Over-the-Counter Topical Skincare Products: A Review of the Literature

February 2012 | Volume 11 | Issue 2 | Original Article | 220 | Copyright © February 2012

Topical "anti-aging" products, with their seemingly limitless list of ingredients, make extensive claims to reduce wrinkles, fine lines, and sun damage, among others. Sales in the United States alone for cosmeceutical products are expected to increase by 7.4% per year to $8.2 billion by 2012. However, in this enormous industry, there has been a significant lack of rigorous controlled trials of efficacy. It is difficult for both dermatologists and consumers to make informed decisions in a market that is yet to be clearly defined and regulated. We elucidate the scientific basis for, as well as the literature behind, common active ingredients found in products intended to reverse photoaging, discuss some interesting new activities, and provide a review of several comprehensive studies on over-the-counter (OTC) products.

J Drugs Dermatol. 2012;11(2):220-224.


Ultraviolet (UV) radiation generates reactive oxygen species (ROS) in the skin that can oxidize nucleic acids, lipids, and proteins. This oxidative stress in the skin is associated with photoaging and skin cancer.1 UV radiation also has been shown to induce matrix metalloproteinases (MMPs), which degrade dermal collagen and elastin. One of the ways skin naturally protects itself against UV damage is with antioxidants that neutralize the ROS that cause damage.1 Based on this scientific evidence, the cosmetic skin care industry has popularized anti-aging creams and serums, many with added vitamins and other antioxidants. We provide a synopsis of many of these ingredients as well as an evaluation of the literature discussing their use in the treatment of photoaged skin.

Common Cosmeceutical Active Ingredients

Retinoids and Vitamin A
There is extensive literature on the use of topical retinoids, which are derivatives of vitamin A, a naturally occurring antioxidant in the skin. Tretinoin, or all-trans retinoic acid, is the biologically active form of vitamin A and one of the few therapeutic agents proven to repair photodamage.2 It has been shown to improve fine facial wrinkles, mottled hyperpigmentation, and skin roughness. 3 However, tretinoin is often associated with skin irritation and is available only in prescription formulations. Retinoids available in OTC formulations, which include retinol, retinaldehyde, and retinyl palmitate, are less potent than tretinoin.
Retinol is oxidized into retinaldehyde and then into retinoic acid, the biologically active form of vitamin A. A 2000 study found that treatment with 1% retinol reduces MMP expression and stimulates collagen synthesis in both sun-protected and photoaged skin.4 Also, randomized controlled trials found significant improvement in fine wrinkles after 12 and 24 weeks of treatment, respectively.5-7 Retinol is one of the best-studied active in OTC products and consistently has been shown to improve photoaged skin.
Retinal or retinaldehyde is the aldehyde form of vitamin A. Retinaldehyde is often an intermediate during the conversion of retinol to retinoic acid.8 Studies have shown that retinaldehyde can produce significant improvement in the appearance of both fine and deep wrinkles.9,10
Retinyl Palmitate
Retinyl palmitate is the ester of retinol and palmitic acid. Although retinyl palmitate has not yet been proven to be an effective anti-aging agent, it has been shown to inhibit the formation of thymine dimers in the presence of UVB rays.11 It also is one of the active ingredients in an OTC product that was shown to produce significant fibrillin-1 deposition in a clinical study.12

α-Hydroxy Acids

α-Hydroxy acids (AHAs) are a class of compounds that consist of a carboxylic acid substituted with a hydroxyl group on the adjacent carbon. They are commonly seen on many OTC product labels as glycolic acid, malic acid, lactic acid, citric acid, α-hydroxyethanoic acid, α-hydroxyoctanoic acid, hydroxycaprylic acid, α-hydroxycaprylic acid, and hydroxyl fruit acids.