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Retinoids in skin aging: a review of clinical effectiveness and safety

The skin, the largest organ of the body, protects all other organs from the external environment. The skin is a complex organ with numerous structures and cell types divided into three layers: epidermis, dermis, and subcutaneous tissue .

In addition to external protection from radiation, the functions of the skin include:

heat regulation,

immune reaction

biochemical synthesis,

touch receptor,

regulation of absorption/loss of water and electrolytes

The stratum corneum is formed from non-viable cornocytes and plays a major role. Keratin combines with disulfide macrowaves together with filaggrin, the main protein component of the keratolytic granule. The cells create the cornea by crossing involucrin and keratohyalin. Lamellar lipids accumulate in intercellular spaces, which are completely hydrophobic. The combination of keratinized hydrophilic cells with hydrophobic intercellular substance forms a barrier to external hydrophilic and hydrophobic substances.

As we age, the skin's natural repair process slows down dramatically, and the skin becomes thinner, drier and less elastic. You can read about how a face ages here.

Aging process

Aging is a biological depletion at the cellular level that results in a decrease in reserve power and the ability to perform normal functions that are performed throughout the lifespan of organisms, increasing the likelihood of death. Aging is the result of a genetic program or clock that is embedded in the genetic structure of each species. It should also be remembered that cumulative damage to genes and proteins derived from them leads to disruption of function and homeostasis. This causes the body to undergo premature aging and death, which in turn will depend on the reparative system.

The skin, as the primary protective barrier between internal organs and the environment, is exposed to ultraviolet radiation (UV) and, to a lesser extent, to other DNA-damaging agents such as cigarette smoke, exhaust fumes, and occupational exposure. UV irradiation leads to the formation of pyrimidine dimers, and benzopyrene from cigarette smoke leads to the formation of nucleotide pair adducts. (Facial photodamage and treatment are scientifically written about in this article). All this is accompanied by damage from endogenous agents such as reactive oxygen and nitrogen species generated by all aerobic cell types as part of normal metabolic processes.

Retinoids

The importance of retinol (vitamin A) was discovered during the First World War, and subsequent studies showed that its deficiency leads to acne and follicular hyperkeratosis. The retinoid drug project was launched in 1968 with the goal of synthesizing compounds similar to vitamin A by chemically modifying its molecule to improve clinical efficacy and safety.

The use of these substances in treatment began approximately 3,000 years ago in Ancient Egypt, where liver was used to treat endemic night blindness. The modern history of retinoids, however, dates back to 1909, when an essential factor in embryo viability was discovered in a fatty extract of egg yolk called vitamin A. Retinoids were finally introduced into the treatment of dermatitis, including photoaging, more than two decades ago.

Tretinoin

Tretinoin has proven to be the retinoid that has been studied more than any other retinoid involved in the treatment of photoaging. Although tretinoin has been used in dermatology since the 1960s, its potential for treating aging was not realized until the 1980s. The effectiveness of tretinoin in the treatment of photoaging was first demonstrated by Kligman and colleagues (1984), using an experimental animal model to study photoaging. The authors note that treating photoaging mouse skin with tretinoin for 10 weeks resulted in significant restoration of an area of new collagen in the papillary dermis, which also correlated with wrinkle smoothing. This interesting observation prompted researchers to explore the potential of tretinoin in the treatment of photoaging.

Much later, ex vivo studies by Fisher and colleagues (1996) helped to understand the molecular basis of this observation. Fisher and colleagues (1996) found that pretreatment of UV-irradiated photoaged skin with 0.1% tretinoin resulted in a complete block of interstitial collagenesis and gelatinase synthesis, thereby preventing collagen degradation.

Following ex vivo observations, Kligman and colleagues (1986) conducted a placebo-controlled, open-label study to evaluate the clinical efficacy of 0.05% tretinoin. The study involved the use of 0.05% tretinoin on photoaging facial and forearm skin for 3-12 months. Interestingly, tretinoin led to clinical improvement in photoaging skin . In addition, histological examination showed the deposition of reticulin fibers and the formation of new dermal collagen (types 1 and 3), accompanied by antiogenesis of the papillary dermis. The encouraging results obtained from this experiment have stimulated scientists to conduct a huge number of clinical trials to confirm the clinical effectiveness of tretinoin in the treatment of photoaging.

