Liaoning Research Institute of Family Planning, Shenyang, Liaoning Province, People's Republic of China.
Int J Nanomedicine. 2013;8:3051-60. doi: 10.2147/IJN.S46748. Epub 2013 Aug 13.
The current investigation aimed to evaluate the transdermal potential of novel testosterone propionate (TP) ethosomes and liposomes prepared by surfactant modification. The effect of hexadecyl trimethyl ammonium bromide and cremophor EL-35 on the particle size and zeta potential of the prepared vesicles was investigated. The entrapment efficiency and stability, as well as in vitro and in vivo skin permeation, were studied with the various techniques, such as differential scanning calorimetry, confocal laser scanning microscopy, transmission electron microscopy, dynamic light scattering, and so on. The results indicated that the ethosomes were defined as spherical, unilamellar structures with low polydispersity (0.100 ± 0.015) and nanometric size (156.5 ± 3.5 nm). The entrapment efficiency of TP in ethosomal and liposomal carriers was 92.7% ± 3.7% and 64.7% ± 2.1%, respectively. The stability profile of the prepared TP ethosomal system assessed for 120 days revealed very low aggregation and very low growth in vesicular size. TP ethosomes also provided an enhanced transdermal flux of 37.85 ± 2.8 μg/cm(2)/hour and a decreased lag time of 0.18 hours across mouse skin. The skin permeation efficiency of the TP ethosomes as further assessed by confocal laser scanning microscopy revealed enhanced permeation of rhodamine red-loaded formulations to the deeper layers of the skin (260 μm) than that of the liposomal formation (120 μm).
本研究旨在评估新型睾酮丙酸（TP）醇质体和由表面活性剂修饰制备的脂质体的经皮潜力。考察了十六烷基三甲基溴化铵和吐温 EL-35 对所制备囊泡的粒径和 zeta 电位的影响。采用差示扫描量热法、共聚焦激光扫描显微镜、透射电子显微镜、动态光散射等多种技术研究了包封率和稳定性，以及体外和体内皮肤渗透。结果表明，醇质体呈球形、单分子层结构，具有低多分散性（0.100 ± 0.015）和纳米级粒径（156.5 ± 3.5nm）。TP 醇质体和脂质体载体的包封率分别为 92.7% ± 3.7%和 64.7% ± 2.1%。对制备的 TP 醇质体系统进行了 120 天的稳定性评估，结果表明其聚集程度非常低，囊泡粒径增长非常低。TP 醇质体还提供了增强的 37.85 ± 2.8μg/cm(2)/小时的经皮通量和 0.18 小时的滞后时间，从而减少了穿过小鼠皮肤的药物传输。通过共聚焦激光扫描显微镜进一步评估 TP 醇质体的皮肤渗透效率，结果表明，与脂质体制剂相比，罗丹明红负载制剂更能渗透到皮肤的深层（260μm）。
