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CYCLODEXTRIN DERIVATIVES AND THEIR USE FOR THE SOLUBILIZATION AND BIOAVAILABILITY ENHANCEMENT OF DRUGS |
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J. Defaye, C. Ortiz-Mellet, J.M. Garcia Fernandez, M. Gomez-Garcia, K. Chmurski, J.-X. Yu
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TECHNICAL DESCRIPTION
This invention describes new branched cyclodextrin derivatives particularly well suited to solubilize hydrophobic guest molecules. These derivatives, which are prepared in a few high yielding steps from native cyclodextrins are homogeneous and pure. The method can easily be adapted to combinatorial strategies to optimize the inclusion of guest molecules as well as interaction of the system with the environment. The technology also involves modular methods for the preparation of diversely branched amino, amido, alkyl, hydroxyalkyl and aryl cyclodextrin derivatives bearing the highly hydrophilic thiourea functionality. This invention is particularly useful for grafting on the cyclodextrin core of multiple copies of tracers and biological recognition markers.
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