Regardless of your ethnic background or skin color, eventually
most of us will struggle with some kind of brown or ashen
pigmentation problem. Skin will either appear lighter
or darker than normal in concentrated areas, or you may
notice blotchy, uneven patches of brown to gray discoloration
or freckling. Skin pigmentation disorders occur because
the body produces either too much or too little melanin.
Melanin is the pigment produced by specific cells (melanocytes).
It is triggered by an enzyme called tyrosinase, which
creates the color of our skin, eyes, and hair. (Melanin
actually has two major forms that combine to create varying
skin tones. Eumelanin produces a range of brown skin and
hair color, while pheomelanin imparts a yellow to reddish
hue.)
As far as skin is concerned, depending on how much is
present, melanin does provide some amount of sun protection
by absorbing the sun's ultraviolet light. This explains
why darker skin colors are less susceptible to sunburn
and the overall effects of sun damage. But less susceptible
doesn't mean immune from problems.
Increased melanin production —also known as hyperpigmentation
—is often referred to as melasma, chloasma or solar lentigenes.
Melasma is a general term describing darkening of the
skin. Chloasma is generally used to describe skin discolorations
caused by hormones. These hormonal changes are usually
the result of pregnancy, birth control pills or estrogen
replacement therapy. Solar lentigenes is the technical
term for darkened spots on the skin caused by the sun.
Solar refers to sunlight and lentigene describes a darkened
area of skin. These spots are quite common in adults with
a long history of unprotected sun exposure.
Aside from sun exposure and hormones, hyperpigmentation
can be caused by skin damage, such as remnants of blemishes,
wounds or rashes (Source: Cutis, August 2005, pages 19-23).
This is especially true for those with darker skin tones.
By far, for all skin colors, the most typical cause of
darkened areas of skin, brown spots or areas of discoloration
is unprotected sun exposure. Once incorrectly referred
to as liver spots, these pigment problems have nothing
whatsoever to do with the liver. In fact, these discolorations
wouldn't have appeared in the first place if skin was
diligently protected from the sun over the years.
On lighter to medium skin tones, solar lentigenes emerge
as small- to medium-sized brown patches of freckling that
can grow and accumulate over time on areas of the body
that receive the most unprotected sun exposure, such as
the back of the hands, forearms, chest, and face. For
those with darker skin colors, these discolorations can
appear as patches or areas of ashen-gray skin. Regardless
of how or why these benign discolorations occur, the thought
is the same worldwide: this is something women want to
get rid of and prevent from recurring (or ever taking
place).
Combination Treatments
Melanin is stimulated by a complex process partially controlled
by an enzyme called tyrosinase. Most skin-lightening treatments
are aimed at inhibiting this enzyme, which can reduce
or block some amount of melanin production. There are
many options to consider when searching for a solution.
The most successful treatments use a combination of topical
lotions or gels containing melanin-inhibiting ingredients
along with a well-formulated sunscreen, and a prescription
retinoid (such as Renova or generic versions containing
tretinoin, a type of retinoid). Depending on how the skin
responds to these treatments, exfoliants—either in the
form of topical cosmetic or chemical peels—and lasers
are also able to further affect pigment and can definitely
enhance results (Sources: Journal of the American Academy
of Dermatology, May 2006, supplemental, pages 272-281;
Dermatologic Surgery, March 2006, pages 365-371; Journal
of Drugs in Dermatology, September-October 2004, supplemental,
27-34; International Journal of Dermatology, December
2003, pages 966-972; and Archives of Dermatology, December
2002, pages 1578-1582).
Sunscreen
Store shelves are lined with products claiming to lighten
skin. But without question, the first line of defense
is smart sun behavior (meaning avoidance) along with the
daily use (365 days a year) and liberal application (and,
when needed, reapplication) of a well-formulated sunscreen.
