复合磷脂组成对香附四物汤活性成分透过脂质体人工皮肤膜行为的影响（英文）

Influence of Phospholipid Composition on the Permeation Behaviors of Active Ingredients from Xiang-Fu-Si-Wu Decoction Through Liposome-Based Artificial Skin Membrane

目的考察蛋磷脂(EPC)与氢化大豆磷脂(HSPC)构成的复合磷脂组成对香附四物汤活性成分透过脂质体人工皮肤膜行为的影响。方法用薄膜分散法制备复合磷脂脂质体,脂质体通过冻-融循环工艺改性聚碳酸酯膜制得脂质体人工皮肤膜,细胞膜电阻仪测定膜电阻,并且考察了香附四物汤5种活性成分阿魏酸、芍药苷、芍药内酯苷、四氢非洲防己碱、延胡索乙素透过不同复合磷脂组成脂质体人工皮肤膜的行为。通过差示扫描量热法(DSC)分析复合磷脂之间的相互作用机制。结果复合磷脂比例对脂质体人工皮肤膜的电阻起到调节作用,在EPC∶HSPC=3∶1摩尔比时达到最大,此时屏障功能最强,香附四物汤活性成分在此复合磷脂比例下的脂质体人工皮肤膜上透过量最少。在EPC∶HSPC=3∶1~1∶3的范围内,脂质体人工皮肤膜的透过量随HSPC的增加而增大。DSC检测结果说明在EPC∶HSPC比例为3∶1时EPC与HSPC融合为均一相。结论应用复合磷脂比例可以有效控制脂质体皮肤膜的屏障功能,从而有可能用于模拟不同状态下的真实皮肤以考察中药活性组分的透皮行为。

OBJECTIVE To investigate the effects of the composition of egg phosphatidylcholine （EPC） and hydrogenated soybean phosphatidylcboline （HSPC） on the permeation behaviors of active ingredients from Xiang-Fu-Si-Wu Decoction （XF- SWD） through liposome-based artificial skin membrane （LASM）. METHODS Liposomes with different phospholipid compo- sitions were prepared by film-dispersion method. The nylon membrane was combined with liposomes by freezing-thawing cycle to obtain LASM and its electrical resistance value was measured by a cell membrane resistance meter. The LASM with differ- ent phospholipid compositions was applied for the measurement of skin permeation behaviors of five active ingredients （ferulic acid, paeoniflorin, albiflorin, tetrahydrocolumbamine and tetrahydropalmatine） from XFSWD. Interaction mechanism between EPC and HSPC was investigated by differential scanning calorimetry （DSC） analysis. RESULTS Phospholipid composition played a regulatory role for the electrical resistance of LASM. The highest barrier function of LASM was obtained at the molar ratio of EPC ：HSPC=3 ： 1, resulting in the lowest permeation values of the active ingredients from XFSWD. The permeabili- ty increased with the increase of HSPC in LASM in the range of the molar ratio of EPC ： HSPC =3 ： 1-1 ： 3. Additionally, DSC analysis revealed that EPC and HSPC could be combined into one homogenous phase at the molar ratio of EPC ： HSPC 3 ： 1. CONCLUSION The barrier function of LASM can be effectively controlled by the modification of phospholipid composi- tion, facilitating the simulation of real skin barrier to investigate the skin permeation behaviors of the active components from traditional Chinese medicine.