Hyperpigmentation results in flat, darkened patches of skin that are light brown to black in colour, and can vary in size and shape. Types of hyperpigmentation include age spots, melasma, and post-inflammatory hyperpigmentation and even lentigo maligna, a form of skin cancer. Hyperpigmentation is one of the biggest skincare concerns today, so if you do have them, know that you are not alone. Read on as Dr Teo Wan Lin addresses your concerns on hyperpigmentation and pigmentation products.
Q1: Do most brightening products target only the top layer of the skin?
It is important to understand from a dermatologist perspective that pigmentation develops from primarily the layer of the skin we call the epidermis. The epidermis itself is further divided into layers, the bottommost layer is known as the stratum basale. It is important scientifically to distinguish that references to the top layer of the skin are actually not accurate because the top layer itself is further divided into five different layers. That being said, the origin of pigmentation is typically from the melanocytes. Melanocytes refer to pigment producing cells – this originates from neural crest cells during the development of the central nervous system via the process of embryogenesis. Pigmentation commonly localises to the stratum basale.
Q2: What are the differences between pigmentation products and brightening products?
In terms of brightening products, one does not use the word brightening in dermatology. However, I understand that it’s a colloquial expression of a topical, that when applied leads to removal of pigmentation, i.e. referring to pigmentation products. This would commonly fall under the category of active ingredients that inhibit the production of melanin, a process we call melanogenesis.
Q3: Do most brightening or pigmentation products make you more sun-sensitive?
I think it’s not to say most. If you were to just zoom in on the synthetic skin lightening pigmentation products, then yes. This is because the most prominent would be hydroquinone and retinoids, both of which could be sun sensitising. Tretinoin which is a form of retinoid and hydroquinone, primarily from its irritating side effects. Having irritated skin means you could be more susceptible to sun damage. On the other hand, botanical or nature derived ingredients that have been scientifically proven to help pigmentation, tend to have little to no side effects. For example, there are certain microorganisms like fungus or kojic acid, that is derived from a fungus in nature, which are helpful in inhibiting melanocyte activity.
Q4: What are the active ingredients in these brightening and pigmentation products?
Most of the active ingredients are tyrosinase inhibitors. Tyrosinase is an enzyme that is actively involved in the production of pigment. Brightening and pigmentation products refer to any active ingredient that has been proven to inhibit the process of melanin formation and melanocyte activity. This would include evidence-based ingredients such as hydroquinone. Hydroquinone has both an epidermal and dermal action when it works in certain conditions such as melasma. In melasma, it is important to emphasise that pigmentation can be both superficial i.e. the top layers, or deep i.e. the dermal layers.
Q5: When pigmentation products advertise that they can effectively treat the cause of hyperpigmentation, are we supposed to believe that?
I think it’s really any descriptive that brands can choose to use. The important thing is the active ingredients the product consist of and the ingredient’s validity based on credible sources. You can carry out a short literature review on the ingredients on a scientific database i.e. Pubmed funded by National Institute of Health (NIH) in the US. If it’s an active ingredient that is scientifically proven, you’ll be able to find more than one paper on that ingredient.
Do note that skincare and cosmetics are not regulated by any authority. The Food and Drug Administration (FDA) in the US and Health Sciences Authority (HSA) in Singapore essentially regulates the incorporation of toxics and banned substances in skincare. They however do not validate claims in skincare. Hence, it is important to first research active ingredients listed in the pigmentation products.
Q6: Do pigmentation products tackle the root of hyperpigmentation or simply “slough off the top layers”?
I believe “sloughing off the top layers” refers to epidermal cell turnover which is the turnover rate of the topmost layer of your skin. There are some active ingredients e.g. glycolic acid, which is a type of AHAs that works well for pigmentation due to its ability to interfere with epidermal cell turnover. Topical retinoids also work by regulating epidermal cell turnover, though via different mechanisms. It targets various pathways in the skin to increase skin elasticity, increase collagen formation as well as decrease deposition of pigmentation.
