期刊
MOLECULES
卷 20, 期 6, 页码 10264-10279出版社
MDPI
DOI: 10.3390/molecules200610264
关键词
cyclodextrin formulations; sevoflurane; sulfobutylether--cyclodextrin; blood-brain barrier; primary microvascular endothelial cells; molecular docking; molecular liphophilicity potential
资金
- IZKF (Interdisziplinares Zentrum fur Klinische Forschung der Universitat Wurzburg) [BMBF01, EO1004]
- BMBF (Bundesministerium fur Bildung und Forschung) [BMBF01, EO1004]
The objective of the present investigation was to study the ability of sulfobutylether--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-SBECD 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 SBECD was confirmed by a minimal Gibbs free energy of binding (G(bind)) value of -1.727 +/- 0.042 kcalmol(-1) and an average binding constant (K-b) of 53.66 +/- 9.24 mM indicating rapid drug liberation from the cyclodextrin amphiphilic cavity.
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