Cosmetic Products Contain with Arbutin: Health Benefits, Risks, Research Facts

Cosmetic products are considered as the first priority items to buy particularly for women. Who doesn’t fell for it? The products promise lots of things that women needs including whitening/brighten, tone, anti-aging, and many more. But wait, do you ever check or want to know the ingredients on the label? Well, that is what you should do from now on. Because there are numerous of beauty products contain with dangerous chemical ingredients such as mercury that can cause severe skin irritation and other health disorders. So, it’s time for you to switch into one of natural ingredients in the cosmetic products that have been proven to be safe. It is arbutin or alpha-arbutin. Here, in this article of ‘Cosmetic Products Contain with Arbutin: Health Benefits, Risks, Research Facts’, we will discuss more and deeper about the excellencies of this nature product, what scientist says, and is there any side effect or not. Check out the details below.



Cosmetic with Dangerous Ingredients Still Out of There

Have you ever heard about Minamata disease? Yes, Minamata disease was remained as important issues in the contemporary Japanese society. Minamata disease is a neurological disease that caused by high level of mercury poisoning. The severe cases was first happened in the mid of 1950s when hundreds of citizens in Minatama city showing symptoms including difficulty to speak, walking, and convulsion.

After deep investigation from scientists of Kumamoto University and British neurologist Douglas McAlpine, it found that the cause was high organic mercury poisoning. Soon known, the water waste production of Chisso Corporation, a big chemical factory in Minamata, has highly contaminated Minamata Bay with dangerous chemical and heavy metals including mercury where the victims have known to consume fish and shellfish that fished from the bay. For those reason, thousands of people reported died suffer from Minamata disease.

Looking from the disaster above, we can conclude that mercury is a chemical that highly poisoning, even lead to death. And now, can you imagine if you apply cosmetics that contain with mercury on to your skin? It is horrific, isn’t it?

In the past years, media particularly in the Asian and African region have been shaken by the discovered of hundreds cosmetic products contained with high mercury level. Mercury is one of the common ingredients found in the skin lightening creams, soaps, mascara, and eye cleansing products. It has been used because the ability to inhibit the formation of melanin in the skin that resulted in the faster lighter skin effect.

According to data of WHO (World Health Organization), although mercury is instantly made the skin brighter, the side effect are very dangerous. The use of mercury in the skin lightening creams or soaps for a long term can cause skin rashes, discoloration, scarring, and reduce resistant to bacterial and fungal infections. Other side effects are including depression, anxiety, peripheral neuropathy, kidney damage, etc.

In European and African nations, the use of mercury in cosmetic products has been banned. Yet, in the U.S and Philippines, it is allowed by limiting to less than 1 mg/kg, while in Canada is less than 3 mg/kg. Other than mercury, other materials such ashydroquinone and rhodamin are also banned as ingredients of cosmetic products.

Arbutin Come as an Alternative

Continuously, cosmetics industries fight to find the safest formulation alternative especially for their skin lightening products. More than ten years ago, DSM Nutritional Products, a Dutch based global company working in life and material sciences, first introduced alpha-arbutin to the cosmetic industry. Its unique activity is believe can promote the appearance of an even skin tone when used for cosmetic application.

So, what is arbutin? Arbutin or Hydroquinone β-D-glucopyranoside is a glucosulated hydroquinone that extracted from the bearberry plant (Arctostaphylos uva ursi), but also naturally find in the pear skins, wheat, some mushrooms, also leaves of blueberries and cranberries. Pure extract of arbutin can be produced synthetically from hydroquinone and acetobromoglucose with the presence of alkali. Historically, the extracts of arbutin have been used for a long time as a diuretic and urinary tract infection, cystitis, also kidney stones treatments as oral remedies.

Arbutin is metabolized to be converted into hydroquinone in the body and mostly excreted in urine. Hydroquinone is a phenolic agent with astringent, antimicrobial, and disinfectant properties. That’s why, topical hydroquinone is commonly used as treatment for hyperpigmentation.

Meanwhile, arbutin is a non-phenolic agent of glycolylated benzoquinone that also effective for hyperpigmentation because it’ll be converted to hydroquinone. Hydroquinone has been used as skin lightening products’ agent commercially since 1960s. Yet, some countries have been controversially banned hydroquinone uses especially above 1% in the cosmetic products.

