Study on the preparation of hyperoside mixed nanomicelles and its intestinal absorption
- VernacularTitle:金丝桃苷混合纳米胶束的制备及其肠吸收研究
- Author:
Yuhang ZHANG
1
;
Zhidong QIU
1
;
Ye QIU
1
;
Weinan WANG
1
;
Yuanyuan DIAO
1
;
Yuwen SHI
1
;
Mengcheng JIANG
1
;
Weipeng LIU
1
;
Ailing JIA
1
Author Information
1. Key Laboratory of Traditional Chinese Medicine Active Ingredient of Ministry of Education,Changchun University of Chinese Med icine,Changchun 130117,China
- Publication Type:Journal Article
- Keywords:
hyperoside;
mixed nanomicelles;
preparation technology;
intestinal absorption characteristics;
Plackett-Burman
- From:
China Pharmacy
2022;33(10):1189-1197
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To prepare hyperoside mixed nanomicelles (Hyp-F127/TPGS) and optimize its preparation technology,and to investigate its intestinal absorption characteristics. METHODS Hyp-F127/TPGS was prepared by thin film dispersion method. Based on single factor test and Plackett-Burman design ,combined with Box-Behnken response surface method , the preparation process was optimized and validated using entrapped efficiency (EE)and drug loading (DL)as evaluation indexes , F127-TPGS mass ratio ,hydration time and the amount of Hyp as factors. The appearance and microscopic morphology of Hyp-F127/TPGS obtained by the optimal technology were observed ,and the particle size ,polydispersity index (PDI)and Zeta potential were also determined. The critical micelle concentration (CMC)of blank micelle (F127/TPGS),in vitro release behavior and preliminary stability of Hyp-F 127/TPGS were investigated ,and absorption characteristics of Hyp-F 127/TPGS were investigated by in situ unidirectional intestinal perfusion model. RESULTS The optimal preparation technology of Hyp-F 127/TPGS included F127-TPGS mass ratio of 2∶1,hydration time of 2 h,and Hyp amount of 9 mg. Results of three validation tests showed that the EE of Hyp-F 127/TPGS was (87.20±0.99)%,and the DL was (5.02±1.20)%,deviations from predicted values were 0.92% and 2.39%. The micelles prepared by optimal technology were yellow ,clear and transparent solution ,with good Tyndall effect ;under transmission electron microscope ,they were spherical ,complete and evenly distributed ;the particle size was (15.02±0.16)nm, the PDI was 0.092±0.031,and the Zeta potential was (-6.67±1.47)mV. The CMC of F 127/TPGS was 21 μg/mL,Hyp-F127/ TPGS was stable after 4 weeks of storage at 4 ℃,and the cumulative release rates of Hyp-F 127/TPGS and Hyp control were (66.30±2.93)%(96 h)and(99.24±0.27)%(60 h),respectively. Hyp-F 127/TPGS and Hyp reference were absorbed in each intestinal segment ,and the main absorption sites were jejunum and duodenum respectively ;drug absorption rate constant andapparent absorption coefficient of the former were significantly higher than those of the latter (P<0.05 or P<0.01). E-mail:zhangyuhangxz@163.com CONCLUSIONS The optimized preparation technology of Hyp-F127/TPGS is stable and feasible ;prepared Hyp-F 127/ TPGS shows a sustained -release effect ,which promotes the intestinal absorption of H yp to a certain extent.