Inclusion Complexation and Solubilization of Paclitaxel by Bridged Bis(β-cyclodextrin)s Containing a Tetraethylenepentaamino Spacer

A novel water-soluble paclitaxel complex has been prepared by inclusion complexation with bridged bis(β-cyclodextrin)s and characterized by means of ¹H 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.