Retinoids in Skincare

By Aznaida L. Tawagon-Pandapatan, MD, DPDS

What are Retinoids?

Retinoids are Vitamin A derivatives. Use of retinoids results to the most sought-after reversal of skin aging. 

How? By organized differentiation and proliferation of skin cells. Think of it as like an organic fertilizer for plants—once applied to the soil, the leaves and fruits will grow faster and with a better quality. 

When applying retinoids, skin cells will grow faster and better (like how your skin used to be when you were younger) and collagen will start to form in your skin dermis, so you can get back that youthful smooth, firm, and glowing skin. 

Currently there are four generations of retinoids:

• First Generation: 

Naturally-occurring: Retinol & Retinaldehyde 

Synthetic: Tretinoin, Isotretinoin, and Alitretinoin

• Second Generation: Etretinate and Acitretin
• Third Generation: Adapalene, Bexarotene and Tazarotene
• Fourth Generation: Trifarotene

What are their uses?

Retinoids are most famous as anti-acne and anti-aging, but amazingly in the medical field, they are also used for other diseases such as in psoriasis, hyperkeratotic conditions and even for cancers. Here we discuss their anti-acne, anti-aging, and anti-melasma actions.

• Anti-Acne

Retinoids have been used for acne vulgaris (pimples) since 1971. Topical Tretinoin & Adapalene are the preferred retinoids for acne. 

These retinoids do their superhero work by normalizing the follicular epithelial differentiation, thus treating the existing pimples and also preventing future pimples to form. New studies also showed that topical retinoids have an anti-inflammatory activity thus further decreasing pimple occurrence.

Adapalene causes less irritation compared to tretinoin, thus it is commonly prescribed for those with sensitive skin and those who cannot tolerate Tretinoin. 

Retinols are milder forms of retinoids. Examples are retinaldehyde & retinyl palmitate. These may be advised for those who cannot tolerate the use of Adapalene & Tretinoin. Studies showed satisfactory results with these retinols, although effects can be slower and milder compared to adapalene and tretinoin.

Oral Isoretinoin (tablet form) is prescription-only and is used for moderate to severe acne that cannot be successfully controlled by creams. Therapy usually lasts for 6 months, and when acne has been controlled, this is shifted by your Dermatologist to topical retinoids as maintenance. 

• Anti-Photoaging (Anti-Aging)

As anti-aging, Tretinoin has been shown to give superior results overall. Fine wrinkles and brown spots are the two targets of retinoids as anti-aging. 

Brown spots or Dyspigmentation], which happens in photoaging, can be treated by retinoids, partially or fully, depending on how severe it is. This is through enhancement of proper cell turn-over of the epidermis, thus shedding off of the darkened/damaged skin cells on top.

Wrinkles can be improved by retinoids by enhancing cell regeneration of the topmost skin layers and by production of new collagen in the dermal layer (lower layer of the skin). This effect on collagen can usually be observed after 6-12 months of regular use.

• Melasma

Melasma has 3 types: EPIDERMAL (affecting the topmost skin layers), DERMAL (affecting lower skin layer), and MIXED epidermal+dermal (affecting both the top and lower layers).

Epidermal type of melasma can be improved by retinoids by enhancing regeneration of new skin cells, thus effectively removing the topmost pigmented cells. Improvement can be 80-100%.

In Mixed type of melasma, the epidermal component can be treated by retinoids by the same mechanism mentioned above, but the lower dermal component does not usually respond to this. Thus the patient can only see a partial improvement of their melasma, about 50-60% improvement.

Dermal type of melasma is difficult to manage with just topical retinoids, it is managed with multiple approaches using lasers and other topicals. 

Retinoids can be combined with other treatment modalities to optimize melasma treatment.

What are the possible side effects of retinoids?

Like many medications, retinoids may have side effects, some are mild and some are severe especially for the first-time users. Here are some of them:

• Dryness
• Peeling, flaky skin
• Irritation: swelling, crusting, blistering when severe
• Skin color changes
• Sensitivity to sunlight
• Redness
• Itchiness
• Burning sensation

Do not let these side effects turn you off from using retinoids. Most of these effects

will usually resolve on their own once the skin adjusts. But for those with severe side effects, your dermatologist will prescribe medications to lessen the effects and guide you when and how to re-introduce it to your regimen.

Tips on proper use of retinoids and how avoid undesirable effects.