Q7: Are the causes of pigmentation on the face and other areas of the body the same? What are the different types of pigmentation?
It is common for a layperson or a non-dermatologist to assume that an area pigmentation vs another area is the same. But to dermatologists, pigmentation itself is a very broad topic and there are 20 or 30 different types of pigmentation. The common ones are mostly cosmetic, thereabouts 4 or 5 types of pigmentation. The most common type of pigmentation is sun spots which is known as solar lentigo. Solar lentigo is dependent on age, genetics and amount of sun exposure. Another common type of pigmentation is ephelides, ephelides are genetically coded freckles which are more common in individuals with red hair.
The other common type of pigmentation in people of coloured skin would be melasma. Melasma is categorised into different types, depending on the various depths of the deposition of the pigment as well as the location of melasma. Other causes of pigmentation would be post-inflammatory hyperpigmentation (PIH) – a mark is left from a pimple or a surgery. PIH has to be treated differently from melasma, solar lentigo and ephelides. There are other types of pigmentation and even autoimmune diseases such as lichen planus. Lichen planus leads to hyperpigmentation of the skin. It is dangerous for anyone to assume that it’s a cosmetic problem and try to treat that with aesthetic dermatology treatment.
Q8: How do I eradicate dark spots and pigmentation on my face?
Firstly, it is important to get a correct diagnosis and knowing when the pigmentation becomes dangerous. It is crucial to not assume dark spots on your face to just be an aesthetic problem that you can burn or laser off. Dermatologists are trained to distinguish between various types of moles which are not obviously cancerous. Thus one should seek professional help before any assumptions are made.
A typical red herring would be a condition known as lentigo maligna. Lentigo maligna has been infamously diagnosed by dermatologists as an cosmetic pigmentation issue. However, it is a fairly aggressive form of skin cancer, melanoma. Melanoma has the ability to spread to your lymph nodes and if discovered at an advanced stage, at the very minimum, it causes severe disfigurement due to the extent of surgical resection needed. At worst, it can lead to mortality.
Q9: Lipodisq has been incorporated safely and efficiently to deliver potent skincare actives into deep layers of the skin. What are your views on nanoparticle drug delivery?
Lipodisq is a nanoparticle delivery system that is patented by a cosmeceutical company in the UK. To my knowledge, it is something which certain cosmetic manufacturers also utilise in the formulation of their products including pigmentation products to increase the cutaneous absorption of active ingredients.
In terms of nanoparticle drug delivery, I would say data is very much limited to the commercial interest that is driving the technology and hence the patent protections as well. Accordingly, I currently do not know of studies by the international dermatology community that independently verify these claims Nonetheless, from what we see with literature provided by the parent company that has researched this technology, the data does seem interesting and the technology itself, a safe and sound form of topical delivery.
1. What is the difference between melasma and hyperpigmentation?
Pigmentation is the discoloration of the skin. Melasma and hyperpigmentation are causes of pigmentation. Melasma tends to be related to changes in hormones such as during pregnancy or after menopause. It is also closely related to genetics and sun exposure. We only use the term “hyperpigmentation” in the context of post-inflammatory hyperpigmentation as a form of scarring following inflammation. Melasma itself is also distributed differently. It tends to appear in a butterfly-like configuration over the cheeks and sometimes spreading to the forehead. It also tends to be very symmetrical, even and diffused, whereas, hyperpigmentation is usually localized to the area of previous injury.
2. Is melasma curable? How about Home remedies?
A cure would mean a one-time treatment that causes all symptoms to go away forever. Most skin conditions are treatable but the underlying root cause has to do with the amount of environmental exposure such as sun exposure in one’s lifetime, genetics, as well as other factors such as hormones.
