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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 effect of complex phospholipid composition composed of phospholipid (EPC) and hydrogenated soya phospholipid (HSPC) on the transdermal delivery of the active ingredients through the liposomes. Methods The phospholipid liposomes were prepared by membrane dispersion method. The liposomes were modified by freeze-thaw cycle to obtain liposome artificial skin membranes. The membrane resistance was measured by membrane resistance meter. The activity of 5 kinds of active ingredients ferulic acid, paeoniflorin, paeoniflorin, tetrandrine and tetrahydropalmatine on liposome artificial skin membrane through different complex phospholipids. The interaction between complex phospholipids was analyzed by differential scanning calorimetry (DSC). Results The ratio of complex phospholipids had a regulatory effect on the resistance of the liposome artificial skin membrane, reaching the maximum at a molar ratio of EPC: HSPC = 3: 1, and the barrier function was the strongest at this time. Proportions of liposomes on the artificial skin membrane transmission through the least. In the EPC: HSPC = 3: 1 to 1: 3 range, the transdermal liposomes increased with the increase of HSPC. The results of DSC showed that EPC and HSPC fused to homogeneous phase when EPC: HSPC ratio was 3:1. Conclusion The application of complex phospholipid ratio can effectively control the barrier function of the liposome skin membrane, which may be used to simulate the real skin in different states to investigate the transdermal behavior of active ingredients of traditional Chinese medicine.