Diligent use of a sunscreen alone allows some repair as
well as protection from further sun damage, which is what
created the problem in the first place (Source: Journal
of the American Academy of Dermatology, May 2005, pages
786-792; American Journal of Epidemiology, April 2005,
pages 620-627; and The British Journal of Dermatology,
December 1996, pages 867-875). No other aspect of controlling
or reducing skin discolorations is as important as being
careful about exposing your skin to the sun and the use
of sunscreen, SPF 15 or greater (and greater is usually
better), with the UVA-protecting ingredients of titanium
dioxide, zinc oxide or avobenzone. Using skin-lightening
products, exfoliants, peels or laser treatments without
also using a sunscreen will prove to be a waste of time
and money. Sun exposure is one of the primary causes of
melasma, and other treatments can't keep up with the sun's
daily assault on the skin. Before you look at any other
option for brown or ashen skin discolorations, applying
sunscreen and reducing sun exposure are the most practical
steps to start with.
Topicals
Topical hydroquinone is the next step in reducing or eliminating
skin discolorations. In fact, topical application of hydroquinone
is considered by many dermatologists to be a safer, as
effective (if not more so), and far less expensive option
than lasers or deep peel treatments. Topical hydroquinone
in 2% (available in cosmetics) to 4% concentrations (available
from a physician or by prescription), alone or in combination
with tretinoin 0.05% to 0.1%, has an impressive track
record. Research has repeatedly shown hydroquinone and
tretinoin to be powerful tools against sun- or hormone-induced
melasma (Source: Dermatologic Surgery, March 2006, pages
365-371).
Some research has shown topical azelaic acid in 15% to
20% concentrations to be as efficacious as hydroquinone
with a decreased risk of irritation. Tretinoin by itself
has also been shown to be especially useful in treating
hyperpigmentation of sun-damaged skin. Kojic acid, alone
or in combination with glycolic acid or hydroquinone,
also has shown good results due to its inhibitory action
on tyrosinase (though kojic acid has had its share of
problems in terms of stability and potential negative
effects on the skin and is rarely being used nowadays).
Several plant extracts and vitamin C also have some research
showing them to be effective for inhibiting melanin production
(Sources: Journal of the American Academy of Dermatology,
May 2006, pages S272-S281; International Journal of Dermatology,
August 2004, pages 604-607; and The American Journal of
Clinical Dermatology, September-October 2000, pages 261-268).
The most reliable and best ones by far to look for are
reviewed below.
Hydroquinone
Hydroquinone deserves more discussion because it has long
been established as the most effective ingredient for
reducing and potentially eliminating melasma. Over-the-counter
hydroquinone products can contain 0.5% to 2% concentrations
of hydroquinone, while 4% (and sometimes even higher)
concentrations are available only from a physician.
In medical literature, hydroquinone is considered the
primary topical ingredient for inhibiting melanin production.
Using it in combination with the other options listed
in this section —especially tretinoin—can greatly reduce
and even eliminate skin discolorations (Sources: Cutis,
March 2006, pages 177-184; Journal of Drugs in Dermatology,
September-October 2005, pages 592-597; Journal of Cosmetic
Science, May-June 1998, pages 208-290; and Dermatological
Surgery, May 1996, pages 443-447). Interestingly, hydroquinone
is not only a hero for those with sun- or hormone-induced
melasma, but its components have potent antioxidant abilities
(Source: Journal of Natural Products, November 2002, pages
1605-1611).
Hydroquinone is a strong inhibitor of melanin production
(Source: Journal of Dermatological Science, August, 2001,
supplemental, pages 68-75), meaning that it prevents skin
from making the substance responsible for skin color.
Hydroquinone does not bleach the skin, which is why calling
it a bleaching agent is a misnomer as it can't remove
pigment from the skin cell. Hydroquinone can only disrupt
the synthesis and production of melanin hyperpigmentation,
which is actually true of any skin-lightening ingredient.
