TY  - JOUR
A1  - Markenstein, Lisa
A1  - Appelt-Menzel, Antje
A1  - Metzger, Marco
A1  - Wenz, Gerhard
T1  - Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES): Synthesis, cytotoxicity and inclusion of anaesthetic actives
JF  - Beilstein Journal of Organic Chemistry
N2  - The mono-6-deoxy-6-azides of 2,6-di-O-methyl-beta-cyclodextrin (DIMEB) and randomly methylated-beta-cyclodextrin (RAMEB) were conjugated to propargylated hydroxyethyl starch (HES) by Cu+-catalysed [2 + 3] cycloaddition. The resulting water soluble polymers showed lower critical solution temperatures (LCST) at 52.5 degrees C (DIMEB-HES) and 84.5 degrees C (RAMEB-HES), respectively. LCST phase separations could be completely avoided by the introduction of a small amount of carboxylate groups at the HES backbone. The methylated CDs conjugated to the HES backbone exhibited significantly lower cytotoxicities 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.
KW  - midazolam
KW  - supermolecular carrier systems
KW  - beta-cyclodextrin
KW  - pharmaceutical applications
KW  - gamma-cyclodextrin
KW  - anaesthetics
KW  - complexation
KW  - cyclodextrin
KW  - LCST
KW  - lower critical solution temperature
KW  - acid dissociation
KW  - drug
KW  - rat
KW  - cycloaddition
KW  - occupancy
KW  - polymer
KW  - sevoflurane
KW  - solubility
KW  - starch
Y1  - 2014
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-114280
SN  - 1860-5397
VL  - 10
ER  -