| Blood-brain barrier (BBB) is a barrier which can make the environment of brain relative stable and prevent the exogenous substances from transferring into brain. At the same time, it is a big challenge to treat diseases of brain. Because of the special structure of cyclodextrins with the shape of runcated cone, they are able to encapsulate most of drugs to form the CD-drug complexes which could improve water-soluble of drugs, increase the concentration of drugs in blood and go through the BBB.In this paper, threeβ-cyclodextrin derivatives labeled by fluorophores were synthesized and characterized, and their spectral properties and the abilities to breakthrough BBB into the central nervous (CNS) as a drug carrier were evaluated. Three kinds of fluorophores widely used in biomedical field, boron-dipyrrolemethene, 1,8-naphthalimide and coumarin, respectively, were chose to modifyβ-cyclodextrin. In addition, PEG was used to modifyβ-cyclodextrins to increase solubility in water and improve biocompatibility. The structures of the compounds had been determined by mass spectrometry,1H-NMR and FT-IR spectroscopy. And spectral properties of the compounds were studied between the small fluorephore and cyclodextrin derivatives, especially the change of the absorption and emission spectra in aqueous solution. Futhermore, glioma cells (BT-325) cells were chose to study and evalute the ability to breakthrough BBB by the methods of fluorescent imaging and flow cytometry. The results indicated that within a certain concentration range, the average of fluorescence intensity and the ratio of staining of cells increased with the increase of the concentration of the studied compounds.β-Cyclodextrin derivatives were able to enter BT-325 cells and had a certain ability to go through BBB, which was a foundation for futher investigation of CD complexes used as the drug delivery system to treat brain diseases. |
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