Preparation and in vitro anti-hepatic fibrosis evaluation of herpetone nanosuspensions.
10.19540/j.cnki.cjcmm.20181224.001
- Author:
Jie-Jie ZUO
1
;
Cheng-Ying SHEN
1
;
Bao-de SHEN
2
;
Yuan LIU
3
;
Rui-Na ZHONG
1
;
Xiao LIU
3
;
Xiao-Han WANG
1
;
Hai-Long YUAN
3
Author Information
1. College of Pharmacy,Chengdu University of Traditional Chinese Medicine(TCM) Chengdu 611137,China Department of Pharmacy,Air Force General Hospital Beijing 100142,China.
2. Department of Pharmacy,Air Force General Hospital Beijing 100142,China Key Lab of Modern Preparation of Traditional Chinese Medicine under Ministry of Education,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China.
3. Department of Pharmacy,Air Force General Hospital Beijing 100142,China.
- Publication Type:Journal Article
- Keywords:
apoptosis;
cell cycle;
dissolution;
hepatic stellate cells;
herpetone;
nanosuspension
- MeSH:
Animals;
Cell Line;
Hepatic Stellate Cells;
Lignans;
Liver Cirrhosis;
Rats
- From:
China Journal of Chinese Materia Medica
2019;44(6):1164-1169
- CountryChina
- Language:Chinese
-
Abstract:
Herpetone( HPT) is a bioactive lignan extracted from Herpetospermum pedunculosum,which can protect liver,lower aminotransferase and inhibit hepatitis B virus. However,HPT has a poor oral bioavailability due to its poor water solubility. And there is no report about whether HPT has an anti-hepatic fibrosis activity. To improve the dissolution of HPT and study its anti-hepatic fibrosis activity and mechanism,the study group prepared herpetone nanosuspensions( HPT-NS) by the miniaturized media milling method. The formulation and process of HPT-NS were optimized by the single factor experiment. Scanning electron microscopy was used to observe morphology of HPT-NS. Dialysis method was used to study dissolution of HPT-NS in vitro. CCK8 method was used to assess the effect of HPT-NS on proliferation of the rat hepatic stellate cells( HSC-T6). Flow cytometry was used to assess the effect of HPT-NS on apoptosis and cell cycle of HSC-T6. The mean particle size of optimized HPT-NS was( 196±7) nm with a polydispersity index of 0.279±0.009.SEM showed that HPT-NS was in a regular rod shape. The cumulative dissolution rate of HPT-NS reached 93% in 18 h,and was higher than that of herpetone coarse suspensions( HPT-CS,28%). CCK8 experiment showed that the inhibition rate of HPT-NS on HSC-T6 was higher than that of HPT-CS. Flow cytometry showed that HPT-NS could block HSC-T6 cells in G2/M phase and induce apoptosis of HSC-T6 cells,with a significantly stronger effect than HPT-CS. The results revealed that HPT-NS significantly increased the in vitro dissolution of HPT,and enhanced the inhibitive effect on HSC-T6 cell proliferation by blocking cells in the G2/M phase and inducing late apoptosis.
