8-甲氧补骨脂素脂质体凝胶皮肤渗透性实验  

Experimental Study on the Percutaneous Permeability of 8-Methoxypsoralen Liposomal Gels

作　　者：阳长明[1] 冯长根[1] 向大雄[2,3] 邓霞飞[1] 赵梦丹[4] 董丽[4] 

机构地区：[1]北京理工大学机电工程学院 [2]中南大学湘雅二医院天然药物研究室 [3]中南大学药学院,长沙410011 [4]中南大学药学院

出　　处：《中国天然药物》2007年第1期56-58,共3页

基　　金：湖南省科技厅资助项目(04SK1007-25)~~

摘　　要：目的研究8-甲氧补骨脂素脂质体凝胶体外皮肤渗透性,为剂型选择和处方筛选提供依据。方法采用改良Franz扩散池法,观察8-甲氧补骨脂素酊剂、脂质体、脂质体凝胶、凝胶对离体小鼠皮肤的渗透性能,高效液相色谱测定加药0.5,1.0,2.0,3.0,5.0,7.0,11.0,13.0h后接收池中8-甲氧补骨脂素浓度,并在实验末期将皮肤组织匀浆,测定皮肤组织中的药物滞留量,同时在不同时间点取少量接收液,透射电镜观察透皮液有无脂质体存在及形态。结果接收液中药物浓度在前3h以脂质体组最高,酊剂次之,脂质体凝胶第三,测得滞留于皮肤内的8-甲氧补骨脂素脂质体组、脂质体凝胶组分别是酊剂组2.7倍、1.8倍,是凝胶组的6.2倍和4.1倍,在接收池中没有观察到完整的脂质体形态。结论8-甲氧补骨脂素脂质体、脂质体凝胶和酊剂均有较强的小鼠离体皮肤渗透性,凝胶剂渗透性较弱;8-甲氧补骨脂素脂质体、脂质体凝胶对于皮肤细胞有特殊的亲和力,有助于药物在皮肤聚集;脂质体可能不是直接透过皮肤进入血液,而是在皮肤中释放药物,然后药物再渗透、穿过皮肤。AIM： To study the permeability of liposomal gel encapsulated 8-methoxypsoralen in vitro. METHODS： The improved Franz diffusing cells were chosen to study percutaneous permeability of 8-methoxypseralen tincture, lipeseme, liposemal gel and gel in mice in vitro was observed. The concentration of 8-methoxypseralen into the receptor cells after administration from 0.5 h to 13.0 h was determined by HPLC. The drug resident percentage in the cutaneous tissue homogenate was measured. And the shape and existence of liposome in different time after administration was observed by using TEM too. RESULTS： The drug concentration of the first three hours into the receptor cells of the liposeme group is highest ,the tincture group is second and the liposomal gel group is the last one; the drug resident percentage in the cutaneous of liposomal group and liposomal gel group are respectively 2.7 and 1.8 times than the tincture group, 6.2 and 4.1 times than gel group; complete liposome is not observed. CONCLUSION： All the three dosage forms have the percutaneous permeability, gel dosage form is feeble; liposome and liposomal gel have especial affinity to the cutaneous cells, and conduce to the assumption of the drug, lipesome probably permeate the cutaneous after metabolism and release but not directly.

关 键 词：8-甲氧补骨脂素 脂质体 脂质体凝胶 皮肤渗透性 

分 类 号：R944[医药卫生—药剂学]