氧化苦参碱脂质体在体透皮研究

Percutaneous Penetration of Oxymatrine Liposomal Formulation in Vivo

目的研究氧化苦参碱脂质体及洗剂经小鼠皮肤给药后药物在皮肤中的分布。方法在体条件下分别局部外用氧化苦参碱脂质体与传统洗剂,测定药物在皮肤内及角质层中的分布情况。结果相同条件下,脂质体制剂在皮肤内药物滞留率较普通洗剂高,在角质层中较普通洗剂低;1.0%,1.5%,3.0%氧化苦参碱脂质体在皮肤内药物滞留率分别为(25.2±1.2)%,(40.1±2.4)%,(22.4±1.5)%,在角质层中药物滞留率分别为(10.3±1.1)%,(16.5±1.8)%,(34.2±1.6)%。结论脂质体制剂能有效透过皮肤角质层,持续发挥局部药物作用。

Objective To study in vivo permeability of oxymatrine topical liposomal and lotion formulations. Methods Distributions of oxymatrine in skin and stratum corneum were determined by SPE- HPLC after topical administration of liposome and common lotion formulations in rats. Results In vivo, the concentration in skin was higher and the concentration in stratum corneum was lower from liposomal formulation than those from gel formulation（P 〈 0. 01）. The residence ratio in skin was （25.2± 1.2）%, （40. 1±2.4）% and （22.4 ± 1.5）% respectively and the residence ratio in stratum corneum was （10. 3 ± 1. 1% ）, （16. 5 ±1.8）% and （34. 2 ± 1.6）% respectively for 1.0%, 1.5% and 3.0% liposomal formulations. Conclusion The liposomal formulation of oxymatrine can penetrate through skin more effectively comparing with lotion formulation.