Alpha‐tocopherol (AT) is the vitamin E homologue with the highest in vivo biological activity. AT protects against the carcinogenic and mutagenic activity of ionizing radiation and chemical agents, and possibly against UV‐induced cutaneous damage. For stability consideration, alpha‐tocopherol is usually used as its prodrug ester, alpha‐tocopherol acetate (ATA), which once absorbed into the skin is hydrolyzed to alpha‐tocopherol, the active form. The objective of this research was to characterize in vitro the permeation properties of ATA from various solutions and gel formulations. Permeation studies were conducted using modified Franz diffusion cells and human cadaver skin as the membrane. Specifically, 5% (w/w) alpha‐tocopherol acetate was formulated in the following vehicles: ethanol, isopropyl myristate, light mineral oil, 1% Klucel_gel in ethanol, and 3% Klucel_gel in ethanol (w/w). The receiver temperature was 37°C. Samples from the receiver were collected at 2, 4, 6, 8, 12, 24, 30, 36, and 48 h and analyzed by HPLC for concentrations of alpha‐tocopherol acetate and alpha‐tocopherol. The permeabilities of ATA through human cadaver skin were 1.0 × 10–4, 1.1 × 10–2, 1.4 × 10–4, 2.1 × 10–4, and 4.7 × 10–4 cm/h for the ethanol solution, isopropyl myristate solution, light mineral oil solution, 1% Klucel_gel, and 3% Klucel gel, respectively. The results show that the formulation had relatively minor effects on the permeability coefficients of ATA through cadaver skin in all cases except for the isopropyl myristate solution.
