Common Whitening Skincare Ingredients

Skin Whitening Products: Understanding the Risks and Misconceptions

The beauty industry often promotes the idea of achieving a lighter complexion, leading to a rise in the popularity of skin whitening products. However, it can be difficult to determine if these products are using safe and effective ingredients to achieve the desired results.

Many Asian women feel societal pressure to have a pale complexion and may resort to extreme measures to avoid sun exposure and use whitening creams, masks, gloves, or seek professional treatments. These products work by reducing the melanin pigment in the skin, resulting in a lighter skin tone.

Melanin levels in the body determine the color of a person's skin, hair, and eyes, and the enzyme tyrosinase controls the production of melanin. Skin whitening cosmetics are often used to reduce the appearance of age spots, acne scars, and hormonal discoloration. However, it is crucial to understand the risks and misconceptions surrounding these products to make informed decisions about their use.

Hydroquinone (HQ)

Combining hydroquinone (HQ) with steroid creams or tretinoin is more effective in lightening the skin compared to using HQ alone. However, it is recommended to obtain prior approval from the Health Sciences Authority (HSA) as HQ can cause side effects and be considered unsafe.

Retinoids

Retinoids are a group of compounds derived from vitamin A that are believed to be essential for maintaining skin health and immunity. They come in various forms such as retinol, retinal, and retinyl esters, and are available in both natural and synthetic varieties.

Retinoids can be found in mild formulations that can be purchased over-the-counter to treat acne or reduce the visible signs of aging. Stronger retinoids, which require a doctor's prescription, are mainly used to treat severe forms of chronic skin conditions like psoriasis. They can help reduce inflammation and lead to smoother, better-looking skin.

Combination treatments, such as creams and gels that contain retinoids, hydrocortisone, and tretinoin, are especially effective in treating acne, pigmentation, and photoaging. Tretinoin, in particular, helps to speed up skin regeneration and disperse pigment granules.
Indications and Effects

To achieve their desired effects, these ingredients employ complex mechanisms of action, which include:

- Inhibiting inflammation
- Increasing production of procollagen, a precursor of collagen
- Opening clogged pores
- Regulating cell proliferation
- Delaying skin aging caused by ultraviolet radiation

Application

Retinoids have various applications in cosmetology and dermatological therapy. They are commonly used to treat mild to moderate acne by opening the pores of the skin, allowing topical antibiotics to penetrate and eradicate acne-causing bacteria. Retinoids are also effective in reducing wrinkles, inflammation, and other signs of aging due to increased production of procollagen.

Retinoids can alleviate inflammation and the increased rate of skin cell production associated with psoriasis. Furthermore, they can control pigment-producing cells, which reduces symptoms of melasma and actinic lentigines, small pigmented spots commonly seen on arms and hands. According to the American Cancer Society, retinoids can also limit the chances of developing certain skin cancer types, such as Kaposi's sarcoma and cutaneous T-cell lymphoma.

However, doctors only prescribe oral retinoids to those at high risk of skin cancer as they can cause birth defects. Lastly, retinoids are one of the treatments that can reduce inflammation and irritability that can occur after hair removal.

Side Effects:

When using retinoids to treat certain conditions, it is highly recommended to exercise caution, especially for those with skin allergies, dryness, or sensitivity. It is best to consult a dermatologist before using any product containing retinoids. Prolonged and large doses of topical retinoids can cause skin irritation, resulting in redness, intense dryness, scaling, and itching.

In rare cases, other side effects may occur, such as acne, increased skin sensitivity to the sun, discoloration, eczema, and swelling of the skin, affecting less than 10% of people.

Pregnant or intending-to-be-pregnant individuals should avoid using oral retinoids as they can cause birth defects, which is the most concerning side effect associated with them. To minimize the risk, a period of two months to three years is necessary before conception after taking the oral retinoid, depending on the type involved. Additionally, people using oral retinoids should refrain from taking blood tests.

Taking oral retinoids can lead to potentially debilitating side effects, such as mental disorders, muscle, joint, and bone pain, headaches, decreased night vision, abdominal pain, nausea, and diarrhea. Those taking acitretin (Soriatan) for psoriasis may experience worse symptoms initially and may also have increased cholesterol levels, bumpy nails, and skin burning.

Directions for use.

To ensure optimal use of retinoids, it is crucial to follow the instructions on the package for over-the-counter products or the doctor's advice for prescription retinoids. When using a prescription retinoid, apply a thin layer of cream or lotion to the affected skin only once a day, preferably at night to minimize exposure to sunlight.

For best results, individuals should ensure that the skin properly absorbs the product, use only the recommended amount, and use the product as directed for the prescribed time.

