Enhanced transdermal bioavailability of testosterone propionate via surfactant-modified ethosomes

Abstract

Shu Meng,1 Zaixing Chen,2 Liqun Yang,1 Wei Zhang,1 Danhua Liu,1 Jing Guo,1 Yanmin Guan,1 Jianxin Li11Liaoning Research Institute of Family Planning, Shenyang, Liaoning Province, People's Republic of China; 2School of Pharmacy, China Medical University, Shenyang, Liaoning Province, People's Republic of ChinaAbstract: 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/cm2/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).Keywords: testosterone propionate, surfactant-modified ethosomes, liposomes, confocal laser scanning microscopy