Some home remedies that have been proposed to treat melasma are quite dangerous. Apple cider vinegar has been proposed as one of the solutions as it contains acetic acid which is proven by research to be effective in lightening skin pigmentation. However, the method and form of acetic acid in apple cider vinegar only causes skin irritation, the most severe form being irritant contact dermatitis or even facial eczema and chemical burn.
The usage of aloe vera is unlikely to be harmful. However, many aloe vera products contain certain compounds such as alcohol that helps to maintain the product in a gel form.
The key thing to understand about these DIY remedies is that while the source and raw ingredients may contain an active ingredient, proven to lighten pigmentation in laboratory studies, it is often not in the correct form for it to be effective on the skin. It can also cause severe irritant reactions that can causes pigmentation to worsen.
3. How should one treat melasma?
For melasma to be effectively treated, you have to use a combination of therapies. To me, the most effective treatment is a combination of the use of a q-switched laser, a 1064nm laser toning device, spaced at weekly intervals, together with topicals, such as hydroquinone to help remove underlying pigmentation, and cosmeceutical skincare. The Radiancé Fluide™ Hydrating Emulsion contains oligopeptides that help reduce the hyperpigmentation while increasing the function of the pigment removing cells. The Vitá C GOLD™ Serum contains nano-formulated sodium ascorbyl phosphate, a stable and effective derivative of Vitamin C, well known for its amazing ability to treat hyperpigmentation and photoageing.
Meet with Dr Teo Wan Lin, an accredited dermatologist at TWL Specialist Skin & Laser Centre, for a thorough consultation to determine the most suitable treatment for your skin.
To book an appointment with Dr Teo, call us at +65 6355 0522, or email firstname.lastname@example.org. Alternatively, you may fill up our contact form here.
In this series of articles, I shall expound on the science and chemical aspects of skin lightening agents used for hyperpigmentation, both prescription and over-the-counter alternatives such as cosmeceuticals. In the first installment, we shall cover the commonest prescription medications used for skin lightening – hydroquinone, and its derivatives.
Cosmeceuticals are topicals that have both cosmetic and pharmaceutical effects. They enhance the beauty through constituents that provide additional health-related benefit. Cosmeceuticals are commonly used for hyperpigmentation. Hyperpigmentation involves the need for skin lightening agents which includes cosmeceuticals. Cosmeceutical agents selectively target hyperplastic melanocytes and inhibit key regulatory steps in melanin synthesis.
Cosmeceuticals are commonly used for hyperpigmentation. Pigmentary disorders are the third most common dermatologic disorder and cause significant psychosocial impairment. These disorders are generally difficult to treat, hence, the need for skin lightening agents including cosmeceuticals.
Common active ingredients in cosmeceuticals for treating hyperpigmentation include the following: Ascorbyl phosphate (Vitamin C), Niacinamide (derivative of Vitamin B12) and plant-derived (phyto-antioxidants) which include grape seed extracts, white flower complexes and grape fruit extracts.
What Are Some Prescription Medications For Treating Hyperpigmentation?
Here are some compounds found in prescription medications that have been used to treat hyperpigmentation.
Hydroquinone competitively inhibits melanin synthesis by inhibiting sulfhydryl groups and acting as a substrate for tyrosinase and dermatologists have traditionally relied on prescription medication hydroquinone at concentrations of 1-4% to treat cases of hyperpigmentation.
What is hydroquinone and what is it used for?
Hydroquinone (HQ) is a chemical belonging to the family of phenols. Hydroquinone competitively inhibits melanin synthesis. Specifically, it blocks sulfhydryl groups and acts as a substrate (receptor) for tyrosinase, an enzyme involved in pigmentation.
Dermatologists have traditionally relied on prescription medication such as hydroquinone at concentrations of 1-4% to treat cases of hyperpigmentation, especially those related to solar lentigo, freckles (ephelides) and melasma.
It is also sometimes prescribed to treat post-inflammation hyperpigmentation. However, the use of hydroquinone is not without side effects of skin irritation. There have also been cases of skin de-pigmentation, a form of permanent scarring.
