洛美沙星透皮吸收制剂对仔猪皮肤表皮结构的影响

Effect of percutaneous absorption preparation of lomefloxacin with laurocapram on epidermal morphology of piglet skin

在 10-12日龄同品种仔猪的腹部皮表区域涂搽含氮酮的洛美沙星透皮吸收制剂和不含氮酮的洛美沙星水溶液,分别于涂药前、涂药后 2、4、6、12、24、48和 72h在体取皮,应用普通光镜和扫描电镜对皮肤表皮结构的变化进行对比观察,探讨氮酮促进洛美沙星透皮吸收的作用机理.结果表明,氮酮通过以下途径促进药物透皮吸收: (1)作用于表皮角质层细胞间脂质,导致细胞结构变得疏松,外层细胞脱落,角质层变薄,降低了皮肤对药物渗透的屏障作用; (2)作用于毛囊,导致毛囊口附近角质疏松,药物易于在此部位储存并经毛囊缓慢渗透入皮下,但毛囊在本制剂经皮渗透中为非主要途径.研究还发现,含有氮酮的洛美沙星透皮吸收制剂对仔猪皮肤的主要作用时段是在给药后 6h内,但氮酮的作用可以维持 72h以上.由氮酮引起皮肤结构的改变是一个非损伤性可逆过程.

To clarify the mechanism of action of laurocapram in lomefloxacin percutaneous absorption preparation, the effect of laurocapram on the epidermal morphology of piglet was investigated in vivo by using optical microscope (LM) and scanning electron microscope (SEM). The results demonstrated the mechanism of action of laurocapram as a penetration enhancer are as follows: (1) Laurocapram disrupts the highly ordered lipid structure of stratum corneum (SC) and makes it loose, which results in the outermost cell of SC easy to exfoliate, decreases the barrier function of skin for the transdermal absorption of this preparation. (2) Meanwhile, laurocapram makes the SC around hair follicles loose, which creates a storage for this preparation and results in transdermal absorption by hair follicle path. But, hair follicle is a minor penetration route in this preparation. The study also discovered that the major acting time of laurocapram is within 6 hours after medication, and that the barrier struture of SC is still in the state of recovery at 72 hours. The structural change of epidermis caused by laurocapram is a non-damnifing and reversible course.