Department of Pharmacy, 1st Hospital of Lanzhou University, Lanzhou, 730000, China.
Arch Pharm Res. 2010 Apr;33(4):567-74. doi: 10.1007/s12272-010-0411-2. Epub 2010 Apr 27.
The aim of this study was to investigate the lipophilic prodrug as a means of promoting acyclovir (ACV) that exhibited biphasic insolubility into the ethosomes for optimum skin delivery. Acyclovir Palmitate (ACV-C(16)) was synthesized as the lipophilic prodrug of ACV. The ethosomal system and the liposomal system bearing ACV or ACV-C(16) were prepared, respectively. The systems were characterized for shape, zeta potential value, particle size, and entrapment efficiency. Franz diffusion cells and confocal laser scanning microscopy were used for the percutaneous absorption studies. The results showed that the entrapment efficiency of ACV-C(16) ethosomes (87.75%) were much higher than that of ACV ethosomes (39.13%). The quantity of drug in the skin from ACV-C(16) ethosomes at the end of the 24 h transdermal experiment (622.89 microg/cm(2)) was 5.30 and 3.43 times higher than that from ACV-C(16) hydroalcoholic solution and ACV ethosomes, respectively. This study indicated that the binary combination of the lipophilic prodrug ACV-C(16) and the ethosomes synergistically enhanced ACV absorption into the skin.
本研究旨在探讨作为一种将阿昔洛韦（ACV）递送至皮肤的最佳方法的亲脂前药，以提高 ACV 的两亲溶解性。合成了 ACV 的亲脂前体棕榈酸阿昔洛韦（ACV-C（16））。分别制备了载有 ACV 或 ACV-C（16）的醇质体系统和脂质体系统。对这些系统的形状、ζ电位值、粒径和包封效率进行了表征。Franz 扩散池和共聚焦激光扫描显微镜用于经皮吸收研究。结果表明，ACV-C（16）醇质体的包封效率（87.75%）远高于 ACV 醇质体的包封效率（39.13%）。在 24 小时透皮实验结束时，ACV-C（16）醇质体中药物在皮肤中的量（622.89 μg/cm（2））分别比 ACV-C（16）水醇溶液和 ACV 醇质体高 5.30 和 3.43 倍。本研究表明，亲脂前体 ACV-C（16）与醇质体的二元组合协同增强了 ACV 向皮肤的吸收。
