Bleaching and Lightening Creams: Lightening Hyperpigmentation
Bleaching products fade areas of unwanted pigmentation by disrupting the production and distribution of melanin in the skin by targeting overactive melanocytes (pigment-producing cells). There are a variety of ways to accomplish this and studies have shown that the best results occur when using a combination of two or more of these ingredients.
Tyrosinase Inhibitors: Tyrosinase is a copper enzyme that stimulates melanin production in the melanocyte. Most whitening agents fall under this category, as they interfere with the enzyme's function thereby reducing pigment production in the melanocyte.
Hydroquinone (HQ) is a hydroxyphenolic compound that has been widely used for skin lightening for 50 years. It is the only FDA-approved product for skin bleaching on the market and a prescription is required to obtain products with a concentration above 2%. HQ is the most widely studied bleaching agent available, and its effectiveness is solidly supported through scientific studies, but its use can come at a cost. The product can be very irritating to sensitive skin and in some cases, can even cause pigmentation to darken and get worse, particularly in those with very dark skin types. Long term use of HQ, particularly in higher concentrations of 4% or more, can lead to the development of a permanent condition known as exogenous ochronosis. HQ also is very difficult to stabilize and will oxidize quickly if exposed to light and air. If a product containing HQ has darkened from an off-white or a creamy, pale yellow to a gold or brown color, it is longer effective and should be discarded. It is best to start using HQ products gradually, every couple of days or so, and build up a tolerance. As the skin adjusts, you can then increase to daily use. PrecisionMD VIVATIA Brightening Complex (2% HQ) matches the performance of 4% HQ in its lightening effect of the skin.
When using hydroquinone it is imperative to stay out of the sun as much as possible in order for the treatment to work. Exposure to sun deteriorates the HQ, and renders it ineffective. Always wear a full spectrum sunblock and if you must go outside, be sure to wear a hat. Elta MD UV Clear Broad-Spectrum SPF 46 is a light weight, oil-free and non-comedogenic sunscreen that is easy to use under makeup.
Kojic acid, a by-product of rice fermentation, was first discovered in Japan in 1907. Kojic acid is the second most common bleaching agent, and is a more natural and gentle alternative to the stronger effects of the more frequently used hydroquinone. It penetrates the upper skin layers and inhibits the production of epidermal melanin. Kojic acid does pose the risk of causing allergic or sensitizing reactions in a small number of people.
A natural skin brightener found in wheat, rye, and barley, azelaic acid (AZA) is most effective in concentrations of 20%, which is closely comparable in activity to 4% hydroquinone. In a study consisting of 329 melasma sufferers, half were treated with a 20% azelaic acid solution, and half were treated with a 4% hydroquinone solution. 56% of patients treated with AZA had good to favorable results while 73% treated with HQ had a similar result. However, when the AZA was combined with tretinoin or alpha hydroxy acids, the results were noticeably improved, and rivaled the results of the high-concentration HQ. Azelaic acid also is antibacterial and anti-inflammatory, so it is effective in the treatment of rosacea and acne.
Arbutin (also known as alpha arbutin, bearberry extract or uva ursi extract)
A botanical, naturally-occuring cousin to hydroquinone, arbutin is derived from the bearberry plant (also known as uva ursi plant). Compared to HQ, arbutin has been shown to be significantly less cytotoxic to the melanocyte — making it a much safer, yet very effective alternative to hydroquinone. In a clinical trial involving Japanese women with melasma, a 3% concentration of arbutin produced good to excellent results in 71.4% of patients within a three month period.
One of the safest and most gentle bleaching agents available, licorice extract is a potent anti-inflammatory and antioxidant. The ingredients responsible for the skin whitening aspect of the plant are known as glabradin and liquiritin. Liquiritin (in a 20% concentration) has been shown to provide good to excellent results in 70-90% of patients with hyperpigmentation and melasma — with minimal side effects and only minor irritation.
Mulberry extract is derived from the root bark of the mulberry tree, Morus Alba L. Studies have confirmed it to effectively reduce tyrosinase activity at much lower concentrations than either hydroquinone or kojic acid.
N-acetyl glucosamine is a more stable form of glucosamine, an agent most widely known as an arthritis treatment. Recent studies have shown it to successfully reduce the amount of melanin in melanocytes by blocking tyrosinase conversion. Interestingly, the product's results improve significantly when combined with niacinamide (see below)..
Inhibition of Melanosome Transfer: Some skin bleaching agents lighten unwanted pigmentation by interfering with the transfer of melanosomes from the melanocyte to the keratinocytes. Niacinamide (or nicotinamide) is a biologically active form of niacin (vitamin B3) that has been shown to interrupt melanocyte transfer by 35-68%. The company Nia24 has built an entire brand around this key ingredient. NIA24 Intensive Recovery Complex is ultra hydrating and helps rebuild the skin's lipid barrier while effectively decreasing dark spots.
RWJ 50353 - RWJ 50353 is a thrombin-inhibitor used in medication as an anticoagulant. It also has been found to effectively reduce melanocyte uptake with no irritation or side effects.
Soybean Trypsin Inhibitor - Soybean Trypsin Inhibitor (STI) is a depigmenting agent derived from soybeans. STI reduces pigment in the skin by inhibiting the activation of a pathway necessary for the melanosome transfer to take place. In addition, STI has been shown to prevent UVB-induced pigmentation.
Other skin lightening
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