Common questions about skin lightening.
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Sat Aug 06, 2005 4:40 pm

Good day, I was wondering if you guys could help me with a couple of questions about skin lightening.

I have my eye on lemon juice, and have been using it for a couple of weeks. I have lightened a little bit, but not how I'd like.
Unlike most people, I am trying to lighten my overall skin colour and not just freckles. Here are my questions:

1. Does leaving lemon juice on the face overnight make any difference?

2. Does leaving it on for one hour give it it's fading potential or must it be on longer?

3. Does it take a while? Should I keep using it?

4. Anyone have any other suggestions about how to lighten skin without using Hydroquinone (I am afraid of it because I hear it harms the skin)

5. Does wearing 60+ SPF sunscreen 24/7 help?

I am a white male with a heavy tan (even in the winter), the the areas of my skin that doesn't receive much sunlight (i.e. upper arms, feet, legs) are ivory, and I was very fair when I was a little kid, does that mean that I can potentially get my face that way? I tan very easily, but want to be very light. Is it possible? Any feedback would be appreciated, thanks.

Brandt

Sat Aug 06, 2005 8:25 pm

If your skin is naturally very fair then you should be able to get that back. I think the most critical product would be a very high SPF sunblock and also wearing hats, long sleeves etc to protect those areas from the sun, and trying to stay out of the sun more in general.

Lemon juice in itself does not sound like a good idea because it is very drying for the skin. Perhaps you could look into products that have Kojic Acid (natural alternative to Hydroquinone)?

Sat Aug 06, 2005 8:59 pm

Well, you see the thing is that like I said, places like my upper arms, legs and feet are very white because they have not been exposed to the sun in a long time. Does that mean I could get my face that way? I have medium brown hair, but dye it blonde because my skin has a lot of rosyness in it so it works well, and I am not REALLY dark.

Part of the reason I am always so tan is probably because I live in New Mexico, which gets a great deal of sunlight. But doesn't that fact that some parts of are white (and it's an even white, not blotchy) mean that I can get my face that way? Really dark people do not get white anywhere.

Sun Aug 07, 2005 3:31 am

Well, I think you can in theory but it's going to be difficult to get it AS white because the other parts are never exposed to the sun. High SPF, regular exfoliation (with something skin brightening like Dermalogica Microfoliant for example), should help you. Kojic Acid might help as well.

free skin care · Sun Aug 07, 2005 5:38 am

I agree with Mabsy. Lemon juice is really not a good idea in my opinion. I would use a cleanser with glycolic acid. It will mildly exfoliate everyday. As well, you need a high SPF sunscreen. Like an SPF 60. I use and love La Roche Posay Fluide Extreme 60 for superior protection. It is not available in the States, so it has to be order online from Europe. I usually buy 4 or 5 at a time as I don't want to run out. It has totally saved my skin this summer. On your body, you don't need the FE; just the regular LPR 60 cream would be good.

I also think the Kojic acid is a good idea. Check out some of these products from Skin Terra. There are many with AHAs/BHAs and Kojic Acid. All of these things will help you over time. http://www.skinterra.com/product/lines/peterthomasroth2.html
It won't be over night, but you will get results after a few months. Don't forget the sunscreen though. 10 Mins without it will undo all the repairing you have done. Also, I don't think 24/7 is necessary. Just during the day time. When it is dark, you don't need it. And, don't forget to re-apply when you spend time outside. Very Happy

Sun Aug 07, 2005 12:15 pm

Anyone know is cucumber juice has the same effect? I was wondering because I heard about it on a different website.

Also, has anyone here USED kojic acid? Any bad side effects?

free skin care · Sun Aug 07, 2005 5:58 pm

Kojic Acid is one of the ingredients in my C serum. I have used it for months without any ill effects. I haven't noticed any whitening really, but I am already super fair. I have an African American friend that uses the same C serum. She likes it because she says it helps fade any scars, which are darker, but it does not alter her actual skin colour.

free skin care · Mon Aug 08, 2005 10:06 am

If you live in New Mexico, even if you are able to get your skin to lighten, you are constantly going to be fighting your skin's natural tendency to tan. In order to achieve real skin lightening, you need a holistic approach:

1. Lightening Agent: You need to be using a treatment product that is designed to break up the melanin in your skin. Kojic acid is good for uneven pigmentation (freckles, sun spots), but will not lighten large areas of your body evenly. Hydroquinone will lighten large areas of your skin, but is not photostable. What that means is if you use hydroquinone alone, you will get rebound pigmentation whenever you are in the sun - even for a short time.
Also, for either of these to have the drastic effects that I think you may be looking for, they would need to be applied in a high concentration (4% starts prescription strength) over an extended treatment period. If you would be using them on your arms, legs, back, etc. then I would be concerned about toxicity issues as well. They are safe for use on small skin areas (face or tops of hands), but may cause a hyper immune response in some sensitive individuals, and possible liver stress if used over an extended period of time (years) in people with existing liver dysfunction or fatty livers.

2. Pigmentation Supressor: This is the second most important aspect of skin lightening. In hyper-pigmented areas, the mature melanocyte has a definitive “memory”. It is the belief of the scientific community that this “memory” can cause a rapid reverse to the original condition of pigmentation if the treatment course is not supported by the use of an FDA approved sunscreen, when exposed to even the most moderate sun exposure.

