This article on skin brighteners is a follow up to my blog on topical retinoids for skin restoration.  The primary focus will be the treatment of solar lentigenes (“liver spots,” “freckles”), melasma and post inflammatory hyperpigmentation.  This article is not intended to address other pigmented lesions such as moles, seborrheic keratoses, or anything that could be cancerous.  It is always best to seek the advice of a board certified dermatologist for the proper initial diagnosis and treatment plan.

Hydroquinone

Unwanted brown freckles or splotches typically appear in sun-exposed areas such as the face, upper chest, arms and hands.  The foundation of any treatment program for unwanted skin pigmentation includes sun protection, and usually a topical retinoid.  In addition to these, hydroquinone is the gold standard for treating brown spots.  While hydroquinone is the subject of controversy regarding its safety, this article will not address these issues because it has a long-term record of safe use in the United States.  Hydroquinone is available over-the-counter in a 2% formulation and by prescription in a 4% formulation.  It can also be compounded in higher strengths by some compounding pharmacies.  Adverse reactions to hydroquinone include skin rash in approximately 5% of users and exogenous ochronisis, a permanent idiosyncratic darkening of the skin.

Azelaic Acid

Azelaic acid is another useful treatment for unwanted pigmentation.  This naturally-derived substance has been shown to be beneficial for the treatment of acne vulgaris, acne rosacea, and melasma.  The only FDA approved topical prescription formulations are Azelex (20% Azelaic acid cream, $413/30 gm) for the treatment of acne vulgaris, and Finacea (15% Azelaic acid gel, $330.49/50 gm) for the treatment of acne rosacea.

Azelaic acid is also useful for hyperpigmentation, although published information seems to favor its efficacy more for melasma and post inflammatory hyperpigmentation than for sun spots.  The FDA has not approved it for over-the-counter use in concentrations of 15% or greater and no claims can be made for over-the-counter azelaic acid products for the treatment of acne.  Glytone has a product, Glytone Enhance Brightening Complex, containing 12% azelaic acid with 3% glycolic acid which costs $70/oz.  This combination of azelaic acid and glycolic acid should provide synergy for the treatment of unwanted pigmentation.  The manufacturer cites internal studies showing benefit but does not permit dissemination of the details of this information.

Topical Vitamin C

Topical vitamin C is another treatment option.  There are several research studies showing the benefits of certain formulations of topical vitamin C for the treatment of hyperpigmentation, restoration of collagen and elastic tissue, and reduction of fine lines.  In my opinion, high-quality vitamin C products are less effective than topical retinoids for this purpose because of their high price (SkinCeuticals C E Ferulic 15% vitamin C $165/oz, Glytone Age-Defying Vitamin C + E Serum with 20% THD ascorbate $130/oz, Revision Vitamin C Lotion with 30% THD ascorbate $109/oz) relative to their efficacy.  Still, for those who wish to spend the money, they do have utility when used with topical retinoids.

Effectiveness and Use of Skin Brighteners

Here’s how I rank these compounds in terms of cost effectiveness for skin brightening:

  1. Topical 4% hydroquinone
  2.  Revision Vitamin C lotion 30% or Glytone Enhance Brightening Complex with 12% azelaic and 3% glycolic acid

I recommend starting with 4% topical hydroquinone and a topical retinoid.  After a month or two, replace the hydroquinone with a topical vitamin C or an azelaic acid product.

 

Some of us remember the 1980’s Wendy’s advertisements where the customer looks at her fast food burger and asks “Where’s the beef?”  Well, that’s my question when it comes to topical products for skin restoration.  Does the product have ingredients with proven efficacy and safety to justify the cost?

Maintaining one’s best appearance starts with preventing sun-related problems.  For a discussion about preventing sun-related skin problems, please refer to my blog on sun protection.  My curent core list of proven effective compounds for skin restoration includes topical retinoids, hydroquinone, azelaic acid, alpha hydroxy acids and vitamin C.  Hydroquinone, azelaic acid, alpha hydroxy acids and vitamin C are the topic of Topical Treatments for Skin Restoration Part 2.  In my opinion, if tolerated, topical retinoids should be the foundation of any skincare program intended to restore skin quality.  They have been shown to help restore collagen and elastic tissue and to reduce fine lines and tan spots.  Additionally, they provide synergy when used in conjunction with other topical skin care products such as skin lighteners.   It should be emphasized that oral retinoids result in severe birth defects if taken during pregnancy.  Variable quantities of topical retinoids are absorbed through the skin into the bloodstream.  Consequently, women contemplating pregnancy, or who are pregnant, should not use topical retinoids.

Topical Retinoids

Topical retinoids include over the counter retinol (vitamin A), retinaldehyde, Differin (adapalene 0.1% gel) and prescription tretinoin and tazarotene.

Currently, I am aware of only three FDA approved prescription topical retinoids for skin restoration:

  1. Renova (0.02% tretinoin), approximately $290.22/40 gm, for the “palliation of fine wrinkles.”
  2. Refissa (0.05% tretinoin), approximately $106.91/20 gm, for the “palliation of fine wrinkles, mottled hyperpigmentation and tactile roughness of facial skin”
  3. Avage (0.1% tazarotene), approximately $387.73/30 gm, for the “mitigation of fine wrinkles, mottled hyperpigmentation and lentigenes”

Most other formulations of topical retinoids can be sold with no claims other than that they “reduce the appearance of fine lines and brown spots.”  Differin 0.1% gel (adapalene) was recently approved by the FDA for the over the counter treatment of acne and became available at approximately $30/30 gm tube in January 2017.  The availability and price of this medication is a game changer in terms of topical retinoid treatment, not only for its approved use in the treatment of acne but also the non approved use for the treatment of sun damaged skin.  There is a large, prospective, randomized, controlled study showing improvement in actinic keratoses, solar lentigenes and photoaged skin with adapalene.  Refissa, if available at $106.91/20 gm, with its FDA indications for skin restoration is also a strong option.

From most evidence to least evidence for efficacy in the treatment of sun damaged skin, I rank the topical retinoids as follows:

  1.  Tretinoin and tazarotene
  2. Adapalene and retinaldehyde (Avene Retrinal 0.1%, $70/30 ml)
  3. Retinol

From least irritating to most irritating, I rank these products as follows:

  1.  Retinol
  2.  Adapalene and retinaldehyde
  3.   Tretinoin
  4.   Tazarotene

In terms of cost effectiveness, I rank them as follows:

  1.  Adapalene
  2.  Refissa or retinaldehyde
  3.  Tretinoin
  4.  Tazarotene

How to Use

To reduce skin irritation, and for maximum effect, I recommend the following:

  1.  Start using the product every other night for two weeks, then nightly if tolerated.  If necessary, take periodic breaks in the treatment.
  2.  Use gentle skin cleanser.
  3.  Use a moisturizer in the evenings and a facial moisturizer with sunscreen in the morning.  Simple unscented skin cleansers and moisturizers are best.
  4.  Apply the products lightly and evenly over the entire face, except around the eyes.

Topical retinoids will intensify the effects of chemical peels, microdermabrasion, or laser treatments and should be stopped at least one week prior to these procedures.