Skin bleaching ingredients, Arbutin and ɑ-Arbutin, and their restrictions in cosmetic products - new amendment to EU Regulation 1223/2009
Arbutin and ɑ-Arbutin - their use in skincare and recent amendment to EU Regulation 1223/2009
On 4 April 2024, the Official Journal of the European Union published a new amendment to the Regulation (EC) No 1223/200 addressing the use of Arbutin and ɑ-Arbutin in cosmetic products.
As usual, this amendment was preceded by an analysis provided by the Scientific Committee on Consumer Safety (SCCS), which shed more light on the safety of these two ingredients.
But let's start with a brief explanation what exactly are Arbutin and ɑ-Arbutin and why they are used in skincare.
What should every cosmetic chemist and formulator know about Arbutin and ɑ-Arbutin?
Both are glucopyranoside derivatives of hydroquinone and they differ only in the way the glucopyranose* ring is attached. Arbutin, aka β-Arbutin, contains bond formed by β-glucopyranose, while in ɑ-Arbutin, the connection includes the other stereoisomer - ɑ-glucopyranose.
*BTW, glucopyranose is just glucose existing in a closed, ring structure.
Only Arbutin has natural origin and can be found in leaves and barks of many plants (that's actually not a big surprise, since nature always promotes the synthesis of only one type of stereoisomer).
On the contrary, ɑ-Arbutin can only be produced in lab environment by enzymatic glycosylation of hydroquinone.
How do Arbutin and ɑ-Arbutin act on skin?
Both are considered skin bleaching agents and are able to block synthesis of skin pigment - melanin.
About melanin biosynthesis - this process has multiple steps but everything starts from the reaction between tyrosine and skin enzyme - tyrosinase.
Since Arbutin shares some structural similarities with tyrosine, it may compete over the binding to enzyme. Moreover, Arbutin can be easily hydrolyzed to glucose and hydroquinone and yesssss, hydroquinone is another “tyrosine-competitor” and skin bleaching agent.
And what about synthetic ɑ-Arbutin?
Well, it is also able to compete with tyrosine and act as an enzyme inhibitor. However, because the structure of ɑ-Arbutin includes α-glycosidic configuration, it is not that prone to be hydrolyzed. In this case, only α-glucosidases found in human skin fibroblasts may enable such a reaction.
The use of Arbutin and ɑ-Arbutin in cosmetic formulas
Ok, so now when the “nerdy” part of this post is done, we can move on to the more practical aspects.
Both isomers are used in skincare and both for the same reason - to achieve the skin bleaching effect.
As the SCCS mentioned in its final opinion, the concentration of Arbutin in face creams and lotions is usually up to 7%. Whereas, ɑ-Arbutin is often applied up to 2% in face/neck care products and up to 0.5% in body lotions.
What are the main concerns about Arbutin and ɑ-Arbutin?
Actually, these concerns do not relate to Arbutin and ɑ-Arbutin themselves, but to their metabolite - hydroquinone.
Hydroquinone has many properties. I already mentioned that it works as a tyrosinase inhibitor. But due to its structure, hydroquinone is actually a powerful antioxidant and electron donor. That is why it is often used as a liquid component in the artificial nail systems, because it allows the polymerization of the methacrylate monomers to be completed.
However, this does not change the fact that safety of hydroquinone is quite debatable. As reported in Cosmetic Ingredients Review, hydroquinone can be rapidly absorbed through the skin from any aqueous solutions, and once metabolized, its derivatives are believed to have nephrotoxic and immunotoxic properties.
That is why hydroquinone has been listed in entry 1339 of Annex II to the Cosmetic Regulation, and has been banned as a cosmetic ingredient. There is only one exception (entry 14 in Annex III) - hydroquinone is allowed to be used in professional artificial nail systems with a maximum concentration up to 0.02% in the finished formula.
But moving back to Arbutin and ɑ-Arbutin - their ability to release hydroquinone raised a lot of understandable concerns and that was the main reason why SCCS and EU Commission decided to take a closer look at those two ingredients.
Arbutin and ɑ-Arbutin - what was the final SCCS`s conclusion and what are the new EU restrictions?
✅ Based on the opinion of SCCS from 31 January 2023, the European Commission decided to limit the use of Arbutin and ɑ-Arbutin in cosmetic products by introducing the following restrictions:
➡️ ɑ-Arbutin can be used in face creams at maximum concentration of 2% and in body lotions up to concentration of 0.5%.
➡️ Whereas for Arbutin the maximum level equals 7% in face cream products.
➡️ Combined exposure of Arbutin and ɑ-Arbutin was also found to be safe for consumers.
➡️ Last but not least, it has been emphasized that presence of Hydroquinone in any formula containing Arbutin and/or ɑ-Arbutin should remain as low as possible and not higher than unavoidable trace levels.
Based on that, Annex III of Regulation 1223/2009 has been extended to include now Arbutin and ɑ-Arbutin.
What are the deadlines?
🗓️ 1 February 2025 - since this day, any cosmetic products that contain Arbutin and ɑ-Arbutin and are not complying with following restrictions shall not be placed on the EU market.
🗓️ 1 November 2025 - from this day, any cosmetic products that includes Arbutin and ɑ-Arbutin and is not compliant with following restrictions shall not be made available for EU consumers.
Does your product contain Arbutin or ɑ-Arbutin? Maybe you are planning to work with these ingredients?
Contact me if you have any questions or doubts.
*Reference
SCCS (Scientific Committee on Consumer Safety), Opinion on the safety of alpha- (CAS No. 84380-018, EC No. 617-561-8) and beta-arbutin (CAS No. 497-76-7, EC No. 207-8503) in cosmetic products, preliminary version of 15-16 March 2022, final version of 31 January 2023, SCCS/1642/22
Amended Safety Assessment of Hydroquinone as Used in Cosmetics - Cosmetic Ingredient Review, June 23, 2014
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