3. Exfoliation: In addition to the lightening agent & pigmentation supressor (sunscreen), the addition of a peel of some type will expedite the lightening process. Appropriate peels & regenerative agents would be: ascorbic acid, glycolic acid, salicylic acid, retinoic acid, and activated enzymes.

In short, lemon juice would do nothing except irritate & dry out your skin. It also is a photosensitizer, so the next time you went out in the sun (even with sunscreen), you would most likely burn & then that would tan anyway.
If you did start a lightening regimen, you would have to be diligent & do it every day (except the peels, of course). Sunscreen is a must, as others have said. Also it is suggested that you limit your sun exposure to no more than 15 minutes a day. Wide-brimmed hats, long sleeves, and long pants will help, although are probably not practical given the climate where you live.

I hope I was able to help a little bit. Serious skin lightening is very tricky and can very easiy backfire. If you are serious, I would suggest getting professional treatments from a medical esthetician. Drastic lightening of large skin areas is not something you can achieve with lemon juice in your shower.
Good luck!
-Darren
Smile

free skin care · Mon Aug 08, 2005 11:16 am

I have used Skinceuticals phyto+ with kojic acid with great results. It is also good for oily acnaic skin.

Fri Aug 26, 2005 12:58 pm

Could some one intsruct Skinceuticals phyto+ with kojic acid and SPF 60 ?

I have same problme as above. I face color is different from Bodya and my Neck too. Plz help.

Fri Aug 26, 2005 12:59 pm

is this a good Sunblock cream ?

http://www.walgreens.com/store/product.jsp?id=prod600131&CATID=100802&skuid=sku600118&V=G&ec=frgl_695409

free skin care · Sat Aug 27, 2005 10:58 pm

EliteBlondeSociety, I don't mean to offend but I'm curious as to why you have that as your pseudonym when you mentioned you are not blonde, but had your hair colored blonde.

If you like just to even out your skin color on all parts of your body, it would be easier to tan the lighter areas than to lighten the darker areas. But if you prefer to be lighter, you may want to investigate some regimen from users at

http://excoboard.com/exco/forum.php?forumid=65288&PHPSESSID=76eb848396357d3afacc71a82d20756e

or

http://www.askmehelpdesk.com/forum/forumdisplay.php?f=296&page=1&sort=lastpost&order=&pp=20&daysprune=365

The most popular products there are Makari and Dermisoft (O'tentika & Hypercreme). A few mentions of Godiva, Thienna, Herbal Inn, Glutathione pills, Fair&Flawless, Fair&White, WhiterSkin, Cellbone Technology, Magic Cream, Sennine, Awanshine, among others.

Here's an article I got from Biochemistryof Beauty.com which is a pay forum.

Quote:

Non-phenolics

Azelaic acid
Azelaic acid (15-20%) has been used to treat melasma, but is FDA-approved only for acne. It has selective skin lightening effects on excessively active melanocytes; there are minimal effects on normally pigmented skin. It can be a photosensitizer and may otherwise irritate. It is isolated from Pityrosporum ovale and is a weak inhibitor of tyrosinase. It is prescribed topically as a 20% cream and has been combined with glycolic acid (15% and 20%), its efficacy has been compared with HQ 4% in the treatment of hyperpigmentation in dark-skinned patients. The combination is as effective as HQ 4% cream, with a slightly greater irritation. Low concentrations of azeleic acid are used in many OTC lightening products.
Studies have shown that topical 20 percent azelaic acid is superior to 2 percent hydroquinone[48] and as effective as 4 percent hydroquinone for melasma [49] without the undesirable side effects. Tretinoin enhances the effect, yielding more skin lightening after three months than azelaic acid alone, with a greater proportion of excellent response. The effect of azelaic acid can be attributed to its ability to inhibit the energy production and/or DNA synthesis of hyperactive melanocytes, and partially to its antityrosinase activity.[50] This may also account for the beneficial effect on postinflammatory hyperpigmentation. The combination can also destroy malignant melanocytes.[51]
Azelaic acid is a naturally occurring saturated dicarboxylic acid. It has an antiproliferative and cytotoxic effect on the human malignant melanocyte, and may arrest the progression of cutaneous malignant melanoma. The mechanism may possibly be related to its inhibition of mitochondrial oxidoreductase activity and DNA synthesis.[52], [53] One study found that topical azelaic acid led to complete and durable resolution of lentigo maligna in more than 50 patients.[54]

Kojic acid (5-hydoxy-4-pyran-4-one-2-methyl)