When you prevent melanin from being generated, as new
skin cells are formed and move to the skin's surface,
they do not contain the excess pigment (melanin), therefore
reducing or eliminating these darkened areas.
Some concerns about hydroquinone's safety on skin have
been expressed, but the research when it comes to topical
application indicates negative reactions are minor or
a result of using extremely high concentrations or from
other skin-lightening agents such as glucocorticoids or
mercury iodine. This is particularly true in Africa where
adulterated skin lightening products are commonplace (Sources:
British Journal of Dermatology, March 2003, pages 493-500
and Critical Reviews in Toxicology, May 1999, pages 283-330).
According to Howard I. Maibach, M.D., professor of dermatology
at the University of California School of Medicine, San
Francisco, "Overall, adverse events reported with
the use of hydroquinone... have been relatively few and
minor in nature.... To date there is no evidence of adverse
systemic reactions following the use of hydroquinone.
and it has been around for over 30 years in skin-care
products." Maibach also has stated that "hydroquinone
is undoubtedly the most active and safest skin-depigmenting
substance..." Research supporting Maibach's contentions
was published in the Journal of Toxicology and Environmental
Health (1998, pages 301-317). Concern about hydroquinone
having carcinogenic properties is mostly from industrial-grade
materials and uses. For cosmetic use there appears to
be no similar evidence.
Despite hydroquinone’s impressive track record and efficacy,
in September 2006, the Food and Drug Administration (FDA)
recommended that products containing hydroquinone be sold
only with a prescription due to their opinion that it
posed certain health risks. The FDA asserts there are
animal studies showing it may be a possible carcinogen,
and studies from Africa showing risk of a skin disorder
called ochronosis (Source: http://www.fda.gov/OHRMS/DOCKETS/98fr/E6-14263.htm).
More than 200 products containing hydroquinone are currently
sold in the United States, and, according to Dr. Susan
Taylor, founding director of the Skin of Color Center
in New York City and assistant professor of dermatology
at Columbia University, "Hydroquinone is the gold
standard for treating pigmentation disorders and has been
for many years. I consider it to be very safe and effective"
(Source: Pittsburgh Post-Gazette, Wednesday, September
6, 2006).
I concur. There is abundant research from reputable sources
that shows hydroquinone to be safe and extremely effective
(Sources: Cutis, August 2006, Supplemental pages 6–19;
Journal of Cosmetic Laser Therapy, September 2006, pages
121–127; American Journal of Clinical Dermatology, July
2006, pages 223–230; and Journal of the American Academy
of Dermatology, May 2006, Supplemental, pages 272–281).
Surprisingly, there is even research showing that workers
who handle pure hydroquinone actually have lower incidences
of cancer than the population as a whole (Source: Critical
Reviews in Toxicology, May 1999, pages 283–330). Research
to the contrary was done either using products contaminated
with other ingredients or was performed on mice using
high concentrations of hydroquinone—and that doesn’t equate
to the levels of hydroquinone used in topical, over-the-counter
skin-care products. Further evidence that this proposed
ban doesn’t make sense comes from the American Academy
of Dermatology (AAD), who doesn’t agree with the FDA’s
proposal—yet the AAD stands to gain the most if consumers
can only obtain hydroquinone products with a dermatologist’s
prescription.
The negative research about hydroquinone and the frightening
assertions being levied in the media are not related to
how this effective ingredient is used in skin-care products
sold in the United States. It has been, and still is,
the most effective topical agent for fading and/or eliminating
sun- or hormone-induced brown skin discolorations.
Because of hydroquinone's action on the skin, it can
be a skin irritant, particularly in higher concentrations
of 4% or greater and predictably when combined with tretinoin.
Some medications have been created that combine 4% hydroquinone
with tretinoin and a form of cortisone. The cortisone
is included as an anti-inflammatory. The negative side
effect of repeated application of cortisone is countered
by the positive effect of the tretinoin so it doesn't
cause thinning of skin and damage to collagen (Source:
Drugs in Dermatology, July-August 2004, pages 377-381).
