Alpha Arbutin: Helpful Guide for Skin Brightening

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Have you always wondered why your face and hands are much pigmented and darker than the rest of your body? It is due to increased melanin production in your skin due to sun damage, acne or burns/injuries. This leads to hyperpigmentation and you get uneven skin tone that does not match the natural tone of your skin. Do you want to have the same natural skin tone on your face, neck and hands? Meet Alpha Arbutin.

Quick Glance

Type of Ingredient: Skin Brightener (Tyrosinase Inhibitor), Antioxidant, Anti-inflammatory (good for acne)

Benefits: Brightens dark spots and scars, prevents further dark spots, evens out skin tone and complexion

Skin Type: Good for all Skin Types

Frequency of Use: Daily, twice a day on cleansed and dry skin after cleansing/exfoliation.

Recommended to use with: Vitamin C, Niacinamide or AHAs/BHAs

What is alpha-arbutin

Alpha Arbutin (a.k.a Hydroquinone β-D-glucopyranoside) is a naturally derived antioxidant that comes from bearberries. Alpha Arbutin is a derivative of Hydroquinone. It is an effective and safe ingredient in the treatment of post-inflammatory hyperpigmentation of the skin.

What is alpha arbutin for skin

Melanin, Tyrosinase, Melanocytes and melanogenesis in a visual diagram

Alpha Arbutin is an anti-inflammatory, antioxidant tyrosinase inhibitor (controls melanin production) that is considered a safe and effective ingredient for treating hyperpigmentation. It is a skin brightener as it reduces the melanin formation in your skin which in turn improves the appearance of spots, freckles, melasma and post-inflammatory hyperpigmentation.[source]

 

Alpha Arbutin is a derivative of Hydroquinone.  Alpha Arbutin is not as effective as Hydroquinone but it is still very effective in treating hyperpigmentation. Unlike Hydroquinone, Alpha Arbutin is not toxic to our skin cells and does not have any side effects or irritation. Less irritation and less inflammation of the skin keeps your melanocytes calm and happy. 

 

Alpha-Arbutin’s parents (the infamous Hydroquinone) have had a very bad reputation. So before we introduce you more to the gentle Alpha Arbutin, let us tell your first about his bad infamous parent - the Hydroquinone.

What is Hydroquinone

Alpha Arbutin versus Hydroquinone - The Good and the Bad Graphic

Hydroquinone is the “gold standard” in fighting Hyperpigmentation because it is the most studied and most potent anti-pigmentation ingredient that we have. However, it comes with a lot of side-effects

 

The biggest problem with Hydroquinone is “rebound hyperpigmentation” which means the hyperpigmentation seems to go away when you are treated with Hydroquinone, but comes back worse within a few months. HQ is toxic to skin cells (Cytotoxic) and it is banned almost everywhere around the world; including Australia, the UK, the EU, Asia. HQ is available in the USA over-the-counter at 2%.

 

Side-effects of Hydroquinone are:

  • Irritant Contact Dermatitis
  • Allergic Contact Dermatitis
  • Postinflammatory Hyperpigmentation
  • Exogenous Ochronosis (blue-black pigmentation)
  • Leukoderma (white patches)

How Alpha Arbutin Works

When applied topically on the skin, Alpha Arbutin slowly metabolizes in our skin. This slow breakdown of alpha arbutin in our skin is a key factor that makes it less irritating and very safe from the side effects that Hydroquinone poses.

Melanin, Tyrosinase, Melanocytes and melanogenesis in a visual diagram

Tyrosinase is an enzyme that tells melanocytes to produce melanin. Melanin is what gives us color. When melanin is overproduced, we see pigmentation on our skin. The solution is to control the rate of melanogenesis (production of melanin). Alpha Arbutin works as a tyrosinase inhibitor. It slows down the maturation of the melanosome (the carrier of melanin from melanocytes to keratinocytes - the skin cells).