Kojic acid is a fungal metabolic product produced by many species of Aspergillus (used in the production of miso, shoyu, and sake), Acetobacter, and Penicillium. Kojic acid is a free radical scavenger used as a food additive to prevent enzymatic browning. It acts as a competitive and reversible inhibitor of polyphenol oxidases, xanthine oxidase, and D- and some L-amino acid oxidases, [55] including the catecholase activity of tyrosinase, the rate-limiting, essential enzyme in the synthesis of melanin. It may involve the rapid formation of an enzyme inhibitor complex that undergoes a relatively slow reversible reaction.[56] It is effective in concentrations of 1-4%.
Although it is an effective lightener, it is also a sensitizer and irritant. A clinical trial evaluated the efficacy of glycolic acid/hydroquinone and glycolic acid/kojic acid for 39 melasma patients. Patients were treated with kojic acid on one side of the face and hydroquinone in a similar vehicle on the other side of the face. Fifty-one percent of the patients responded equally to hydroquinone and kojic acid. Twenty-eight percent had a more dramatic reduction in pigment on the kojic acid side; whereas 21% had a more dramatic improvement with the hydroquinone formulation. The kojic acid preparation was more irritating.[57]
On exposure to air or sunlight, or water kojic acid turns brown and loses efficacy. Efficacy also declines with product age.[58] Some manufacturers use kojic dipalmitate instead kojic acid because it is more stable, but there have been no clinical trials demonstrating its efficacy. If kojic acid is used, it should be in a waterless vehicle and it should be applied only at night.
Scientists have synthesized a stable derivative of kojic acid, 5-[(3-aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one (Kojyl-APPA), which is converted to kojic acid enzymatically in cells. In melanoma cells, Kojyl-APPA decreased melanin content to 75% of control and in normal human melanocytes, decreased neomelanin synthesis to 43% of control. Its permeation through skin is nearly an order of magnitude higher than that of kojic acid.[59]
Kojic acid has recently been banned for use as a depigmenting agent in Korea because Japanese dermatologists have found that kojic acid may promote liver cancer. The ban will remain in effect until the Korea Food and Drug Administration proves the safety of the ingredient.[60],[61]

Niacinamide
Niacinamide (nicotinamide) is an effective skin lightener that works by inhibiting melanosome transfer from melanocytes to keratinocytes. Proctor and Gamble reported on the efficacy of of 3.5 percent niacinamide with retinyl palmitate for hyperpigmentation and wrinkles at the 2002 American Academy of Dermatology meeting. Clinical trials involving 18 Japanese subjects with hyperpigmentation who used 5% niacinamide or vehicle, and 120 subjects with tans who used vehicle, sunscreen and 2% niacinamide, or sunscreen alone revealed that niacinamide significantly decreased hyperpigmentation and increased skin lightness compared with vehicle alone after 4 weeks.[62]

Green Tea and other polyphenols
Some manufacturers are selling green tea and other polyphenols as lighteners. Kanebo includes green tea in its Koakuma whitening serum, but there may be other herbs in the formula. Asian cosmetic firms tend to be secretive about their formulations. Until there is full compliance with EU labelling regulations and clinical trials are conducted, the details will remain a mystery.[63]

Paper mulberry
A 0.4% concentration of paper mulberry extract inhibits tyrosinase by 50% compared to 5.5% for HQ and 10.0% for kojic acid. At 1% paper mulberry extract is not a significant irritant.[64]

Licorice extracts
Glabridin, the main ingredient in licorice extract, is an inhibitor of tyrosinase activity. It is not cytotoxiic. A 0.5% concentration has been shown to inhibit UV-B–induced pigmentation and erythema. It is also an anti-inflammatory due to ihibition of superoxide anion production and cyclooxygenase activity.[65]
Glabrene and isoliquiritigenin also inhibiti tyrosinase-dependent melanin biosynthesis and may serve as skin-lightening agents.[66]
In a clinical trial, 20 women with melasma were treated with liquiritin on one side of the face and vehicle on the other side twice daily for 4 weeks. Subjects avoided sun exposure and/or used topical sunscreen during the treatment. Researchers concluded that liquirtin improved melasma.[67]

Alpha tocopherol and alpha tocopherol ferulate

Oral vitamin E (alpha tocopherol) may effectively treat hyperpigmentation, especially when combined with vitamin C. In addition to its antioxidant activity, iti is also an inhibitor tyrosinase activity. Alpha tocopheryl ferulate is an ester of alpha tocopherol with ferulic acid. Ferulic acid is also an antioxidant and can absorb UV, which results in enhanced stability. Both alpha tocopherol and alpha tocopherol ferulate inhibit melanin formation efficiently when compared to arbutin, kojic acid, magnesium L-ascorbyl 2-phosphate and tranexamic acid. They suppress tyrosinase activity and polymerization of 5,6-dihydroxyindole-2-carboxylic acid to melanin.[68],[69],[70]

Arctostaphylos patula and Arctostaphylos viscida
Fifty percent extracts in ethanol from the leaves of 2 Arctostaphylos plants, A. patula and A. viscida, showed potent inhibition against tyrosinase in the labe. They not only inhibited the production of melanin from dopachrome by autoxidation, but also exhibited superoxide dismutase-like activity as well as moderate absorbance in UVB.[71] The effective topical concentration for hyperpigmentation disorders is not known. A. uva ursi is also effective, but slightly less so. Pentapharm markets a product called Melfade containing A. uva ursi and magnesium ascorbyl phosphate.

