Human in vivo pharmacology of topical retinoids

Griffiths, C.E.M.; Voorhees, John J.

doi:10.1007/bf00370719

Cited by 20 publications

(8 citation statements)

References 66 publications

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“…Retinoic acid, for instance, is known to increase cell proliferation and decrease ceramide biosynthesis leading to skin xerosis, at least in the short term [10].…”

Section: Discussionmentioning

confidence: 99%

Effect of lactic acid isomers on keratinocyte ceramide synthesis, stratum corneum lipid levels and stratum corneum barrier function

et al. 1996

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Alpha-hydroxy acids are effective agents for the treatment of skin xerosis and it is known that, following treatment with lotions containing D,L-lactic acid, the stratum corneum prevents xerosis more effectively. To date, the relative efficacy of the different isomers of lactic acid has not been evaluated and the mode of action of lactic acid in improving stratum corneum resilience is not known. The objective of the present studies was to determine the effects of lactic acid isomers on keratinocyte ceramide biosynthesis, stratum corneum barrier function and the resistance of the stratum corneum to the appearance of skin xerosis. In vitro, lactic acid enhanced the production of ceramides by keratinocytes. L-Lactic acid was more effective than the D isomer (300% increase vs 100% increase). Carbon label from lactic acid was incorporated into all keratinocyte lipid species and a greater incorporation of label into ceramides was achieved with L-lactate than with D-lactate. In vivo, lactic acid increased the levels of stratum corneum ceramides. Whereas, lotions containing L-lactic acid resulted in the greatest increase (48% increase) followed by D,L-lactic acid (25% increase), D-lactic acid had no effect on stratum corneum ceramide levels. The increases in stratum corneum ceramide levels following lactic acid treatment also led to improvements in stratum corneum barrier function, measured by transepidermal water loss following a challenge to the skin with SLS and in the regression phase of a moisturization efficacy study. Significant improvements in barrier function and resistance to the appearance of skin xerosis were observed following L-lactic acid and D,L-lactic acid, but not following D-lactic acid treatment. From these results we believe that lactic acid, particularly the L isomer, stimulates ceramide biosynthesis leading to increased stratum corneum ceramide levels which results in superior lipid barrier and a more effective resistance against xerosis.

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“…Retinoic acid, for instance, is known to increase cell proliferation and decrease ceramide biosynthesis leading to skin xerosis, at least in the short term [10].…”

Section: Discussionmentioning

confidence: 99%

Effect of lactic acid isomers on keratinocyte ceramide synthesis, stratum corneum lipid levels and stratum corneum barrier function

et al. 1996

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“…This once-daily treatment reverses the abnormal follicular desquamation and inflammatory responses involved in the pathogenesis of acne [8][9][10][11][12]. Adapalene gel 0.1% applied on the skin of patients with acne vulgaris is thought to exhibit retinoid-like activity by initiating a sequential process consisting of binding to the nuclear retinoic acid receptors g, activating the transactivation function in the cell nucleus, normalizing the abnormal keratinization of follicular epithelial cells leading to the reduction of the formation and development of comedones thus reducing the number of comedones [13]. The efficacy and safety of adapalene has been established in numerous clinical trials [12,[14][15][16][17][18][19][20][21][22][23][24][25].…”

Section: Introductionmentioning

confidence: 99%

Adapalene gel 0.1% is effective and safe for Japanese patients with acne vulgaris: A randomized, multicenter, investigator-blinded, controlled study

Kawashima

Harada

Loesche

et al. 2008

Journal of Dermatological Science

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“…These ligand-dependent transcription factors bind retinoids either as homodimers (RAR/RAR, RXR/RXR) or heterodimers (RAR/RXR) [4], which then can induce subsequent target gene expression by binding to the retinoid-responsive elements (RAREs and RXREs) in the promotor region of such genes [5, 6, 7]. They also inhibit the expression of genes without retinoid-responsive elements by downregulating the action of other transcription factors such as activator protein-1 (AP-1) and nuclear factor for interleukin-6 (NF-IL6), probably through mechanisms of competition for commonly required co-activator proteins [8, 9, 10].…”

Section: Topical Retinoidsmentioning

confidence: 99%

Topical Treatment in Acne: Current Status and Future Aspects

Gollnick

Krautheim²

2003

Dermatology

110

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During the last 20 years, the number of topical and systemic drugs for the treatment of acne vulgaris has been enriched. Topical drugs on the one hand have been newly discovered or further developments of already available agents such as in the group of retinoids or galenic formulation have improved efficacy or local tolerance. Topical retinoids are a mainstay in acne treatment since 1962. All-trans retinoic acid was the first and is still in use. Its irritative potential has led to the new galenics, i.e. incorporation in microsponges and in propolyomers, which increased the tolerability significantly. The isomer of tretinoin, isotretinoin, has the same clinical efficacy, but also a lower irritancy. A real breakthrough was adapalene, a retinoid-like agent, with a different retinoid receptor-binding profile, but in addition to the same clinical efficacy on inflammatory and non-inflammatory acne lesions compared to tretinoin, a better tolerability and, therefore, compliance. Unfortunately, over the past years topical retinoids have been less used in inflammatory acne than they should be, taking the the mechanisms of action into account. Topical antimicrobials, in particular topical antibiotics, should be used less often than in the past and only for short periods to avoid the development of resistances. It seems better to combine those agents with topical retinoids, with BPO or with azelaic acid to enhance the efficacy and slow down the development of resistance. BPO is still the gold standard for papular-pustular acne of mild-to-moderate type in concentrations of 2–5%. Azelaic acid is an alternative with efficacy on the comedo and is antibacterial without development of resistances. Finally, the physical removal by electrocautery or CO₂ laser of multiple densely packed closed comedones, macrocomedones and microcysts is necessary to enhance the efficacy of topical comedolytic agents and to speed up the therapeutic results. Photodynamic therapy has not yet been proven efficacious in controlled studies. Blue and red light can probably be used in association with local agents but enhancement of the irritative potential of topical and systemic agents has to be considered.

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Human in vivo pharmacology of topical retinoids

Cited by 20 publications

References 66 publications

Effect of lactic acid isomers on keratinocyte ceramide synthesis, stratum corneum lipid levels and stratum corneum barrier function

Effect of lactic acid isomers on keratinocyte ceramide synthesis, stratum corneum lipid levels and stratum corneum barrier function

Adapalene gel 0.1% is effective and safe for Japanese patients with acne vulgaris: A randomized, multicenter, investigator-blinded, controlled study

Topical Treatment in Acne: Current Status and Future Aspects

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