The toxicity of monosubstituted n-alkyldimethylammonium-beta-cyclodextrins (DMA-C(n)-CD with n=2, 4 and 12) towards endothelial cells of an in vitro model of the blood-brain barrier (BBB) was evaluated and compared to that of the native beta-CD. DMA-C(12)-CD was found to be non-toxic below 10mM due to the self-inclusion of the alkyl chain in the CD cavity. A high percentage of passage (30%) of DMA-C(12)-CD through the endothelial cells has been measured.