Melatonin
Melatonin is secreted by the pineal gland in response to sunlight. It is an inhibitor of melanogenesis. It does not affect tyrosinase activity; but may work at the posttyrosinase step in melanin biosynthesis. It inhibits adenosine 3',5'-cyclic phosphate (cAMP) driven processes in pigment cells. The concentration for hyperpigmentation disorders has not been established, however, a cosmetic manufacturer reports melatonin as an effective antioxidant at a concentration of 1%. It is also anti-inflammatory.[72],[73]

Magnesium ascorbyl phosphate
Ascorbic acid (AA) is a known inhibitor of melanogenesis. However, AA oxidizes rapidly in aqueous solutions and is not generally useful as a depigmenting agent. One study investigated the depigmenting ability of magnesium-L-ascorbyl-2-phosphate (VC-PMG), a stable derivative of AsA. 10% VC-PMG cream provided significant lightening effect in 19 of 34 patients with chloasma or senile freckles and in 3 of 25 patients with normal skin.[74] MAP has a protective effect against skin damage induced by UV-B irradiation.[75]
A total of 120 Japanese female volunteers aged 25-60 years with solar lentigines were treated for 6 months with 3% magnesium ascorbyl phosphate (MAP), a stable form of vitamin C, on one side of the face and vehicle on the other side. SLM significantly reduced the total area of hyperpigmented spots after one month of treatment compared to the vehicle, with no significant variation in facial skin colour tone in the areas outside the hyperpigmented spots. The total area of hyperpigmented spots 6 months after discontinuing the treatment had returned to pre-treatment levels.[76]
Researchers investigating novel L-ascorbic acid (vitamin C) derivatives found that a hydrophilic derivative, 2-O-(5-hydroxy-4H-pyran-4-one-2-methyl)-L-ascorbic acid (1), exhibited good thermal stability and inhibitory activities against tyrosinase catalyzed melanin formation, AOS, and free radicals compared to vitamin C and its conventional derivatives (such as the 2-phosphate 6-stearate and 2.6-dipalmitate, and 2-O-octadecylascorbic acid), as well as vitamin E, kojic acid, and arbutin. They also found a synergistic effect when vitamin C and kojic acid were combined.[77]

Tretinoin

Retinoids accelerate desquamation and remove preformed melanin. They are generally, but not always, irritating. Tretinoin (retinoic acid, RA, all-trans retinoic acid) 0.05-0.1% is used in the treatment of acne and to decrease the signs of sun damage and normal aging skin, including roughness, fine lines, and hyperpigmentation. Redness, dryness, and scaling are frequent at onset of therapy. These reactions may decrease with time, but sometimes requires an adjustment in the dose or discontinuation. In depigmentation, tretinoin exfoliates discolorations and provides for better penetration of other actives. In some clinical trials it has been used successfully to combat pigmentation problems on its own but it is often used concomitantly with other depigmenting agents. Other retinoids may also be used, with tazarotene likely to be more successful (and more irritating), while adapalene, retinol, retinaldehyde, and retinyl acetate may be less aggressively corrective of pigmentation problems.
RA does not directly inhibit melanogenesis. Neither does it influence interactions between melanocytes, keratinocytes and fibroblasts in the pigmentation process. The role of RA in bleaching is likely to be due to its promotion of keratinocyte proliferation and acceleration of epidermal turnover.[78] During the course of treatment for photodamaged skin, most of its actions are directed at restoring the skin to the pre-sun-damaged state.[79]
Thirty-eight women completed a randomized, vehicle-controlled study, in which they applied 0.1% tretinoin or vehicle cream once daily to the face for 40 weeks. At the end of treatment 68% of the tretinoin-treated patients were clinically rated as improved or much improved, compared with 5% in the vehicle group. Significant improvement first occurred after 24 weeks. Epidermal pigment was reduced 36%, compared with a 50% increase with vehicle. Side effects of erythema and desquamation occurred in 88% of tretinoin-treated and 29% of vehicle-treated patients. Topical 0.1% tretinoin produces significant clinical improvement of melasma, mainly due to reduction in epidermal pigment, but improvement is slow.[80]
In another study, 15 middle aged or elderly patients with chronic solar damage of the skin, eight patients with melasma and three patients with xeroderma pigmentosum were treated with topical tretinoin for 6 months. No significant change was induced in melasma despite the improvement in smoothness of the skin surface.[81]
For liver spot treatment, 58 patients completed a 10-month study in which they applied either 0.1 percent tretinoin or vehicle cream daily. After one month of treatment the patients treated with tretinoin had significant lightening of hyperpigmented lesions as compared with the patients who received vehicle. After 10 months, 83 percent of patients treated with tretinoin had lightening of their lesions, compared with 29 percent of the patients who received vehicle. Compared with vehicle, tretinoin caused a significant decrease in the degree of epidermal pigmentation. Lesions that had disappeared during the first 10 months of tretinoin treatment did not return in any patient, and patients who continued to use tretinoin had further improvement.[82]
A study on emollient cream formulations of topical tretinoin at concentrations of 0.05% and 0.01% were examined in 251 subjects with mild to moderate photodamaged skin. Seventy-nine percent of the subjects who received 0.05% tretinoin for 24 weeks showed overall improvement in photodamaged skin compared with improvement in 48% of the vehicle-treated control subjects. Significant reductions were found in melanin content and mottled hyperpigmentation after 0.05% tretinoin therapy when compared with controls. Side effects of erythema, peeling, and stinging were usually mild and well tolerated.[83]
A study on black patients examined the efficacy of topical 0.1% all-trans-retinoic acid (tretinoin) in the treatment of melasma in Twenty-eight patients in a 10-month, randomized, vehicle-controlled clinical trial in which they applied either 0.1% tretinoin or vehicle cream daily to the entire face. After 40 weeks, there was a 32% improvement compared with a 10% improvement in the vehicle group. The skin epidermal pigmentation was decreased in the tretinoin group compared with the vehicle group. Side effects were limited to a mild "retinoid dermatitis" occurring in 67% of tretinoin-treated patients.[84]
In 40-week trial on topical tretinoin (0.1 percent retinoic acid cream), 24 subjects applied tretinoin daily and 30 subjects applied vehicle cream. The facial post-inflammatory hyperpigmented lesions of the tretinoin-treated subjects were significantly lighter after the 40 weeks of therapy than those of the vehicle-treated subjects; overall improvement was first noted after four weeks of treatment. A 40% lightening in lesions toward normal skin color was observed in the tretinoin-treated lesions, as compared with an 18% lightening in vehicle-treated lesions. Epidermal melanin content in the lesions decreased by 23% with tretinoin and by 3% with vehicle. Normal skin was minimally lightened by tretinoin as compared with vehicle. Retinoid dermatitis developed in 12 of the 24 tretinoin-treated subjects but diminished as the study progressed.[85]
A trial to assess the efficacy of 0.1% tretinoin cream treatment for hyperpigmented lesions associated with photoaging was conducted on Chinese and Japanese patients. Forty-five photoaged patients applied 0.1% tretinoin cream and 24 applied vehicle cream once daily for 40 weeks. At the end of treatment, hyperpigmented lesions were lighter or much lighter in 90% of patients receiving tretinoin compared with 33% receiving vehicle. a 41% decrease in epidermal pigmentation with tretinoin therapy as compared with a 37% increase in the vehicle group.[86]