Hydroquinone can be an unstable ingredient in cosmetic
formulations. When exposed to air or sunlight it can turn
a strange shade of brown. Therefore, when you are considering
a hydroquinone product, it is essential to make sure it
is packaged in a non-transparent container that doesn't
let light in and minimizes air exposure. Hydroquinone
products packaged in jars are not recommended because
they become ineffective shortly after opening.
Alternatives to Hydroquinone
Although hydroquinone has the highest efficacy and a long
history of safe usage behind it, there are other alternatives
that have shown some promise for lightening skin. But
these have been far less researched and often pale in
comparison to hydroquinone. It is interesting to point
out that some of these alternative ingredients are, ironically,
derivatives of hydroquinone. They include Mitracarpus
scaber extract, Uva ursi (bearberry) extract, Morus bombycis
(mulberry), Morus alba (white mulberry), and Broussonetia
papyrifera (paper mulberry)—all of which contain arbutin
(more technically known as hydroquinone-beta-D-glucoside)—which
can inhibit melanin production. Pure forms of arbutin
are considered more potent for affecting skin lightening
(alpha-arbutin, beta-arbutin, and deoxy-arbutin).
Other options with some amount of research regarding
their potential skin lightening abilities are licorice
extract (specifically glabridin), azelaic acid, and stabilized
vitamin C (L-ascobic acid, ascorbic acid, and magnesium
ascorbyl phosphate). What has not been conclusively established
for most of these hydroquinone alternatives is how much
is needed in a cosmetic lotion or cream to obtain an effect.
There is also a small amount of research showing oral
supplements of pomegranate extract, ellagic acid, vitamin
E, and ferulic acid can inhibit melanin production. All
of these options are worth considering and experimenting
with. However, compared to the extensive research concerning
hydroquinone's effect on inhibiting melanin production,
these alternatives may very well disappoint, but their
natural allure is hard for consumers to ignore (Sources:
Experimental Dermatology, August 2005, pages 601-608;
Bioscience, Biotechnology, and Biochemistry, December
2005, pages 2368-2373; International Journal of Dermatology,
August 2004, pages 604-607; Journal of Drugs in Dermatology,
July-August 2004, pages 377-381; Facial and Plastic Surgery,
February 2004, pages 3-9; Dermatologic Surgery, March
2004, pages 385-388; Journal of Bioscience and Bioengineering,
March 2005, pages 272-276; Journal of Biological Chemistry,
November 7, 2003, pages 44320-44325; Journal of Agriculture
and Food Chemistry, February 2003, pages 1201-1207; International
Journal of Cosmetic Science, August 2000, pages 291-303;
and Anti-Cancer Research, September-October 1999, pages
3769-3774).
Arbutin
A bit more information on arbutin is warranted. As mentioned
above, arbutin contains a form of hydroquinone derived
from the leaves of bearberry, cranberry, mulberry or blueberry
shrubs, and also is present in most types of pears. Because
of arbutin's hydroquinone content it can have melanin-inhibiting
properties (Source: The Journal of Pharmacology and Experimental
Therapeutics, February 1996, pages 765-769). Although
the research describing arbutin's effectiveness is persuasive
(even if most of the research has been done in vitro),
concentration protocols have not been established. That
means we don't know how much arbutin it takes to lighten
skin when it is added to a cosmetic formulation. Moreover,
most cosmetics companies don't use "arbutin"
in their products because there are patents controlling
its use for skin lightening. To get around this problem
many cosmetics companies use plant extracts that contain
arbutin. Unfortunately, there is little to no research
showing the plant extract source of arbutin as having
any impact on skin, especially not in the tiny amounts
used in cosmetics.
