灯盏花素脂质载体凝胶的小鼠在体透皮及皮肤局部药代动力学考察

Transdermal Test and Topical Skin Pharmacokinetic Investigation of Breviscapine Lipid Carrier Gel in Mice

目的:考察灯盏花素普通凝胶与固体脂质纳米粒凝胶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代动力学,探讨固体脂质纳米粒凝胶促进灯盏花素经皮渗透的作用机制。方法:建立皮肤中灯盏花素滞留量的测定方法,比较灯盏花素固体脂质纳米粒凝胶与普通凝胶的在体透皮皮肤滞留量,采用DAS药动学软件拟合药物动力学参数,初步探讨2种凝胶皮肤局部药代动力学。结果:普通凝胶24 h内单位面积皮肤滞留量为固体脂质纳米粒凝胶的1.73倍;固体脂质纳米粒凝胶和普通凝胶皮肤局部动力学过程分别以二室、一室模型拟合效果较好,AUC0-24分别为17.804,24.675 mg.L-1.h,T1/2分别为10.855,15.534 h。结论:固体脂质纳米粒凝胶中灯盏花素透过皮肤进入体内的程度和速度均较普通凝胶大,对药物渗透皮肤有促进作用。

Objective：To investigate relationship between deposition amount and time of breviscapine common gel and solid lipid nanoparticle（SLN） gel in mice abdominal skin,and their topical pharmacokinetic of transdermal drug delivery.To investigate mechanism of SLN gel in enhancing breviscapine to penetrate into skin. Method： To set up an assaying methodology of breviscapine deposition amount in skin and compare accumulation deposition amount of breviscapine in skin between common gel and SLN gel,pharmacokinetics parameters were fitted by DAS software,in order to discuss topical pharmacokinetic of these two gels. Result： Within 24 h,per unit area deposition amount of breviscapine in skin of common gel were 1.73 times more than SLN gel;Dermatopharmacokinetic process of SLN gel and common gel were fitted with tow-compartment model and one-compartment model,respectively, AUC0-24 were 17.804,24.675 mg·L-1·h and T1/2 were 10.855, 15.534 h, respectively. Conclusion： Transdermal degree and speed of SLN gel were greater and faster than common gel,which showed that SLN gel had function to enhance drug to penetrate into skin.