【摘要】 目的制备黄藤素脂质体,考察其体外透皮行为。方法薄膜分散法制备黄藤素脂质体,测定其粒径、Zeta电位、包封率、体外释放度,考察包封率测定方法,使用改良Franz扩散池考察体外透皮特性,以及皮肤滞留情况。结果鱼精蛋白法测得包封率为59.22%,阳离子交换树脂法测得包封率为45.53%。大豆磷脂1.0 g、胆固醇0.15 g、黄藤素0.02 g以薄膜分散法制得黄藤素脂质体为球状或类球状粒子,平均粒径215.2 nm,Zeta电位-20.5 mV。体外释放结果表明,黄藤素脂质体释药与黄藤素溶液剂相比,呈缓释行为,符合Weibull模型(r=0.993 0);体外透皮吸收试验显示,黄藤素脂质体、黄藤素溶液剂中黄藤素8 h累积释放量分别为(53.42±5.96)、(12.72±3.28)μg·cm-2,平均皮肤蓄积率分别为0.93%、0.45%。结论与黄藤素溶液剂相比,黄藤素脂质体可以显著提高黄藤素透皮吸收速率,增加皮肤蓄积量,在皮肤外用中具有潜在的优势。更多还原

【Abstract】 Objective To prepare the palmatine liposomes and to investigate the in vitro transdermal behavior.Methods For the palmatine liposomes prepared by thin film dispersion method,the particle size,Zeta potential,encapsulation efficiency and in vitro release were determined. The determination method of encapsulation efficiency was investigated. The modified Franz diffusion pool was use to conduct an in vitro transdermal absorption experiment to investigate the transdermal absorption behavior and skin retention. Results The entrapment efficiency was59.22% determined by protamine method and 45.53% by cation exchange resin. What’s more, the palmatine liposomes prepared from soybean phospholipid 1.0 g,cholesterol 0.15 g and palmatine 0.02 g by film dispersion method demonstrated an average particle size of 215.2 nm and Zeta potential of-20.5 mV. In vitro release experiments showed that,compared with the solution,the palmatine liposomes showed sustained release behavior,which conformed to the Weibull equation(r=0.993 0). In vitro transdermal absorption test showed that the 8-hour cumulative permeation per unit area of palmatine liposomes and palmatine aqueous solutions were(53.42 ±5.96)and(12.72 ± 3.28)μg · cm-2, respectively, and the average skin accumulation rates was 0.93% and 0.45%,respectively. Conclusion The palmatine liposomes can increase the transdermal absorption rate of the palmatine and increase the skin accumulation compared with the aqueous solution,which has potential advantages in external use of skin.更多还原