Tretinoin peel

In a trial on peeling with tretinoin, after five sessions of twice weekly peeling in concentrations of 1-5% on 15 females, good results for melasma were orbtained. The peels were practical, quick, and easily accomplished with no side effects.[87]

isotretinoin

A trial investigated the efficacy of topical 0.05 per cent isotretinoin gel (Isotrex) in the treatment of melasma in Thai patients. Thirty patients with moderate to severe melasma entered a 40-week, randomized, vehicle-controlled clinical trial in which they applied either 0.05 per cent isotretinoin gel, or its vehicle base together with a broad spectrum sunscreen (SPF 2 Cool

daily to the entire face. After 40 weeks, there was no statistically significant difference between the isotretinoin and vehicle groups. Side effects were limited to a mild transient "retinoid dermatitis" occurring in 27% of isotretinoin-treated patients. Daily use of broad spectrum sunscreen alone had a significant lightening effect on melasma in Thai patients.[88]

Retinol

Ten-percent ROL gel was used in a trial incorporating a two-phased bleaching protocol (bleaching and healing phases); 5% hydroquinone and 7% lactic acid ointment were used along with ROL gel in the bleaching phase (2 to 6 weeks). Five-percent hydroquinone and 7% ascorbic acid ointment were used alone during the healing phase (4 to 6 weeks). Improvement of pigmentation was seen in 16 of 18 patients after an average treatment period of 11.3 weeks, and in 6 patients, pigmentation was almost eliminated after treatment. Erythema and scaling were seen.[89]

Glycolic acid

Multiple creams and lotions are available that contain lower concentrations of glycolic acid, often in combination with other skin lightening agents. Glycolic acid can cause skin irritation, scaling, redness and itching. It helps other actives to penetrate better, can provide light exfoliation and also helps treat conditions like acne or aging skin changes. Many lightening formulations include it.

Mandelic acid

Mandelic acid at 10% has been reported to improve melasma up to 50% after 1 month of treatment. Faintly pigmented lentigenes respond much more slowly-a result characteristic of treatment with other AHA products-with gradual fading over a period of weeks or months. Dermal melasma, which is normally resistat to treatment, was also improved with mandelic acid, but responded much more slowly than epidermal melasma. Mandelic acid may be particularly useful in darker skin types.[90]

Peels

Peels that are more than very superficial are risky therapy for those with pigmentation problems. The skin may become blotchy and uneven. Many damaged melanocytes are in dermis where peels cannot reach. Peeling may provide good initial results but with time, hyperpigmentation may worsen. Peeling may kill epidermal hyperpigmented cells but the deeper melanocytes that remain untouched will find other cells to attach to and transfer pigment to so that hypepigmentation is likely to return.[91]
Glycolic when applied as a 50-70% solution can reduce pigmentation in the skin after the peeling process subsides. Some chemical peels of moderate depth, using low-concentration trichloroacetic acids or Jessner's solution, may reduce the epidermal pigmentation of melasma. Weak chemical peels containing alpha hydroxy acids do not generally provide any improvement.
One trial evaluated the efficacy of superficial peels in conjunction with topical tretinoin and hydroquinone in patients with melasma. There was an overall decrease in melasma area and severity of 63%; peels hastened the effects of topical therapy.[92]

