Abstract
The hemolytic properties of naturalcyclodextrins, especially of the more commoncyclomaltoheptaose entity, severely hamper theirpotential use as carriers in pharmaceuticalapplications where parenteral administration isconcerned. A systematic investigation on the role ofchemical modifications with regard to the hemolyticcharacter was carried out involving C-6 branchedneutral, anionic, cationic and amphoteric derivatives.From these data, conclusions have been drawnabout the charge and the geometry of the modification: (i)Substitution at primary hydroxyl groups usuallydecreases the hemolytic character and the geometry ofthe substituent affects the hemolytic property; (ii)introduction of an amino group, resulting in apositive charge at physiological pH, decreases thehemolytic character; (iii) negative charges arecomparatively less effective in reducing the hemolyticcharacter; (iv) zwitterionic groups seem to enhancethe hemolytic character of the cyclodextrin molecule.
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Bost, M., Laine, V., Pilard, F. et al. The Hemolytic Properties of Chemically Modified Cyclodextrins. Journal of Inclusion Phenomena 29, 57–63 (1997). https://doi.org/10.1023/A:1007919719275
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DOI: https://doi.org/10.1023/A:1007919719275