When using topical retinoids for acne treatment, start by applying a thin layer – approximately the size of a pea – every other day for the first 2-4 weeks. After the initial phase, rinse the product off the skin after 30-60 minutes and finish by using a gentle, non-clogging moisturizer.

For oral retinoids, it is crucial to follow the doctor's advice on how and when to take them. For example, it is recommended to take acitretin once a day with milk after the main meal. Drinking milk is important as the body needs fat for optimal absorption of the medication.

Retinol

Retinol, a form of retinoid, is a medication based on vitamin A1 that has gained popularity in recent times for its ability to promote healthy aging, improve skin tone, and combat acne. Topical retinol is available in the form of serums, gels, creams, and moisturizers, which can be applied to the skin to achieve various skin benefits.

The American Academy of Dermatology (AAD) specifies that over-the-counter retinol up to 2% is available, while stronger varieties may require a prescription.

Retinol is a popular option for topical skin care products as it can penetrate both the outermost layer of the skin, known as the stratum corneum, and the deeper layer of skin called the dermis. According to a research review conducted by a reliable source, when applied to the skin, retinol is converted to retinoic acid, which promotes cell regeneration and prevents the breakdown of collagen, a protein that provides skin elasticity.

Application:

Retinol's ability to penetrate the stratum corneum and dermis of the skin makes it a widely used treatment for acne, a common chronic skin condition caused by blocked skin follicles affected by dead skin cells, oil glands, and bacteria that can lead to inflammation. A systematic review has found that topical retinoids, including retinol, reduce abnormal skin flaking, a key factor in treating acne. People with severe acne may require a stronger retinoid than retinol, such as isotretinoin, which requires a prescription from a dermatologist.

Retinol is also effective in treating skin aging, as it reduces fine lines, wrinkles, and sagging skin and blocks molecules that produce inflammation. When fighting skin aging, external factors such as UV radiation, smoking, and pollution should be taken into account.

According to the AAD, age spots can appear on skin exposed to UV rays. The application of topical retinol with a concentration of 0.4% improves epidermal thickness and blood flow in affected areas. Retinol also stimulates collagen and elastin production and inhibits water loss from the skin, giving it a youthful appearance. After 8 weeks of treatment, retinol visibly reduced facial wrinkles around the eyes and neck.

A small study compared the effects of retinol and retinoic acid and found that retinol was less effective, but it increased epidermal thickness and collagen expression. Analysis of facial images also demonstrated a significant reduction in expression lines after participants implemented a retinol regime for at least 12 weeks. Retinol can even out the texture and tone of the skin by stimulating collagen production and influencing skin cell regeneration.

Moreover, it can make the skin brighter and more luminous, which helps reduce the appearance of wrinkles and further smooths out the tone and texture of the skin. For individuals who used a serum containing 0.3% or 0.5% of retinol for 8 weeks, pigmentation and irregularities were minimized, but those who used the 0.5% serum displayed a higher tendency to display symptoms.

An examination of individuals with darker skin who were given a 3% retinol peel showed significant progress in terms of skin pigmentation and tone. The results suggest that this type of treatment can be applied to all skin types without compromising safety.

The AAD advises caution when using retinol, particularly on dark-skinned individuals, as it may cause inflammation and pigmentation issues.

Retinol use provides many advantages, such as treating keratosis pilaris, a skin condition characterized by rough and bumpy patches. Research has also found that it can reinforce the epidermis and protect the skin from the adverse effects of external factors, such as air pollution. Additionally, the AAD has reported that retinol can greatly reduce the visibility of acne scars and shrink the size of pores.

However, long-term use or excessively high concentrations of retinol may lead to negative side effects such as skin dryness, redness, itching, and peeling. After using retinol, individuals may be prone to less common side effects, including discoloration, sensitivity to the sun, acne breakouts, swelling, and tingling or blistering of the skin. The AAD recommends wearing sunscreen and protective clothing after every application to prevent sunburn.

Arbutin

Arbutin, a powerful active ingredient found in the leaves of plants like cranberry, bilberry, and bearberry, interferes with the production of melanin in the skin by blocking the activity of tyrosinase, an enzyme that is essential for melanin production, and halting the maturation of melanosomes.

Those interested in brightening their skin, evening out their skin tone, and reducing the appearance of discoloration may find this natural solution beneficial. Arbutin is well-known for its brightening capabilities and can be found in its most concentrated form derived from hydroquinone, a topical bleaching agent. It can also be synthesized reproducibly in the laboratory or extracted directly from certain plants of the azalea family.

Arbutin evens out, brightens, and lightens skin tone, dark spots, and scars by interacting with melanin, the pigment naturally produced by the skin. Excessive melanin production can result in dark patches on the skin (hyperpigmentation), which can be caused by sun exposure, pregnancy, and some medications.

