Tazarotene

Tazarotene is a newer retinoid that is nevertheless one of the best-researched. Its anti-aging effects include, but is not limited to, improving both fine and deep wrinkles, lightening pigmented spots and smoothing the skin. Tazarotene is also well-known for treating acne and psoriasis.

Effects


Grade Level of Evidence
A Multiple double-blind, controlled clinical trials.
B 1 double-blind, controlled clinical trial.
C At least 1 controlled or comparative clinical trial.
D Uncontrolled, observational, animal or in-vitro studies only.
Grade Effect Size of Effect Comments

A

Wrinkle treatment

Strong

Improves fine and coarse wrinkling by increasing collagen synthesis.

A

Increased skin thickness

Strong

Increases the rate of epidermal proliferation and the number of cell layers.

A

Psoriasis treatment

Strong

Therapeutic effect on plaque, palmoplantar and nail psorasis, by restoring normal keratinocyte proliferation and lowering epidermal inflammation.

A

Acne treatment

Strong

Reduces inflammatory and non-inflammatory lesion counts. Also successful in treating post-inflammatory hyperpigmentation.

A

Skin lightening

Moderate

Improves mottled pigmentation and lightens lentigines.

A

Smoother skin

Moderate

Reduces the number of peaks and valleys on the skin surface, possibly by compacting the basket-weave morphology of the stratum corneum.

B

Smaller pores

Moderate

Reduces pore size, presumably by promoting the clearance of comedones and microcomedones.

D

Tighter skin

Moderate

12 weeks of treatment with 0.1% tazarotene improves skin laxity by 25%.

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Scientific Research


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Table of contents:

1. Sources

Tazarotene is a synthetic compound that is part of the acetylenic retinoids, a non-isomerizable class of retinoic acid receptor (RAR)-specific retinoids.[1][2]

2. Bioavailability

Tazarotene is available in gel, cream and foam formulations.[3] Topical application provides direct delivery of tazarotene into the skin; 10 hours after topical application of tazarotene gel, 4-6% of the dose was found to reside in the stratum corneum and 2% distributed to the viable epidermis and dermis.[4]

Tazarotene is rapidly metabolized in the skin to tazarotenic acid, its primary and active metabolite.[5] The systemic bioavailability of tazarotenic acid is low, approximately 1% after single and multiple topical applications to healthy skin.[4] Experiments show that the maximum average plasma concentrations of tazarotenic acid after topical application of tazarotene cream 0.1% to the face were less than 0.25 µg/L.[6] Dosing with tazarotene gel and foam also leads to low plasma concentrations of tazarotenic acid, though the concentration is significantly higher for gel versus foam.[3]

Tazarotenic acid does not accumulate in adipose tissue, but undergoes further metabolism to its sulfoxide and to other polar metabolites and is rapidly eliminated via both urinary and faecal pathways with a terminal half-life of about 18 hours.[4]

3. Effects on the skin

3.1 Anti-wrinkle effect

Tazarotene has significant anti-wrinkle effects. One large multicenter, randomized, double-blind, vehicle-controlled parallel comparison of 0.01%, 0.025%, 0.05% and 0.1% tazarotene creams against 0.05% tretinoin emollient cream (Renova) and vehicle cream found that all tazarotene formulations and tretinoin were associated with significantly higher proportions of subjects having at least a 1-grade improvement from baseline versus vehicle cream, for fine wrinkling.[7] This corroborates the results from two later studies, which similarly found that tazarotene treatment led to clinical improvements in both fine and coarse wrinkling.[8][9]

In another study, 0.1% tazarotene gel increased the distribution of plateaus, transitional areas between wrinkles.[10]

Tazarotene's efficacy in reducing wrinkling has been attributed to its induction of transforming growth factor β (TGF-β), which results in the activation of fibroblasts, increasing collagen synthesis.[8] It has also been hypothesized that the increased epidermal thickness brought about by tazarotene may be instrumental in wrinkle effacement.[11]

3.2 Lightening effect

Numerous studies have demonstrated that treatment with 0.1% tazarotene ameliorated mottled pigmentation in individuals with photodamage.[7][8][9][10] Likewise, other studies found that 0.1% tazarotene improved the appearance of irregular depigmentation and lentigines.[8][9][12]

0.1% tazarotene appears to be as efficacious as 0.05% tretinoin in this respect.[9] The adjunctive use of hydroquinone also enhances tazarotene's efficacy in lightening lentigines and mottled hyperpigmentation.[12]

3.3 Smoothing effect

Tazarotene reduces the number of peaks and valleys on the skin surface, thereby smoothing the skin.[10] A number of studies have also consistently shown that treatment with 0.1% tazarotene led to a greater incidence of patients achieving clinical improvement in tactile roughness, supporting this finding.[8][12][13]

Histologically, tazarotene treatment tends to compact the basket-weave morphology of the stratum corneum, which is thought to have led to the observed reduction in skin roughness.[11]

3.4 Reduced pore size

In one controlled, double-blind study of 563 patients, close to 40% treated with 0.1% tazarotene achieved at least a 1-grade improvement in pore size, compared to close to 30% of those treated with vehicle after 24 weeks, with further clinical improvement observed over another 28 weeks of treatment.[8] These results are supported by 2 other double-blind studies, which also found an improvement in the appearance of pore size following treatment with 0.1% tazarotene.[9][13]