In the cosmetic products, arbutin has the ability to inhibit the production of melanin when used as topical application with minimal systemic absorption like mercury and hydroquinone, yet of course, in the safest level. Or compared with other natural ingredients brightener such as kojic acid (derived from mushrooms) and licorice root (derived from licorice plant), they have the same the same function as tyrosinase inhibitors that provide the effects of skin lightening and brightening.

The Differences between Alpha Arbutin and Beta Arbutin

When you check on the ingredients label of your skin-lightening products, you might read that it doesn’t simply writtern by arbutin, but alpha-arbutin or beta-arbutin. But, what are the differences between them? Check the answer below.

About Beta-Arbutin

Beta-arbutin is a beta-glucopyranoside derivate of hydroquinone that found in the bark and leaves of various plants especially bearberry (uva ursi). Beta-arbutin is also often referred as arbutin itself. Although arbutin is a derivate of hydroquinone, it has been proven to be safer as skin-lightening agent.

It’s because arbutin breaks down into hydroquinone slowly compared to applying skin-lightening contain with hydroquinone. Although beta-arbutin is quite cheaper than alpha-arbutin but the skin-lightening effect is less than its counterpart. This is why many cosmetic industries prefer to use alpha-arbutin than beta-arbutin.

About Alpha-Arbutin

Alpha-arbutin is considered as the “cousin” or alpha-isomer of beta-arbutin. It’s a synthetic substance that produced by hydroquinone enzymatic glycosylation in the presence of dextrin and alpha-Amylase. Alpha-arbutin is an ingredient that pure, water-soluble and produced in a powder form.

According to some research, alpha-arbutin is a stronger (up to 10 times more effective) inhibitory than beta-arbutin. It’s due the a-glucosidic bond in the alpha-arbutin is more stable and efficient than the b-form in the beta-arbutin. The different mechanism of alpha-arbutin causes the skin-whitening to be active faster and more efficient than only existing single components.

Although alpha-arbutin is more expensive even at the very low concentration, but the power of inhibitory activity of tyrosinase make this ingredient to be more promising as skin-whitening agent. Alpha-arbutin has alpha-glycosidic configuration that won’t be expected to be a substrate for beta-glucosidases and it can prevent the hydrolysis sterically. However, when alpha-glucosidases can be found in the human skin lysosomes and fibroblasts, the release of hydroquinone can be occurred.

Health Benefits of Arbutin

Like has been mentioned briefly above, arbutin is natural ingredients that brings several health benefits including:

  1. Skin Brightening Agents

Tyrosinase is an enzyme contained in the melanocytes that contributed to the production of melanin (pigment) in skin cells. By the direct contact with UV lights, tyrosinase will be activated. If you have a long term sun exposure, you will notice sun spots and freckles on your skin start to develop.

Here, topical application of arbutin will help to inhibit tyrosinase to activate, so the production of melanin will be decreased and resulted in brighter skin. Especially alpha-arbutin, it has stronger skin-brightening ability than beta-arbutin. This inhibitory activity of arbutin is due to the similar structural of hydroquinone group of tyrosine, the natural substrate of tyrosinase.

In addition, since arbutin is gentler than other skin-brightening ingredients, so the side effects are fewer. The active component of arbutin is acted as reservoir that released hydroquinone slowly. When arbutin absorbed into the skin, the enzymes in the body will split the sugar group from arbutin and release hydroquinone.

It can work like built-in safety valve that preventing from hydroquinone exposure at once in the skin, so the irritation side effect is less than other agents. Moreover, it works for all skin colors, so it’s like a miracle especially for those with sensitive skin conditions.

  1. Promote Urinary System Health

Uva ursi or bearberry, the plant from arbutin is extracted, has medical properties as oral medication. The glucoside arbutin compound in the plant also helps to promote diuretic action. Arbutin is mostly absorbed unchanged and excreted by kidneys. During this excretion process, arbutin works as antiseptic on urinary mucous membrane.

As the main active compound in Uva ursi, arbutin, a derivate of hydroquinone, is absorbed and converted into a substance that has astringent, antimicrobial, and disinfectant properties. Although arbutin can work effective alone, but as the main active compound, it plays the big role.

