肉桂油非离子表面活性剂囊泡经皮给药系统的研究

Percutaneous permeability of cinnamon volatile oil niosomes

目的:考察以非离子表面活性剂囊泡(niosomes)为载体的肉桂挥发油经皮给药的可行性以及浓度、促渗剂种类对药物渗透速率的影响。方法:制备非离子表面活性剂囊泡后,以SD♂大鼠皮肤为媒介,Franz单室扩散池为体外模型,用HPLC法测定透过皮肤的包合物含量。结果:按司盘40(Span40)与胆固醇(Chol)的用量为比1∶1形成的囊泡对适量肉桂油的平均包封率可以达到85%左右。肉桂油含量为0.1,0.5,2.0,5.0g.L-1的非离子表面活性剂囊泡,透皮速率分别为(4.8±0.3),(39.4±8.0),(86.3±17.4),(184.6±33.0)μg.h-1.cm-2。加入5%的二甲基甲酰胺、二甲基亚砜、月桂氮卓芯酮+丙二醇等促渗剂后,其透皮速率分别为对照组的1.17,1.27,1.30倍。结论:非离子表面活性剂囊泡能有效克服肉桂易挥发的特点,与促渗剂联合应用时能提高肉桂在皮肤中的滞留量,非离子表面活性剂囊泡制剂有望开发为肉桂新的经皮给药系统。

OBJECTIVE To investgate the possiblility of percutaneous transport of niosomes inclusion of cinnamon volatile oil and the inluence of the concentrations and the type of penetration enhancer on the permeation rate. METHODSNiosomes were performed by Span40 and Chol. With the skin of 813 male rat, the penetration experiments in vitro were performed on modified Franz diffusion cells. The amount of drug penetration concentrations of inclution compound was determined by HPLC. RESULTS Niosomes prepared by span40 and Chol According to 1 ： 1 ratio, the Average encapsulation efficiency can be achieved a bout 85%. The steady permeation rate of niosomes which Cinnamon oil content 0. 1,0. 5,2. 0,5.0 g.L ^-1 were （4. 8 ± 0. 3）, （39. 4 ±8. 0）, （86. 3 ±17. 4）, （ 184. 6 ± 33. 0）μg. h ^-1 cm ^-2 respectively. With addition of penetration enhancer such as N, N- DMF（5%） DMSO（5%） ,azone（5Y0） ＋ 1,2 trimethylene glycol（5%）, it was 1.17,1.27,1.30 higher than that of the control group. CONCLUSION Niosomes can effectively overcome the characteristics of volatile cinnamon oil increase the skin accumu lation of drug.