期刊
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
卷 95, 期 13, 页码 2678-2685出版社
WILEY
DOI: 10.1002/jsfa.7002
关键词
capsaicin; microemulsion; in vitro release; irritation; bioavailability
资金
- National Natural Science Foundation of China [30973677]
- Ministry of Education of China [20113227110012]
- college Natural Science Research Foundation of Jiangsu Province [14KJB350002]
- Special Funds for 333 [BRA2013198]
- 331 projects
- Industry-University-Research Institution Cooperation in Jiangsu Province [JHB2012-37, GY2012049, GY2013055]
- Industry-University-Research Institution Cooperation in Zhenjiang City [JHB2012-37, GY2012049, GY2013055]
BACKGROUNDCapsaicin, as a food additive, has attracted worldwide concern owing to its pungency and multiple pharmacological effects. However, poor water solubility and low bioavailability have limited its application. This study aims to develop a capsaicin-loaded microemulsion to enhance the oral bioavailability of the anti-neuropathic-pain component, capsaicin, which is poorly water soluble. RESULTSIn this study, the microemulsion consisting of Cremophor EL, ethanol, medium-chain triglycerides (oil phase) and water (external phase) was prepared and characterized (particle size, morphology, stability and encapsulation efficiency). The gastric mucosa irritation test of formulated capsaicin was performed in rats to evaluate its oral feasibility, followed by the pharmacokinetic study in vivo. Under these conditions, the encapsulated capsaicin revealed a faster capsaicin release in vitro coupled with a greater absorption in vivo when compared to the free capsaicin. The oral bioavailability of the formulated capsaicin-loaded microemulsions was 2.64-fold faster than that of free capsaicin. No significant irritation was observed on the mucosa from the pathological section of capsaicin-loaded microemulsion treated stomach. CONCLUSIONThese results indicate that the developed microemulsion represents a safe and orally effective carrier for poorly soluble substances. The formulation could be used for clinical trials and expand the application of capsaicin. (c) 2014 Society of Chemical Industry
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据