 

Since Alpha Arbutin is also an antioxidant, it also prevents free radicals (the oxygen species on skin that come from pollution and UV radiation) which can trigger melanocytes and cause hyperpigmentation - making it the perfect treatment for fighting hyperpigmentation. 

What does alpha arbutin do to skin

When you apply Alpha Arbutin on your skin,our skin converts it into Glucose and Hydroquinone - a form that is not so strong and irritating like the synthetic hydroquinone. Alpha Arbutin works with your skin - it literally has to slowly break it down into Glucose and Hydroquinone. When you apply Alpha Arbutin on your skin, it goes through this process throughout the day. Tyrosinase is the enzyme that tells the melanocytes (packets in the skin that hold melanin) to produce melanin. What Alpha Arbutin does is it inhibits tyrosinase - stopping it from triggering the melanocytes which controls and prevents hyperpigmentation on your skin

When and How to use alpha arbutin

Alpha Arbutin can be applied twice a day; at night as well as in the morning (AM and PM) because it is not photosensitive like Hydroquinone. It is recommended to be applied twice a day to keep the function of tyrosinase inhibition active in the skin and all the studies relating to Alpha Arbutin also suggest the use twice a day.

 

The Alpha Arbutin comes in the treatment stage of your skincare routine so first cleanse, then hydrate using a toner or cleansing water. Next you can exfoliate, and then finally apply Alpha Arbutin serum followed by your other serums and finally apply a moisturizer. If you are using Alpha Arbutin at AM, make sure you apply a broad-spectrum Sunscreen in the end.

 

  1. Cleanse
  2. Tone
  3. Exfoliate (you can use AHA/BHA with Alpha Arbutin)
  4. Serums (Alpha Arbutin is applied now + any other serums you may be using. Use Alpha Arbutin as your first serum for maximum absorption)
  5. Moisturizer
  6. Sunscreen (in the morning)

 

Take 2-3 drops of Alpha arbutin serum in your palm, rub gently, and gently pat on your face.

 

If you feel your skin texture as tacky and sticky, this is an indication that you have used too much of the product. If your skin is flaking, that’s not actually your skin but it's actually the dried out products that you have applied on your face. This is also a good indication that you are using too much than your skin can absorb into the pores.

Mixing Alpha Arbutin with Other Actives

You can use Alpha Arbutin and any active ingredient or exfoliant in the same routine without any side effects.

Alpha arbutin vs niacinamide

There is no comparison to say which one is better since they both help in treating hyperpigmentation and dark spots in different ways and both are recommended to be used in your skincare routine to treat hyperpigmentation. 

Alpha Arbutin prevents production of melanin while Niacinamide prevents the already produced melanin from reaching the surface of your skin. 

 

Niacinamide prevents melanosomes (packets of melanin) from reaching the keratinocyte cells (cells in the top layer of skin - epidermis). This means the melanin is prevented from reaching the surface of your skin so you don’t see the hyperpigmentation on your face.

 

Alpha Arbutin is a tyrosinase inhibitor. It stops the tyrosinase enzyme from triggering melanocytes to produce melanin.

Alpha Arbutin + Vitamin C

You can use Alpha Arbutin serum with Vitamin C. It is a great combination and recommended to be used in your skincare regimen as both are antioxidants and complimenting the benefits of Vitamin C as a skin brightening agent can add to the overall goal of treating hyperpigmentation. 

 

Both work slightly differently. Alpha Arbutin is a slow release so it works throughout the day, while Vitamin C starts working the moment you apply it to your skin. 

 

If you are using a The Ordinary Vitamin C suspension, use it AFTER Alpha Arbutin serum. 

Why alpha arbutin turns yellow

Alpha Arbutin serums can turn yellow to brown with time. However, it does not degrade the quality or effectiveness of the product with the change in color. Alpha Arbutin is extremely sensitive to degrading in the presence of water as it is water soluble.

