Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes
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 li...
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MDPI AG
2015-11-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/20/11/19694 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Eszter Róka |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-10T23:06:36Z |
| format | Article |
| id | doaj.art-6f3edd0d79334feaa6d1a9ea9e7aa483 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T23:06:36Z |
| publishDate | 2015-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-6f3edd0d79334feaa6d1a9ea9e7aa4832022-12-22T01:30:02ZengMDPI AGMolecules1420-30492015-11-012011202692028510.3390/molecules201119694molecules201119694Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human ErythrocytesEszter Róka0Zoltán Ujhelyi1Mária Deli2Alexandra Bocsik3Éva Fenyvesi4Lajos Szente5Ferenc Fenyvesi6Miklós Vecsernyés7Judit Váradi8Pálma Fehér9Rudolf Gesztelyi10Caroline Félix11Florent Perret12Ildikó Katalin Bácskay13Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, Temesvári körút 62, Szeged H-6726, HungaryDepartment of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, Temesvári körút 62, Szeged H-6726, HungaryCyclolab Ltd., Illatos út 7, Budapest H-1097, HungaryCyclolab Ltd., Illatos út 7, Budapest H-1097, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryDepartment of Pharmacology and Pharmacodynamics, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryUniversity Lyon 1, ICBMS, Equipe CSAp, 43 Boulevard du 11 Novembre 1918, Villeurbanne F-69622, FranceUniversity Lyon 1, ICBMS, Equipe CSAp, 43 Boulevard du 11 Novembre 1918, Villeurbanne F-69622, FranceDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, Debrecen H-4032, HungaryCyclodextrins, 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.http://www.mdpi.com/1420-3049/20/11/19694α-CD derivativescytotoxicityCaco-2 cell linehemolysisRT-CES |
| spellingShingle | 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 Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes Molecules α-CD derivatives cytotoxicity Caco-2 cell line hemolysis RT-CES |
| title | Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes |
| title_full | Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes |
| title_fullStr | Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes |
| title_full_unstemmed | Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes |
| title_short | Evaluation of the Cytotoxicity of α-Cyclodextrin Derivatives on the Caco-2 Cell Line and Human Erythrocytes |
| title_sort | evaluation of the cytotoxicity of α cyclodextrin derivatives on the caco 2 cell line and human erythrocytes |
| topic | α-CD derivatives cytotoxicity Caco-2 cell line hemolysis RT-CES |
| url | http://www.mdpi.com/1420-3049/20/11/19694 |
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