Uva ursi has the ability to reduce bad bacteria in the urine. When the bacteria have been reduced, it can reduce inflammation (swelling) and astringent (drying) effect on the tissues. These medical properties make uva ursi can treat urinary tract disorders, including kidney, bladder, and urethra infections, urinary tract inflammation, increased and painful urination, and urine that contains with excess urine acid or others. Constipation and bronchitis also can be treated with this plant.

Read More:  The Role of Folic Acid in The Life

Uva ursi is safe for the consumers through oral administration or when consumed by mouth in short term (up to one month). The possible side effects can cause to nausea, stomach discomfort, vomiting, and greenish-brown discoloration of urine. Meanwhile, it can be possibly unsafe when consumed in high doses for a long term. The worse side effects can cause liver damage, breathing and eye problems, convulsions, even the worst is death. Children and women who pregnant and breast-feeding are strictly avoid consuming this oral remedy.

  1. Anticancer Agent

In the study titled “Proteomics analysis of A375 human malignant melanoma cells in response to arbutin treatment,” that investigated anticancer effect of arbutin showed a good result. By using 8 microg/ml of arbutin for 24, 48, and 72 hours treatment on protein expression profile in A375 cells outlined that there was an interaction of protein correlated with the downstream regulation of tumor suppressor and cell apoptosis. It found 3 up-regulated and 5 down-regulated proteins in the cells that treated by arbutin. They were the proteins that play important roles in the suppression development of the cancer.

Read more: Cryotherapy Skin Benefits and All Facts You Must Know

Is There Any Possible Risks?

The German Federal Institute for Risk Assessment (BfR) revealed in their assessment that skin-lightening product use beta-arbutin has posed health risk. The reason is because the application of arbutin on to skin will be metabolized later in the body and converted to D-glucose and hydroquinone. Hydroquinone is suspected as a carcinogenic substance for human that can cause the risk of cancer. But, is it true?

As mainly turn into a big concern for safety use, hydroquinone has been banned by U.S Food and Drug Association (FDA) and European Union Cosmetic Regulation. In the 1982, skin bleaching drug products contain with 1.5 to 2% of hydroquinone is still categorized as generally recognized as safe and effective (GRASE).

Yet, from the later study in 2006 indicated that hydroquinone may act as carcinogen or cancer-causing agent after so many concern appeared. It was because the topical hydroquinone known to cause some medical disease including skin darkening and disfiguration called as ochronosis.

Furthermore, FDA conducted a new study under National Toxicology Program (NTP) to learn more about hydroquinone side effects. Yet, the following studies were done under oral administration on rats, not topical application. Since the concerns of hydroquinone only based on oral ingestion, FDA come into conclusion that hydroquinone can’t be rule out as potential carcinogen over topical application.

If the products are using the standard rule of hydroquinone concentration and directed under supervision of licensed physician, then topical toxicity and carcinogenesis of hydroquinone can’t be validated. Moreover, there have been no cancer cases reports regarding topical application of skin products contain with hydroquinone.

That’s why, tyrosinase inhibitors such as arbutin (from the leaves of bearberry) is better tolerated cosmetic product ingredients than hydroquinone. Hydroquinone may has proven to be the cause of some skin problems especially ochronosis, but it doesn’t apply the same for arbutin. Although it’s true that arbutin will be converted to hydroquinone in the skin, but the process is slower than direct application of skin-whitening contain with hydroquinone. Since arbutin is extracted from natural products, so the possible side effects are fewer than hydroquinone in the similar concentration, presumably due to more the gradual release.

How Scientists Prove that Arbutin is Safe?

Mostly, the concerns about arbutin are due to the facts that it hydrolyses to hydroquinone, the suspected toxic skin-whitening agents. As these concerns become such a hot debate in the cosmetic industries, research about health benefits and risks start to be conducted from various sources, like in the following studies:

  1. Scientific Committee on Consumer Safety (SCSS)

Arbutin has become the hot topic of safety discussion in European Union. In the Annex II/1339 of the Cosmetic Regulation No 1223/2009, it has banned the use of hydroquinone for skin whitening products except for one strictly permitted use in artificial nail systems in the final product up to 0.02%. Meanwhile, beta-arbutin is suspected to be the potential of hydroquinone production.

