Alpha Arbutin and Beta Arbutin in Skin Care Products

The two types of arbutin, alpha arbutin and beta arbutin, are cosmeceutical ingredients in skin care products that are tyrosinase inhibitors used to treat hyperpigmentation. Arbutin serums and arbutin creams are popular skin care products used to lighten dark spots on the skin, especially when using hydroquinone is undesirable. Compounding pharmacies may make a skin lightening product that has hydroquinone and arbutin together, but you will no longer see hydroquinone available without a prescription.

Arbutin is one of the most commonly used skin care ingredients to lighten skin that is available over the counter without a prescription.

There are two forms of arbutin found in skincare. They have the same chemical structure but different rotational configurations which gives them slightly different effects on melanin production.

1. Alpha arbutin (4-hydroxyphenyl alpha-glucopyranoside)-  
2. Does not occur naturally so will not be found in natural or organic skin care products
3. Is synthetic
4. Is a stronger tyrosinase blocker than the beta arbutin form
5. Studies have demonstrated that synthetic α-arbutin is 10 times more effective than natural arbutin.[6]
6. Beta arbutin (4-hydroxyphenyl beta-glucopyranoside)-  
7. Occurs naturally in plants.
8. Found in the dry leaves of bearberry, cranberry, blueberry, wheat, and other plants.[1],[2]
9. This is the form used in natural and organic skin care creams and serum.

Arbutin is primarily used for depigmenting, or skin lightening, but also can serve as a protective agent against the sun.

Arbutin is structurally very similar to hydroquinone

Arbutin is hydroquinone bound to a sugar molecule

Both hydroquinone and both forms of arbutin block tyrosinase activity which leads to less production of skin pigment.

If you are allergic to hydroquinone, you may also be allergic to arbutin but it is less likely

Arbutin has less melanocytotoxicity than hydroquinone and less skin irritation.

Arbutin does not cause ochronosis like hydroquinone can

Arbutin has antioxidant, anti-inflammatory, and skin lightening properties.[3],[4] While naturally occurring beta arbutin has garnered attention in the cosmetic and therapeutic realms as an alternative to HQ, evidence suggests that a synthetic version of the botanical agent called alpha arbutin is even more effective.

Its anti-inflammatory, antioxidant, and, in particular, anti-tyrosinase properties make it useful in skincare regimens designed to lighten skin. This is because inflammation can lead to hyperpigmentation so soothing the skin helps prevent dark spots on the skin.

Both forms of arbutin are used to treat hyperpigmentation skin problems such as:

• Melasma
• Postinflammatory hyperpigmentation (PIH)

Arbutin is thought to be a safe alternative to HQ according to the US FDA. It is allowed in cosmetic products while hydroquinone is not. However, it has been banned for safety reasons in European Union, Japan, Australia, and some African countries due to its similarity in chemical structure to hydroquinone. If you have an allergy to hydroquinone, you should avoid arbutin.

Side effects of arbutin include stinging and allergic dermatitis. The Environmental Working Group (EWG) gives arbutin a 1 rating (safe).

Arbutin is a glycosylated hydroquinone derivative. Unlike hydroquinone, which is a potent depigmenting agent with higher risks, arbutin releases hydroquinone slowly and in much smaller amounts, reducing potential toxicity. When applied topically, arbutin has low systemic absorption, meaning it does not significantly enter the bloodstream and therefore poses minimal risk to the fetus. There are no known studies indicating teratogenic (birth defect-causing) effects of arbutin when used topically. Its safety profile is generally considered acceptable, especially in comparison to other more aggressive skin-lightening agents.

DRPT, DRPW, DSPT, DSPW, ORPT, ORPW, OSPT, OSPW

Although it is much better to shop by your Baumann Skin Type, you can find the best arbutin serums and creams here.

Find the best products with arbutin such as Arbutin serums and creams

The source of arbutin in skin care differs. Alpha arbutin is made in the laboratory. Beta arbutin is primarily extracted from the bearberry plant (Arctostaphylos uva-ursi) but is also found in blueberry, cranberry, wheat, and other plants. Other arbutin derivatives, such as deoxyarbutin, are synthesized by chemical and enzymatic methods.[5]

Arbutin is structurally very similar to hydroquinone. They both have benzene rings.

Arbutin is hydroquinone bound to a sugar molecule

Arbutin is either one of these:

• α--D glucopyranoside
• β-D glucopyranoside

It is not well established what impact the cultivation of arbutin sources has on the environment. Similarly, it is not yet known how the culling of plants containing arbutin for the processing of synthetic forms of the ingredient affects the environment. There are no known environmental concerns.

Skin penetration is an issue with many ingredients including arbutin. Various methods have been used to enhance skin penetration.[7]

The hydrophilic nature of arbutin limits penetration into human skin. Arbutin should be used with penetration enhancing ingredients when possible such as hyaluronic acid and oleic acid. When designing a skin care routine, care should be taken to design the order of steps in the routine to increase absorption of arbutin. Saturated fatty acids in moisturizers may decrease effectiveness of arbutin, so look for moisturizers with unsaturated fatty acids like linoleic acid.

Several clinical studies have indicated that arbutin used in combination with another depigmenting agent or therapy to treat melasma or other skin hyperpigmentation conditions is as effective as monotherapy while less likely to induce side effects.[8]

In other words: arbutin works bets when combined with other skin lightening and whitening ingredients.

Used traditionally in Japan, arbutin is one of the best skin whitening ingredients in the Unites States. It is less effective than hydroquinone but safer than HQ. Synthetic versions of arbutin compare with HQ in effectiveness, but natural arbutin is also effective especially when combined with other tyrosinase inhibitors. Arbutin is found in many skin care products to treat melasma, skin aging, and to protect the skin from the damage from sun exposure.

Is Arbutin right for you? You need to take the skin care quiz to find out.

[1] Sheth VM, Pandya AG. Melasma. A comprehensive update Part II. J Am Acad Dermatol. 65: 699, 2011.

[2] Draelos ZD. Skin lightening preparations and the hydroquinone controversy. Dermatol Ther. 20:308, 2007.

[3] Bauman L. Chapter 35, Arbutin. Cosmeceuticals and Cosmetic Ingredients. McGraw Hill 2014.

[4] Baumann L. Chapter 41, Depigmenting Ingredients. Baumann’s Cosmetic Dermatology. McGraw Hill, 2022.

[5] Seo DH, Jung JH, Lee JE, et al. Biotechnological production of arbutins (α- and β-arbutins), skin-lightening agents, and their derivatives. Appl Microbiol Biotechnol. 95:1417, 2012.

[6] Saeedi M, Khezri K, Seyed Zakaryaei A, Mohammadamini H. A comprehensive review of the therapeutic potential of α-arbutin. Phytother Res. 2021 Aug;35(8):4136-4154.

[7] Wiechers JW, Kelly CL, Blease TG, et al. Formulating for efficacy. Int J Cosmet Sci. 26:173, 2004.

[8] Saeedi M, Khezri K, Seyed Zakaryaei A, Mohammadamini H. A comprehensive review of the therapeutic potential of α-arbutin. Phytother Res. 2021 Aug;35(8):4136-4154.