Cosmeceuticals for Hyperpigmentation - Naturopathic Perspectives

Although it has been fraught with debate, and even distain on occasion, the use of airbrushing of photos emanating from the marketing world of skin care and beauty tells us one thing…our society has a desire for evenness in skin appearance.  Fortunately, more facial beauty photos are being taken au-naturel, with minimal post-photo adjustment.  However, the interest in achieving that even skin tone remains, even as we demand more honesty from our commercial beauty images.  The world of Naturopathic Aesthetics has much to offer in the management of various forms of pigmentation concerns, from various topical cosmeceuticals, through to key lifestyle considerations.  Our focus for this article will be on how these play a role in mitigating common hyperpigmentation concerns such as melasma, post-inflammatory hyperpigmentation, ‘age spots’, ‘mottled’ skin, and general skin tone unevenness.  

A brief review…

Increases in skin pigmentation (hyperpigmentation) generally represent alterations in the biochemical processes which control skin pigment (melanin) production and placement into the skin cells.  It can be represented by an increase in melanocytes (cells in skin making melanin); melanosome production (melanin-containing ‘droplets’ transferred from melanocyte to skin cells); synthesis of melanin itself; and increase number of melanocytes or their dendritic ‘arms’ interweaving between skin cells.  There are a variety of both common and rare medical causes of hyperpigmentation, as such it is always recommended to confirm the diagnosis

of any pigmentation concern with your local dermatologist and skin care provider.  Our interest and focus will fall on some of the more common causes of hyperpigmentation, with a brief review of each below:

à Melasma: Represents an area(s) of circumscribed hypermelanosis, typically with symmetric brown or tan-colored skin patches.  It occurs most frequently over the face, but can be found on the arms as well.  It affects women more-so than men, and tends to develop and progress slowly.  It is more common, and can persist longer, among those of higher Fitzpatrick phototypes, such as Hispanic, East Indian, Asian, African, and Middle Eastern populations.  Exacerbating factors include hormonal changes (ex. pregnancy, oral contraceptive use), exposure to ultraviolet (UV) light, and heat ^[1].

à Post-Inflammatory Hyperpigmentation (PIH): Represents an acquired hyperpigmentation which involves areas of prior skin inflammation.  Experienced as asymptomatic spots/areas of skin discoloration ranging in color from tan to dark brown, through to blue-gray to gray-brown, depending on how deep in the skin the melanin is deposited.  Among the most common inflammatory triggers is acne.  However, PIH can also occur after allergic contact & irritant reactions; skin-based drug reactions; trauma such as burns and friction; as well as after cosmetic procedures (ex. chemical peels, laser/light therapy, injections, or skin reaction/irritation from topical preparations).  Hyperpigmentation develops and appears in areas of inflammation once the initial redness/swelling subsides (ex. around the spot of a previous acne pimple).  PIH affects all skin types, women and men equally, but like melasma is more apparent, and longer lasting, in higher Fitzpatrick phototypes (darker skin tones) ^[1].

à Solar Lentigines (‘Age-spots’, ‘Liver spots’):  These represent the experience of well-demarcated flat to slightly raised, tan to brown or even blackened small areas of skin.  Often round or oval, they can range in diameter from 3mm to 2cm and become confluent.  Typically occurring with increased age and sun exposure, more than half of those over age 64 will have at least one solar lentigo present, with most experiencing more than one.  Sun-exposed skin, such as the back of the hands, forearms and face, are the most common areas affected ^[2,3].   

Cosmeceuticals for Hyperpigmentation

A number of topical products are available as a means of improving and managing the appearance of various forms of hyperpigmentation, along with other skin appearance benefits. These are collectively, and appropriately, known as cosmeceuticals.  On store shelves, these are often referred to as ‘skin lightening’ ingredients or products.  In general, cosmeceutical products for hyperpigmentation can lighten skin (reduce pigmentation) through various means. This includes the interference of melanin synthesis, the inhibition of melanin transfer into skin cells, as well as by speeding the exfoliation of melanin-containing skin cells closer to the skin surface ^[4].  We will now review some of the more common and well-researched cosmeceutical actives (ingredients) used for hyperpigmentation.  Quite often, cosmeceutical manufacturers will combine these actives together into a formula designed for skin lightening benefit.  The information reviewed is recommended to first be discussed with your local (skin) healthcare provider to confirm its appropriateness in your case.  

