Some Pharmaceutical Properties of a New Branched Cyclodextrin,6-O-alpha-(4-O-alpha-D-Glucuronyl)-D-glucosyl-beta-cyclodextrin

摘要

Some physicochemical and biological properties of a new branched cyclodextrin,6-O-alpha-(4-O-alpha-D-glucuronyl)-D-glucosyl-beta-cyclodextrin GUG-beta-CyD)were investigated.Further,the interaction of GUG-beta-CyD with several drugs was studied by the solubility and spectroscopic methods,and compared with those of parent bdet-CyD and 6-O-alpha-maltosyl-beta-CyD(G_2-beta-CyD).The hemolytic activity of GUG-beta-CyD on rabbit erythrocytes was lower than thosee of beta-CyD and G_2-beta-CyD.GUG-beta-CyD and G_2-deta-CyD showed negligible cytotoxixity on Caco-2 cells up to at least 0.1 M.The inclusion ability of GUG-beta-CyDto neutral and acidic drugs was comparable to or slightly smaller than those of beta-CyD and G_2-beta-CyD,probably because of a steric himdrance of the aranched sugar.On the other hand,GUG-beta-CyD showed greater affinity for the basic drugs,compared with deta-CyD and G_2-beta-CyD,owing to the electrostatic interaction of its carboxylate anion wiht posiitive charge of basic brugs.Thus GUG-beta-CyD may be useful as a safe solubilizing agent particularly for basic drugs.