Updated: May 7, 2020
As an aesthetician, I come across a lot of cases where people are trying to improve their hyperpigmentation. Approximately 15% of the world’s population is investing in skin whitening agents, mostly Asia, and the global market is expected to be worth $23 billion by next year. Age spots, freckles, sun damage and post-inflammatory scarring is a common situation that happens to every one of us. UV exposure, drugs and hormones are known to be the main cause, but hormones and skin trauma can also play a part in the overproduction of melanin.
What is melanin?
Melanin is responsible for the pigment in human skin and eyes and is produced by something called melanocytes during a sophisticated set of chain reactions known as melanogenesis. Tyrosinase plays a crucial part in the creation of melanin and this is why it is a main target when treating skin pigmentation.
What are tyrosinase inhibitors?
Tyrosinase inhibitors slow down the process of melanogenesis and are not only used in cosmetic manufacturing but also found in the food and agriculture industry, to stop the browning of compounds and prevent disease that is caused by the production of melanin.
If you are trying to treat melasma, sun damage, age spots or post-inflammatory pigmentation then scroll down to see the most popular and best ingredients to treat these conditions, the risks and which treatment will be better suited to you.
Also known as tocopheryl acetate this ingredient has been used in the medical industry for over 50 years for treating pigmentation and is the only FDA-approved product for skin bleaching. This tyrosinase inhibitor is made from crude oil and is available on prescription in many countries worldwide – banned in some. It is often combined with tretinoin, a retinoid that encourages skin shedding and boosts the skin’s renewal process.
For many dermatologist’s hydroquinone is the front runner for treating hyperpigmentation despite the stigma that is attached to using it. Some studies suggest that hydroquinone can lead to cancer risk and toxicity to the organs and respiratory tract, and the ingredient has also been associated with the skin disorder ochronosis.
Common side effects like redness, itching, extreme dryness and flaking of the skin is a frequent occurrence after using this ingredient, particularly in the first 2-6 weeks.
Day 17 of a nuderm journey via thina77
Hydroquinone is an aggressive approach to treating skin hyperpigmentation and because of this, skin pigmentation can have a bounce-back effect after a course of using it, particularly in darker skin types. For this reason, nature-derived acids and skincare have been more favoured in recent years for treating uneven skin tone, those of which I will be mentioning in this post.
PROS: The only FDA-approved whitening skincare ingredient, considered the gold standard treatment for improving severe cases hyperpigmentation
CONS: Aggressive downtime, medical advice is needed, risk of pigmentation ‘bouncing back’
How long does it take to see a result? Usually within 2-4 weeks of using hydroquinone you can see a universal brightening of the skin and some improvement in hyperpigmentation. The course time can vary from patient to patient, depending on the severity of pigmentation being treated, usually a course is not prescribed for anything longer than 5 months.
Obagi Nuderm 12-week transformation using hydroquinone via obagi.com
Arbutin is often noted as the ‘cousin’ of hydroquinone and a common alternative. There are two types; alpha arbutin and beta arbutin – alpha arbutin is thought to be a more stable and effective product.
This is a biosynthetic ingredient, derives from bearberry leaves and works by breaking down into hydroquinone when applied to the skin.
This ingredient is commonly paired with other tyrosinase inhibiting ingredients like kojic acid, vitamin C and niacinamide. It is certainly gentler on the skin than hydroquinone however users can often experience irritation and a tingling feeling when they first start using it.
As well as treating hyperpigmentation, alpha arbutin has been known to contain anti-cancer properties.
PROS: Less toxic than hydroquinone, can be combined with other tyrosinase inhibitors for maximum results
CONS: May cause skin irritation that can develop into acne
How long does it take to see a result? 2-3 months
Alongside hydroquinone, kojic acid is one the most-studied tyrosinase inhibiting ingredients for treating hyperpigmentation. It is developed in a lab using strains of the Aspergillus fungi, it is anti-microbial and anti-fungal and perfect for treating athlete’s foot, ringworm and cases of acne.
However, this particular ingredient is known to be highly irritating on the skin – dermatitis is a common side effect. One medical study has shown how when kojic acid is applied in high concentrations on mice, it can cause tumours to develop. Due to its low absorption rate in humans, there is a small chance this can happen to us, however like many cosmetic ingredients and supplements on the market today, there simply isn’t enough evidence to know for sure what the risk is.
With that being said, kojic acid has been proven over and over again to be a successful ingredient of treating hyperpigmentation. Its derivatives play an antioxidant and anti-inflammatory role on the skin, has antiviral, antiparasitic and pesticidal properties.