What are the concerns involving the usage of hydroquinone?
As hydroquinone is carcinogenic and may cause DNA Damage, over-the counter skin bleaching agents containing hydroquinone are banned, and should be used under strict medical supervision for a period of time only. Clinical studies supporting these side effects were based on ingested and injected forms of hydroquinone which are not used clinically in dermatologists’ offices. There has been no evidence of skin cancer or organ cancers developing as a result of hydroquinone applied topically.
However, I have phased out the use of hydroquinone for treating most pigmentation problems in my practice and relied more on over-the-counter active ingredients in cosmeceuticals which are mainly plant-derived and still demonstrate clinical efficacy for the treatment of pigmentation problems.
With the recent safety concern regarding the use of hydroquinone, the need for alternative natural, safe and efficacious skin lightening agents is becoming all the more necessary.
What is it?
It is a derivative of hydroquinone. Its mechanism of action is unclear. It acts as a substrate for tyrosinase, thereby inhibiting the formation of melanin precursors.
What is it?
A phenol that blocks tyrosinase activity (pigment cell producing activity).
1. Kojic Acid
What is it?
Kojic acid occurs in nature as a water-loving fungus byproduct. It helps to block the progression of pigmentation by stopping the production of the enzyme tyrosinase. It is also a powerful antioxidant which means that it engulfs free radicals that are responsible for skin aging.
What is it?
Arbutin is one of the most widely prescribed skin-lightening and depigmenting agent worldwide. It is a derivative of hydroquinone, and is a naturally occurring plant derived compound.
How does it work?
Arbutin prevents the growth and maturation of the cell component responsible for hyperpigmentation known as the melanosome. Notably, it is less toxic to the pigment cells than hydroquinone. Melanosomes are the pigment granules confer skin with colour and sun protection. They are also the cell engines whereby the body produces, stores and transports pigments known as melanin. The use of arbutin is limited by its concentration. While higher concentrations may be more effective, there is a greater risk for hyperpigmentation which can occur as a paradoxical side effect.
Is it effective?
Although there have been no randomized controlled trials on using arbutin for treating hyperpigmentation, it has been proven in many clinical studies to still be effective.
Dr.TWL Pharmacy is a proprietary specialist skincare pharmacy run by Dr. TWL Dermaceuticals, providing custom compounded prescriptive cosmeceuticals for common skincare concerns. It is located on-site at TWL Specialist Skin & Laser Clinic, a Ministry of Health accredited dermatology practice headed by dermatologist Dr. Teo Wan Lin. The pharmacy formulates skincare prescriptives for the treatment of various skin concerns including acne, hyperpigmentation, anti-ageing, excessive oil production, age spots and skin sensitivity/redness.
Melanin is the culprit behind the dark spots that give us an uneven complexion. It is a brown pigment found in the basal layer of the epidermis.
This pigment is synthesised by melanocytes. The process of melanin synthesis is termed melanogenesis. Melanocytes go through different stages of maturation, becoming more pigmented at each stage.
Certain stimulants trigger a gene to produce more of tyrosinase, a copper-containing enzyme that converts tyrosine into melanin. Stimulants that activate the melanocyte include hormones, inflammation (such as acne) and external environmental conditions (ultraviolet light that causes the production of free radicals).
One simple way to reduce melanin production is to use broad-spectrum sunscreens with zinc oxide, titanium dioxide or iron oxide. These substances help block UVA and UVB light, thus impeding the stimulation of melanocytes.
Pigmentary disordersfrom melanin
Common hyperpigmentation disorders that involve the darkening of an area of skin due to increased melanin include melasma, lentigo, and post-inflammatory hyperpigmentation.
Melasma is usually caused by chronic exposure to ultraviolet radiation or a spike in hormones due to pregnancy or the use of oral contraception. It can be found at the epidermis, dermal layer or mixed, depending on the location of the pigment.
