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Molecules 2015, 20(11), 20269-20285; doi:10.3390/molecules201119694

Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes

1
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, Hungary
2
University Lyon 1, ICBMS, Equipe CSAp, 43 Boulevard du 11 Novembre 1918, Villeurbanne F-69622, France
3
Department of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, Temesvári körút 62, Szeged H-6726, Hungary
4
Cyclolab Ltd., Illatos út 7, Budapest H-1097, Hungary
5
Department of Pharmacology and Pharmacodynamics, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, Hungary
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 October 2015 / Revised: 29 October 2015 / Accepted: 2 November 2015 / Published: 11 November 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1977 KB, uploaded 11 November 2015]   |  

Abstract

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. View Full-Text
Keywords: α-CD derivatives; cytotoxicity; Caco-2 cell line; hemolysis; RT-CES α-CD derivatives; cytotoxicity; Caco-2 cell line; hemolysis; RT-CES
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Róka, E.; Ujhelyi, Z.; Deli, M.; Bocsik, A.; Fenyvesi, É.; Szente, L.; Fenyvesi, F.; Vecsernyés, M.; Váradi, J.; Fehér, P.; Gesztelyi, R.; Félix, C.; Perret, F.; Bácskay, I.K. Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes. Molecules 2015, 20, 20269-20285.

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