In another trial, serial glycolic acid peels were found to provide additional improvement when combined with a time-tested topical regimen, a modification of Kligman's formula (hydroquinone 5%, tretinoin 0.05%, hydrocortisone acetate 1% in a cream base). Forty Indian melasma patients were divided into two groups of 20 each. One group received serial glycolic acid peel combined with a topical regimen, modified Kligman's formula. The other, a control group, received only modified Kligman's formula. The group receiving the glycolic acid peels showed a trend toward more rapid and greater improvement, with statistically significant results. Only a few side effects were observed in the peel group.[93]
A trial using 10 Asian women with moderate to severe melasma investigated twice daily applications of a cream containing 10% glycolic acid and 2% hydroquinone (Neostrata AHA Age Spot and Skin Lightening Gel) to both sides of the face, and glycolic acid peels every 3 weeks (20-70%) to one-half of the face using Neostrata Skin Rejuvenation System. All patients had to use a sunblock (SPF 15). At 26 weeks (or after eight peels) the degree of improvement of pigmentation and fine facial wrinkling on each side of the face were assessed. Melasma and fine facial wrinkling improved on both sides of the face. The side that received glycolic acid peels did better but the results were not statistically significant.[94]
A trial on 25 nonpregnant Indian females involved the use of daily application of SPF15 sunscreen and 10% glycolic acid lotion at night for 2 weeks. Patients were then treated with 50% glycolic acid facial peel once per month for three consecutive months. Improvement in melasma was observed in 91% of patients. Patients with epidermal-type melasma demonstrated a better response to treatment than those with mixed-type melasma. The prepeel program followed by 50% glycolic acid facial peel once per month for three consecutive months proved to be an effective treatment modality in Indian patients without any significant side-effects.[95]
Twenty-one Hispanic women with bilateral epidermal and mixed melasma were enrolled in a split-faced prospective trial lasting 8 weeks to assess the efficacy of 4% hydroquinone cream vs 4% hydroquinone cream combined with glycolic acid peels. Patients underwent 20% to 30% glycolic acid peels every 2 weeks to one side of the face only in addition to twice-daily full-face application of 4% hydroquinone cream and SPF 25 sunscreen each morning. Hydroquinone treatment alone and treatment with the combination of hydroquinone and glycolic acid had a significant effect in reducing skin pigmentation compared with baseline. However, no significant difference was found using combination therapy compared with hydroquinone alone.[96]

TCA - tretinoin

A trial was conducted using 16 men with actinic damage including actinic keratoses. They were treated with a 40% trichloroacetic acid (TCA) chemical peel. Half were pretreated for 6 weeks with topical tretinoin; they also used tretinoin after the peel. Some improvement was noted in all patients. More rapid and even frosting was observed in the patients pretreated with tretinoin. Solar lentigines, actinic keratoses, and skin texture were the features of photoaging most affected. No statistically significant difference was found between patients treated with TCA and tretinoin (before and after peel) and those with TCA alone.[97]

TCA - tretinoin - salicylic

A methyl salicylate-buffered, croton oil-containing 50% salicylic acid ointment peel, following pretreatment with topical tretinoin and localized 20% trichloroacetic acid, is effective for removal of lentigines, pigmented keratoses, and actinically damaged skin from the hands and forearms. The ease of application, uniform results, decreased risk of scarring, and one-time application of this peel.[98]

Phenol

Deep phenol peels impair melanin synthesis, have a bleaching effect, and can obliterate actinic keratoses, mottling, and freckling.[99] However, they are likely to result in hypertrophic scarring if used on highly pigmented individuals.

Lasers

Currently available laser treatments generally aggravate melasma and are, therefore, best avoided. One study evaluated the erbium:YAG laser resurfacing in the management of refractory melasma. Ten female patients with melasma unresponsive to previous therapy of bleaching creams and chemical peels were included in this study. Full face skin resurfacing using an erbium: YAG laser (2.94 microm) was performed. There was marked improvement of the melasma immediately after laser surgery using the parameters outlined; however, between 3 and 6 weeks postoperatively, all patients exhibited post-inflammatory hyperpigmentation, Significant clinical improvement in the melasma was seen compared to the preoperative evaluation. Erbium:YAG laser resurfacing effectively improves melasma; however, the almost universal appearance of transient post-inflammatory hyperpigmentation necessitates prompt and persistent intervention. The use of this laser therapy is recommended only for refractory melasma.[100]
In patients with vitiligo, sometimes the greatest part of the skin has already lost its melanocytes. The remaining pigmented patches can be removed by using strong bleaching creams, but many adverse events have been reported with this treatment.. Eight patients with remaining pigmentation of the arms, hands, and face were treated once with a Ruby laser. In patients with a positive Koebner phenomenon, a permanent state of depigmentation was reached after laser therapy. None of the treated patients showed severe side-effects. Ruby laser treatment can be an effective, fast, and safe method for removing cosmetically disturbing remnants of normal pigmentation in vitiligo patients with a positive Koebner phenomenon.[101]

Kinetin
Kinerase may provide some improvement in fine lines and discolorations. It is very gentle but may be useful for dry or sensitive skin types.

Neogarobiose

Japanese researchersa at Kose recently found that Neoagarobiose, a disaccharide mouse cells, exhibited low cytotoxicity, and has a water-binding capacity exceeding that of hyaluronic acid.[102]

Steroids

15 patients with melasma were treated with betamethasone 17-valerate in a cream base containing DMSO. One patient with secondary pigmentation was also entered in the trial. In nine patients results were favourable and in three results were moderate.[103]

Cinnamic acid

One study evaluated the effects of aloin, cinnamic acid and 15 other kinds of natural chemicals on the activity of tyrosinase, in order to provide new insight for lightening agents in the treatment of hyperpigmentation disorders and cosmetic additives. Cadabine, paeonal, farrerol, evodin, cinnamic acid, aloin and sophorcarpidine had different levels of inhibition of tyrosinase. The inhibitory rates of cinnamic acid (2 mmol/L, 0.5 mmol/L), aloin (2 mmol/L) and the rest were significantly higher than that of hydroquinone (0.5 mmol/L) (P < 0.05). Tyrosinase activity can be greatly inhibited by cinnamic acid, aloin and sophorcarpidine.[104]