A lentigo is a light or dark brown area of discoloration that can range from 1mm to 1cm across, and is caused by an increased number of melanocytes. Its outline is usually discrete, but can also be irregular. Simple lentigines arise mostly during childhood on areas not exposed to the sun. Solar (or senile) lentigines are found on the backs of hands or on the face, most commonly after middle age.
Post-inflammatory hyperpigmentation (PIH) is the skin’s response to inflammatory skin disorders. Common causes are acne and atopic dermatitis. PIH is caused by the overproduction of melanin caused by skin inflammation.
Treating hyperpigmentation from melanin
Hydroquinone: For 50 years, hydroquinone has been the gold standard treatment for hyperpigmentation. This compound inhibits tyrosinase activity, thus limiting the amount of melanin to be produced. It also alters melanosome formation, possibly degrading melanocytes.
However, prolonged use of topical hydroquinone has shown to have side effects such as ochronosis and permanent depigmentation. Ochronosis is a disorder with blue-black discoloration. As such, hydroquinone is banned in cosmetic formulations and only available through a prescription that should be carefully managed by an accredited dermatologist.
Retinoids are forms of vitamin A that can treat acne, photodamage and PIH. They have various pathways that lead to skin lightening effects, such as accelerating epidermal turnover, reducing pigment transfer and slowing the production of tyrosinase.
With common side effects being erythema, skin irritation, dryness and scaling, it is recommended to use a retinoid only under the supervision of an accredited dermatologist. Corticosteroids (steroid hormones) have anti-inflammatory abilities and are often prescribed along with retinoids to prevent excess irritation.
Arbutin is a botanically derived compound found in cranberries, blueberries, wheat and pears. Though arbutin is a derivative of hydroquinoine, it has shown to be a more controlled way of inhibiting the synthesis of melanin as it does not permanently destroy melanocytes.
Kojic acid is a naturally occurring fungal substance. Its skin-lightening ability works by inhibiting the activity of tyrosinase. However, frequent use can cause side effects of contact dermatitis or erythema (redness of the skin).
Azelaic acid is known to be effective for treating PIH and acne. Azelaic acid depigments the skin in several ways. It can inhibit tyrosinase or reduce levels of abnormal melanocytes. This means that azelaic acid does not influence normal skin pigmentation but only acts on the proliferation of unwanted melanocyte activity. Side effects are mild and only last for a short period of time. Irritation, burning sensation or mild erythema may emerge, taking 2 to 4 weeks to subside.
Niacinamide is a derivative of vitamin B3. It works by decreasing the transfer of melanosome to keratinocytes. Niacinamide is a stable ingredient as it is unaffected by light, moisture or acids. This ingredient is often incorporated into cosmeceuticals due to its safety profile.
Vitamin C or L-ascorbic acid is a naturally occurring antioxidant that helps with skin lightening. It prevents tyrosinase from converting tyrosine to melanin. Vitamin C is also favored for its anti-inflammatory and photoprotective properties. However, L-ascorbic acid is highly unstable and rapidly oxidized. It is not used in the treatment of PIH.
Stable forms of vitamin C include magnesium ascorbyl phosphate or sodium ascorbyl phosphate. For safe and effective results, consider a dermatologist-formulated serum VITA C GOLD™ Serum,a formulation tested for bio-activity in a laboratory.
As seen above, there are various treatment options to treat common hyperpigmentation disorders. Recognizing the underlying cause for pigmentation is critical for proper treatment and choosing the best-suited therapy. Visit an accredited dermatologist for effective and safe treatments catered to your condition.
Vitamin C is likely to be no stranger to any of us, we see it present in plenty of fruits and vegetables like oranges, grapefruits or pineapple. Yet, it is rather new to most of us to have it on our face. This obsession with this skincare ingredient could be why you are googling up on this article now, and what we are about to tell you.
The vitamin brings benefits to the skin that we love: antioxidative, photoprotective, antiaging, and anti-pigmentary effects.
