应用不同类型脂质体作为姜黄素经皮给药载体的实验研究

Experiment on using different types of liposomes as carriers for curcumin transdermal delivery

目的:探讨不同脂质体作为姜黄素经皮给药载体药物透皮吸收及皮肤沉积效果,优化得到姜黄素经皮给药最佳脂质体载体。方法:注入法制备了3种类型脂质体——一般脂质体、乙醇脂质体(醇质体)和丙二醇脂质体,并对其粒径、包封率、体外释放率等理化性质进行了考察。采用大鼠腹部皮肤及franz扩散池进行体外透皮实验,HPLC法测定10 h内皮肤姜黄素透皮量及在皮肤的积蓄量,并加以比较。结果:各种不同脂质体的粒径大小次序为:一般脂质体(1 345.7±1 257.8)nm>乙醇脂质体(963.5±702.4)nm>醇水相体积比为1:2的丙二醇脂质体(506.6±326.7)nm。各种脂质体的姜黄素包封率大小为:丙二醇脂质体>醇质体>一般脂质体,其中醇水相体积比为1:2时制备的丙二醇脂质体粒径最小,包封率最高(92.74%±3.44%),且体外稳定性好,10 h内姜黄素透皮量和在皮肤的积蓄量与姜黄素乙醇溶液结果无明显差别。结论:醇相和水相体积比为1:2制备的丙二醇脂质体粒径小,包封率高,是姜黄素经皮给药的最佳载体。

Objective： To probe different types of liposomes and their practicability as curcumin transdermal delivery vectors.Methods： With curcumin as a target drug,three types of liposomes——traditional liposomes,ethosomes and propylene glycol liposomes（PGL）,were prepared by injection method.Their morphology,particle size and encapsulation effi-ciency were investigated.Drug release rate in vitro was measured using dissolution apparatus.Rat abdominal skin was used to evaluate drug transdermal quantity and deposition quantity in skin.Results： The order of particle size of different liposomes was： traditional liposomes（1346.7±1257.8）nmethosomes（963.5±702.4）nmPGL with glycol-wa-ter volume ratio of 1：2（506.6±326.7） nm.The sequence of encapsulation efficiency was： PGL ethosomestraditional liposomes.Liposomes prepared at 1：2 alcohol-water volume ratio had the highest encapsulation efficiency of 92.74±3.44%.From penetration test results,PGL made at propylene glycol-water volume ratio of 1：2 showed small particle size,high encapsulation efficiency and good stability.There was no significant difference between curcumin ethanol solution and optimum PGL in drug transdermal quantity and skin deposition quantity in 10 h.Conclusion： PGL with simple preparation and high encapsulation efficiency maybe an effective transdermal drug delivery carrier.