肉桂提取物醇质体凝胶经皮给药研究

Study on Percutaneous Permeation of Ethosomes Gel of Cinnamon Extract

目的制备肉桂提取物醇质体凝胶,考察肉桂提取物醇质体凝胶的透皮速率影响因素。方法采用注入法制备肉桂提取物醇质体,将醇质体与羟丙基甲基纤维素(HPMC)凝胶混合制备肉桂提取物凝胶,采用♂SD大鼠皮肤和Franz单室扩散池作体外经皮研究,HPLC测定不同时间点接受池的肉桂酸含量,考察不同HPMC浓度、不同促渗剂和促渗剂浓度对肉桂提取物醇质体凝胶渗透速率的影响。结果不同HPMC浓度作为肉桂提取物醇质体基质时经皮渗透速率:2%HPMC>3%HPMC>4%HPMC>5%HPMC≈醇质体。2%氮酮-丙二醇(1∶1)处理显示最好的促渗效果,渗透速率与醇质体相比:(4.38±0.47)μg·h-1·cm-2 vs(1.53±0.31)μg·h-1·cm-2。结论 2%HPMC制备的肉桂提取物醇质体凝胶,能提高肉桂透皮速率,醇质体凝胶有望开发为肉桂提取物经皮给药剂型。

OBJECTIVE To investigate the effect of HPMC on the penetration rate of Cinnamon Cortex extract and the synergistic effect of cinnamon cortex extract ethosome gel and the chemical enhancers on enhancement of Cinnamon Cortex extract permeation. METHODS Cinnamon Cortex extract ethosomes gel was prepared by injection method and admixed with HPMC gel. With the skin of SD male rats, the penetration experiments in vitro were performed on modified Franz diffusion cells. The amount of penetrated cinnamon cortex extract was determined by HPLC. The steady penetration rate was calculated. RESULTS The penetration rate shows 2%HPMC〉3%HPMC〉4%HPMC〉5%HPMC^ethosome. 2% Azone-propanediol（1 ： 1） pretreated in ethosomal form dramatically enhanced the skin permeation of Cinnamon Cortex extract in vitro compared with ethosomes[（4.38±0.47）μg.h ^-1.cm^-2 vs （1.53±0.31）μg.h^-1·cm^-2]. CONCLUSION Ethosome gel could be developed as the new dosage form in cinnamon cortex extract transdermal delivery.