How long does alpha arbutin take to work

Alpha Arbutin is dose-dependent. Most of the studies show that Alpha Arbutin is most effective at 2.5% to 3% and a pH of about 4.9. A study conducted within the 12 weeks of using Deoxyarbutin showed “a significant or slight reduction in overall skin lightness and improvement of solar lentigines in a population of light skin or dark skin individuals, respectively”.

 

Alpha Arbutin is definitely going to even out your skin tone over time as it slowly starts to control the rate of melanin production so you should not expect the results from Day 1. It would take about 6 to 12 weeks to see the results as the skin naturally turns over in 30 days, the pigment will be removed from the skin and because you were using Alpha Arbutin all this while, the melanin on the surface of your skin won’t be replaced with the same amount as before. So overtime you will see that brightening and even tone on your face.

What happens if you stop using Alpha Arbutin

There is no study till date that confirms the length of effectiveness of prolonged use of Alpha Arbutin in tyrosinase inhibition so it is not yet clear that if you are using alpha arbutin for 6 months, you see results and then you stop using it, will it continue to inhibit tyrosinase for an n number of months or not.

The ideal solution to this question would be use a product that contains Alpha Arbutin in a moisturizer or in your cleanser; so you always keep getting the tyrosinase inhibition and avoid any hyperpigmentation from occurring due to sun damage or acne.

Fun Fact

Mainly derived from bearberries, Alpha Arbutin can also be derived from blueberries, cranberries, pear or from wheat.

Top 10 Alpha Arbutin Products

  1. The Ordinary Alpha Arbutin 2% + HA ($11 | 30ml)

The Ordinary Alpha Arbutin 2% with Hylaronic Acid

This is a great formulation at 2% Alpha Arbutin with Hyaluronic Acid. The purpose of HA here is to act as a penetration enhancer to assist in topically delivering the Alpha arbutin more effectively into the deeper layers of your skin.

  1. The Ordinary Ascorbic Acid 8% Alpha Arbutin 2% ($10 | 30ml)

Alpha Arbutin 2% and Vitamin C 8%

This is a great combination of 2 different antioxidants that will make sure your skin is free from free radicals, along with added benefits of skin brightening.

  1. The Inkey List Alpha Arbutin ($12 | 30ml)

The Inkey List Alpha Arbutin for dark spots and pigmentation

If you don’t like the sticky feeling of The Ordinary Alpha Arbutin, you will like The Inkey List as an alternative.

  1. Sunday Riley’s Tidal Brightening Enzyme Water Cream ($22 | 15g)

Brightening Cream

If you are not looking for Alpha Arbutin all by itself in a serum, and want a more comprehensive formulation to target your dark spots while hydrating your skin, then this formulation of moisturizer by Sunday Riley is amazing - especially for pigmented and dry skin. It has Hyaluronic Acid, Alpha Arbutin, Tamarind Seed Extract (for hydration), Papain (for exfoliation of top layer of skin) and Horse Chestnut Seed Extract (for even tone).

Recommended Videos on Alpha Arbutin

Citations

  1. The Use of Botanical Extracts as Topical Skin-Lightening Agents for the Improvement of Skin Pigmentation Disorders
  2. The unravelling of the complex pattern of tyrosinase inhibition
  3. Mechanisms Regulating Skin Pigmentation: The Rise and Fall of Complexion Coloration
  4. Opinion on α-Arbutin: SCCS, European Commission
  5. Cosmeceuticals for Hyperpigmentation: What is Available?
  6. Inhibitory effects of arbutin on melanin biosynthesis of α-melanocyte stimulating hormone-induced hyperpigmentation in cultured brownish guinea pig skin tissues
  7. Anti-inflammatory effects of arbutin in lipopolysaccharide-stimulated BV2 microglial cells
  8. Effects of hydroquinone and its glucoside derivatives on melanogenesis and antioxidation: Biosafety as skin whitening agents
  9. Hydroquinones cause specific mutations and lead to cellular transformation and in vivo tumorigenesis
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