50 Years of Topical Retinoids for Acne: Evolution of Treatment

Baldwin, Hilary; Webster, Guy F.; Gold, Linda F Stein; Callender, Valerie D.; Cook‐Bolden, Fran; Guenin, Eric

doi:10.1007/s40257-021-00594-8

Cited by 48 publications

(49 citation statements)

References 51 publications

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“…Topical retinoids, such as adapalene, are a mainstay of acne treatment; they normalize keratinocyte proliferation, block several inflammatory pathways, promote comedolysis, and reduce microcomedonal formation. While they are generally well tolerated, their use can be limited by dryness, irritation, and erythema [ 8 , 17 ]. Adapalene—a third-generation retinoid that modulates cellular keratinization, differentiation, and proliferation [ 8 , 18 ]—has the advantage of being one of the most tolerable retinoids [ 19 ] that also retains its stability in the presence of BPO [ 9 ].…”

Section: Discussionmentioning

confidence: 99%

“…While they are generally well tolerated, their use can be limited by dryness, irritation, and erythema [ 8 , 17 ]. Adapalene—a third-generation retinoid that modulates cellular keratinization, differentiation, and proliferation [ 8 , 18 ]—has the advantage of being one of the most tolerable retinoids [ 19 ] that also retains its stability in the presence of BPO [ 9 ]. Benzoyl peroxide is an antibacterial agent with mild comedolytic activity, keratolytic effects, and good efficacy and tolerability [ 2 , 20 – 22 ]; it is unaffected by C. acnes resistance, [ 20 ] and has been used in combination with topical and oral antibiotics because of its ability to reduce resistant C. acnes populations [ 23 ].…”

Section: Discussionmentioning

confidence: 99%

“…Formulated as an aqueous gel, with no alcohol, preservatives, occlusive agents, or surfactants, it is pH balanced for the skin and contains propylene glycol, a hydrating humectant. As a smaller particle size allows for better penetration of the pilosebaceous unit [ 7 , 8 ], BPO and adapalene have been micronized. Additionally, all ingredients are contained within a polymeric gel to allow for even distribution on the skin.…”

Section: Introductionmentioning

confidence: 99%

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Efficacy and Safety of a Fixed-Dose Clindamycin Phosphate 1.2%, Benzoyl Peroxide 3.1%, and Adapalene 0.15% Gel for Moderate-to-Severe Acne: A Randomized Phase II Study of the First Triple-Combination Drug

et al. 2021

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Background A three-pronged approach to acne treatment-combining an antibiotic, antibacterial, and retinoid-could provide greater efficacy and tolerability than single or dyad treatments, while potentially improving patient compliance and reducing antibiotic resistance. Objectives We aimed to evaluate the efficacy and safety of triple-combination, fixed-dose topical clindamycin phosphate 1.2%/benzoyl peroxide (BPO) 3.1%/adapalene 0.15% (IDP-126) gel for the treatment of acne. Methods In a phase II, double-blind, multicenter, randomized, 12-week study, eligible participants aged ≥ 9 years with moderate-to-severe acne were equally randomized to once-daily IDP-126, vehicle, or one of three component dyad gels: BPO/adapalene; clindamycin phosphate/BPO; or clindamycin phosphate/adapalene. Coprimary endpoints were treatment success at week 12 (participants achieving a ≥ 2-grade reduction from baseline in Evaluator's Global Severity Score and clear/almost clear skin) and least-squares mean absolute changes from baseline in inflammatory and noninflammatory lesion counts to week 12. Treatment-emergent adverse events and cutaneous safety/tolerability were also assessed. Results A total of 741 participants were enrolled. At week 12, 52.5% of participants achieved treatment success with IDP-126 vs vehicle (8.1%) and dyads (range 27.8-30.5%; P ≤ 0.001, all). IDP-126 also provided significantly greater absolute reductions in inflammatory (29.9) and noninflammatory (35.5) lesions compared with vehicle or dyads (range inflammatory, 19.6-26.8; noninflammatory, 21.8-30.0; P < 0.05, all), corresponding to > 70% reductions with IDP-126. IDP-126 was well tolerated, with most treatment-emergent adverse events of mild-to-moderate severity. Conclusions Once-daily treatment with the novel fixed-dose triple-combination clindamycin phosphate 1.2%/BPO 3.1%/ adapalene 0.15% gel demonstrated superior efficacy to vehicle and all three dyad component gels, and was well tolerated over 12 weeks in pediatric, adolescent, and adult participants with moderate-to-severe acne. Clinical Trial Registration ClinicalTrials.gov identifier NCT03170388 (registered 31 May, 2017).

