Combined effect of d-limonene pretreatment and temperature on the rat skin permeation of lipophilic and hydrophilic drugs.
Combined effect of d-limonene pretreatment and temperature on the rat skin permeation of lipophilic and hydrophilic drugs.
复制标题
d-柠檬烯预处理和温度对亲脂性和亲水性药物大鼠皮肤渗透的联合影响。
DOI：
10.1248/bpb.18.439
复制
发表时间：
1995
影响因子：
2
通讯作者：
T. Nagai
中科院分区：
文献类型：
--
作者：
N. Ohara;K. Takayama;T. Nagai
本文研究了d-柠檬烯和温度联合作用对亲脂性和亲水性渗透剂的体外透皮性能的影响。以强的松龙为亲脂性渗透剂，以葡萄糖和异烟肼为亲水剂。当皮肤用不含d-柠檬烯的30%乙醇处理时，由于渗透性很低，各渗透剂的稳态渗透系数(P)很难计算。另一方面，当皮肤用1.5%d-柠檬烯在30%乙醇中预处理时，每种渗透剂的累积量随着温度的升高而增加。葡萄糖和异烟肼的P值在Arrhenius曲线上呈线性关系，经皮渗透的活化能分别为87.6和66.5kJ/mol。然而，当强的松龙作为渗透剂时，P值的阿累尼乌斯曲线呈凸曲率。这可能表明，d-柠檬烯和温度的联合使用有效地改变了角质层非极性通路的屏障结构，而对极性通路没有观察到协同作用。
The combined effect of d-limonene and temperature on the skin permeation of lipophilic and hydrophilic penetrants has been investigated in rats in vitro. Prednisolone was used as a lipophilic penetrant, and glucose and isoniazid were used as hydrophilic ones, respectively. When the skin was pretreated with 30% ethanol without d-limonene, the steady state permeability coefficient (P) of every penetrant through the skin was difficult to calculate because of very low permeability. On the other hand, the cumulative amount of each penetrant increased with an increase in temperature when the skin was pretreated with 1.5% d-limonene in 30% ethanol. The Arrhenius plots of P values for glucose and isoniazid showed a linear relationship, and the activation energies of skin permeation were estimated to be 87.6 and 66.5 kJ/mol, respectively. When prednisolone was used as penetrant, however, the Arrhenius plot of P values exhibited a convex curvature. This may suggest that the combined use of d-limonene and temperature effectively changes the barrier structure of the non-polar pathway in the stratum corneum, while no synergistic effect was observed on the polar pathway.