Pharmacognosy Magazine

ORIGINAL ARTICLE
Year
: 2014  |  Volume : 10  |  Issue : 37  |  Page : 9--17

Effect of various absorption enhancers based on tight junctions on the intestinal absorption of forsythoside A in Shuang-Huang-Lian, application to its antivirus activity


Wei Zhou1, Xuan Xuan Zhu2, Ai Ling Yin3, Bao Chang Cai3, Hai Dan Wang2, Liuqing Di1, Jin Jun Shan4 
1 College of Pharmacy, Nanjing University of Chinese Medicine; Jiangsu Engineering Research Center for Efficient Delivery System of TCM; Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, Nanjing, China
2 Department of Pharmacology, Affiliated Hospital of Nanjing University of Chinese Medicine, Nanjing, China
3 College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China
4 First Medicine College, Nanjing University of Chinese Medicine, Nanjing, China

Correspondence Address:
Liuqing Di
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046
China

Background: Forsythoside A (FTA), one of the main active ingredients in Shuang-Huang-Lian (SHL), possesses strong antibacterial, antioxidant and antiviral effects, and its pharmacological effects was higher than that of other ingredients, but the absolute bioavailability orally was approximately 0.72%, which was significantly low, influencing clinical efficacies of its oral preparations seriously. Materials and Methods: In vitro Caco-2 cell and in vivo pharmacokinetics study were simultaneously performed to investigate the effects of absorption enhancers based on tight junctions: sodium caprate and water-soluble chitosan on the intestinal absorption of FTA, and the eventual mucosal epithelial damage resulted from absorption enhancers was evaluated by MTT test and morphology observation, respectively. The pharmacological effects such as antivirus activity improvement by absorption enhancers were verified by MDCK damage inhibition rate after influenza virus propagation. Results: The observations from in vitro Caco-2 cell showed that the absorption of FTA in SHL could be improved by absorption enhancers. Meanwhile, the absorption enhancing effect of water-soluble chitosan may be almost saturable up to 0.0032% (w/v), and sodium caprate at concentrations up to 0.64 mg/mL was safe, but water-soluble chitosan at different concentrations was all safe for these cells. In pharmacokinetics study, water-soluble chitosan at dosage of 50 mg/kg improved the bioavailability of FTA in SHL to the greatest extent, and was safe for gastrointestine from morphological observation. Besides, treatment with SHL with water-soluble chitosan at dosage of 50 mg/kg prevented MDCK damage after influenza virus propagation better significantly than that of control. Conclusion: Water-soluble chitosan at dosage of 50 mg/kg might be safe and effective absorption enhancer for improving the bioavailability of FTA and the antivirus activity in vitro in SHL.


How to cite this article:
Zhou W, Zhu XX, Yin AL, Cai BC, Wang HD, Di L, Shan JJ. Effect of various absorption enhancers based on tight junctions on the intestinal absorption of forsythoside A in Shuang-Huang-Lian, application to its antivirus activity.Phcog Mag 2014;10:9-17


How to cite this URL:
Zhou W, Zhu XX, Yin AL, Cai BC, Wang HD, Di L, Shan JJ. Effect of various absorption enhancers based on tight junctions on the intestinal absorption of forsythoside A in Shuang-Huang-Lian, application to its antivirus activity. Phcog Mag [serial online] 2014 [cited 2022 Jan 23 ];10:9-17
Available from: http://www.phcog.com/article.asp?issn=0973-1296;year=2014;volume=10;issue=37;spage=9;epage=17;aulast=Zhou;type=0