What is it about?
Lopinavir is an important drug molecule of limited physicochemical properties for the treatment of HIV infected patients. Although a wide range of (2-hydroxy)propylated cyclodextrins are used in the solubilization of drugs they have been found to be poorly usable for this guest molecule. Theoretical studies of the (2-hydroxy)propylated cyclodextrins the high degree of substitution version of gamma-cyclodextrin was found to be a suitable target although their synthesis is difficult, due to the high reactivity of the (2-hydroxy)propyl substituent.
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Why is it important?
A new in silico method is presented and a practical example demonstrated its usability. The synthesis of highly substituted cyclodextrin and the use of the supercritical assisted spary-drying technique in the cyclodextrin complex preparation is described.
Perspectives
The guest specific design and synthesis of highly hydroxypropylated cyclodextrin derivatives, the most common host molecules, can be achieved by the presented method.
Dr Laszlo Jicsinszky
University of Turin, DSTF
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This page is a summary of: Cyclodextrin solubilization and complexation of antiretroviral drug lopinavir: In silico prediction; Effects of derivatization, molar ratio and preparation method, Carbohydrate Polymers, January 2020, Elsevier,
DOI: 10.1016/j.carbpol.2019.115287.
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