Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

Bagatin, Ediléia; Wagemaker, Tais A. L.; Júnior, Nelson dos Reis Aguiar; Gianeti, Mirela D.; Gonçalves, Erika Maria Berardo; Campos, Patrícia Maria Berardo Gonçalves Maia

doi:10.1590/s1984-82502015000100009

Cited by 6 publications

(10 citation statements)

References 23 publications

(21 reference statements)

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“…It is widely used for the topical treatment of various skin disorders, such as acne vulgaris and skin aging caused by UV radiation (photo-aging) [ 2 ]. It may also be used in so-called off-label indications, such as psoriasis, ichthyosis, follicular keratosis, stretch marks, verruca vulgaris, cutaneous warts [ 3 ], cutaneous lupus erythematosus [ 4 ], melasma (hyperpigmentation) [ 5 ], and squamous cell carcinoma [ 6 ]. Beyond that, it seems to be helpful in the prevention of non-melanoma skin cancer [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

et al. 2023

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Background: Tretinoin (TRE) is, for its anti-comedogenic and comedolytic activity, widely used in the topical treatment of acne vulgaris. The effect lies in the regulation of sebum production and collagen synthesis. The study is devoted to the formulation of dermal gels containing TRE using microemulsion as the drug solubilizer. Methods: The aim was to evaluate the effect of the reference microemulsion (ME) and lecithin-containing microemulsion (MEL) on the release of TRE through the synthetic membrane (in vitro) and the pig’s ear skin (ex vivo) through the Franz cell diffusion method. Subsequently, after an ex vivo study, the amount of the drug in the skin influenced by the applied formulation was determined. In addition, the impact of ME on the microscopic structure, texture, and rheological properties of gels was evaluated. Results: On the basis of the analysis of texture, rheological properties, and drug release studies, Carbopol formulations appear to be more appropriate and stable. Considering the synthetic membrane as a stratum corneum, the Carbopol gel penetrated about 2.5-higher amounts of TRE compared to the Xanthan gel. In turn, ex vivo studies suggest that MEL slows the drug transfer to the dissolution medium, simulating absorption into the blood, which is a desirable effect in local treatment. The drug retention study proved the highest amounts of TRE in the skin to which microemulsion-Carbopol formulations were applied. Conclusion: The results confirm the benefit of TRE solubilization in ME due to its bioavailability from the tested dermal formulations.

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Section: Introductionmentioning

confidence: 99%

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

et al. 2023

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“…A study from 2015 showed that most of the tretinoin peel was retained in the stratum corneum. 44 This might explain why tretinoin peels do not cause burning, stinging, pain or irritation at such high concentrations - which is commonly seen in home use of commercial formulations of the same agent at low concentrations. This very superficial retention of tretinoin peel implies that its only effect is an exfoliation of the stratum corneum, without action on the RAR of viable keratinocytes from the deeper layers of the epidermis.…”

Section: Tretinoin and Aging Skinmentioning

confidence: 99%

“…This very superficial retention of tretinoin peel implies that its only effect is an exfoliation of the stratum corneum, without action on the RAR of viable keratinocytes from the deeper layers of the epidermis. 31 , 43 , 44 Therefore the sequential peels effect may not be similar to daily use of standard concentrations of tretinoin cream for melasma and photoaging.…”

Section: Tretinoin and Aging Skinmentioning

confidence: 99%

Tretinoin peel: a critical view

Sumita

Leonardi

Bagatin

2017

An. Bras. Dermatol.

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The tretinoin peel, also known as retinoic acid peel, is a superficial peeling often performed in dermatological clinics in Brazil. The first study on this was published in 2001, by Cuce et al., as a treatment option for melasma. Since then, other studies have reported its applicability with reasonable methodology, although without a consistent scientific background and consensus. Topical tretinoin is used for the treatment of various dermatoses such as acne, melasma, scars, skin aging and non-melanoma skin cancer. The identification of retinoids cellular receptors was reported in 1987, but a direct cause-effect relation has not been established. This article reviews studies evaluating the use of topical tretinoin as agent for superficial chemical peel. Most of them have shown benefits in the treatment of melasma and skin aging. A better quality methodology in the study design, considering indication and intervention is indispensable regarding concentration, vehicle and treatment regimen (interval and number of applications). Additionally, more controlled and randomized studies comparing the treatment with tretinoin cream versus its use as a peeling agent, mainly for melasma and photoaging, are necessary.

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“…To the best of our knowledge, there is still a lack of validated, simple, and suitable methods to assay TTN in different porcine skin layers for penetration/retention studies from dermatological formulations, such as creams and gels. Most studies have not evaluated TTN penetration in different skin layers, separately [24,25,26], or they used other skin models [27,28]. Porcine is the most used skin model for penetration/permeation studies due to its similarity to human skin in terms of its anatomical and physiological characteristics [29,30].…”

Section: Introductionmentioning

confidence: 99%

Liquid chromatography method to assay tretinoin in skin layers: validation and application in skin penetration/retention studies

Oliveira

Andrade

Oliveira

et al. 2020

Heliyon

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A B S T R A C TA liquid chromatography (LC) method for the quantification of tretinoin (TTN) in different matrices (adhesive tape, cotton and porcine skin layers, stratum corneum, viable epidermis, and dermis) was validated and applied in in vitro porcine skin penetration/retention studies. This study proposes, for the first time, a method for assaying TTN in separated porcine skin layers (stratum corneum, viable epidermis, and dermis). The skin studies were carried out using tape stripping and cutaneous retention techniques. The procedures for the extraction of TTN from dermatological formulations (creams and gels) and biological and non-biological matrices used with the tape stripping and retention techniques were also evaluated. The LC method consisted of a mobile phase composed of a mixture of methanol, water, and glacial acetic acid (85:15:1, v/v); a C18 column used as the stationary phase; a flow rate of 1.0 mL min À1 ; an injection volume of 100 μL; and TTN detection at 342 nm. The method was linear in the range of 0.05-15.00 μg mL À1 (r ¼ 0.9999), and it was precise and accurate. The limit of detection (LOD) and limit of quantification (LOQ) were 0.0165 μg mL À1 and 0.0495 μg mL À1 , respectively. TTN was extracted from different matrices, showing good precision [relative standard deviation (RSD) of <5%] and accuracy (89.4-113.9%). This method was successfully applied in the evaluation of TTN skin retention/permeation from dermatological formulations (cream and gel). A higher penetration of TTN through the skin was achieved with the gel rather than the cream, showing the influence of the dosage form. Therefore, the developed method can easily be applied in porcine skin penetration/retention studies of dermatological formulations containing TTN, and it is able to discriminate the behaviours of the different formulations.

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Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

Cited by 6 publications

References 23 publications

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

Tretinoin peel: a critical view

Liquid chromatography method to assay tretinoin in skin layers: validation and application in skin penetration/retention studies

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