期刊
CARBOHYDRATE RESEARCH
卷 343, 期 7, 页码 1180-1190出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carres.2008.03.014
关键词
cyclodextrin; inclusion complexes; A-007 prodrugs; molecular aggregation; NOESY
One- and two-dimensional NMR spectroscopy was used to demonstrate the formation of inclusion cyclodextrin complexes with several A-007 prodrugs. These complexes are comprised from the encapsulation of the two phenol moieties of the A-007 prodrugs within the cyclodextrin cavity. Considering the size of the two phenol moieties of the A-007 prodrugs compared to the sizes of (alpha-, beta-, and gamma-cyclodextrin cavities, we observed complementary binding of the A-007 prodrug with only beta-cyclodextrin, which was also demonstrated spectroscopically. The beta-cyclodextrin inclusion complexes increased the prodrug solubility and modified the prodrug half-life in water. Therefore, beta-cyclodextrin inclusion complexes can be used as an essential form of A-007 prodrug delivery. (c) 2008 Elsevier Ltd. All rights reserved.
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