Study on transdermal absorption and anti-inflammatory activity of Compound Sanguis Draxonis Microemulsion in vitro
DANG Xueliang1 JIA Lihua2 SONG Yanfeng1 ZHAO Jun1 WANG Qingwei1
1.Department of Pharmacy, the Second Affiliated Hospital of Air Force Medical University, Shaanxi Province, Xi′an 710038, China;
2.Shaanxi Institute for Food and Drug Control, Shaanxi Province, Xi′an 710065, China;
Abstract:Objective To investigate the transdermal absorption of main active components of Compound Sanguis Draxonis Microemulsion with different concentrations in vitro, and provide experimental basis for further study of the preparation. Methods According to the random number table, twenty-four SD rats were randomly divided into 3 groups, which were high-dose group (5.0%), medium-dose group (2.5%) and low-dose group (1.0%) of Compound Sanguis Draxonis Microemulsion, with 8 rats in each group. The isolated rat skin of the same part was taken as the permeation barrier, and the content of ligustilide, the main active ingredient of Compound Sanguis Draxonis Microemulsion, was determined by HPLC using modified Franz diffusion cell. The transdermal absorption of Compound Sanguis Draxonis Microemulsion was investigated by calculating the cumulative permeation amount of ligustilide in vitro. Forty SD rats were randomly divided into 5 groups according to their body weight, which were model group, Dexamethasone Acetate Cream group, high-dose group (5.0%), medium-dose group (2.5%) and low-dose group (1.0%) of Compound Sanguis Draxonis Microemulsion with 8 rats in each group. Experiment of paw swelling in rats induced by carrageenan was operated to observe inflammation inhibited by Compound Sanguis Draxonis Microemulsion, Dexamethasone Acetate Cream group as positive control group. Results The cumulative permeabilities of ligustilide, the main active ingredient of low-dose, medium-dose and high-dose groups of Compound Sanguis Draxonis Microemulsion, within 24 h were (153.000±6.586), (311.200±14.520) and (454.100±23.440) μg/cm2 respectively. The transdermal rate constants Jss were (6.8130±0.2196), (13.7100±0.5953), (20.1900±0.9491) μg/(cm2·h), respectively. Compared with the positive control group, the high-dose group of Compound Sanguis Draxonis Microemulsion significantly inhibited carrageenan-induced paw swelling in rats (P < 0.01). Conclusion Compound Sanguis Draxonis Microemulsion has good transdermal performance and anti-inflammatory activity in vitro. The cumulative permeability per unit area within 24 h increased with the content of ligustilide, and the transdermal permeation behavior conformed to the zero-order kinetic equation.