Arbutin inhibits the melanin pathway, the complex process responsible for creating pigment. It not only stops the activity of tyrosinase, but studies have also suggested that its whitening effect is likely due to its antioxidant properties, which protect the skin from oxidative stress.

In conclusion, arbutin has been shown to be more effective than any other tested alternatives in reducing age spots.

Comparison of α-arbutin and β-arbutin.

Skin care product labels may contain either α-arbutin or deoxy-arbutin, which are synthetic, or β-arbutin, which is sourced from plants. All forms of arbutin inhibit melanin production, but α-arbutin is more efficient, believed to be ten times more effective than β-arbutin, according to academic research.

Compared to arbutin, hydroquinone, kojic acid, and vitamin C are also known for their skin-lightening qualities, but each has its own effects and should be considered when treating the skin. Hydroquinone, a typical whitening agent, is banned in certain countries and can cause irritation, tingling, contact dermatitis, and skin discoloration.

Arbutin slowly releases hydroquinone, meaning that the skin is not exposed to large amounts of the chemical, which sets it apart from hydroquinone. Kojic acid is a bleaching agent, and although arbutin has a more stable effect, kojic acid is generally thought to be more effective. However, both ingredients can be used together.

Vitamin C is an antioxidant that, when combined with arbutin, boosts the effects of both ingredients and brightens the skin.

Using Arbutin in skincare?

In skincare, arbutin is a safe ingredient to use in face creams at concentrations of up to 2% and in body lotions at up to 0.5%. However, many countries such as the European Union, Japan, Australia, and some African countries prohibit the use of hydroquinone in cosmetic products at concentrations above 1%.

Reparative ingredients such as retinol can also be used in lightening treatments with arbutin, and there are no known interactions between arbutin and other ingredients. It is recommended to apply arbutin once or twice a day to the entire face or as a spot treatment to specific areas.

To evaluate results, it is suggested to give arbutin two to three months of consistent use before consulting a licensed dermatologist for the perfect routine that suits individual skin concerns.

Azelaic Acid

Azelaic acid, a natural dicarboxylic acid that can be isolated from the lipophilic yeast Pityrosporum ovale, has antibacterial, anti-inflammatory, and skin-clearing properties. It is effective at treating skin conditions such as acne and rosacea and can be found in cereals such as barley, wheat, and rye. It is accessible in gel, cream, and foam form, with the two most prominent brands being Azelex and Finacea.

Physicians typically prescribe products containing at least 15% azelaic acid, while some over-the-counter products contain much less. However, due to the time required for azelaic acid to take effect, many dermatologists do not use it as their first choice in treating acne. Furthermore, azelaic acid can have side-effects such as burning, dryness, and flaking of the skin.

Azelaic acid reduces inflammation, evens out skin tone, and kills acne-causing bacteria. It has a soothing effect on the skin and helps to neutralize free radicals that can cause inflammation. Additionally, azelaic acid inhibits the enzyme tyrosinase, which can darken the skin, making it ideal for treating acne scars and melasma. Its bacteriostatic and bactericidal properties limit the production and kill Propionibacterium bacteria, which is integral to the occurrence of acne.

Azelaic Acid for Acne and Acne Scars:

For the treatment of acne and acne scars, azelaic acid is available in different formulations such as creams, gels, and foams. It works by eliminating irritation-causing bacteria, aiding skin healing, and encouraging the regeneration of skin cells to reduce breakouts, redness, rashes, and inflammation. The instructions for using azelaic acid in any form are the same. It can also be used to treat acne scars by boosting the cell regeneration process, reducing the severity of scars, and blocking the creation of pigmented cells that change skin color. If various treatments have been unsuccessful in curing blemishes or scars, azelaic acid may be worth trying.

How to Use:

To use azelaic acid, wash the affected area of skin with a mild soap or soap-free cleanser and pat it dry with a soft towel. Avoid using cleansers containing alcohol, dyes, abrasive substances, astringents, and exfoliating ingredients, especially if you have rosacea, and ask your physician for a recommended cleanser. Thoroughly shake the azelaic acid foam before use and apply a thin layer of gel, foam, or cream to the affected area, lightly massaging it in. Do not cover the area with bandages, plasters, or any other sort of cloth. Leave the foam to dry before reapplying any makeup and wash your hands afterward.

Astringent or deep cleansing products should not be used during the application of azelaic acid.

Azelaic acid may cause the following side effects

Azelaic acid may cause side effects such as burning, tingling, and peeling of the skin at the site of application, as well as dryness, redness, and blisters. Joint tightness, pain, hives, itching, fever, and difficulty breathing may also occur. Using azelaic acid can cause the skin to become thinner and more sensitive to damage when exposed to the sun, so using sun protection with SPF is important. Discontinue use and contact a medical professional immediately if any of these unwanted effects occur.