The most important cosmeceutical…sun protection!

The temptation may be there to automatically assume, and reach for, skin lightening products in the management of hyperpigmentation.  However, if there is one take-away from this article, it’s that protection from the sun’s ultra violet light is paramount in your quest for reducing pigmentation concerns.  This cannot be emphasised enough given its direct connection to the persistence and worsening of hyperpigmentation through its role in activating melanocytes and promoting melanin deposition in the skin.  This means regular sunscreen use…yes, even in the winter months, through to sun protection measures via clothing and sun avoidance whenever possible.  Year-round sunscreen use and sun reduction may necessitate periodic checking of Vitamin D levels through your physician or Naturopathic Doctor, do discuss this with them.  In this way, from a topical product standpoint, you could think of sunscreens as a primary cosmeceutical for controlling hyperpigmentation.

The Gold-Standard cosmeceutical…Effective, but potentially flawed

Hydroquinone is by far the preeminent topical therapy used in managing hyperpigmentation.  It is available both over-the-counter (OTC), and in higher strengths, as a prescription. When prescribed, it is often combined with topical forms of a retinoid (Vitamin A derivative) and steroid ^[5].  Hydroquinone is a potent inhibitor of the enzyme tyrosinase, essential for the chemical conversion and pathway through which melanin is formed.  Where the debate comes in, however, and hence the ‘potentially flawed’ mention above, is in relation to hydroquinone’s potential side effects.  This includes the likes of skin irritation/dermatitis; a rare pigmentary reaction known as Exogenous Ochronosis; and possibly of most concern, is that of animal studies suggesting cell toxicity and mutagenicity effects.  The true degree and impact of these concerns is debatable, however it has been enough for certain countries and regions, like Japan and the European Union, to enforce restrictions and/or bans regarding its inclusion into skin lightening products ^[4,6].  From this, the result has become the search for more, and safer, skin lightening alternatives, and that is what we will turn to next…       

The search for safer alternatives brings us to…

There are numerous compounds which have been explored for their role in offering skin lightening benefits, while avoiding some of the concerns associated with hydroquinone.  In general, most of these skin lightening ‘actives’ offer weak depigmentation effects on their own, but are amplified when combined together as part of a formula.  Some of the more common actives you may encounter in the skin lightening market include: 

• Vitamin C & derivatives:  Through its ability to interfere with the creation of melanin, vitamin C has been shown effective in reducing hyperpigmentation concerns like melasma and post-inflammatory hyperpigmentation.

This effect seems to extend to vitamin C in many of its chemical forms.  From pure ascorbic acid, to variants designed to offer improved chemical stability and tolerability on the skin, such as Magnesium Ascorbyl Phosphate (MAP) and Sodium Ascorbyl Phosphate (SAP).  Those with more sensitive skin may need to consider the use of better tolerated derivatives such as these ^[7,8].