DSM Personal Care, the first promoter of arbutin, is trying to prove that arbutin is safe for cosmetic use by providing the extensive safety dossier. Then, Scientific Committee on Consumer Safety (SCSS) processed the document and did the deeper toxicity research. In May 2015, SCSS officially released their opinion about arbutin that contain with:

  1. The use of alpha-arbutin is SAFE for cosmetic products in a concentration up 2% for face creams and up to 0.05% for body lotion.

In the studies of local toxicity with human volunteers, they use the topical application of cosmetic formulation contain with 1% alpha-arbutin for 30 days or 12 weeks. The studies showed that the products were well-tolerated and no adverse reactions observed.

  1. The use of beta-arbutin is SAFE for cosmetic products in a concentration up to 7% for face creams. In the condition that the contamination of hydroquinone is remain below 1 ppm in the cosmetic formulations.

The studies used a single patch test on human volunteers with 10% beta-arbutin in water and 7 and 10% in cosmetic formulation. The repeated application tests were also done with 10% beta-arbutin in the cosmetic formulation with and without sunlight exposure. All the tests revealed to be non-irritating, well-tolerated by the voluntees and showed no adverse reactions.

  1. Scientific Publication by FDA Staff

In September 2015, FDA released a study research with the title is “Comparative studies on the chemical and enzymatic stability of alpha and beta arbutin.” The study was aimed to establish comparative analysis of chemical and enzymatic stability between alpha-arbutin and beta-arbutin, as the potential source of hydroquinone. The study analyzed various cosmetics formulations including creams, gels, lotions, and sera for the arbutin and hydroquinone content with an array of techniques including HPLC-PDA, optical rotation, and nuclear magnetic resonance.

The study results showed that both arbutins possess similar stability profiles. They were more prone to in vivo rather than in chemico degradation. There was no hydroquinone found after enzymatic hydrolysis and no epimerization in any tested conditions. It showed the potential use of optical rotation (OR) and nuclear magnetic resonance (NMR) along with more established HPLC methods, works as complementary investigate tools for the stability and safety assessment of arbutin.

  1. Study released in the Biological & Pharmaceutical Bulletin

In the study titled ‘Inhibitory effects of alpha-arbutin on melanin synthesis in cultured human melanoma cells and a three-dimensional human skin mode,’ also indicate that alpha-arbutin is safe and effective for skin-lightening ingredients. From the study resulted:

– At a concentration below 1.0 mM of alpha-arbutin showed no inhibitory effect on HMV-II cell growth.

– At a concentration 0.5 mM of alpha-arbutin treated melanin synthetis in cells decreased to 76% in non-treated cells. The cellular tyrosinance activity of HMV-II cells is also significantly decreased.

– The use of 250 microgram of alpha-arbutin as human skin model treatment didn’t inhibit cell viability, while melanin synthesis was reduced to 40%.

  1. Article Published in Journal of Cosmetic Science

In 2005, some researchers from Department of Chemistry, University of Cincinnati released an article titled “Comparative efficacy and safety of deoxyarbutin, a new tyrosinase-inhibiting agent.” In the article provide the evidence that arbutin (deoxyarbutin/dA) is less cytotoxicity than standard skin-whitening ingredients in the market such as hydroquinone. Compared to hydroquinone, cytotoxicity of dA didn’t associate with high degenerative changes in the keratinocytes morphology. It resulted in the conclusion that dA is potentially safer and more effective as depigmenting agent and the alternative of hydroquinone.

Because there is no recent health disorder case reports for the topical application of skin whitening products contain with arbutin and proven to be safe by several researches, there is no countries that specifically banned the use of arbutin. Recently, only the use of hydroquinone strictly limited by some countries especially U.S and European Union.

Now, It’s Time to be a Smart Consumer

In summary, we can conclude that the use of arbutin is actually safe when it’s used in a safer concentration for cosmetics products under legal production standard. When it’s beyond the concentration, you should start to worry. That’s why, you, as a customer who are going to buy and use cosmetic product should be very careful. Always look at the label of ingredients, avoid when you see no label, do not buy when you see the concentration of arbutin, hydroquinone, even mercury is higher than legally state laws recommended.

There is no amazing things come in an instant. Something instants tend to result with no good end. This is also applied for beauty care, whitening skin, or such as. Everything needs time and effort. After reading about arbutin health benefits, risk, and research facts, now you should be able to take more consideration before choosing your skin lightening products, don’t you? Be a smart cosmetic products’ consumer.


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