Sevoflurane-Sulfobutylether-β-Cyclodextrin Complex: Preparation, Characterization, Cellular Toxicity, Molecular Modeling and Blood-Brain Barrier Transport StudiesReport as inadecuate




Sevoflurane-Sulfobutylether-β-Cyclodextrin Complex: Preparation, Characterization, Cellular Toxicity, Molecular Modeling and Blood-Brain Barrier Transport Studies - Download this document for free, or read online. Document in PDF available to download.

1

Department of Anaesthesia and Critical Care, University of Würzburg, 97080 Würzburg, Germany

2

CycloLab Cyclodextrin Research & Development Laboratory Ltd., H-1097 Budapest, Hungary

3

Sapiotec Ltd., 97078 Würzburg, Germany





*

Author to whom correspondence should be addressed.



Academic Editor: Derek J. McPhee

Abstract The objective of the present investigation was to study the ability of sulfobutylether-β-cyclodextrin SBEβCD 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-SBEβCD 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 Papp. In addition, SEV binding affinity to SBEβCD was confirmed by a minimal Gibbs free energy of binding ΔGbind value of −1.727 ± 0.042 kcal·mol−1 and an average binding constant Kb of 53.66 ± 9.24 mM indicating rapid drug liberation from the cyclodextrin amphiphilic cavity. View Full-Text

Keywords: cyclodextrin formulations; sevoflurane; sulfobutylether-β-cyclodextrin; blood-brain barrier; primary microvascular endothelial cells; molecular docking; molecular liphophilicity potential cyclodextrin formulations; sevoflurane; sulfobutylether-β-cyclodextrin; blood-brain barrier; primary microvascular endothelial cells; molecular docking; molecular liphophilicity potential





Author: Sergey Shityakov 1,* , István Puskás 2, Katalin Pápai 3, Ellaine Salvador 1, Norbert Roewer 1,3, Carola Förster 1 and Jens-Albert Broscheit 1,3

Source: http://mdpi.com/



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