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Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES): Synthesis, cytotoxicity and inclusion of anaesthetic actives
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-114280
- 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 toThe 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.…
Autor(en): | Lisa Markenstein, Antje Appelt-Menzel, Marco Metzger, Gerhard Wenz |
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URN: | urn:nbn:de:bvb:20-opus-114280 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Medizinische Fakultät / Lehrstuhl für Tissue Engineering und Regenerative Medizin |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | Beilstein Journal of Organic Chemistry |
ISSN: | 1860-5397 |
Erscheinungsjahr: | 2014 |
Band / Jahrgang: | 10 |
Seitenangabe: | 3087 - 3096 |
Originalveröffentlichung / Quelle: | Beilstein Journal of Organic Chemistry 2014, 10, 3087–3096. doi:10.3762/bjoc.10.325 |
DOI: | https://doi.org/10.3762/bjoc.10.325 |
PubMed-ID: | https://pubmed.ncbi.nlm.nih.gov/25670977 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
Freie Schlagwort(e): | LCST; acid dissociation; anaesthetics; beta-cyclodextrin; complexation; cycloaddition; cyclodextrin; drug; gamma-cyclodextrin; lower critical solution temperature; midazolam; occupancy; pharmaceutical applications; polymer; rat; sevoflurane; solubility; starch; supermolecular carrier systems |
Datum der Freischaltung: | 26.06.2015 |
Lizenz (Deutsch): | CC BY: Creative-Commons-Lizenz: Namensnennung |