Pros: Is great for treating acne as well as hyperpigmentation, a well-studied ingredient
Cons: A high chance of developing skin irritation following use
How long will it take to see a result? 6-12 weeks
This skin-lightening ingredient is naturally found in grains, barley, wheat and rye and is considered a safe and effective ingredient for treating hyperpigmentation. This superior treatment has been shown to be more effective than hydroquinone is some studies due to its toxic effect on melanocytes.
Azelaic acid is comedolytic and has been used a prescriptive product to treat acne for a number of years. It is the ultimate multi-tasking ingredient; as well as treating pigmentation and acne, the ingredient has been shown to improve cases of rosacea and boost cell renewal. Azelaic acid also works well in combination with niacinamide.
Although azelaic acid is a blockbuster ingredient in high street skincare, there has been limited research to suggest how effective low concentrated and non-prescriptive products can be.
Pros: Can also be used to treat rosacea and acne
Cons: Lack of studies to prove the efficiency of low-concentrated azelaic acid-based products
How long will it take to see a result? General brightening of the skin can be seen in just one week, but it can take just up to a month to see a significant change in hyperpigmentation. When treating acne, it could take up to several months before noticing an improvement
Liquorice extract is one of the gentlest tyrosinase inhibitors on this list and is perfectly safe to use on all skin types. It is derived from the root of the Glycyrrhiza glabra plant and although liquorice is renowned for its sweet taste in confectionary, this extract is favoured in skincare too, because of its soothing and brightening agents.
Liquorice root via maxpixel
Liquorice contains the skin-lightening compound glabridin whilst glycyrrhizin reduces redness and swelling by releasing steroid hormones in the skin. It is also an antioxidant and anti-fungal ingredient.
Pros: Can also be used to soothe skin rashes, insect bites and stings, safe to use on all skin types
Cons: It is questionable whether ‘extracts’ in skincare are efficient at all
How long will it take to see a result? 2 months
This multi-tasking ingredient is a form of the vitamin B3 and is widely used in skincare and health supplements. Niacinamide is a well-studied tyrosinase inhibitor and is an ingredient that is easily delivered into the skin.
This skin lightener has also been studied to improve acne and rosacea due to its anti-bacterial and anti-inflammatory properties – niacinamide also helps assist increase ceramide production in the skin, boosting hydration levels. It is also considered a non-irritating exfoliating ingredient, as it aids desquamation and boosts cell renewal.
One study, amongst many others has shown that niacinamide can inhibit melanosome transfer by 35-68% and significantly decreased the appearance of hyperpigmentation in just 4 weeks.
Pros: Moisturising, great for treating acne & rosacea, non-acidic and gentle for most skin types
Cons: It is not a miracle product in comparison to the other high-strength ingredients on this list, mild irritation may occur in the first week or two of using niacinamide
How long will it take to see a result? 4-8 weeks
Paper Mulberry extract
This extract derives from the white mulberry tree and has been used in Chinese medicine for thousands of years – the bark of the tree is so strong it is also used in paper and cloth manufacturing. In skincare, paper mulberry is often concentrated with glycerin and water and can be found in serums, essences, cleansers and face masks.
Paper mulberry extract is also a nourishing antioxidant, but it is best known for its effect on treating the overproduction of melanin. In 2013 a randomised, single-blind, placebo-controlled trial on 50 patients showed improvement of pigmentation at week 8, after using a 75% white mulberry extract oil. Paper mulberry extract has also been studied many times on tricky melasma cases and showed positive results. This ingredient can also be combined with liquorice extract, kojic acid and alpha arbutin to maximise its effect on pigmentation.
Pros: Can be used in conjunction with other tyrosinase inhibitors, a gentle and nourishing ingredient
Cons: There is limited study on the effectiveness of products containing a low concentrate of paper mulberry extract
How long will it take to see a result? 2 months
It is important to remember that the toleration to these skincare ingredients, differs from person to person and therefore should be introduced gradually into your skincare routine, particularly inhibitors like kojic and azelaic acid and niacinamide. If you experience a strong reaction from the ingredient’s discussed in this post, (except for arbutin and hydroquinone) it may be a good idea to reduce your use of the product or stop completely until the irritation clears.
Results will also vary from each case – hyperpigmentation is notoriously difficult to treat, particularly hormonal-based conditions like melasma.
Also, in most cases particularly when using more aggressive ingredients like hydroquinone, alpha arbutin and kojic acid, the pigmentation can appear significantly darker for some time before it lightens.
If hyperpigmentation is a concern, consider professional treatments with an aesthetician like laser facials, skin peels and microneedling to enhance your results.
An SPF should always be used for the duration of the time you are using these ingredients and especially if you are wanting to brighten your skin and lighten darker patches. If a sunblock isn’t applied regularly throughout the day, then results will be very limited and you will run the risk of developing more pigmentation.