Cyclodextrin (CD) complexes of cholesterol--their potential use in reducing dietary cholesterol intake

The main objective of this investigation was to test and see if cyclodextrins, a type of molecule which form inclusion complexes, could effectively prevent the absorption of food derived cholesterol. Cyclodextrins are nontoxic and easily tolerated, having only a slight sweet taste. alpha,beta,gamma-Cyclodextrins, 2-Hydroxypropyl-beta-cyclodextrin (2-HPCD), and heptakis-O,O-dimethyl-beta-cyclodextrin (DMCD) were tested in solutions of different concentrations. These solutions were then saturated with cholesterol and the excess cholesterol was removed. The clear solutions left were then analyzed by HPLC to assess the amount of cholesterol in the solutions, and compared to a standard. DMCD gave the best results in successfully dissolving (complexing) most of the cholesterol followed by HPCD and alpha-cyclodextrin. Beta- and gamma-CD showed nearly insignificant complex formation. After administration of 10 mg of cholesterol to mice through a gastric tube, the cholesterol level increased about 125-130%, and only 15-20%, if the cholesterol was administered together with 20 mg of DMCD. That means, the DMCD formed complexes with approximately 80-85% of the cholesterol administered in the mice gastrointestinal tract.