Anti-aging & Cosmeceutical Corner

Remarkable Retinoids

By Navin M. Geria, Senior Technical Advisor and Principal Doctors Skin Prescription | December 3, 2013

Global anti-aging product sales are forecast to grow 26% from 2011-2016 to $28 billion. During this time, US anti-aging sales will climb 24% to $3.6 billion, according to Euromonitor International. Some of the most potent, collagen-boosting raw materials are peptides and forms of vitamin A.

Although they are completely synthetic, they are among the most potent anti-aging ingredients and are used extensively by dermatologists and consumer health care companies. This column will briefly review retinol, which is rightly considered the gold standard of anti-aging raw materials.

According to Mintel, during the past three years, there have been 185 skin care product launches in North America, which cite retinol as an ingredient. These launches have occurred across all channels of distribution, from mass to class. Synthetic forms of vitamin A called retinoids have been used as drugs for a long time, and one of them, tretinoin (aka all-trans-retinoic acid) has proved effective for treatment of acne and wrinkles. Retinol became well known shortly after Retin-A made headlines as a prescription wrinkle cream back in 1987. Tretinoin is the active ingredient in Retin-A (Renova). Topical tretinoin is approved for the treatment and prevention of photo-aging.

Vitamin A, found primarily in red and green vegetables, is converted by the body from beta-carotene into retinol and then into retinoic acid. Retinol is a natural form of vitamin A that stimulates cell repair, regulates skin functions and is necessary for skin cell regeneration. It is incorporated into serums and moisturizers to stimulate collagen production. Its side effects include redness and irritation. Retinol is not active when applied to skin. Applying retinol to damp skin does not maximize its potency. Retinol potency is related to skin chemistry and retinol receptors.

Skin cells receive the retinol, and hold on to it until needed, converting only the needed amount into retinoic acid. This attribute can dramatically reduce the adverse effects of retinoic acid, which include peeling, flaking, sun-sensitivity and redness. Despite these temporary side effects, ultimately, retinol generates beneficial skin results. Retinol-induced skin flaking is not like the exfoliation you get from use of glycolic acid. Retinol is gentler than retinoic acid. Biochemically, it accomplishes the same objective as retinoic acid, but at a slower pace. Retinol is the most studied and most common ingredient found in cosmeceuticals. Retinoic acid is a very small molecule that easily penetrates all layers of the skin, prompting rapid cell-turnover and exfoliation in the process. This mechanism helps explain its efficacy in repairing photoaging, treatment of brown spots, acne and roughness. Its regular application improves the signs of photo-aging and chronological skin aging. Retinoic acid is marketed in three concentrations: 0.025%, 0.05% and 0.1%. Avoid physical contact with eyes, mouth and during pregnancy.

Retinoids work at a much more profound level by affecting gene expression and causing enhanced production of collagen and hyaluronic acid, two of the main components of dermis, which give skin firmness, fullness, skin smoothing, even skin pigmentation while also slowing the age-related loss of these two components, resulting in proactively preventing lines and wrinkles that have not yet formed. Retinoids cannot alter the gene itself or its DNA, hence you must keep using them to retain anti-aging effects.
Furthermore, they prevent the production of collagenase, the enzyme that breaks down collagen after UV exposure. It takes an average of 12 weeks of use to produce noticeable changes in the skin. Several clinical research studies have shown that retinoids trigger changes in the skin to make it look clearer and youthful. On the subject of skin lightning, retinol and retinoic acid are well known for their ability to increase skin-cell turnover. They are added to many skin lightning formulations to speed the removal of pigment granules and accelerate the effects of other whitening agents.

Some Caveats
They must be used continually for best results. It is important to remember that retinoids breakdown in sunlight, which is why they are packaged in opaque packaging and are best applied at night. It is better to use micro-encapsulated retinol in the formula because it remains protected from light, oxygen, moisture etc. When the finished product is applied on face, the polymeric encapsulation film is broken, releasing free retinol to show its benefits.

Retinoids make skin thinner, and thus more vulnerable and sensitive to sun exposure. Always use a sunscreen if you choose skin lightener that is formulated with retinoids. Dryness can also be a problem.

According  to Kate Spetrino, the skin care marketing manager with BASF, claims that are currently used in the marketplace include: anti-aging, collagen boosting, reduce fine lines, increase cell turn over, even out skin tone, repair, smooth, firm, illuminate and protect the skin, boost skin’s radiance, visibly lift skin, enhance skin texture for smoothness and softness, brighten skin tone, firming and illuminating.

Retinoic acid was originally intended for acne treatment. Clinical studies surprisingly proved that retinoic acid not only prevented skin aging but also improved pre-existing skin damage. Vitamin A and retinoic acid are both the mainstay of prescription medical treatment for acne. They affect the production and cohesiveness of cells that line and plug the follicle, thus preventing the progression of acne from becoming severe. Retin-A (tretenoin) works by decongesting follicular debris, helping to clear the follicles of comedones and opening up clogged pores. It is also an excellent agent for oily skin and pimples. Tretinoin, available in cream, gel and liquid form, requires a physician’s prescription.

The question arises: if retinol works as well as well as the label promises, then why would you ever need to use Retin-A or Renova? Tretenoin addresses only one aspect of aging skin, which is bound to generate skin irritation and inflammation.

To avoid this, just remember to use a moisturizer that is formulated with sunscreens, antioxidants, and anti-inflammatory agents. It is safe to caution consumers that over-use of retinoids would thin the skin, causing chronic inflammation leading to premature aging.

Supporting this thought is the comment made by well-known dermatologist Tina Alster that too much skin inflammation breaks down collagen leading to more lines and sagging.

Navin M. Geria
Senior Technical Advisor and Principal Doctors Skin Prescription

Navin Geria, ex-Pfizer Research Fellow, is senior technical advisor and principal of the dermatological research company, Doctors Skin Prescription (DSP), Boston, founded by dermatologist David J. Goldberg, MD JD and plastic surgeons William P. Adams, MD FACS and Jason Pozner, MD. Geria has more than 30 years of experience in the personal care industry and was previously with Clairol, Warner-Lambert, Schick, Bristol-Myers and most recently, Spa Dermaceuticals. He has earned nearly 20 US patents, has been published extensively and has been both a speaker and a moderator at cosmetic industry events.