Cyclodextrins as diethylstilbestrol carrier system: characterization of diethylstilbestrol-cyclodextrins complexes.
OBJECTIVE
The in vitro formation of DES-cyclodextrins inclusion complexes was characterized using lipoxygenase as enzymatic system.


METHODS
DES-cyclodextrins complexes were obtained in aqueous solution.


RESULTS
The addition of cyclodextrins to the reaction medium had an inhibitory effect on DES oxidation by lipoxygenase due to the drug's complexation into the cyclodextrin cavity. This inhibitory effect depends on the complexation constant between DES and the cyclodextrins type used. In this case, beta-, 2-hydroxypropyl-beta- and gamma-cyclodextrins have similar complexation constants and therefore produce the same inhibitory effect. Moreover, depending on the type of cyclodextrins used, the solubility of DES can be enhanced up to 956 times, while the lipoxygenase activity remains constant.


CONCLUSIONS
These results suggest that the system described may be used as a controlled-release delivery system for DES, since it may diminish the local and systemic adverse side effects caused by high concentrations of the drug.
Núñez-Delicado
E
E
Department of Biochemistry and Molecular Biology-A, Faculty of Biology, University of Murcia, Spain.
Sojo
M
M
Sánchez-Ferrer
A
A
García-Carmona
F
F
D003505:Cyclodextrins / Q000008:administration & dosage / Q000378:metabolism*; D004054:Diethylstilbestrol / Q000008:administration & dosage / Q000378:metabolism*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006861:Hydrogen Peroxide; D008084:Lipoxygenase / Q000378:metabolism
D003505:Cyclodextrins; D004337:Drug Carriers; D004054:Diethylstilbestrol; D006861:Hydrogen Peroxide; D008084:Lipoxygenase