Novel nanocapsule of α-lipoic acid reveals pigmentation improvement: α-Lipoic acid stimulates the proliferation and differentiation of keratinocyte in murine skin by topical application

Exp Dermatol. 2019 Feb;28 Suppl 1:55-63. doi: 10.1111/exd.13828.


α-Lipoic acid is amphipathic with low molecular sulphur-containing fatty acid and has strong antioxidant effects. It has been used at the purposes of anti-ageing, treatment of diabetic neuropathy, and supplement as antioxidant. Though α-lipoic acid is normally administered in oral or injection, it has not been used in a topical use via skin because of its bad penetration. We developed the novel nanocapsule of α-lipoic acid, named α-lipoactive (nLA), to improve skin permeability. The nLA is constructed as micelles of α-lipoic acid mixed with the non-ionic surfactant, and its surface of the micelles was coated with inorganic metal salts. It is water soluble and has a diameter of approximately 8-15 nm. After nLA was applied to the murine skin, epidermal thickening was observed. It was confirmed that this effect is caused by α-lipoic acid molecule, but not by the raw material used for encapsulation. In in vivo experiments, it was found that nLA is very effective for improving UV-induced pigmentation and epidermal thickening. Our findings suggest that nanoencapsulation of α-lipoic acid is considerably effective for topical application.

Keywords: keratinocyte; nanocapsule; skin turnover; topical application; α-lipoic acid.

Publication types

  • Review

MeSH terms

  • Administration, Topical
  • Animals
  • Antioxidants / pharmacology
  • Cell Differentiation / drug effects*
  • Cell Proliferation / drug effects*
  • Cosmetics
  • Fatty Acids / chemistry
  • Gene Expression Profiling
  • Guinea Pigs
  • Keratinocytes / cytology
  • Keratinocytes / drug effects*
  • Male
  • Mice
  • Nanocapsules*
  • Nanomedicine
  • Permeability
  • Signal Transduction
  • Skin / drug effects*
  • Skin Pigmentation / drug effects*
  • Sulfur / chemistry
  • Thioctic Acid / chemistry
  • Thioctic Acid / pharmacology*
  • Ultraviolet Rays


  • Antioxidants
  • Cosmetics
  • Fatty Acids
  • Nanocapsules
  • Sulfur
  • Thioctic Acid