At the moment, Tretinoin is the most studied retinoid .

Tazarotene

Tazarotene is a new acetylene retinoid effective in the topical treatment of psoriasis and acne. Tazarotene is a prodrug that is rapidly metabolized to the active metabolite tazarotenic acid. Due to its rigid polyaromatic structure, it does not undergo isomerization or conformational changes in the skin. Sefton and colleagues (2006) were the first to conduct a pilot, double-blind, randomized trial to evaluate the effectiveness of tazarotene 0.1% in 10 healthy women with moderate levels of photoaging of the forearm. At the end of 12 weeks, the tazarotene treatment group experienced a significant reduction in age spots, fine lines and skin roughness. Moreover, histological examination showed a decrease in keratinocyte atypia and restoration of its polarity.

Adapalene

Adapalene is considered a third generation synthetic retinoid that contains naphthoic acid. Unlike retinoic acid, adapalene shows selectivity for the nuclear retinoic acid receptor (RAR). It targets pathological skin desquamation, modulates cellular differentiation and has anti-inflammatory properties. In addition, due to its receptor selectivity, it causes less skin irritation. Adapalene has been successfully used in the treatment of acne. However, not much has been done to explore its potential in aging/photoaging. To date, only one study has been conducted to determine the photoaging potential of alapalene.

Kahn and colleagues (2003) conducted a two-center, randomized, placebo-controlled, masked, parallel-group study in 83 patients suffering from actinic keratosis and solar lentigo and other symptoms of photoaging to evaluate the therapeutic potential of adapalene (0.1% or 0. 3%) or placebo for 4 weeks, followed by twice daily dosing, if well tolerated, for up to 9 months. Significant relief of solar lentigo was observed in patients receiving adapalene compared with patients receiving placebo gel within one month of treatment. After 9 months, 57% and 59% of patients had milder lesions in the adapalene 0.1% and 0.3% group, respectively, compared with only 36% in the placebo group.

In addition, histological evaluations showed improved cellular atypia and decreased epidermal melanin in the adapalene-treated group compared with the placebo group. A retrospective evaluation of paired clinical photographs (before and after nine months of treatment) showed significant improvement in wrinkles and other clinical signs of photoaging of the skin with adapalene, compared with placebo.

As you would expect, adapalene was very well accepted by the patients participating in the study. Thus, adapalene can be used as an adjuvant treatment for photoaging, mainly in patients who demonstrate extreme intolerance to conventional retinoids.

However, large-scale clinical trials must be conducted to test the effectiveness of adapalene.

Side effects from topical retinoid

The most common and frequent side effect of topical retinoid, known as “retinoid reaction,” is characterized by itching, burning at the application site, erythema, and peeling. Another side effect associated with retinoin therapy is photosensitivity, which usually occurs early in therapy. Patients on retinoid therapy are advised to avoid excessive sun exposure and take precautions (eg, use of sunscreen) to protect themselves from the sun.

However, after several months of therapy, the skin's response to UV radiation returned to normal. Irritable conjunctivitis has been observed in some cases when the retinoid was applied close to the eye. Over the past 30 years, no systemic side effects have been observed with long-term treatment with topical retinoids in young adults.

In addition, Lattarino and colleagues (1997) found that topical tretinoin had no significant effect on endogenous plasma levels of tretinoin or its metabolites. This is mainly due to the limited transdermal absorption of these agents. Pregnant women or women of childbearing potential should use topical retinoids with caution as they are known to cause teratogenicity/embryotoxicity through systemic exposure.

However, in more than 25 years of using topical tretinoin to treat acne, there has been no history of teratogenicity. Additionally, in one case-control study of 215 mothers who were exposed to topical tretinoin treatment in the first trimester of pregnancy, the prevalence of major fetal malformations in the tretinoin-treated group was 1.9% versus 2.6% in the control group, which indicates the safety of topical tretinoin .

Dealing with Adverse Effects

To counteract the symptoms of a retinoid reaction, it is generally recommended to reduce the frequency of retinoid use or switch to a less irritating one. Additionally, the addition of 3% indomethacin or 1% hydrocortisone to retinoids has also been suggested for symptomatic relief. However, if the patient cannot tolerate even the weakest concentration of retinoids, then treatment should be discontinued.