酮洛芬醇质体凝胶与脂质体凝胶的体外经皮渗透动力学的比较研究

目的比较酮洛芬醇质体(KPFE)凝胶与脂质体(KPFL)凝胶的体外经皮渗透行为,以期为筛选出较优的KPF外用制剂奠定基础。方法制备KPFE凝胶与KPFL凝胶;以离体鼠皮为屏障,采用Franz扩散池法对KPF这2种凝胶的体外经皮渗透行为进行比较研究。结果 2种凝胶的经皮渗透动力学均符合Higuchi方程,KPFL凝胶剂:Q=28.65 t1/2-16.88(R2=0.995);KPFE凝胶剂:Q=35.22 t1/2-20.62(R2=0.988),稳态透皮速率分别为28.65μg·cm-2·h-1和35.22μg·cm-2·h-1,在经皮渗透24 h后,皮肤中的蓄积量分别为22.16μg·cm-2和19.95μg·cm-2,凝胶层中的残留量为56.25μg·cm-2和50.62μg·cm-2,4个指标之间比较差异均有统计学意义(P<0.05)。结论与KPFL凝胶相比,KPFE凝胶在促进药物经皮吸收方面具有更好的效果。

Comparative study on in vitro transdermal penetration of ketoprofen ethosomal gels and liposomal gels

Objective To compare the in vitro transdermal penetration of ketoprofen ethosomal(KPFE) gels and liposomal(KPFL) gels to screen the optimal external preparation for KPF.Methods KPFE gels and KPFL gels were prepared.Skipped mouse skin as the barrier,the in vitro transdermal penetration of the two gels was studied and compared by using Franz diffusion cells.Results Both the in vitro transdermal penetration of the two gels was fitted with Higuchi equation,Q=28.65 t1/2-16.88(R2=0.995) for KPFL gels and Q=35.22 t1/2-20.62(R2=0.988) for KPFE gels.The stability penetration rate was 28.65 μg·cm-2·h-1 and 35.22 μg·cm-2·h-1,respectively.After 24 h transdermal penetration,the KPF cumulative amount in skin and residual amount in the gels was 22.16 μg·cm-2 and 19.95 μg·cm-2,56.25 μg·cm-2 and 50.62 μg·cm-2,respectively.The above indices all showed significant difference between the two gels.Conclusion Compared with KPFL gels,KPFE gels exhibited better transdermal enhancement in the transdermal drug delivery systems.