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CHEMICAL WHITENING AGENTS
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Mequinol (4-hydroxyanisole; 4-Methoxyphenol; Hydroquinone Monomethyl Ether; MEQ), is a Skin Lightening Agent. Mequinol is a synthetic derivative of hydroquinone and works as a depigmenting agent if used at high doses over a long period of time. Although the exact mechanism of the depigmenting effects of mequinol remains unclear, it may exert its effect by oxidation of tyrosinase to cytotoxic products in melanocytes. Mequinol may also act by competitively inhibiting the formation of melanin precursors. Mequinol can be used to whiten skin semi-permanently if used in conjuntion with high-dose hydroquinone skin lighteners. There is a product called ‘Solage’ that is used to remove age spots and liver spots on people with FITZ I skintones. Solagé contains mequinol 2% and tretinoin 0.01%. There are other brands that sell mequinol creams with higher doses. Most brands are reported as “burning” as soon as it toches the skin. Burning can cause more hyperpigmentation, which defeats the purppose of useing it. You can s always purchase mequinol powder to make your own MEQ creamthat aren’t as harsh & caustic, but just as effective.
Glabridin is a powdered natural skin lightening agent & antioxidant extracted from the Glycyrrhiza Glabra (Licorice) Root. Glabridin whitens skin by inhibiting the activity of tyrosinase and dopachrome tautomerase (TRP-2). Glabridin is often used in skincare because of it’s skin lightening, anti-inflammatory (reduce redness), and humectant (moisturizing) properties. Glabridin-40 is also used in eye makeup and haircare formulations for those same benefits. Glabridin 0.5% cream reduces UVB-induced pigmentation and erythema (redness) after 3 weeks of use. In other words, Glabridin 0.5% heals sunburns and gets rid of suntans in about 3 weeks. Therefore a stronger percentage, like Glabridin 10%, could fully eradicate a suntan and heal your sunburned skin within 7 days easy! Glabridin has been shown in vitro to have a skin lightening effect 16 times greater than that of hydroquinone , which is great on top of being an “Herbal Skin Lightener”. Glabridin is much more expensive than hydroquinone ($30/gram!) which is why you don’t see as many merchants selling Glabridin cream. And you don’t see a very high content of Glabridin (like 1%-3%) in the creams that are being sold, and none are under $100/bottle. Glabridin is an organic chemical, but it is also classified under “Herbal Skin Whiteners” because it isn’t a byproduct of anything. Glabridin is found “as is” in nature and doesn’t have to be synthesized like hydroquinone.[Resource]
Hydroquinone is a topical lightening product found in OTC (over-the-counter) products, and is used to correct skin hyperpigmentation including melasma, post-inflammatory hyperpigmention, sunspots, age spots, and freckles. It can be used alone, but is more frequently found in combination with other agents such as alpha-hydroxy acids and retinoids to increase efficacy. Hydroquinone has come under scrutiny due to many myths about skin damage associated with its use. Including dermal irritation, exogenous onchronosis, and carginogenicity. As a result of these false findings, hydroquinone has been banned in the United Kingdom, Ireland, Africa, and other parts of europe. This all due to scam merchants using Mercury as the skin whitening agent, but claiming it is authentic “hydroquinone” cream. This is because mercury is VERY cheap, very easy to obtain, and causes rapid skin whitening. But several weeks after applying this poisonous mercury skin whitener, the skin starts turning blue-black, stretch marks appear, blisters. The skin is completely destroyed (Exogenous ochronosis).
