肉桂提取物β-环糊精包合物经皮渗透性的研究

Study on Percutaneous Permeability of Cinnamon Extract in β-Cyclodextrin Composite Ethosomes

目的考察以醇质体为载体的肉桂提取物β-环糊精包合物经皮给药的可行性以及醇浓度、促渗剂对药物渗透速率的影响。方法制备肉桂提取物β-环糊精后,采用注入法制备醇质体,以SD雄性大鼠皮肤为媒介,Franz单室扩散池为体外模型,用HPLC测定透过皮肤的肉桂酸含量。结果含醇20%,30%,40%和50%的醇质体稳态透皮速率分别为(5.06±1.29),(8.08±3.76),(10.05±1.76)和(17.89±0.15)μg.h-1.cm-2,与包合物水溶液[(5.00±0.75)μg.h-1.cm-2]相比,其增渗倍数分别为1.01,1.62,2.01和3.58倍。加入促渗剂如二甲基亚砜、1,2-丙二醇增渗倍数分别为1.50,1.83倍,但也有渗透速率变小的。结论β-环糊精包合物联合醇质体能显著促进肉桂提取物经皮渗透,有望成为肉桂提取物新的经皮给药系统。

OBJECTIVE To investigate the possibility of percutaneous transport of Cinnamon extract inβ-cyclodextrin（β-CD） composite ethosomes. And to determine the effect of the concentration of ethanol and penetration enhancers on the permeation rate. METHODS β-CD composite ethosomes was prepared by injection method. With the skin of SD male rat,the penetration experiments in vitro were performed with modified Franz diffusion cells. The penetration concentrations ofβ-CD composite ethosomes was determined by HPLC. RESULTS The steady permeation rate ofβ-CD composite ethosomes with 20% , 30% , 40% and 50% ethanol were （5.06 ± 1.29）, （8. 08 ±3. 76）, （ 10. 05 ± 1.76） and （ 17.89 ±0. 15） μg· h^-1·cm^-2 respectively. And it was 1.01,1.62,2. 01 and 3. 18 times as that of （ 5.00 ± 0.75 ） μg·h^-1·cm^-2 β-CD aqueous solution. Penetration enhancer of DMSO and 1,2-trimethylene glycol increased the permeability by 1.50 and 1.83 times, compared with that ofβ-CD composite aqueous solution. CONCLUSION Ethosomes can improveβ-CD inclusion permeation, and increase the skin accumulation of the drug.