十一酸睾酮二元醇质体体外透皮特性及其安全性研究

In vitro Transdermal Penetration and Safety of Testosterone Undecanoate Binary Ethosomes

目的:对十一酸睾酮(TU)二元醇质体的体外透皮特性进行考察,并对其皮肤安全性进行研究。方法:采用注入法制备TU二元醇质体;以小鼠皮肤为屏障,采用Franz扩散池法对其体外透皮特性进行考察;以豚鼠为实验动物,对其皮肤刺激性、过敏性、毒性进行考察。结果:TU二元醇质体平均包封率为(79.14±0.66)%;体外透皮实验中,累积释药百分率Q与时间t的关系符合一级动力学方程:Q=8.57t+8.26(r=0.998 6),稳态透皮速率为8.57μg·cm-2·h-1;24 h后TU在皮肤中的滞留量为(208.8±55.26)μg·g-1;TU二元醇质体无明显局部刺激性、致敏性及急性毒性。结论:TU二元醇质体表现出较好的体外透皮渗透性,且安全性理想,值得进一步研究。

Objective： To study the in vitro transdermal penetration and skin safety of testosterone undecanoate （TU） binary etho- somes. Methods： TU binary ethosomes were prepared by an ethanol injection method. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes. The local skin irritation, hypersensitivity and toxic- ity were studied in guinea pigs. Results： The entrapment efficiency of TU binary ethosomes was （79.14 ± 0.66） %. The in vitro trans- dermal penetration was fitted a first-order equation： Q = 8. 57t ＋ 8. 26 （ r = 0.998 6） with the stable penetration rate of 8.57 μg · cm- 2 · h-1. After 24 h, the amount of TU in skin was （208.8 ± 55.26） μg · g-l. No significant local irritation, sensitization and acute toxicity were shown for TU binary ethosomes. Conclusion： TU binary ethosomes exhibit promising in vitro transdermal penetration with high safety, which are valuable to be studied further.