摘要
Abstract
Objective To compare the in vitro stability and transdermal penetration of ketoprofen (KPF) ethosomal (KPFE) gels versus binary ethosomal (KPFBE) gels for screening the optimal external preparation for KPF.Methods KPFE gels and KPFBE gels were prepared.The stability of the two KPF gels was studied and compared after centrifugation,high temperature (60 ℃),low temperature (4 ℃) or strong light.With skipped mouse skin as the barrier,the in vitro transdermal penetration of the two gels was studied and compared using Franz diffusion cells.Results After the centrifugation,the two gels showed no layer separation phenomenon.The stabilities of KPFE at low temperature and strong light were good,while at high temperature,the drug concentration and mean size of KPFE were increased with the testing time.Under the above experimental conditions,the stability of KPFBE was promising.Both the in vitro transdermal penetration of the two gels was fitted zero-order kinetic equation,Q =38.04t + 12.32 (r =0.999 6) for KPFE gels and Q =54.68t-21.19 (r =0.998 5) for KPFBE gels.The steady state penetration rate (J) was 38.04 μg/(cm2 · h) for KPFE and 54.68 μg/(cm2 · h) for KPFBE.After 24 h transdermal penetration,the KPF cumulative amount in skin was 18.36 μg/cm2 for KPFE gels and 16.79 μg/cm2 for KPFBE gels (P > 0.05),and residual amount in the gels was 2.45 mg and 1.34 mg,respectively (P < 0.05).Conclusion Compared with KPFE gels,KPFBE gels exhibit better stability and in vitro transdermal penetration in the transdermal drug delivery systems.关键词
酮洛芬/一元醇质体/二元醇质体/稳定性/体外经皮渗透Key words
ketoprofen / ethosomes / binary ethosomes / stability / in vitro transdermal penetration分类
医药卫生