Some Pharmaceutical Properties of a New Branched Cyclodextrin, 6- O-α-(4- O- α-D-Glucuronyl)-D-glucosylβ-cyclodextrin.

Autor: Sumitra Tavornvipas, Hidetoshi Arima, Fumitoshi Hirayama, Kaneto Uekama, Toshihiro Ishiguro
Zdroj: Journal of Inclusion Phenomena & Macrocyclic Chemistry; Dec2002, Vol. 44 Issue 1-4, p391-394, 4p
Abstrakt: Some physicochemical and biological properties of a new branched cyclodextrin, 6-O-α-(4-O-α-d-glucuronyl)-d-glucosyl-β-cyclodextrin GUG-β-CyD) were investigated. Further, the interaction of GUG-β-CyD with several drugs was studied by the solubility and spectroscopic methods, and compared with those of parent β-CyD and 6-O-α-maltosyl-β-CyD (2-β-CyD). The hemolytic activity of GUG-β-CyD on rabbit erythrocytes was lower than those of β-CyD and 2-β-CyD. GUG-β-CyD and 2-β-CyD showed negligible cytotoxicity on Caco-2 cells up to at least 0.1 M. The inclusion ability of GUG-β-CyD to neutral and acidic drugs was comparable to or slightly smaller than those of β-CyD and 2-β-CyD, probably because of a steric hindrance of the branched sugar. On the other hand, GUG-β-CyD showed greater affinity for the basic drugs, compared with β-CyD and 2-β-CyD, owing to the electrostatic interaction of its carboxylate anion with positive charge of basic drugs. Thus GUG-β-CyD may be useful as a safe solubilizing agent particularly for basic drugs. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index