The only products available with a rather high concentration
of arbutin (about 5%) are Shiseido's Whitess Intensive
Skin Brightener ($120 for 1.4 ounces), Shiseido's Luminizing
Night Essence ($75 for 1.3 ounces), and Shiseido's Cle
de Peau The Cream ($500 for 1 ounce). Despite the pricing
disparity, these formulations have far more in common
than they do differences. Be forewarned: The Cream comes
in jar packaging, which will not keep the arbutin stable
for very long after opening.
Tretinoin
A great deal of research has shown that the use of tretinoin
(also known as all-trans retinoic acid as found in the
prescription medication Renova and Retin-A) can only be
somewhat effective in treating skin discolorations (Sources:
Dermatologic Surgery, March 2006, pages 365-371; Acta
Dermato-Venereologica, July 1999, pages 305-310; International
Journal of Dermatology, April 1998, pages 286-292; and
Journal of the American Academy of Dermatology, March
1997, pages S27-S36). However, the skin's response to
tretinoin is far more noticeable and impressive when it
is used in combination with hydroquinone or azelaic acid.
Because of this, tretinoin is generally not recommended
as the only topical option for melasma but is best used
for the purpose of reducing darkened areas of skin in
combination with other effective topicals, particularly
sunscreen and hydroquinone (Source: eMedicine Journal,
www.emedicine.com http://www.emedicine.com, November 15,
2001).
Even though tretinoin by itself can be disappointing
for skin lightening, this should in no way diminish its
role in the improvement of skin's healthy cell production,
collagen production, elasticity, texture, and dermal thickness.
Tretinoin, combined with more effective skin-lightening
treatments, is a powerful ally in the battle against sun-damaged
and aged skin.
Alpha Hydroxy Acids
Alpha hydroxy acids (AHAs)—primarily in the form of lactic
acid and glycolic acid—are the most researched forms of
AHAs because they have a molecular size that allows effective
penetration into the top layers of skin. It is generally
assumed that in and of themselves AHAs in concentrations
of 4% to 15% are not effective for inhibiting melanin
production and won't lighten skin discolorations in that
manner. Rather, it is believed that their benefit is in
helping cell turnover rates and removing unhealthy or
abnormal layers of superficial skin cells (exfoliation)
where hyperpigmented cells can accumulate. However, other
research has shown that lactic and glycolic acids can
indeed inhibit melanin production separate from their
actions as an exfoliant on skin (Source: Experimental
Dermatology, January 2003, supplemental. pages 43-50).
Either way, there is a good amount of evidence that in
combination with other treatments—such as hydroquinone,
azelaic acid, laser resurfacing, and, of course, an effective
sunscreen—AHAs can be very effective for improving the
overall appearance of sun-damaged skin and possibly helping
other ingredients better penetrate skin. While there is
no comparative research in regards to salicylic acid (BHA)
and its effect on melasma, it makes sense to assume that
because salicylic acid exerts a similar action on skin
as AHAs, it will have similar results for improving skin
color.
Much like laser treatments, alpha hydroxy acid peels
(using 50% concentrations or greater) have impressive
results for removing skin discolorations (Sources: Dermatologic
Surgery, February 2005, pages 149-154; Journal of Cutaneous
Medicine and Surgery, April 2004, pages 97-102; Cutis,
February 2004, supplemental, pages 18-24; Dermatologic
Therapy, June 2004, pages 196-205; and Dermatological
Surgery, June 1999, pages 450-454). Only a physician should
perform these types of facial peels.