[Read – Hydroquinone is Safe]Hydroquinone is a very potent “master antioxidant”, and is the primary active ingredient used for inhibiting melanin production in most skin whitening products. Hydroquinone is a strong inhibitor of melanin production; it prevents dark skin from making the substance responsible for skin color (melanin). Hydroquinone does not bleach the skin but lightens it and can only disrupt the synthesis and production of melanin hyperpigmentation.Another reason hydroquinone gets a bad reputation, is because when a person uses a cream with more than 4% hydroquinone. Rebound-hyperpigmentation occurs. meaning, the skin becomes red and then darkens. This because the skin has to become acclimated to doses higher than 5$ hydroquinone. Rebound-hyperpigmentation can be avoided by diluting high-dose HQ with a plain/regular body lotion. Then slowing increasing the dosage over the next few weeks. After that hydroquinone cream of any dosage can be applied to the skin without any side effects. can be avoided [Read – Diluting Your HQ Cream]
NOTE: Understand that Arbutin exists in two isomers. Or, there are two different types of Arbutin. Alpha-Arbutn (α-Arbutin CAS# 84380-01-8) and Beta-Arbutin (β-Arbutin CAS# 497-76-7). Beta-Arbutin isn’t as potent as “α-Arbutin”. The purity of α-Arbutin is higher, and the process for synthesizing α-Arbutin is a lengthier more labor intensive one. Which is why α-Arbutin is more expensive than β-Arbutin. The alpha isomer offers higher stability over the beta isomer and is the preferred form of Arbutin for skin whitening.Arbutin is found naturally in the leaves of bearberry, cranberry, mulberry, blueberry shrubs, and is most present in pears. In china and other countries, arbutin and other plant extracts are commonly used as safe alternatives to banned whitening agents like hydroquinone. Which is why China is the biggest producer of arbutin (both alpha & beta). Arbutin is a tyrosinase inhibitor, shown to be less cytotoxic to melanocytes in comparison to hydroquinone. In other words, arbutin isn’t as strong as hydroquinone. Arbutin is an anti-oxidant found in foods, over-the-counter drugs, and herbal dietary supplements. Arbutin has also been used as an anti-ineffective for the urinary tract, as well as a diuretic.Arbutin is found naturally in certain fruits and shrubs (see above) but pears have proven to have the highest content of arbutin. Arbutin is especially concentrated in the skin of the pear. This is why arbutin is sourced from pear skins You can literally lighten your skin by eating arbutin containing foods, like pears. Arbutin was found to be extensively absorbed from the gastrointestinal tract where it is primarily converted to hydroquinone. [Read – “Hydroquinone is Safe”] Fresh pear peels were reported to contain an arbutin content of approximately 0.1%! So if you peel or scrape the skin from a pear, 0.1% of what you have there is organic Arbutin. You can extract the arbutin out of the pear skins using the same method as any herbal extract. [Resource]
RESORCINOL
Resorcinol, is often used in skin lightening products in countries where hydroquinone is prohibited. Phenylethyl resorcinol {4-(1-phenylethyl)1,3-benzenediol} or ‘PR’ is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. Meaning it degrades as soon as sunlight hits it, and it’s hard to melt/dissolve so that it can be formulated into a usable cream.
PR has been shown to serve as a whitening and brightening ingredient in skin care products, hair lightening products, and cosmetics. It is a synthetic compound that is partially derived from natural skin lightening compounds found in Scotch Pine bark. According to research, it is one of the highest tyrosinase inhibitors, 22 times more potent than kojic acid. When directly compared to β-arbutin (Beta-Arbutin), PR was shown to be over 100 times as effective at lightening hair. Also, it served as an antioxidant agent—better than vitamin E, vitamin C , and butylated hydroxytoluene. However, the application problems of PR were due to its light instability and poor water solubility. The poor water solubility may limit its absorption, while its photo instability may render the topically applied PR ineffective. Therefore, there is a need for appropriate delivery vehicles that can improve the photo stability and water solubility of PR. [Resource]
Liquiritin, another component of licorice, is also a tyrosinase inhibitor. A 20% Liquiritin cream used twice daily (1 gram/day) for 4 weeks can whiten skin 1-2 shades. Liquiritin isn’t as strong as Glabridin or Hydroquinone or even a-Arbutin, liquiritin is more of a co-whitener. Liquiritin is an organic chemical, but it is also classified under “Herbal Skin Whiteners” because it isn’t a byproduct of anything. Liquiriten is found “as is” in nature and doesn’t have to be synthesized like hydroquinone. [Resource]
Kojic acid is a by-product in the fermentation process of malting rice for use in the manufacturing of sake, the Japanese rice wine. Kojic acid exhibits antioxidant properties, and has shown to be effective for inhibiting melanin production. However, kojic acid is an unstable ingredient in cosmetic formulations. Upon exposure to air or sunlight, it can turn brown and will no longer be effective. Also, in high doses kojic acid can cause skin irritation. That’s why you never see creams with percentages higher than 3% kojic acid content. Many cosmetic companies use “Kojic Acid Dipalmitate” as an alternative because it is more stable in formulations. However, there is no research showing kojic dipalmitate to be as effective as kojic acid, although it is also an antioxidant. Further, some controversial research has suggested that kojic acid may have carcinogenic properties in large doses.[100] Other further studies show that kojic acid is not carcinogenic but can cause allergic contact dermatitis[101] and skin irritation.Kojic Acid is a metabolic product of the fungal species Acetobacter, Aspergillus, and Penicillium. KA is used in cosmetic skin whiteners and is also used as a food additive to prevent browning in fruit. Over the years, there have been mixed reports on the efficacy of KA. Kojic Acid has been shown to be more beneficial in combination with other ingredients. In other words, it seems Kojic Acid is more of a “co-whitener”. A recent comparative study by Monteiro et al21 evaluated the efficacy of once-daily application of 4% HQ and 0.75% KA cream, which contained 0.75% KA and 2.5% vitamin C, in the treatment of melasma. Sixty patients were enrolled in this 12-week study. The authors found that at Week 4, patients responded earlier to the HQ cream than to the KA cream. And at Week 12, the HQ cream had overall superiority in lightening skin compared to the KA cream. [Resource]
