Study on the preparation of hyperoside mixed nanomicelles and its intestinal absorption / 中国药房
China Pharmacy
; (12): 1189-1197, 2022.
Article
en Zh
| WPRIM
| ID: wpr-924071
Biblioteca responsable:
WPRO
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.
Texto completo:
1
Banco de datos:
WPRIM
Tipo de estudio:
Prognostic_studies
Idioma:
Zh
Revista:
China Pharmacy
Año:
2022
Tipo del documento:
Article