4.7 Article

Inclusion complexation and solubilization of paclitaxel by bridged bis(β-cyclodextrin)s containing a tetraethylenepentaamino spacer

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JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 22, 页码 4634-4637

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AMER CHEMICAL SOC
DOI: 10.1021/jm034148f

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A novel water-soluble paclitaxel complex has been prepared by inclusion complexation with bridged bis(beta-cyclodextrin)s and characterized by means of H-1 NMR, SEM, powder X-ray diffraction patterns, TG-DTA, DSC, FT-IR, and 2D NOESY. The cyclodextrins were able to solubilize paclitaxel to levels as high as 2 mg/mL. Furthermore, the cytotoxicity of the novel complexes was assessed using a K562 leukemia cell line which indicated that drug concentrations of 10 pg/mL elicited an inhibitory effect.

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