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Molecules 2015, 20(6), 10264-10279; doi:10.3390/molecules200610264

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

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
Received: 12 April 2015 / Accepted: 25 May 2015 / Published: 3 June 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [5530 KB, uploaded 3 June 2015]   |  

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
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Shityakov, S.; Puskás, I.; Pápai, K.; Salvador, E.; Roewer, N.; Förster, C.; Broscheit, J.-A. Sevoflurane-Sulfobutylether-β-Cyclodextrin Complex: Preparation, Characterization, Cellular Toxicity, Molecular Modeling and Blood-Brain Barrier Transport Studies. Molecules 2015, 20, 10264-10279.

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