Inclusion complexation and solubilization of paclitaxel by bridged bis(beta-cyclodextrin)s containing a tetraethylenepentaamino spacer.
A novel water-soluble paclitaxel complex has been prepared by inclusion complexation with bridged bis(beta-cyclodextrin)s and characterized by means of (1)H 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.
Liu
Yu
Y
Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, P. R. China. yuliu@public.tpt.tj.cn
Chen
Guo-Song
GS
Li
Li
L
Zhang
Heng-Yi
HY
Cao
Dong-Xu
DX
Yuan
Ying-Jin
YJ
D000970:Antineoplastic Agents / Q000737:chemistry*; D001952:Bridged-Ring Compounds / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D003505:Cyclodextrins / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008855:Microscopy, Electron, Scanning; D008958:Models, Molecular; D017239:Paclitaxel / Q000737:chemistry*; D011073:Polyamines / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013818:Thermogravimetry; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D001952:Bridged-Ring Compounds; D003505:Cyclodextrins; D011073:Polyamines; D017239:Paclitaxel