Document Detail

Cyclodextrins as diethylstilbestrol carrier system: characterization of diethylstilbestrol-cyclodextrins complexes.
MedLine Citation:
PMID:  10397605     Owner:  NLM     Status:  MEDLINE    
PURPOSE: 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.
E Núñez-Delicado; M Sojo; A Sánchez-Ferrer; F García-Carmona
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Pharmaceutical research     Volume:  16     ISSN:  0724-8741     ISO Abbreviation:  Pharm. Res.     Publication Date:  1999 Jun 
Date Detail:
Created Date:  1999-08-18     Completed Date:  1999-08-18     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  854-8     Citation Subset:  IM    
Department of Biochemistry and Molecular Biology-A, Faculty of Biology, University of Murcia, Spain.
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MeSH Terms
Cyclodextrins / administration & dosage,  metabolism*
Diethylstilbestrol / administration & dosage,  metabolism*
Drug Carriers
Drug Delivery Systems*
Hydrogen Peroxide
Lipoxygenase / metabolism
Reg. No./Substance:
0/Cyclodextrins; 0/Drug Carriers; 56-53-1/Diethylstilbestrol; 7722-84-1/Hydrogen Peroxide; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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