title: Enhanced transdermal bioavailability of testosterone propionate via surfactant-modified ethosomes.
abstract: 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).
authors.affiliation: Liaoning Research Institute of Family Planning, Shenyang, Liaoning Province, People's Republic of China.
authors.forename: Shu
authors.initials: S
authors.lastname: Meng
authors.forename: Zaixing
authors.initials: Z
authors.lastname: Chen
authors.forename: Liqun
authors.initials: L
authors.lastname: Yang
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Danhua
authors.initials: D
authors.lastname: Liu
authors.forename: Jing
authors.initials: J
authors.lastname: Guo
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Guan
authors.forename: Jianxin
authors.initials: J
authors.lastname: Li
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001682:Biological Availability; D000077286:Cetrimonium; D002593:Cetrimonium Compounds / Q000737:chemistry; D004355:Drug Stability; D000431:Ethanol; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D018613:Microscopy, Confocal; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000737:chemistry / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D043343:Testosterone Propionate / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D002593:Cetrimonium Compounds; D008081:Liposomes; D013501:Surface-Active Agents; C022131:cremophor; D000431:Ethanol; D011092:Polyethylene Glycols; D043343:Testosterone Propionate; D000077286:Cetrimonium
keywords: Testosterone propionate; confocal laser scanning microscopy; liposomes; surfactant-modified ethosomes