Vitamin C in our body
Vitamin C is the most abundant antioxidant in human skin. Antioxidants work to reduce the damage that free radicals can bring to our skin cells. We are unable to synthesize the antioxidant as we do not have the enzyme needed to do so. Even as we consume high doses of vitamin C supplements, only a small fraction of it will remain in our body and skin cells. This brings us to rely on external supplements, with topical application being the most common form.
What should the concentration of my Vitamin C be?
When choosing a product, you may come across different concentrations of the active ingredient available. Of what percentage of the ingredient should we be using? That really depends on the type of Vitamin C in use. Conventional Vitamin C formulations such as Ascorbic Acid in its raw form may require 10 to 20 percent to have any reasonable efficacy. This is limited inherently by the fact that higher concentrations, for instance above 20 percent, may cause irritation to the skin. On the other hand, studies have shown that a mere 1 percent concentration of Sodium Ascorbyl Phosphate – considered to be a new generation of ascorbic acid derivatives, has strong antimicrobial efficacy against acne.
What are the common forms of Vitamin C?
Out of all the various forms of Vitamin C, L-ascorbic acid is conventionally recognised as one of the most biologically active molecules. This compound is likely to be found at a pH below 3.5 for greater stability and permeability. Above that, the acid becomes very unstable in aqueous solutions and is prone to immediate oxidation, turning to a brown colour when oxidized.
Other formulations available are magnesium ascorbyl phosphate, ascorbyl-6-palmitate and sodium ascorbyl phosphate. These formulations are stable at neutral pH of 7. As a water-soluble derivative, magnesium ascorbyl phosphate is more stable in water but less potent than L-Ascorbic acid.
Sodium Ascorbyl Phosphate is one of the most stable and effective forms of available. As it will not oxidize as easily, it is a preferable choice for skin care formulations. A well-formulated product allows sodium ascorbyl phosphate to penetrate the skin epidermis without causing irritation. You may consider a dermatologist-formulated product such as Vita C Gold™ Serum, which is a Sodium Ascorbyl Phosphate formulation that has been tested for bio-activity in a laboratory, for safe and effective results.
Different formulations of Vitamin C exists, and you may decide which forms would be preferable in your skincare by weighing in on the cost, potency, texture or formulation. Although the conventional L-ascorbic acid is perhaps the most potent derivative of Vitamin C, it oxidizes too quickly when exposed to oxygen to be much efficacy on the skin. One may prefer newer Vitamin C derivatives – Sodium Ascorbyl Phosphate, which are much more stable and able to deliver better efficacy even at lower concentrations.
Vitamin C helps to produce collagen
The nutrient is required by our bodies to produce collagen, making it crucial for anti-ageing. Think of it as an anti-ageing shield your skin needs to reduce the damage your skin suffered, and also to prevent future damage. The vitamin also facilitates enzymes that lead to the stability of collagen fibers. In addition, it increases expression of collagen and synthesizes inhibitors to block enzymes from degrading collagen.
Vitamin C has anti-pigmentary effect
Vitamin C plays an important role in skin-lightening, as it inhibits an enzyme called tyrosinase. This enzyme works by converting tyrosine into melanin, so by reducing the activity of tyrosinase, our skin cells produce less melanin.
Should I DIY my own serum?
According to Dr Teo Wan Lin, an accredited dermatologist at TWL Specialist Skin and Laser Centre, she says: “Concocting your own serum of Vitamin C can be dangerous as it can lead to phytophotodermatitis, a condition where itchy blisters and reddened patches appear on the exposed skin. The redness and blistering will settle down in a few days, but it leaves pigmentation at the same sites. Phytophotodermatitis results from the action of UV radiation on a plant chemical called furocoumarins. Citrus fruits such as lemon, lime or bergamot oranges are often responsible for the reaction.”
It is best to avoid DIY recipes or you may end up with rashes that scar for a long time.