Preparation，characterization and gastric mucosal permeability of evodiamine phospholipid complex self- microemulsifying drug delivery system
- VernacularTitle:吴茱萸碱磷脂复合物自乳化药物递送系统的制备、表征及胃黏膜渗透性研究
- Author:
Shuoyao SONG
1
,
2
;
Guiqian YANG
1
,
2
;
Ling TAO
1
,
2
;
Xiangchun SHEN
1
,
2
;
Huan ZHANG
1
,
2
;
Herong LI
1
,
2
;
Shouli WANG
1
,
2
;
Huiyun SHI
1
,
2
;
Wen LIU
1
Author Information
1. School of Pharmacy，Guizhou Medical University，Guiyang 550025，China
2. Guizhou Province Key Laboratory for Optimal Utilization of Natural Medicine Resources，Guiyang 550025，China
- Publication Type:Journal Article
- Keywords:
self-microemulsifying drug delivery system
- From:
China Pharmacy
2022;33(9):1056-1062
- CountryChina
- Language:Chinese
-
Abstract:
OBJE CTIVE To prepare and characterize evodiamine phospholipid complex self-microemulsifying drug delivery system（EVO-PC-SMEDDS），and to investigate its gastric mucosal permeability. METHODS EVO-PC-SMEDDS was prepared ， and particle size ，polydispersity（PDI）and Zeta potential were tested ，and microscopic observation was carried out. The stability of EVO-PC-SMEDDS in simulated gastric liquid with different pH （1.2，2.0，4.0，7.0）was investigated. The entrapment efficiency and drug-loading amount of the preparation were determined ，and the in vitro release was investigated. The gastric mucosal permeability of EVO-PC-SMEDDS was studied by combining rat gastric mucosal tissue and Ussing Chamber technology. RESULTS The particle size of EVO-PC-SMEDDS was （53.63±1.51）nm，PDI and Zeta potential were 0.217±0.017 and （－12.20±0.15）mV，entrapment efficiency was （95.25±0.97）％ and drug-loading amount was （19.30±1.21）mg/g. EVO-PC- SMEDDS exhibited a uniformly dispersed round spherical shape under transmission electron microscope. Stability experiments showed that EVO-PC-SMEDDS exhibited no significant change in particle size ，PDI and Zeta potential under the simulated gastric fluid with different pH and showed excellent stability. Results of in vitro release test showed that compared with evodiamine （EVO），in vitro accumulative release of EVO-PC-SMEDDS were enhanced 6.83-fold，which was in line with the first-order kinetic release model. Results of gastric mucosal permeability showed that gastric mucosal permeation transport ，permeation rate ， permeation flux and area under curve of cumulative permeability of EVO-PC-SMEDDS were higher than those of EVO ， respectively. CONCLUSIONS EVO-PC-SMEDDS is prepared N successfully and shows good stability. It could significantly improve the release behavior and gastric mucosal permeability of EVO.
