banner img3

Lighteners and Brighteners.

Posted November 06, 2014 in Products


Pigmentation problems (dark or light changes in the skin) are the third most common dermatologic disorder and are more common in women.  This has a number of causes, but sun exposure is one of the most common.  So, most people will notice changes in the summer.  The most important thing anyone can do to prevent and treat pigmentation changes is a sunscreen with zinc or titanium with SPF 30.  In addition to sunscreen, an antioxidant product and a lightener can help your skin be radiant.  We are bombarded with products that claim to reduce browspots at the drugstore, make up counter and in advertisements.  What do these contain, how do they work and, most importantly, do they really work?

Prescription Products

Hydroquinone, the “gold standard”

Hydroquinone is a prescription cream that blocks the pathway that creates melanin (pigment) in melanocytes (cells that create pigment).  Since, it remains the gold standard in treatment of dark spots and is the “go to” for most physicians; it can be found in many of our medicine cabinets.  It comes in a range of concentrations, usually from 2-4%, but can be higher.  It can also be combined with a steroid and retin-A.  This can result in more dramatic effects, but can also be more irritating to the skin.  Hydroquinone works very well, but you must be careful about not going in the sun for extended periods of time and when you do use sunscreen and a hat, if possible.  Hydroquinone makes the skin very sensitive to the sun’s effects and can cause the pigmentation to worsen, if you sunbathe.  Other potential side effects include including change in nail color, and impaired wound healing.  Therefore, the industry has made a concerted effort to find alternatives.


Retinols and retin-A are derived from Vitamin A.  So, they are natural and have been well studied to improve pigmentation as well as skin texture and sun damage.  Lower concentrations can be found in cosmeceuticals and even cosmetic products, but the more efficacious higher concentrations require a prescription.  However, they do have side effects such as redness, flaking and skin irritation, particularly with retin-A.  An active area of product development is to make formulations with more active form available for efficacy and less skin irritation.  With those of us used to retin-A, it takes getting used to the idea that these new products are working even if there isn’t the characteristic flaking phase.

Lightening Ingredients in Cosmeceuticals (non-prescription)

Synthetic Compounds

Mequinol is a derivative of hydroquinone.  It blocks the pigment pathway, but the exact way it does so is not clear.  It can be combined with retin-A and has been shown to be effective in scientific studies.  The side effects are similar to hyroquinone.  N-acetyl-4-S-cysteaminylphenol, NCAP, takes approximately 2-4 weeks to take effect, has been found to be effective and causes less skin irritation than hydroquinone.

Common Natural Compounds


Kojic acid, Arbutin, Vitamin C, Vitamin E and Niacinamide are some of the most common lightening compounds that are not prescriptions, but have scientific studies showing that they can improve pigmentation. Therefore, they are considered cosmeceuticals.  These tend to be gentler on the skin and have less side effects than hydroquinone or the retinols.   Kojic acid is a naturally occurring product that comes from certain fungi.  It blocks the pigment pathway, as well as acting as a powerful antioxidant.  Kojic acid can be combined with hydroquinone, but there have been no head-to-head studies comparing it to hydroquinone treatment alone.  Arbutin is one of the most widely prescribed skin-lighteners worldwide.  It is derived from the leaves of a number of different plants including bearberry, blueberry, cranberry and pear trees.  Arbutin blocks the pigmentation pathway in a way that is less toxic to the cell producing pigment.  Arbutin is gentler, which is good for your skin, but is not as effective as kojic acid.  Vitamin C is a naturally occurring compound that not only reduces free radicals, but blocks several steps in the production of the pigment.  Vitamin C penetrates best in an acidic environment, which the skin is not.  Therefore, it has to be in high concentration and in a form that will penetrate.  These criteria are met in cosmeceutical forms, but often not in the cosmetic brands found in grocery stores or drug stores.  Not all Vitamin C is the same!  Vitamin E is an antioxidant that has been shown to have photo-protective effects, as well as block the pigment pathway at multiple steps.  Vitamin E and Vitamin C work together to activate each other.  This was demonstrated by a double-blinded clinical study found that Vitamin E and C improved melasma and pigment better than each on their own.  So, a combination product is best.  Niacinamide is the physiologically active version of niacin (vitamin B3). Clinical trials have shown that 2% niacinamide reduces the total area of hyperpigmentation after 4 weeks.  There is a plateau of the effect, so can be a product that is rotated in and out of your skin care regimen.

Plant extracts

As we become more aware of the effects and side-effects that can be associated with synthetic products, products from natural sources will become more popular and available.  These have not been studied as widely, but from preliminary findings may have similar efficacy to the other treatments.  These are frequently found in cosmeceuticals, but can be in cosmetics also.

A number of natural compounds have been found to have a lightening effect without many of the side effects seen with synthetic products.  These include orchid extract, aloe vera, pycnogenol from the French pine tree, marine algae extract, cinnamic acid, coffeeberry, mulberry extract, soy, licorice extract, umbelliferone from carrots and coriander, boswellia from the Boswellia serrate tree in India and Africa, and N-Acetyl Glucosamine in combination with niacinamide.  Grape seed extract is a powerful antioxidant that has not been studied as a topical application, but has been shown to improve melasma if ingested for at least 6 months.  Flavonoids can come from green tea leaves, eucalyptus strawberries and aloe.  These are amazing compounds and have anti-inflammatory, antioxidant, antiviral and anti-carcinogenic properties.  Most studies on these compounds are preliminary or observational, rather than comparative to existing treatments, at this time, but the literature is growing as they become more popular.


Although hydroquinone remains the gold standard treatment for hyperpigmentation, there are a growing number of natural ingredients being used with efficacy in some studies.  Check the label of your products to see if these compounds are included in the active ingredients.  Of course, when in doubt, ask your Dermatologist, Plastic Surgeon or skin care specialist.  We are always happy to take a look at it!

Posted in: Products