• Follow the instructions given by your Dermatologist.
• Do a Patch Test or ROAT (Repeat Open Application Test) before you apply on your face. How? Apply a small amount of the product on the inner forearm or back of the ears, every other day for 3 consecutive instances (example: Mon-Wed-Fri). If there are no allergic reactions, you may start using it on the face twice a week.
• A pea-sized amount is adequate for the whole face.
• Dry your skin first before application, this will lessen irritation.
• Apply thinly. 
• Avoid application on sensitive areas around the eyes such as the eyelids and eyebag areas, and the neck. These areas are very sensitive. There are milder retinol formulations that are better suited for these areas.
• As a beginner, use it twice a week for a month; then every other day for another month, and if there are no bad reactions, you may use it daily.
• Make sure to use it at night only—this is to avoid inactivation by UV light and to avoid UV sensitivity effects in daytime (sunburns & irritation).
• Wear a broad-spectrum sunscreen SPF 30 (or higher) during daytime, and don’t forget to reapply the sunscreen (lunch breaks are great time for reapplication; and every 2 hours when swimming). This is again, to avoid the UV inactivation and UV sensitivity effects of retinoids.
• When on retinoids, avoid the sun in general. If you have to be outdoors, limit the time & avoid the extreme sun from 10am to 2pm. Wear protective gear too, such as wide-brimmed hats, sunglasses and UV-blocking masks and umbrella.
• In general, while your skin is still adapting to retinoids, it is best not to try new products yet. Once your skin has stabilized with retinoid use (could take 2-6 months), then you may start using other products. 
• If starting new products, use one product at a time. Example, a new niacinamide toner, try just this (after proper ROAT/Patch test) for 2-4 weeks before adding another product to your routine. This is to avoidirritation and losing what you have gained from retinoids.
• The following are active ingredients that should not be applied together with retinoids: alpha-hydoxy acids (glycolic, lactic, mandelic), beta hydroxy acids (salicylic, vitamin C, and benzoyl peroxide.
• It takes 3-6 months of regular use (at least every other day) before initial improvements are seen, remarkable results are observable after 6-12 months.
• Avoid retinoids if you have severe eczema, and those with broken, and sunburned skin.
• Purging is not common, but it can happen for a few people, this is noted as worsening of acne on the first 2-4 weeks of retinoid use. If this happens, you may contact your dermatologists so she can advise you on what to do.
• If allergic reactions such as redness, stinging, blistering and inflammation become persistent (lasts for more than a day, or worse enough to disturb your daily activities), stop using retinoids and contact your Dermatologist for advice on what to do.

Myths about retinoids in skincare:

• Retinoids will make the skin thin. 
• No, it will not thin the skin out, it will do the opposite. It will ensure proper, continuous skin cell growth, to maintain normal skin thickness so your get younger-looking skin.
• Retinoids are only for mature skin.
• Retinoids can be used as early as teenage years, mostly for acne especially if indicated and prescribed by a Board-Certified Dermatologist.
• The more product you apply, the faster and better the results.
• Nope. Doing so will not increase its effectiveness, it will only increase chances of side effects such as redness, flaking, dryness and stinging. A pea-sized amount is enough for the whole face.

Facts about retinoids in skincare:

• Major desired effects on the skin as anti-acne can be observed in 2-4 months, so you have to have patience.
• Major desired effects on skin as anti-aging (fine lines, dyspigmentation) and anti-melasma can be observed in 6-12 month.
• Avoid the use of oral retinoids, establish first a proper effective contraception and get guidance from a board-certified dermatologist. These have high tendency to cause fetal death and malformations.
• Avoid the use of topical retinoids when pregnant or breast-feeding. According to a large population-based study done by Jick et. al., there was no risk of birth defects in offspring born to mothers who were exposed to topical tretinoin during pregnancy. Despite this, use of topical retinoids in pregnancy and breast-feeding is still discouraged to avoid even the smallest possible risk of fetal death and malformations. No risk is worth taking, when dealing with new life.
• If in doubt, always communicate with a board-certified Dermatologist, we always have your best interests at heart!

References

1. Bolognia, Jean, et. al. Dermatology 3^rd ed. New York. Elsevier Saunders. 2012.
2. Kang, Sewon, et. al. Fitzpatrick’s Dermatology 9^th ed. New York. McGraw Hill Education. 2019.
3. Kiser, Philip D.; Golczak, Marcin; Palczewski, Krzysztof (11 July 2013). “Chemistry of the Retinoid (Visual) Cycle”. Chemical Reviews. 114 (1): 194–232. doi:10.1021/cr400107q. PMC 3858459. PMID 23905688.
4. Stefanaki C, Stratigos A, Katsambas A (June 2005). “Topical retinoids in the treatment of photoaging”. J Cosmet Dermatol. 4(2): 130–4.
5. Orfanos CE, Zouboulis CC, Almond-Roesler B, Geilen CC. Current use and future potential role of retinoids in dermatology. Drugs. 1997 Mar;53(3):358-88. doi: 10.2165/00003495-199753030-00003. PMID: 9074840.
6. Jick SS, Terris BZ, Jick H. First trimester topical tretinoin and congenital disorders. Lancet. 1993;341(8854): 1181-1182.