An approach to vectorisation of pharmacologically active molecules: The covalent binding of leu-enkephalin to a modified β- cyclodextrin.

A hexagonal columnar packing structure of C7 symmetric supramolecules: a superstructure of a 2:3 complex of heptakis‐(6‐O‐tert‐butyldimethylsilyl)‐β‐cyclodextrin and ethyl acetate

“…However, β-cyclodextrin (β-CD) and its derivatives, typical cylindrical molecules widely used as clathrate hosts [16][17][18][19][20][21], do not generate a hexagonal columnar structure in crystal. The following occurrences cause the distortion of their symmetric cylindershapes; 1) holding of a guest molecule among the seven C6-hydroxy groups with hydrogen bonds, 2) inclusion of a large non-symmetric molecule in their cavities, and 3) remaining of a large unoccupied inner space [22][23][24]. Therefore, the protection of the C6-hydroxy groups and the filling of the inner space of β-CD by inclusion of the symmetrical molecules could be effective to get a hexagonal columnar superstructure.…”

Cyclodextrins as templates for the presentation of protease inhibitors

“…This property has been extensively exploited to change the physicopharmaceutical properties of lipophilic drugs such as water solubility, bioavailability, improved stability and effectiveness [2], and cyclodextrins at present are widely used as transportactive additives. The covalent attachment of bioactive peptides to cyclodextrins has also been proposed [3,4], although their grafting to the relatively large cyclodextrin carrier might impair recognition by receptor molecules. In fact, covalent linkage of an enkephalin analog to [3-cyclodextrin was found to lower significantly the receptor affinity and selectivity, but the clearance rate was reduced [5].…”

Improvement of Drug Properties by Cyclodextrins

“…140,141 CyD derivatives coupled to drugs such as enkephalin, doxorubicin, methicillin, ibuprofen and nucleobase were synthesized for modifi cation of biological potencies. [142][143][144][145][146] In this section, recent results on sitespecifi c delivery using CyDs are described.…”