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Cytotoxicity of different types of methylated β-cyclodextrins and ionic derivatives
T. Kiss 1, F. Fenyvesi 2, N. Pasztor 1, P. Feher 1, J. Varadi 1, R. Kocsan 1, L. Szente 3, E. Fenyvesi 3, G. Szabo 4, M. Vecsernyes 1, I. Bacskay 1
Affiliations
Article Info
1 Department of Pharmaceutical Technology, University of Debrecen, Debrecen, Hungary
2 Department of Pharmaceutical Technology, University of Debrecen, Egyetem ter 1. P.O. box 78, Debrecen, H-4010, Hungary, Email: fenyvesi@king.pharmacol.dote.hu
3 Cyclolab Ltd., Budapest, Hungary
4 Department of Biophysics and Cell Biology, Medical and Health Science Center, University of Debrecen, Debrecen, Hungary
Abstract
Cyclodextrins (CDs) are widely used materials and still in the focus of drug development. In spite of the extensive studies, there is limited information about the cytotoxic effect of different derivatives. This study compares the cytotoxic effect of methylated β-CDs and some ionic derivatives. The methylated CDs involved in this study differ in the number and position of the methyl substituents. Heptakis(2,6-di-O-methyl)-β-CD (DIMEB) with a degree of substitution (DS) of 14 has two methyl groups in all of the seven glucose subunits mostly at O-2 and O-6 position, each OH group is methylated in heptakis(2,3,6-tri-O-methyl)-β-CD (TRIMEB) (DS = 21), ?twb=0.25wand an unsystematic substitution is realized in randomly methylated β-CD (RAMEB). DS is defined as the number of substituents per cyclodextrin ring. Using the above definition, the DS for RAMEB is 12.6. To see the effect of the ionic groups an anionic and a cationic CD derivative were also investigated: (2-hydroxy-3-N,N,N-trimethylamino)propyl β-CD (QABCD) (DS = 2) and carboxymethylated β-CD (CMBCD) (DS = 3,5). The in vitro cell toxicity decreases in the order of DIMEB > TRIMEB ≥ RAMEB > QABCD > CMBCD. Ionic β-CDs were less toxic than the methylated derivatives.