Preparation of herpetolide A nanosuspension lyophilized powder and evaluation of its anti-hepatitis B virus activity.
10.19540/j.cnki.cjcmm.20191221.306
- Author:
Yu-Ji ZHONG
1
;
Qing-Chuan LIU
2
;
Ting ZHANG
1
;
Xiao LIU
3
;
Li-Qiang WANG
4
;
Hai-Long YUAN
3
Author Information
1. Huaqiao University Quanzhou 362021, China Department of Pharmacy,Air Force Medical Center,PLA Beijing 100142, China.
2. Fifth Medical Center of Chinese PLA General Hospital Beijing 100039, China.
3. Department of Pharmacy,Air Force Medical Center,PLA Beijing 100142, China.
4. Huaqiao University Quanzhou 362021, China.
- Publication Type:Journal Article
- Keywords:
HepG2.2.15;
anti-hepatitis B;
herpetolide A;
lyophilized powder;
nanosuspension
- MeSH:
Coumarins/pharmacology*;
Cucurbitaceae/chemistry*;
Hep G2 Cells;
Hepatitis B virus/drug effects*;
Humans;
Nanoparticles;
Particle Size;
Phytochemicals/pharmacology*;
Solubility;
Suspensions
- From:
China Journal of Chinese Materia Medica
2020;45(5):1076-1081
- CountryChina
- Language:Chinese
-
Abstract:
To prepare the herpetolide A nanosuspension lyophilized powder(HPA-NS-LP), in order to investigate its anti-hepatitis B virus(HBV) activity and the dissolution in vitro. Herpetolide A nanosuspension(HPA-NS) was prepared by ultrasonic precipitation method. The formulation and process of HPA-NS were optimized by the single factor experiment. Lyophilized powder(HPA-NS-LP) was prepared by freeze-drying method. Scanning electron microscopy was used to observe morphology of HPA-NS-LP. Paddle method was used to determinate the dissolution of HPT-NS-LP in vitro. The anti-HBV activity of herpetolide A coarse suspension lyophilized powder(HPA-CS-LP) and HPA-NS-LP was evaluated by HepG2.2.15 cell model. The mean particle size of optimized HPA-NS was(173.46±4.36) nm, with a polydispersity index of 0.110±0.012. After redispersion, the mean particle size and the polydispersity index of HPA-NS-LP increased, with changes within a rational range. Scanning electron microscopy showed that HPA-NS-LP was spherical in shape. Cumulative dissolution rate of HPA-NS-LP was more than 90% in 2 hours, which was higher than that of HPA-CS-LP. Both HPA-CS-LP and HPA-NS-LP could effectively inhibit the secretion of HepG2.2.15 cell antigens(HBsAg and HBeAg), and the inhibitory effect of HPA-NS-LP was significantly higher than that of HPA CS-LP(P<0.05). HBV-DNA test showed that high, medium and low-dose HPA-NS-LP(50, 25, 12.5 mg·kg~(-1)) significantly decreased the level of HBV-DNA(P<0.05), and the effect was better than that of the same dose of HPA-CS-LP(P<0.05). The results revealed that HPA-NS-LP exhibited anti-HBV activity in vitro, and its effect was superior to that of HPA-CS-LP.
