天山雪莲传递体的制备及其小鼠皮肤给药药动学特点

Dermato-pharmacokinetic studies of Saussurea involucrate transfersomes in rat topical skin

目的:制备天山雪莲传递体,考察天山雪莲在小鼠腹部皮肤的滞留量与时间的关系及其局部经皮给药的药动学。方法:采用注入-高剪切分散法制备天山雪莲传递体,测定样品的平均粒径、粒径分布等理化性质;以绿原酸、芦丁为指标性成分,采用HPLC法测定不同时间给药皮肤中绿原酸、芦丁生物滞留量,DAS软件拟合药动学参数。结果:天山雪莲传递体中以绿原酸为指标的包封率为83.95%、载药量为4.65%,以芦丁为指标的包封率为71.90%、载药量为3.94%,平均粒径为152.6nm,PDI值为0.202,Zeta电位为-3.29mV;在小鼠皮肤中滞留量的动力学过程符合二室模型。结论:天山雪莲传递体中有效成分能较快渗透进入皮肤,并在皮肤局部较长时间蓄积。

OBJECTIVE Saussurea involucrate transfersomes was prepared to study the relationship between deposition and time of Sa^ssurea involucrate in rats＇ abdominal skin and its topical pharmacokinetics. The function of transfersomes in enhancing the transdermal absorption of the encapsulated drug was investigated. METHODS The Saussurea involucrata was prepared by combining injection technique with high shear scattered method. The characteristics of prepared Saussurea involucrate transfersomes was determined including mean particle size, particle size distribution and zeta potential, respectively. The relationship between deposition and time of Saussurea involucrate in rats＇ abdominal skin was studied by selecting both chlorogenic acid and rutin in extracts of Saussurea involucrate as indexes with HPLC and the pharrrlacokinetic parameters were fitted by DAS. RESULTS The chlorogenic acid and rutin entrapment ef ficiency and drug loading of the prepared Saussurea involucrate transfersomes were 83. 95%, 71.90% and 4. 65%, 3. 94% respectively. The characteristics of prepared Saussurea involucrate transfersomes including mean particle size, particle size distribution and zeta potential, was 152. 6 nm, 0. 202 and - 3. 29 mV. Depositions of different time in rats＇ abdominal skin was studied could be fitted with the two compartment model. CONCLUSION The active ingredients of Saussurea involucrate transfermmes can permeate through the skin effectively and stay long time.