Linoleic acid

Lincomycin (LM) and linoleic acid (LA) can inhibit melanogenesis. Researchers investigated the efficacy of topical application of LM and LA in combination with betamethasone valerate (BV) in melasma patients. Forty-seven Korean females with melasma were enrolled in a 6-week, double-blind, randomized clinical trial. Patients were treated with one application of the vehicle (group A), 2% LM mixed with 0.05% BV (group B), or 2% LM mixed with 0.05% BV and 2% LA (group C) on the face every night. After 6 weeks, in comparison with the pre-treatment the average pigmentation score was 68.9%, compared with 98% in vehicle and 85.4% in group B. Seven patients (43.7%) in group C revealed more than moderate improvement in objective assessment, compared with none in group A and two patients (12.5%) in group B. There were no significant side effects.[105]

tannins

Low molecular weight tannins may prove to be effective as skin-lightening agents.[106]

soy

Soybean-derived serine protease inhibitors and soybean extracts alter skin pigmentation, suggesting that soymilk could be used as a natural alternative to skin lightening.[107]
Researchers examined natural agents that could exert their effect via the PAR-2 pathway. They found that soymilk and the soybean-derived serine protease inhibitors, soybean trypsin and Bowman-Birk, inhibit PAR-2 cleavage and reduce keratinocyte ingestion of melanin.[108]
One study tested azelaic acid, glycolic acid, and soy extract, which is reported to reduce pigmentation through interaction with the PAR-2 of keratinocytes. Azelaic acid and the soy extract led to significant skin lightening after a 3-week treatment. By contrast, glycolic acid showed an inconsistent effect. The depigmenting effect observed with the soy extract indicates that the inhibition of PAR-2 may new way to approach certain pigmentary disorders of the skin.[109]

20% azelaic acid v 5% ascorbyl glucosamine, 1% kojic acid and alpha-hydroxyacid esters v soy

In an Asian study, 50 women with solar lentigines applied products twice daily for 2 or 3 months. A 20% azelaic acid formulation, and one with 5% ascorbyl glucosamine, 1% kojic acid and alpha-hydroxy acid esters were not effective. A stabilized soy extract showed better but modest lightening effects.[110]

Licorice vs arbutin vs hydroquinone

A study evaluated the efficacy of topical arbutin 7% twice daily, licorice extract 0.1% twice daily, and 4% HQ once at night in 30 female patients with epidermal melasma. All subejcts received weekly MAP iontophoresis on the melasma areas of the right half of the face, avoided sun exposure and used SPF 28 every morning for 3 months. Improvement was statistically significant both in the HQ and arbutin group but the HQ group was significantly better than the arbutin group. No significant improvement was noted in the licorice group. Topical application of arbutin and licorice appeared to have marginal effect in treating melasma when compared to HQ, while MAP iontophoresis did not provide additional benefit.[111]

Pycnogenol
Pycnogenol is a standardized extract of the bark of the French maritime pine (Pinus pinaster), a well-known, potent antioxidant. Pycnogenol is several times more powerful than vitamin E and vitamin C. In addition, it recycles vitamin C, regenerates vitamin E and increases the endogenous antioxidant enzyme system. Pycnogenol protects against UV radiation. Its efficacy in the treatment of melasma was investigated in a clinical 30-day trial in which 30 women took one 25 mg tablet of Pycnogenol with meals three times daily. The average melasma area of the patients decreased by 25.86 mm(2) and the average pigmentary intensity decreased by 0.47 units. The general effective rate was 80%. No side effect was observed. The results of the blood and urine test parameters at baseline and at day 30 were within the normal range. Fatigue, constipation, pains in the body and anxiety were also improved.[112]

A new vitamin E derivative

A novel vitamin E derivative, (6"-hydroxy-2",5",7",8"-tetramethylchroman-2"-yl)methyl 3-(2',4'-dihydroxyphenyl)propionate (TM4R) inhibits tyrosinase activity. Its ability to scavenge hydroxyl radicals is nearly the same as that of alpha-tocopherol. Researchers noted an efficient lightening effect following topical application of TM4R to UVB-irradiated skin. TM4R may be an efficient whitening agent, possibly by inhibiting tyrosinase activity and biological reactions caused by reactive oxygen species.[113]

the search for safer topicals

Researchers have evaluated alkyl esters of gentisic acid (GA), a relative of methyl gentisate (MG), and four putative tyrosinase inhibitors, utilizing mammalian melanocyte cell cultures and cell-free extracts. They sought non-cytotoxic compounds with melanogenesis inhibiting activity in cells, preferably due to tyrosinase inhibition. Of the six esters synthesized,

the smaller esters (methyl and ethyl) were more effective enzyme inhibitors

hydroquinone (HQ), was a less effective enzyme inhibitor and was highly cytotoxic to melanocytes in cell cultures at low concentrations.

Kojic acid did not reduce pigmentation in cells.

Both arbutin and magnesium ascorbyl phosphate were ineffective in the cell-free and cell-based assays.

MG inhibits melanogenesis primarily through tyrosinase inhibition.

