Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES): Synthesis, cytotoxicity and inclusion of anaesthetic actives

• Lisa Markenstein,
• Antje Appelt-Menzel,
• Marco Metzger and
• Gerhard Wenz

Beilstein J. Org. Chem. 2014, 10, 3087–3096, doi:10.3762/bjoc.10.325

• than the corresponding monomeric CD derivatives. Since the binding potentials of these CD conjugates were very high, they are promising candidates for new oral dosage forms of anaesthetic actives. Keywords: anaesthetics; complexation; cyclodextrin; LCST; lower critical solution temperature; midazolam

• conjugation of azido-functionalized methylated β-CD derivatives to propargylated HES, the evaluation of the toxicity of these new polymers and first binding studies for the hydrophobic anaesthetic ingredients sevoflurane and midazolam. Sevoflurane, currently applied as an inhalation anaesthetic [36], could be

• solubilized in water to allow further use in oral or parenteral dosage forms as an analgesic drug. Also the uptake of midazolam could be improved by complexation in CD derivatives [37][38]. Results and Discussion Cyclodextrin polymers were synthesized by copper-catalyzed [2 + 3] cycloaddition of methylated