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Sevoflurane-sulfobutylether-\(\beta\)-cyclodextrin complex: preparation, characterization, cellular toxicity, molecular modeling and blood-brain barrier transport studies

Please always quote using this URN: urn:nbn:de:bvb:20-opus-148543
  • The objective of the present investigation was to study the ability of sulfobutylether-\(\beta\)-cyclodextrin (SBECD) to form an inclusion complex with sevoflurane (SEV), a volatile anesthetic with poor water solubility. The inclusion complex was prepared, characterized and its cellular toxicity and blood-brain barrier (BBB) permeation potential of the formulated SEV have also been examined for the purpose of controlled drug delivery. The SEV-SBE\(\beta\)CD complex was nontoxic to the primary brain microvascular endothelial (pEND) cells at aThe objective of the present investigation was to study the ability of sulfobutylether-\(\beta\)-cyclodextrin (SBECD) to form an inclusion complex with sevoflurane (SEV), a volatile anesthetic with poor water solubility. The inclusion complex was prepared, characterized and its cellular toxicity and blood-brain barrier (BBB) permeation potential of the formulated SEV have also been examined for the purpose of controlled drug delivery. The SEV-SBE\(\beta\)CD complex was nontoxic to the primary brain microvascular endothelial (pEND) cells at a clinically relevant concentration of sevoflurane. The inclusion complex exhibited significantly higher BBB permeation profiles as compared with the reference substance (propranolol) concerning calculated apparent permeability values (P\(_{app}\)). In addition, SEV binding affinity to SBE\(\beta\)CD was confirmed by a minimal Gibbs free energy of binding (ΔG\(_{bind}\)) value of -1.727 ± 0.042 kcal・mol\(^{-1}\) and an average binding constant (K\(_{b}\)) of 53.66 ± 9.24 mM indicating rapid drug liberation from the cyclodextrin amphiphilic cavity.show moreshow less

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Metadaten
Author: Sergey Shityakov, István Puskás, Katalin Pápai, Ellaine Salvador, Norbert Roewer, Carola Förster, Jens-Albert Broscheit
URN:urn:nbn:de:bvb:20-opus-148543
Document Type:Journal article
Faculties:Medizinische Fakultät / Klinik und Poliklinik für Anästhesiologie (ab 2004)
Language:English
Parent Title (English):Molecules
Year of Completion:2015
Volume:20
Pagenumber:10264-10279
Source:Molecules 2015, 20, 10264-10279. DOI: 10.3390/molecules200610264
DOI:https://doi.org/10.3390/molecules200610264
Dewey Decimal Classification:6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Tag:blood-brain barrier; cyclodextrin formulations; ether; etomidate; formulations; hydrochloride; in vitro; intestinal absorption; molecular docking; molecular liphophilicity potential; pharmaceutical applications; primary microvascular endothelial cells; propranolol; safety; sevoflurane; ulfobutylether-\(\beta\)-cyclodextrin; water
Release Date:2018/11/15
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International