• Licorice extract:  Quickly becoming one of the more popular cosmeceutical actives for depigmentation, extracts from the licorice plant have shown benefit in a few small human trials for melasma and ultra-violet induced pigmentation ^[7].   Compounds sourced from licorice, such as the flavonoids glabridin and liquiritin, are believed to inhibit tyrosinase and disperse melanin.  The extract also can provide anti-inflammatory and antioxidant effects, while also reducing UV-induced skin reddening.  It has been found to be well tolerated, with no known cellular toxicity ^[7].
• Vitamin A derivatives (retinoids): One of the reasons for retinoids being such a popular product is the skin lightening effects it offers in addition to the various benefits seen for the skin, such as fine line and wrinkle reduction, among others. Much of the research has come from prescription forms of retinoids, however OTC forms such as retinol, retinyl palmitate, and even hydroxypinacolone retinoate, are being found to be effective, albeit to a lesser degree as compared to prescription retinoids.  Having said that, OTC retinoids are generally found to be better tolerated as compared, again, to their prescription counterparts.  Methods by which retinoids help reduce excess pigmentation include an inhibition of the tyrosinase enzyme; a reduced transfer of melanin into skin cells; and an enhancement of (upper layer) skin turnover ^{[6, 9]}.  Retinoid-containing products are not recommended during pregnancy or lactation.
• Unfermented soy extract: Fresh/unfermented soy milk extract contains the proteins Soybean Trypsin Inhibitor (STI) & Bowmann-Birk Inhibitor (BBI).  Together, these act to block the ability of melanin to be transferred from the melanocyte (pigment producing cell) into the keratinocyte (skin cell).  Fermentation of soy would render these proteins inactive ^{[6, 10]}.
• Vitamin B3 Derivatives (Niacinamide & Myristyl Nicotinate):  Much like the soy proteins just discussed, derivatives of Vitamin B3 like niacinamide, and possibly myristyl nicotinate, act to also inhibit melanin transfer from melanocytes into keratinocytes.  They are well tolerated, and their topical application offers multiple concurrent benefits for skin health.  This includes skin barrier and moisturization support; anti-inflammatory/anti-facial redness effects; and acne management through control of oil production (a nice bonus while it helps limit acne-based PIH).  Popular combinations of niacinamide and myristyl nicotinate in cosmeceutical products include: hyaluronic acid; N-acetylglucosamine, retinol, and ceramides ^{[11, 12,13]}
• Hydroxy acids:  Easily one of the most popular actives found in skin lightening products are those of the hydroxy acids, including alpha-hydroxy acids (AHAs) such as glycolic and lactic acid, and the poly-hydroxy acids (PHAs) and bionics, such as gluconolactone and lactobionic acid.  In general, AHAs may be more irritating to sensitive skin owing to their smaller chemical size, while PHAs and Bionics are less irritating and provide moisturization and skin barrier supportive effects.  The primary means by which these impart a depigmentation effect is via their role, at lower concentrations found OTC, of providing an enhancement of the exfoliation process. With the melanin pigment sitting in the upper layers of skin cells, speeding their shedding will, by consequence, also hasten the release of the melanin they contain. Stronger chemical peels as offered in a Medical Spa setting, or through a Dermatologist, are used in a similar, but more pronounced, fashion ^[14].

’Rules of Thumb’ regarding skin lighteners and managing hyperpigmentation

• Most often, skin lightener products are recommended to be used after cleansing and toning, but prior to other products such as moisturizers, sunscreen, and makeup
• For facial use, skin lighteners are typically applied over the full face, as skin lightening of non-affected skin is unexpected; avoiding spot treatment will also prevent the chance for ‘bull’s eye’ areas of discoloration ^[1]
• Always follow the label/manufacturer/skincare provider’s recommendations regarding when and how to apply the product as part of your daily regimen; frequency and overall length of use, as differences in formulas ingredients may alter the usage recommendations for a given skin lightener product
• Those with a darker skin phototype looking for skin procedures such as hair removal, laser skin treatment, dermabrasion, chemical peel, etc., should be sure to work with a provider experienced in treating those with darker skin tones. This is for the reason that these procedures, if misapplied, can (ironically) worsen the hyperpigmentation 
• Patience, patience, patience: Although we are a society that loves speedy results, use of skin lightening cosmeceutical products can take a number of weeks and/or months to fully establish a beneficial effect. The degree of change may itself be limited, requiring the exploration of other complementary procedures, such as professionally-administered deeper chemical peels and laser treatments.  Taking regular reproducible photographs, either yourself or through your skincare provider, can help track minor but noticeable changes over time.
• Don’t forget the sun protection!!! 😊