Azelaic acid is a component of grains, such as wheat, rye, and barley. It is applied topically in a cream formulation at a 10–20% concentration. Azelaic acid is used to treat acne, but there also is research showing it to be effective for skin discolorations. Azelaic acid interferes with deoxyribonucleic acid (DNA) synthesis, inhibits mitochondrial oxidoreductase, competitively inhibits tyrosinase, and decreases free radical formation. This agent preferentially targets abnormal and highly active melanocytes with minimal effect on uninvolved skin. In other words, you can use azelaic acid all over your face and it will only target the “hyper” pigmented spots &/or areas. Most clinical trials study azelaic acid as an acne treatment. In a 16-week, baseline-controlled study of 20 patients with Fitzpatrick Skin Types IV to VI, 15% azelaic gel applied twice daily showed a reduction in acne and post-inflammatory hyperpigmentation. [Resource]
Tranexamic acid (TXA), an antifibrinolytic drug, is now gaining popularity as a skin whitening agent. It is a synthetic lysine amino acid derivative which mainly blocks the conversion of plasminogen to plasmin by inhibiting plasminogen activator. This results in less free arachidonic acid production, and hence a reduction in the prostaglandin (PG) levels as well. Thus, by reducing PG production, TXA reduces the melanocyte tyrosinase activity and plays an important role in the treatment of melasma, ultraviolet-induced hyperpigmentation, and other postinflammatory hyperpigmentation. Tranexamic acid has been tried topically, orally, and intradermally in the management of melasma with minimal adverse effects. However, more randomized trials are needed to fully elucidate the exact mechanism of action, ideal route, frequency, and duration of administration of the drug, along with its potential to treat other pigmentary disorders.When tranexamic acid is used as a skin whitener, it is said that a topical solution should contain at least 5% TA. A Tranexamic acid %5 cream is as effective as Hydroquinone 3% cream [Resource]; [Resource]
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HERBAL WHITENING AGENTS
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Licorice extract comes from the root of Glycyrrhiza glabra. Licorice root contains two skin whitening agent. Glabridin and Liqiritin. Glabridin, is a very potent tyrosinase inhibitor. Liquiritin, is also a tyrosinase inhibitor but more of a co-whitener to Glabridin (see above for more info)Most licorice root grows in Greece, Turkey, and Asia. Licorice root extract is commonly used to flavor licorice candy, and is also used as a sweetener in hot berages & in cooking/baking.For centuries licorice root has been used in Greece, China, and Egypt for stomach inflammation and upper respiratory problems. Some people use licorice root as a dietary supplement for digestive problems, menopausal symptoms, cough, and bacterial and viral infections. People also use licorice root as a shampoo. [Resource]
Mulberry extract is an extract derived from dried mulberry leaves, Morus alba. Mulberry leavse contain two active whitening agents- Mulberroside-F and Arbutin. In several East Asian countries, the leaves from mulberry trees are used to feed silkworms and have been used in traditional Chinese and Thai medicine in the treatment and prevention of diabetes. We already know that arbutin whitens skin by inhibiting tyrosinase. But according to in-vitro studies, mulberry leaf’s other active ingredient Mulberroside-F inhibits tyrosinase activity; melanin formation in melan-cells; and melanin transfer. Containing two whitening agents makes mulberry extract a very potent herbal skin whitener.[Resource]
Belides™ ORG is a natural skin-lightening agent, derived from organic daisy flowers (Bellis perennis). It is suitable for any skincare concept providing even and luminous complexion and radiant skin.Belides™ ORG’s action is based on a potent, multifaceted reduction in the activity of melanocytes. Belides™ ORG influences different cellular pathways involved in melanogenesis, encompassing the reduction of cellular signaling, tyrosinase transcription, tyrosinase activity and melanosome transfer. These actions lead to even pigmentation and make age spots less visible.[Resource]
MSM taken orally in high doses will whiten skin several shades. MSM raises glutathione levels in the body. And a side effect of glutithion levels being raise, is noticable skin whitening. Taking Vitamin-C complements & intensifies the effects of MSM. And a side effect of glutithione levels being raised, is noticeable skin whitening. [Read – MSM Skin Whitening]
Vitamin C is an anti-oxidant, and is an effective herbal skin lightener. Vitamin-C (like others) raises glutathione levels in the body. And a side effect of glutithione levels being raised, is noticeable skin whitening. [Read – Best Skin Whitening Pills]
Glutathione is a tripeptide molecule found in mammalian bodies. It is an antioxidant that plays an important role in preventing oxidative damage to the skin. In addition to its many recognized biological functions, glutathione has also been associated with skin lightening. Amongst the many mechanisms postulated to contribute to its antimelanogenic properties, inhibition of tyrosinase enzyme, skewing of melanogenesis from the darker eumelanin to the lighter phaeomelanin, and scavenging of free radicals seem to be the most important. While skin whitening reduces melanin which serves as the natural protection from UV exposure, glutathione’s antioxidant property also protects the skin from UV radiation.
