Transdermal behaviors comparisons among Evodia rutaecarpa extracts with different purity of evodiamine and rutaecarpine and the effect of topical formulation in vivo

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• 作者：Fei Chen^a ; Su Li^a ; Dai Li^b ; Jin-Song Ding^a ; ^{dingjinsong0221@163.com}
• 关键词：ATR-FTIR ; Attenuated Total Reflectance Fourier Transform Infra-Red ; CGRP ; Calcitonin Gene-Related Peptide ; COX-2 ; Cyclooxygenase-2 ; EE ; Evodia rutaecarpa Extract ; EVO ; Evodiamine ; NSAIDs ; Nonsteroidal Anti-Inflammatory Drugs ; PEG-400 ; Polyethylene Glycol
• 刊名：Fitoterapia
• 出版年：2012
• 期刊代码：35_0367326x
• 类别：ch
• 出版时间：July, 2012
• 卷：83
• 期：5
• 页码：954-960
• 文件大小：542 K

摘要

Aim

Evodiamine (EVO) and rutaecapine (RUT), the major active components from Evodia rutaecarpa extract (EE), are recognized as a depended analgesic agent. This study was designed to investigate the effect of purity and chemical enhancers on the transdermal behavior of EVO and RUT, and the pharmacological effect of their topical cream in vivo.

Material and methods

Transdermal delivery across a full thickness pig abdominal skin was detected in vitro by Franz-type diffusion cell, with HPLC for quantification of the permeation of EVO and RUT. The activity of topical cream in vivo was evaluated by a mice pain model induced by formalin and hot plate.

Results

Transdermal characters of EVO and RUT showed a low transdermal rate, long lag time and low cumulative amount. The transdermal rate and cumulative amount could be promoted by lipophilic enhancers, whereas lag time was shortened by hydrophilic surfactant, but these permeation parameters were not markedly influenced by purity of EE (p > 0.05). The effect in vivo was confirmed by analgesic models in topical cream of EE, which produced a significant (p < 0.05) inhibitory effects on pain response in dose-dependent manner.

Conclusion

The purity of EVO and RUT from EE has no significant effect on their permeation through porcine skin, but oleic acid or nerolidol can markedly elevate the transdermal rate of EVO and RUT. High purity of EE is the best choice for topical preparation to increase the drug loading. The effect of EE in vivo is verified by formalin model and hot plate test.