Effect of Electroporation on Percutaneous Permeation of Sinomenine Hydrochloride
10.13422/j.cnki.syfjx.20211448
- VernacularTitle:电致孔方式对盐酸青藤碱经皮渗透的促进作用
- Author:
Sen YAN
1
;
Jian TENG
2
;
Tong-tong SUN
3
;
Li XU
2
;
Ping QIU
2
;
Qing WANG
1
Author Information
1. State Key Laboratory of Fine Chemicals，School of Chemical Engineering， Dalian University of Technology，Dalian 116024，China
2. Hunan Zhengqing Pharmaceutical Group Co. Ltd.，Huaihua 418005，China
3. Dalian Kexiang Technology Development Co. Ltd.，Dalian 116024，China
- Publication Type:Research Article
- Keywords:
sinomenine hydrochloride;
percutaneous permeation in vitro;
electroporation;
intact skin;
stripped skin;
in vitro diffusion cell method
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2021;27(17):146-151
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To investigate the percutaneous permeability of sinomenine hydrochloride （SNH） and optimize the parameters of electroporation to achieve the best permeation enhancing effect on SNH. Method:The percutaneous permeability of SNH and the enhancement effect of electroporation were studied by in vitro diffusion cell method， and the enhancement effect of electroporation was further evaluated by in vivo study in mice. Result:Under steady-state condition， the permeation rates of SNH in stripped skin and intact skin of hairless mice were （385.81±12.88）， （0.88±0.20） μg·cm-2·h-1， respectively. The permeation rate in stripped skin was 438 times higher than that in intact skin. The results of percutaneous permeation kinetics analysis showed that the solubility and diffusion coefficient of SNH in stratum corneum were relatively low， which were （70.82±9.63）×103 g·m-3 and （3.07±1.52）×10-14 cm2·s-1， respectively. Under the optimized electroporation conditions （voltage of 72 V， time of 60 min）， the 24 h cumulative permeation amount of SNH through skin of mice was （10 008.39±1 961.57） μg·cm-2， and the steady-state permeation rate was （456.01±51.26） μg·cm-2·h-1， which were 5.4 times and 5.1 times higher than those of blank group， respectively. In vivo studies in mice showed that the contents of SNH in skin and muscle of electroporation group were 2.0 times and 1.5 times higher than those of blank group. Conclusion:The low solubility and low diffusion coefficient of SNH in the stratum corneum are the main factors hindering the percutaneous permeation of SNH. Electroporation can significantly increase the percutaneous permeation of SNH and its retention in skin and muscle of mice.