Why is azelaic acid prescribed?

Azelaic acid gel and foam are both prescribed to diminish skin dysfunctions, rashes, and swelling caused by rosacea. Azelaic acid cream is used to treat acne and acne-related puffiness. Azelaic acid is part of a group of medications in the dicarboxylic acid family, which efficiently combats redness and inflammation when used to treat rosacea. It also helps limit the development of acne by killing the bacteria that causes it and reducing keratin production.

Before using azelaic acid:

Before using azelaic acid, inform your doctor and pharmacist of any allergies you have to azelaic acid or any other prescription or non-prescription/herbal medications, vitamins, supplements, or herbal products. Let your doctor know if you have had asthma or recurrent forest fire attacks in the past. If you plan to become pregnant or are already pregnant, tell your doctor. Azelaic acid may cause skin discoloration in dark-skinned individuals, so speak to your doctor if you notice any changes in your skin color. Finally, keep all medicines, including azelaic acid, out of the reach of young children, securely fasten protective caps after each use, and store in a safe place (high and out of reach).

Glycolic Acid

Glycolic acid, derived from sugar cane, is a water-soluble alpha hydroxy acid (AHA) and one of the most popular AHAs used in skincare products. These naturally occurring acids consist of small molecules that easily penetrate the skin, making them effective for anti-aging, reducing the visibility of fine lines and wrinkles, and improving skin texture. Low concentrations of glycolic acid can rid the skin of pigmented cells, and 30-70% of it can enable other bleaching elements, such as hydroquinone, to penetrate deeper.

How does glycolic acid work?

Glycolic acid optimizes exfoliation compared to other AHAs due to its small molecular structure. It activates cell renewal and breaks down the bonds connecting dead cells, allowing them to shed at a faster rate. As collagen production in the skin decreases with age and sun exposure hinders collagen production further, regular applications of glycolic acid can help prevent these collagen degrading processes, as it is a major component of the protein that gives body to the skin, making it firm, smooth, and elastic.

There are many product options for those seeking a skincare treatment with glycolic acid. It is available in numerous over-the-counter cleansers, masks, toners, and moisturizers with concentrations of up to 10% found at most drugstores, markets, or spas. For stronger glycolic acid percentages, chemical peels are available at salons and spas ranging from 30-70% concentrations, while the most potent peels can be provided by a dermatologist.

Glycolic acid is very popular for the following reasons:

Glycolic acid has become very popular for its ability to help with anti-aging, moisturizing, preventing sun damage, and brightening the complexion. It can also gently exfoliate the skin, unclog pores, and reduce the appearance of acne. While it cannot erase scars, it can lighten dark spots and make raised and deep scars less noticeable. Physician-administered glycolic acid peels or other professional treatments are typically more effective at treating scars.

While sugar can be gently rubbed on the face to exfoliate and soften the skin, the effects of glycolic acid are much more powerful. Glycolic acid is extracted from sugar cane, but it is not the same as what is found in stores.

Choosing the Glycolic Acid treatment for your skin:

When choosing a glycolic acid product, consider the type of skin and desired outcomes. Over-the-counter products containing glycolic acid can promote a healthier, brighter complexion, prevent breakouts, and reduce the visibility of small lines and wrinkles without the need for professional peels. However, professional peels may be a better choice for addressing specific skin issues such as sunburns, brown spots, acne, or deep wrinkles for faster and more effective results. Professional peels, however, tend to cause more irritation due to higher levels of glycolic acid.

While the percentage of glycolic acid is a factor to consider, the product's pH level is also crucial, as lower pH levels are associated with more potent and helpful effects. Additionally, sun protection is essential when using glycolic acid as it can make the skin more sensitive to light.

It is recommended to start slowly with over-the-counter products, applying them three times a week for a week before increasing the frequency until they can be used daily, or pausing if they cause irritation. With in-office or salon peels, the amount of glycolic acid used initially will likely be smaller before higher concentrations are used.

After the first few peels, the skin may feel rough, but with repeated usage of glycolic acid, the texture will become smoother over time. Topical retinoids and products that exfoliate quickly should not be used with glycolic acid, and it is important to seek the approval of a dermatologist before using glycolic acid products or undergoing a peel.
Resources

1. Do retinoids really reduce wrinkles?
2. The toxicology of hydroquinone--relevance to occupational and environmental exposure
3. How Does Retinol Work on the Skin?
4. Treating Acne with Azelaic Acid
5. Glycolic Acid - Uses, Side Effects, and More