This has been hypothesized to be related to tazarotene's anti-acne activity, i.e. its ability to help normalize the differentiation of follicular epithelium, which promotes the clearance of comedones and microcomedones, preventing further follicular buildup. By clearing follicles, tazarotene may allow them to become visibly smaller.[8]

3.5 Increased epidermal thickness

In one study, 0.1% tazarotene gel increased epidermal thickness by 90% over 12 weeks.[10] A second study focusing on the histological effects of tazarotene also discovered a increase in mean epidermal thickness after 24 weeks of treatment, though the magnitude of this effect was smaller (40%).[11]

This effect appears due to an increase in the rate of epidermal proliferation and the greater number of cell layers.[10][11]

3.6 Tightening effect

One early controlled, double-blind trial found that laxity (looseness) was improved in 0.1% tazarotene-treated skin after 12 weeks, compared with baseline.[10]

3.7 Psoriasis treatment

Tazarotene is effective as a treatment for many variants of psoriasis, a chronic inflammatory skin condition.[14] Although effective as a single agent, evidence is accumulating that combining topical tazarotene with other established antipsoriatic therapies results in enhanced efficacy and reduced adverse events.[15]

The efficacy of tazarotene monotherapy and combination therapies has been thoroughly evaluated with respect to the treatment of plaque psoriasis, the most common form of psoriasis. Multicenter, double-blind, randomized, vehicle-controlled studies have shown that 0.05% or 0.1% tazarotene creams significantly reduce the severity of the clinical signs of psoriasis.[16] 0.1% tazarotene gel has comparable clinical efficacy to crude coal tar ointment[17] and 0.005% calipotriol ointment,[18] but is less effective than 0.05% clobetasol propionate cream.[19]

Tazarotene plus topical corticosteroids as a combination therapy has a greater therapeutic effect than that with tazarotene alone, reduced the irritancy of tazarotene, and decreased the risk of post-treatment disease flare seen with corticosteroids.[20][21][22][23] Tazarotene in combination with phototherapy on the other hand offers a therapeutic option for psoriasis that is faster than phototherapy alone.[24][25][26][27]

Topical tazarotene is also effective in treating psoriasis of the nails (nail psoriasis) and psoriasis of the hands and feet (palmoplantar psoriasis). 0.1% tazarotene gel significantly reduced onycholysis in occluded and nonoccluded nails as well as pitting in occluded nails in one study.[28] Tazarotene formulated as a 0.1% hydrophilic ointment, or as a cream in combination with pulsed dye laser treatment, is similarly efficacious.[29][30] Furthermore, 0.1% tazarotene cream appears to be as effective as clobetasol propionate in treating palmoplantar psoriasis, and is thus a good alternative where hypopigmentation limits the use of clobetasol propionate cream.[31]

Clinical improvements of psoriasis with the topical application of tazarotene is associated with the restoration of normal keratinocyte proliferation and differentation, and a decrease in epidermal inflammation.[32][33]

3.8 Acne vulgaris treatment

Multiple double-blind, vehicle-controlled trials have demonstrated the efficacy of tazarotene gels and creams in reducing both inflammatory and non-inflammatory acne lesion counts.[34][35] Short-contact application of tazarotene gel as well as tazarotene foam, devised to minimize local adverse events, has also been found to be safe and effective methods of acne treatment.[36][37][38] Moreover, 0.1% tazarotene cream successfully treated postinflammatory hyperpigmentation in patients from darker racial ethnic groups.[39]

The efficacy of topical tazarotene has been compared with that of topical adapalene. While some studies have indicated that 0.1% tazarotene had better efficacy than 0.1% or even 0.3% adapalene,[40][41][42] other studies have concluded that tazarotene provided similar efficacy as adapalene.[43][44][45] Studies also differ on the tolerability of tazarotene versus adapalene, with some claiming similar tolerability[40][41][42][44] while others have found adapalene to be better tolerated.[43][46][45]

0.1% tazarotene gel has also been consistently shown to be more efficacious than 0.025% tretinoin gel or 0.1% tretinoin microsponge gel, while having comparable tolerability.[47][48][49] In a more recent study, 0.05% tazarotene cream had equal efficacy, but superior tolerability, compared to 0.04% tretinoin microsphere gel pump in mild to moderate facial acne vulgaris.[50]

Tazarotene together with other anti-acne agents is more effective than tazarotene monotherapy. The adjunctive use of clindamycin and benzoyl peroxide enhances the efficacy of tazarotene, leading to greater reductions in comedo and inflammatory lesion counts.[51][52] This combination is also more effective than tretinoin plus clindamycin.[53] Another promising combination therapy is 0.1% tazarotene cream plus 5% dapsone gel, an anti-inflammatory agent.[54]

4. Side Effects

4.1 Dermatitis

Daily application of tazarotene is associated with minimal local side effects.[55] Adverse events are similar to those induced by other topical retinoids, that is, irritation, erythema, dryness, desquamation and a burning sensation on the treated sites.[9][13]

These tend to be of mild or moderate severity, and occur predominantly in the first few weeks of treatment.[13] Tolerability improves with continued treatment as the skin becomes accommodated to the retinoid.[8] In most cases, the side effects were not serious enough to cause patients to drop-out of the clinical studies.[8][10][13]

Tazarotene foam has also been demonstrated to have low potential for contact sensitization.[56]

Scientific References


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