-cyclodextrin derivatives resulted in concentration-dependent cytotoxicity, so the IC50 values have been determined. Based on our evaluation, the Real Time Cell Electronic Sensing method is the most accurate for describing the time and concentration dependency of the observed toxic effects. Regarding the cytotoxicity on Caco-2 cells, phosphatidylcholine extraction may play a main role in the mechanism. Our results should provide help in selecting those α-cyclodextrin derivatives which have the potential of being used safely in medical formulations.

Original languageEnglish
Pages (from-to)20269-20285
Number of pages17
Issue number11
Publication statusPublished - Nov 11 2015


  • Caco-2 cell line
  • Cytotoxicity
  • Hemolysis
  • RT-CES
  • α-cd derivatives

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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