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Efficacy and Safety of a Fixed-Dose Clindamycin Phosphate 1.2%, Benzoyl Peroxide 3.1%, and Adapalene 0.15% Gel for Moderate-to-Severe Acne: A Randomized Phase II Study of the First Triple-Combination Drug

et al. 2021

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“…Although retinoids offer benefits in terms of effective acne treatment and favorable hyperpigmentation outcomes, they can be irritating—which in itself can contribute to unwanted pigmentary changes [ 30 ]. To address issues of irritation and tolerability, novel lotion formulations were developed for tretinoin and tazarotene [ 31 ]. Tretinoin 0.05% lotion was developed using a polymeric emulsion technology resulting in a honeycomb matrix that provides uniform distribution of the active ingredient (which was micronized for more homogeneous dispersion and to promote diffusion into skin follicular openings), along with a homogeneous dispersion of the moisturizing/hydrating ingredients [ 32 ].…”

Section: Retinoids Acne and Hyperpigmentationmentioning

confidence: 99%

Effects of Topical Retinoids on Acne and Post-inflammatory Hyperpigmentation in Patients with Skin of Color: A Clinical Review and Implications for Practice

et al. 2021

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Acne is a common cause for post-inflammatory hyperpigmentation (PIH), particularly in patients with skin of color (SOC), and PIH is often more distressing to patients than the acne itself. Topical retinoids are approved for the treatment of acne and for pigmentation disorders such as melasma or mottled hyperpigmentation associated with photodamage; moreover, they have been shown to reduce hyperpigmentation in patients with SOC. Therefore, treatment with topical retinoids should be started as early as possible unless contraindicated. Use of novel formulations or application of commonly recommended moisturizers may help reduce irritation. Combining retinoids with other topical agents and procedures such as superficial chemical peels can help to improve hyperpigmentation. Primary acne lesions are likely to improve weeks before PIH resolves and helping patients manage their expectations may reduce frustration. Providing clinicians and researchers with more education about the presentation and management of dermatologic conditions in patients with SOC is also recommended.

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“…They have antiphlogistic, immunomodulatory, antiproliferative, and differentiating effects on keratinocytes, lymphocytes, and sebocytes [1]. the most popular topical therapy is tazarotene [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17], which, chemically, is ethyl-[2-(4,4-dimethylthiochroman-6-yl)-ethynyl] nicotinate. Tazarotene is in organism rapidly hydrolysed by esterases to a biologically active form-tazarotenic acid 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinic acid (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Controlled Release of Tazarotene from Magnetically Responsive Nanofiber Patch: Towards More Efficient Topical Therapy of Psoriasis

et al. 2021

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Electrospun polycaprolactone nanofibers with embedded magnetic nanoparticles were developed for use in the topical delivery of antipsoriatic drugs. To test a hydrophobic drug, a tazarotene has been used, which is an efficient retinoid derivative. Such a smart hyperthermia nanofiber system with self-generated heat from the incorporated magnetic nanoparticles induced drug release in response to on–off switching of alternating magnetic fields for the delivery of tazarotene through the skin, as quantified using Franz cells. This highly efficient external field-controllable system with minimal skin irritation could create a new avenue for the topical therapy of psoriasis.

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50 Years of Topical Retinoids for Acne: Evolution of Treatment

Cited by 48 publications

References 51 publications

Efficacy and Safety of a Fixed-Dose Clindamycin Phosphate 1.2%, Benzoyl Peroxide 3.1%, and Adapalene 0.15% Gel for Moderate-to-Severe Acne: A Randomized Phase II Study of the First Triple-Combination Drug

Efficacy and Safety of a Fixed-Dose Clindamycin Phosphate 1.2%, Benzoyl Peroxide 3.1%, and Adapalene 0.15% Gel for Moderate-to-Severe Acne: A Randomized Phase II Study of the First Triple-Combination Drug

Effects of Topical Retinoids on Acne and Post-inflammatory Hyperpigmentation in Patients with Skin of Color: A Clinical Review and Implications for Practice

Controlled Release of Tazarotene from Magnetically Responsive Nanofiber Patch: Towards More Efficient Topical Therapy of Psoriasis

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