MG and GA were non-mutagenic in Chinese hamster cells, whereas HQ was highly mutagenic and cytotoxic.

The properties of MG, including (1) pigmentation inhibition in melanocytes, (2) tyrosinase inhibition and selectivity, (3) reduced cytotoxicity relative to HQ, and (4) lack of mutagenic potential in mammalian cells, suggest that MG is a candidate skin-lightening agent.[114]

Other botanicals

aloesin, or [2-acetonyl-8-beta-d-glucopyranosyl-7-hydroxy-5-methylchromone], is a constituent of Aloe is is a competitive inhibitior of tyrosinase. In a percutaneous absorption study a finite dose of aloesin penetrated the skin slowly. It holds promise as pigmentation-altering agent for cosmetic or therapeutic applications.[115]

angelica

asian turnip, juice used as a lightening agent

birch (betula alba)

chamomile, an endothelin antagonist

coffee extract

common rue (ruta graveolens)

corktree

cucumber extract

dodder seed

grapefruit extract

indian bread-poria cocos

ivy

lemon

mexican skin tree (mimosa ternuiflora), works on thioredoxin reductase system

papaya (papain), pineapple (bromelain), and banana enzymes

peony extract (Paenia suffruticoda)

plant glycosides

rice bran, Has some melanogenesis-inhibiting properties, Contains also PABA, ferulic, and allantoin (natural sunscreens)

safflower extract

sanchi (panax notoginsen)

strawberry begonia (saxifraga sarmentosa), usually used with other botanicals

scutellaria baicalensis –by inhibiting tyrosinase activity

seabuckthorn – Hippophae rhamnosides, probably due to high linoleic acid content

silk (pteria margaritifera)

thanatkha, From Burma, Tyrosinase inhibitor

nasturtium (tropaeolum majus )

vitis vinifera extract

New Cosmetic Lighteners

Albatin: Aminoethylphosphoric Acid (and) Butylene Glycol (and) Water
by Exsymol

Tyrostat 11™: Field Dock (Rumex spp.) extract, a strong tyrosinase inhibitor. A 1% solution is stated to have anti-tyrosinase activity equivalent to 1% kojic acid and 4% lactic acid and is approximately 3-fold more active than 3% arbutin and 30% more active than 2% tumeric extract.
by Fytokem

Clerilys™: Water (and) Angelica dahurica roots Extract (and) Cucumis sativa (cucumber) Seed extract (and) alba hibiscus bark Extract (and) sabdariffa flower Extract (and) fermented grape Extract
by Greentech Morus

Gigawhite™ : Water, Glycerin, Malva Sylvestris (Mallow) Extract, Mentha Piperita (Peppermint) leaf Extract, Primula Veris Extract, Alchemilla Vulgaris Extract, Veronica Officinalis Extract, Melissa Officinalis Leaf Extract, Achillea Millefolum Extract

Melawhite: Leukocyte Extract with hydroxy acid
by Pentapharm/Centerchem

Dermawhite: Mannitol (and) Arginine HCL (and) Phenylalanine (and) Disodium EDTA (and) Sodium citrate (and) Kojic acid (and) Citric acid (and) Yeast Extract
by Laboratoires Serobiologiques

Gatuline® Whitening (a complex lightening ingredient derived by fermentation of Kojic and Lactic acids with licorice extract)
by Robanda International, Inc

Clariskin: wheat germ extract with glutathione and glutathione reductase as actives; divert melanogenesis to synthesize light-colored pigments, suggested concentration is 3-5%
by RITACORP

Melaslow ™ Citrus unschiu peel Extract (and) glycerin
by CRODA

Asian herbs[116]

Skin lightening formulations have been important in Asia for much longer than tanning in the West. Many herbs have been attributed with skin lightening activity, generally due to inhibition of tyrosinase activity[117],[118]. The herbs, some of which are approved by the MOHW in Japan as skin lighteners, include

Dang Gui (Angelica sinensis)

Bai Zhi (Dahurian angelica)

Chuan Xiong (Ligusticum chuanxiong)

Hua Gu (Szechuan lovage)

shiitake mushroom (Lentinus edodes)

Ling Zhi(Ganoderma lucidum)

Xiao Lian Qiao, Chamomile

Japanese Cinnamon

Chai Hu, rhizome of Szechwan Lovage

and many others. The Song-Yi mushroom (Tricoloma matsutake Singer AKA Matsutake tricoloma) was used traditionally by high-caste families in Japan for whitening. This compound is available from Campo Research in a form suitable for use in cosmetics formulations, from cultured mycelia of the mushrooms. These traditional herbal remedies appear to be effective.

Other depigmenting agents

The following compounds are also used for depigmenting: Mercurials including Mercuric Oxide, Mercuric Chloride, Ammoniated Mercury Chloride which have systemic effects and are a source of severe problems in other countries, catechols, tyrosinase acetate, tyrosinase peptides, chelators such as EDTA, yeast, and peroxides.

free skin care · Sun Aug 28, 2005 12:28 am

thanks for that article, it was very informative

free skin care · Sun Aug 28, 2005 6:55 pm

Thanks eSquire415 for that post Smile

This is a topic I'm very interested in coz I've been trying to figure out how to accelerate the fading of acne marks.

free skin care · Mon Sep 19, 2005 1:10 pm

Are you trying to get whiter to match with your other body parts? Just curious.

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