Preparation,Properties and In Vitro Release Behavior Study of Inclusion Complex of Taxifolin with 2-Hydroxypropyl-β-cyclodextrin
10.19756/j.issn.0253-3820.241006
- VernacularTitle:紫杉叶素与羟丙基-β-环糊精包合物的制备、性能及体外释放行为研究
- Author:
Shui-Xian MA
1
;
Xin TAO
;
Yun-Han YANG
;
Sha XIA
;
Yu-Xiang YANG
;
Li YANG
;
Li-Juan YANG
Author Information
1. 云南医药健康职业学院基础与药学院,昆明 650033
- Keywords:
Taxifolin;
2-Hydroxypropyl-β-cyclodextrin;
Inclusion complex;
Process screening;
Drug release
- From:
Chinese Journal of Analytical Chemistry
2025;53(10):1684-1693
- CountryChina
- Language:Chinese
-
Abstract:
The inclusion complex of taxifolin(TAX)with hydroxypropyl-β-cyclodextrin(HP-β-CD)was prepared by saturated aqueous solution method,and the preparation conditions such as molar ratio,volume ratio of solution,inclusion temperature and inclusion time were selected by single-factor experiment.The orthogonal design of three-level four-factor L9(34)was used to screen the preparation process of the inclusion complex,and the inclusion complex was prepared with optimal preparation process.The prepared inclusion complex was characterized by scanning electron microscopy(SEM),nuclear magnetic resonance(1H NMR,2D NMR),Fourier transform infrared spectroscopy(FT-IR),ultraviolet-visible(UV-Vis)absorption spectroscopy and X-ray powder diffraction(XRD).The inclusion ratio,biostability,solubility and in vitro release of the inclusion complex were investigated.The results of orthogonal experiments showed that the optimum conditions for preparation of the inclusion complex were as follows:the molar ratio of TAX to HP-β-CD was 1:1,the volume ratio of methanol to ultra-pure water was 1:8,the inclusion time was 8 h,and the inclusion temperature was 30℃.Under the optimal conditions,the inclusion ratio between TAX and HP-β-CD was calculated to be 1:1 by Job's curve method.According to the change of UV-vis absorption spectra,the host-guest complexation constant of 4.9488×104 L/mol was obtained by Benesi-Hildebrand curve method.The solubility of TAX increased from 1.2665 mg/mL to 19.3469 mg/mL after inclusion,demonstrating that HP-β-CD could serve as an effective host molecule for TAX,which could significantly enhance the bio-stability and solubility of the formed inclusion complex.