Kojic Acid
Kojic acid is a by-product in the fermentation process
of malting rice for use in the manufacturing of sake,
the Japanese rice wine. There is convincing research—both
in vitro (in a test tube) and in vivo (on a live subject)—showing
kojic acid to be effective for inhibiting melanin production
(Source: Archives of Pharmacal Research, August 2001,
pages 307-311). Glycolic or kojic acid, or glycolic acid
with hydroquinone, are highly effective in reducing the
pigment in melasma patients (Source: Dermatological Surgery,
May, 1996 pages 443-447). So why aren't there more products
available containing kojic acid? Because it is an extremely
unstable ingredient in cosmetic formulations. Upon exposure
to air or sunlight it can turn a strange shade of brown
and lose its efficacy. Many cosmetic companies use kojic
dipalmitate as an alternative because it is far more stable
in formulations. However, there is no research showing
kojic dipalmitate to be as effective as kojic acid, although
is it a good antioxidant. Further, some controversial
research has shown kojic acid to have some carcinogenic
properties (Sources: Mutation Research, Genetic Toxicology
and Environmental Mutagenesis, June 2005, pages 133-1450
and Toxicological Sciences, September 2004, pages 43-49).
Azelaic Acid
Azelaic acid is a component of grains, such as wheat,
rye, and barley. It is effective against a number of skin
conditions when applied topically in a cream formulation
at a 20% concentration. Azelaic acid is recommended to
treat acne, but there also is research showing it to be
effective for skin discolorations. For example, "The
efficacy of 20% azelaic acid cream and 4% hydroquinone
cream, both used in conjunction with a broad-spectrum
sunscreen, against melasma was investigated in a 24-week,
double-blind study with 329 women. Over the treatment
period, the azelaic acid cream yielded 65% good or excellent
results; no significant treatment differences were observed
with regard to overall rating, reduction in lesion size,
and pigment intensity. Severe side effects such as allergic
sensitization or exogenous ochronosis were not observed
with azelaic acid" (Source: International Journal
of Dermatology, December 1991, pages 893-895). Other research
also indicates azelaic acid is an option for inhibiting
melanin production (Source: Journal of the American Academy
of Dermatology, May 2006, supplemental, pages 272-281).
However, additional research suggests that azelaic acid
is more irritating than hydroquinone mixed with glycolic
acid (Source: eMedicine Journal, www.emedicine.com, November
5, 2001). Regardless, azelaic acid is definitely a consideration
for skin lightening if you have had problems using hydroquinone.
Vitamin C
Magnesium ascorbyl phosphate, L-ascorbic acid, ascorbyl
glucosamine, and ascorbic acid are various forms of vitamin
C considered stable and effective antioxidants for skin.
There are very few studies showing them to have benefit
for inhibiting melanin production, but what little there
is has been positive. The problem is that the concentrations
of these ingredients were high (more than 5%), which is
rarely used in cosmetic formulations. However, in combination
with other treatments, vitamin C is an extra step that
can help reduce skin discolorations (Sources: International
Journal of Dermatology, August 2004, page 604; Dermatology,
April 2003, pages 316-320; and Journal of the American
Academy of Dermatology, January 1996, pages 29-33).
Laser Treatments
Both ablative and nonablative lasers can have a profound
effect on melasma. However, the results are not always
consistent, and problems can occur (such as hypo- or hyperpigmentation).
Moreover, laser treatments of this kind often are a problem
for those with darker skin tones. Nonetheless, when laser
treatments work they can have a marked difference in the
skin's appearance, especially when used in combination
with the other topical treatments previously mentioned.
The results can be startling, and though expensive, for
stubborn discolorations, lasers are absolutely worth a
try. There are many types of lasers that can be successful
for this purpose. Which one is optimal for you is best
determined by a skilled dermatologist who has a practice
that incorporates a variety of different lasers (Sources:
Journal of the American Academy of Dermatology, May 2006,
supplemental, pages 262-271; Dermatologic Therapy, January
2001, page 46; Journal of Cosmetic and Laser Therapy,
March 2005, pages 39-43; Journal of Cutaneous Medicine
and Surgery, April 2004, pages 97-102; Journal of Drugs
in Dermatology, November-December 2005, pages 770-774;
Dermatologic Surgery, October 2005, page 1263; and Lasers
in Surgery and Medicine, April 2000, pages 376-379).