Alpha Lipoic Acid (RS-ALA)
About Alpha Lipoic Acid in DIY Skin Care
Alpha Lipoic acid is an antioxidant used to treat and prevent the aging of skin, fine lines, and pigmentation abnormalities. Lipoic acid may decrease the inflammation that leads to accelerated skin aging.
The effectiveness of Alpa Lipoic acid is believed to be due to its by-product, dihydrolipoic acid (DHLA).
Although DHLA has a more powerful antioxidative effect than Alpa Lipoic acid, it is very unstable and is oxidized in the skin within minutes of application.
Alpa Lipoic acid has become popular due to the fact that it is absorbed in a stable form and after entrance into cells, is immediately converted to DHLA
Researchers have identified and emphasized four principal antioxidative properties of Alpa Lipoic acid:
The capacity to chelate metals.
The ability to scavenge reactive oxygen species.
The ability to regenerate endogenous antioxidants such as vitamins C and E.
The ability to repair oxidative
Topical application of 3% Alpa Lipoic acid in a lecithin base has been shown to reduce UVB-induced erythema .
Topical application of lipoic acid could prevent free radical damage to skin, reducing the effects of photoaging and carcinogenesis.
However, it should be noted that research has also indicated that Alpa Lipoic acid is sensitive to UV radiation.
Alpa Lipoic acid should therefore be used as a sun damage treatment, NOT a sun damage prevention product.
From alpha Lipoic Acid to dihydrolipoic acid
- Alpha Lipoic acid is an example of an existing drug whose therapeutic effect has been related to its antioxidant activity. 
- Dihydrolipoic acid [DHLA], formed by reduction of lipoic acid, has more antioxidant properties than does lipoic acid. 
- Both dihydrolipoic acid [DHLA], and Alpha lipoic acid have metal-chelating capacity and scavenge ROS, whereas only DHLA is able to regenerate endogenous antioxidants and to repair oxidative damage. 
- Alpha lipoic acid can act as an antioxidant against the pro-oxidant activity produced by dihydrolipoic acid [DHLA]. 
- Dihydrolipoic acid [DHLA], has the capacity to regenerate the endogenous antioxidants vitamin E, vitamin C and Glutathione. 
- Alpha lipoic acid topically applied to skin penetrated readily, and was reduced to 
- Alpha lipoic acid was converted rapidly by the cells to dihydrolipoic acid. 
Alpha Lipoic Acid is an acid and it may irritate. Start of with small amounts. A slight tingling/burning feeling upon application is common, this should go away after a few minutes. If not, remove from face and use a smaller percentage.
Topically applied Alpha Lipoic Acid may:
- prevent or reduce UVA and UVB sun damage:     
- act as an anti oxidant     
- increase collagen production 
- act as an anti inflammatory 
12. Matsugo S, Bito T, Konishi T.. Photochemical stability of lipoic acid and its impact on skin ageing. Free Radic Res. 2011 Aug;45(8):918-24. Epub 2011 Jun 9. PMID: 21651453
11. Tsuji-Naito K, Ishikura S, Akagawa M, Saeki H. α-Lipoic acid induces collagen biosynthesis involving prolyl hydroxylase expression via activation of TGF-β-Smad signaling in human dermal fibroblasts. Connect Tissue Res. 2010 Oct;51(5):378-87. PMID: 20604712
10. Wada N, Wakami H, Konishi T, Matsugo S. The Degradation and Regeneration of alpha-Lipoic Acid under the Irradiation of UV Light in the Existence of Homocysteine. J Clin Biochem Nutr. 2009 May;44(3):218-22. Epub 2009 Apr 25. PMID: 19430609
9. Davis GD, Masilamoni JG, Arul V, Kumar MS, Baraneedharan U, Paul SF, Sakthivelu IV, Jesudason EP, Jayakumar R. Radioprotective effect of DL-alpha-lipoic acid on mice skin fibroblasts.. Cell Biol Toxicol. 2009 Aug;25(4):331-40. Epub 2008 Jun 13. PMID: 18553143
8. Petersen Shay K, Moreau RF, Smith EJ, Hagen TM. Is alpha-lipoic acid a scavenger of reactive oxygen species in vivo? Evidence for its initiation of stress signaling pathways that promote endogenous antioxidant capacity. IUBMB Life. 2008 Jun;60(6):362-7. PMID: 18409172
7. Ho YS, Lai CS, Liu HI, Ho SY, Tai C, Pan MH, Wang YJ. Dihydrolipoic acid inhibits skin tumor promotion through anti-inflammation and anti-oxidation. Biochem Pharmacol. 2007 Jun 1;73(11):1786-95. Epub 2006 Dec 10. PMID: 17403519
6. Lin JY, Lin FH, Burch JA, Selim MA, Monteiro-Riviere NA, Grichnik JM, Pinnell SR. Alpha-lipoic acid is ineffective as a topical antioxidant for photoprotection of skin. J Invest Dermatol. 2004 Nov;123(5):996-8. PMID: 15482491
5. Beitner H. Randomized, placebo-controlled, double blind study on the clinical efficacy of a cream containing 5% alpha-lipoic acid related to photoageing of facial skin. Br J Dermatol. 2003 Oct;149(4):841-9. PMID: 14616378
4. Podda M, Zollner TM, Grundmann-Kollmann M, Thiele JJ, Packer L, Kaufmann R. Activity of alpha-lipoic acid in the protection against oxidative stress in skin. Curr Probl Dermatol. 2001;29:43-51. PMID: 11225200
3. Biewenga GP, Haenen GR, Bast A. The pharmacology of the antioxidant lipoic acid. Gen Pharmacol. 1997 Sep;29(3):315-31. PMID: 9378235
2. Podda M, Rallis M, Traber MG, Packer L, Maibach HI. Kinetic study of cutaneous and subcutaneous distribution following topical application of [7,8-14C]rac-alpha-lipoic acid onto hairless mice. Biochem Pharmacol. 1996 Aug 23;52(4):627-33. PMID: 8759036
1. Handelman GJ, Han D, Tritschler H, Packer L. Alpha-lipoic acid reduction by mammalian cells to the dithiol form, and release into the culture medium. Biochem Pharmacol. 1994 May 18;47(10):1725-30. PMID: 8204089