Use of alpha-tocopherol esters for topical vitamin e treatment: Evaluation of their skin permeation and metabolism

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Abstract

Objectives The aim of this work was to investigate new pro-vitamins based on α-tocopherol (α-Toc) and fatty acids, and to compare their properties with those of α-tocopherol acetate (α-TAc). Methods Skin levels of α-Toc-fatty acid ester conjugates, total α-Toc and endogenous α-Toc were measured in skin samples taken from separate groups of treated and untreated rats. Multiple and extensive treatment with α-Toc oleate and α-TAc was also carried out to assess the skin accumulation and safety of these esters. Key findings The in-vivo studies revealed that α-Toc-fatty acid conjugates penetrated into the skin quantitatively while being comparable with the permeation of α-TAc. Differences were found between the levels of total α-Toc and endogenous α-Toc after application of α-TAc, α-Toc oleate, α-Toc linoleate, α-Toc-α linolenate and α-Toc palmitate, indicating that α-Toc conjugates of these fatty acids, but not α-Toc γ-linolenate or α-Toc stearate, were hydrolysed to free α-Toc. In long-term and extensive treatment, α-TAc was found to be lethal to rats treated with 1.15 mg/kg of this agent, which had been spread over 16 cm2 of skin. Similar treatment with α-Toc oleate did not produce any side effects. Conclusions This study suggests that α-Toc conjugates with unsaturated fatty acids may be a good alternative as stable vitamin E derivatives, rather than the α-TAc ester.

Original languageEnglish
Pages (from-to)652-658
Number of pages7
JournalJournal of Pharmacy and Pharmacology
Volume65
Issue number5
DOIs
StatePublished - 1 May 2013

Keywords

  • polyunsaturated fatty acids
  • skin permeation
  • α-tocopherol
  • α-tocopherol acetate

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