Glutathione is an ingredient in some cosmetics preparations. Glutathione for skin whitening is available in cream, soap, lotion, nasal spray, and injectable form. Glutathione that is applied on the skin in the form of lotion is not efficiently absorbed by the skin cells as the thiol group undergoes rapid formation of disulfide. When taken orally, glutathione is hydrolyzed (or destroyed) by enzymes in the gastrointestinal tract resulting in reduced bioavailability. As a result, the effectiveness of externally administered glutathione is slowed down by its inability to cross cell membranes efficiently and its rapid degradation by enzymes in the gastrointestinal tract. That’s why glutathione pills don’t work at all. And topical glutathione products work very little for skin whitening. The best route of administration of glutathione is via enema or I.V. Intravenous glutathione delivers very high doses directly into the system and is the preferred mode of administering glutathione. However, the I.V. method of administrating glutathione is only approved in places like Seol South Korea. Glutathione Enema is your only alternative if you live outside of Seol South Korea. There are some shoppes that are selling glutathione enama mixes, but you can always mix your own and purchase enema equipment online.
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Glutathione can be combined with many other whitening agents like N-A-C (N-acetyl cysteine), N-A-G (N-Acetyl Glucosamine), Alpha-Lipoic Acid, Niacinamide, and MSM to intensify it’s efficacy. Some suggest mixing in Vitamin-C but this is incorrect. Vitamin-C is acidic, and acid destroys glutathione. [Read – Best Skin Whitening Pills]
N-acetylcysteine (NAC) is a thiol derivative that stimulates the synthesis of glutathione, an internal antioxidant. NAC has been clinically used as a mucolytic agent as well as an antidote for acetaminophen toxicity. NAC was previously reported to be useful in the treatment of skin diseases including toxic epidermal necrolysis and lamellar ichthyosis. N-A-C Works in synergy with N-A-G, Niacinamide, and MSM in raising glutathione levels. And a side effect of glutithione levels being raised, is noticeable skin whitening. [Read – Best Skin Whitening Pills]
Also known as vitamin B3 and nicotinamide, niacinamide is a water-soluble vitamin that works with the natural substances in your skin to help visibly improve the appearance of enlarged pores, uneven skin tone, fine lines and wrinkles, dullness, and a weakened surface. Niacinamide also reduces the environmental damage & helps skin to repair signs of past damage. Niacinamide inhibits melanosome transfer. Niacinamide 5% cream significantly decreases hyperpigmentation and whitens skin by 1-2 shades after 6 weeks of use. Early research shows that applying a cream containing 2% N-acetyl glucosamine (N-A-G) and 4% niacinamide to the face decreases dark spots caused by aging and sun exposure. [Read – Best Skin Whitening Pills]
Aloin is derived from the aloe vera plant and has been shown to inhibit tyrosinase, tyrosine hydroxylase, and dopa oxidase, according to in-vitro studies. Aloin has direct inhibitory effects on melanogenesis and dose-dependent reductions in melanin content and tyrosinase activity using an in-vitro pigmented skin equivalent. Aloin works synergistically with arbutin. [Resource]
The enzyme lignin peroxidase is derived from the tree fungus Phanerochaete chrysosporium and acts by oxidizing and breaking down melanin. In decaying trees, lignin – structurally similar to melanin, is broken down by lignin peroxidase resulting in decolorization. In one studiey Lignin peroxidase cream had a significantly more rapid and observable skin-lightening effect than 2% HQ. In a more recent randomized paired/controlled/split-face study, the pigment lightening efficacy of lignin peroxidase produced skin lightening superior to HQ 2% cream and HQ %4 cream . Lignin peroxidase also produced superior results in aesthetics when compared to HQ. This includes skin texture, lack of clarity and radiance, roughness, and overall appearance. Lignin peroxidase does show promise as a skin lightener based on these studies, but more studies are warranted. [Resource]
Ellagic acid is a polyphenol antioxidant found in trees, nuts, and fruit. Ellagic acid is especially concentrated in blueberries & cranberries. In-vitro studies suggest that ellagic acid inhibits melanogenesis through the reduction of tyrosinase activity. Two randomized, controlled trials (RCT) have evaluated its skin lightening effects. [Resource]
