Inclusion complexes of azadirachtin with native and methylated cyclodextrins: solubilization and binding ability.
The inclusion complexation behavior of azadirachtin with several cyclodextrins and their methylated derivatives has been investigated in both solution and the solid state by means of XRD, TG-DTA, DSC, NMR, and UV-vis spectroscopy. The results show that the water solubility of azadirachtin was obviously increased after resulting inclusion complex with cyclodextrins. Typically, beta-cyclodextrin (beta-CD), dimethyl-beta-cyclodextrin (DMbetaCD), permethyl-beta-cyclodextrin (TMbetaCD), and hydroxypropyl-beta-cyclodextrin (HPbetaCD) are found to be able to solubilize azadirachtin to high levels up to 2.7, 1.3, 3.5, and 1.6 mg/mL (calculated as azadirachtin), respectively. This satisfactory water solubility and high thermal stability of the cyclodextrin-azadirachtin complexes, will be potentially useful for their application as herbal medicine or healthcare products.
Liu
Yu
Y
Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China. yuliu@public.tpt.tj.cn
Chen
Guo-Song
GS
Chen
Yong
Y
Lin
Jun
J
D003505:Cyclodextrins / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D006358:Hot Temperature; D036701:Limonins / Q000737:chemistry*; D012995:Solubility; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
D003505:Cyclodextrins; D004337:Drug Carriers; D036701:Limonins; C010329:azadirachtin