Turmeric (Curcuma longa) is a widely-used Ayurvedic herbal supplement and spice. The active ingredient in turmeric is curcumin, a hydrophobic polyphenol characterized by yellow pigment. Studies have shown curcumin to possess anti-inflammatory and anti-carcinogenic properties. Recently, an in-vitro study has suggested that curcumin might induce apoptosis of human melanoma cells via mitochondrial pathway and caspases activation. Application of topical turmeric extract reduces the appearance of facial hyperpigmentation, fine lines and wrinkles. Daily application of turmeric facial mask will reduce darkspots & even skintone after 6 weeks. [Resource]
Soybean, a legume commonly grown in East Asia, consists of many biologically active substances, including isoflavones and serine protease inhibitors. In-vitro studies have uncovered the anti-aging, antioxidant, pigment-reducing, photo-protective, and melanosome transfer inhibiting properties of soybean extract. Several clinical studies support the hypothesized skin-lightening role of soybean. In a controlled trial, Hermanns et al52 compared the effect of different topical hypo-pigmenting agents in treating facial hyper-melanosis in 44 Celtic-complexioned men. Soybean extract did show skin-lightening effects in the study. Another study involving Caucasian and Hispanic women found that the application of soy extract to melasma lesions once daily for three months led to an average 12% reduction of hyperpigmentation & melasma. [Resource]
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MARINE WHITENING AGENTS
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Pearls contain an organic protein called ‘nacre’. Nacre is responsible for the iridescence you see in pearls and pearl shells. Nacre produces a whitening effect on your skin. This whitening helps reduce the appearance of age or sun spots, scars and even out skin tone, making your skin look brighter and more vibrant. All without the use of makeup. Pearls also contain many minerals that nourish skin & heal skin. Pearl powder & pearl extract have more anti-aging and skin smoothing effects than skin whitening effects. Pearl extract works in synergy with other stronger skin whitening agents.
N-acetyl glucosamine is a chemical that comes from the outer shells of shellfish. It can also be synthesized in a lab. Don’t confuse N-acetyl glucosamine with other forms of glucosamine, such as glucosamine hydrochloride or glucosamine sulfate. They may don’t have the same effects. You may also see chitosan as an ingredient in some glucosamine products. Chitosan (shells of shellfish are made of chitin) is a form of N-acetyl glucosamine that has been chemically altered. N-A-G has been proven to effectively treat dark spots on skin due to aging and/or sun exposure. Early research shows that applying a cream containing 2% N-acetyl glucosamine and 4% niacinamide to the face decreases dark spots caused by aging and sun exposure. It’s unclear if applying a cream containing only N-acetyl glucosamine would have the same effect. N-A-G is also used to treat inflammatory bowel diseases, including ulcerative colitis and Crohn’s disease. There is some early evidence that if N-acetyl glucosamine is taken by mouth or rectally, may decrease symptoms of IBD in children with Crohn’s disease or ulcerative colitis. N-A-G is also used to treat Knee pain. Taking at least 600mgof NAG will raise glutathione levels by 38%.
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DANGEROUS WHITENING AGENTS
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Many unethical merchant over seas are selling Mercury based skin whiteners. These poisonous creams usually contain the most toxic forms of mercury, such as mercury(II) chloride or ammoniated mercury, because it is the cheapest skin whitening agent available. Mercury for human consumption has been banned in most countries. As late as January 2016, the FDA published a warning not to use a particular brand of whitener, Viansilk’s Crema Piel De Seda (Silky Skin Cream), sold in the United States due to its mercury content. [Resource] Read more about mercury skin whiteners [here].
Topical steroids are never to be used as a skin lightening agent. Topical steroids will almost completely destroy skin skin when used this way. Skin getting lighter or going ‘pale’ in color, is a side-effect of using topical steroids. The skin lightening you see is only temporary. After a few weeks you’ll see stretch marks (on your face!) where ever you’ve been using the steroid creams. Steroids thin the skin. If you get simple paper cut, it will never heals or take months to finally heal completely. For more info about steroid skin whitener, please read – Hydroquinone is Safe