Comedolytic Effect of Topical Retinaldehyde in the Rhino Mouse Model

Fort-Lacoste, L.; Verscheure, Y.; Tisné-Versailles, J; Navarro, Ricardo Navarro

doi:10.1159/000051376

Cited by 24 publications

(21 citation statements)

References 3 publications

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“…A 3-week topical treatment induced a significant decrease in both the size and density of dermal cysts, an effect also observed with topical retinoids on the rhino mouse model [12] or the coaltar-induced comedogenesis in the rabbit ear model [Navarro et al, pers. commun.].…”

mentioning

confidence: 85%

“…Likewise, all-trans-retinaldehyde (RAL) is converted by epidermal cells to both storage (all-trans-retinyl esters) and active (RA) forms of vitamin A and exerts significant retinoid biological activities [5][6][7], with a very good local tolerance even at a concentration of 0.1% [10,11]. On the other hand, RAL showed comedolytic [12] and antibacterial activities [13,14]. Recently, ·-hydroxy acids (AHAs) and particularly glycolic acid (GA) gained importance in dermatological applications, such as products against skin ageing.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

et al. 2005

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Background: Retinoids and α-hydroxy acids (AHAs) are major compounds in topical therapy. They exert distinct but potentially complementary activities. However, their association is limited by their respective irritating potential. Recently, the first association between a retinoid and an AHA has been achieved; this formulation (RALGA) associates retinaldehyde (RAL) – a precursor of retinoic acid (RA) – and glycolic acid (GA) – an AHA. Objective: To study the pharmacological properties of RALGA. Methods: The bioavailability of RAL into the skin after topical RALGA was studied by HPLC, and its bioconversion to RA was analysed by measuring the enzyme activity of retinaldehyde dehydrogenase and the RA content in the epidermis and dermis. The retinoid activity of RALGA was studied on the modulation of Hhb4 keratin mRNA on the tail of C57BL/6 mice, and its comedolytic properties on the size and density of dermal cysts and the morphology of sebaceous glands in hairless mice. Results: Epidermal and dermal concentrations of RAL and RA were higher after RALGA treatment, as compared to both RAL 0.1% alone and RA 0.05% alone; this indicates that the presence of GA favours the bioavailability and biotransformation of RAL into RA. The retinoid activity of RALGA (suppression of Hhb4 mRNA keratin) was similar to that of RAL alone, indicating that the presence of GA does not interfere with specific retinoid activity; GA alone had no effect in this test, which confirms the specificity of Hhb4 mRNA keratin modulation for retinoid activity. The diameter and the density of dermal cysts as well as the size of sebaceous glands were significantly decreased by RALGA. Conclusion: These observations indicate that the addition of an AHA such as GA to a retinoid such as RAL results in a better bioavailability of the retinoid, thus a higher delivery of RA, which potentiates the biological activities of the retinoid. This combination allows a delivery of high amounts of RA in the skin while preventing the side-effects usually observed with high concentrations of topical RA.

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confidence: 85%

Section: Introductionmentioning

confidence: 99%

Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

et al. 2005

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“…RAL has revealed a retinoid-like activity in the stimulation of proliferation and differentiation, comedolysis, inhibition of protein expression (in particular melanin) and increase in epidermal thickness [24,26,27]. RAL also shows a specific antibacterial activity against Propionibacterium acnes [28,29].…”

Section: Retinaldehydementioning

confidence: 99%

RALGA (Diacnéal<sup>®</sup>), a Retinaldehyde and Glycolic Acid Association and Postinflammatory Hyperpigmentation in Acne – A Review

Katsambas¹

2005

Dermatology

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Acne vulgaris affects 3 out of 4 adolescents and usually vanishes at the end of puberty with either no sequelae or mild to moderate sequelae, such as postinflammatory hyperpigmenation (PIH), which may result in psychological and emotional damages. The poor tolerability of the actual treatments (secondary inflammation) is a hindrance to therapy. Retinaldehyde (RAL), a precursor of retinoic acid, has shown depigmenting activity. Glycolic acid (GA) decreases the excess of pigment by a wounding and re-epithelization process. Thus, a synergistic effect was expected from the combination of RAL 0.1% and GA 6% RALGA (Diacnéal^®) in the treatment of acne vulgaris and PIH. Efficacy results of preclinical and clinical trials tend to confirm the expectations for both acne and PIH treatment. A good tolerability was observed. In conclusion, the cosmetic cream Diacnéal is a well-tolerated treatment for the prevention and healing of PIH in acne patients.

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“…RAL is a key intermediate element in the metabolism of natural vitamin A in human and mouse keratinocytes [8][9][10] and leads to measurable biological activity in the skin [11,12]. Moreover, RAL is well tolerated by humans [12], and, in animal models, RAL works at least as well as retinoic acid in resolving comedonal acne [8].…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, RAL is well tolerated by humans [12], and, in animal models, RAL works at least as well as retinoic acid in resolving comedonal acne [8]. In humans, in vivo and in vitro studies have demonstrated that RAL exerts a direct antibacterial activity against Propionibacterium acnes, while retinoic acid does not [10,13].…”

Section: Introductionmentioning

confidence: 99%

Topical Retinaldehyde with Glycolic Acid: Study of Tolerance and Acceptability in Association with Anti-Acne Treatments in 1,709 Patients

et al. 2005

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Background: Retinaldehyde (RAL), a key metabolite between vitamin A and retinoic acid, acts by modulating differentiation and proliferation of keratinocytes, which is of interest in acne lesions, mainly retentional lesions. Glycolic acid increases the exfoliation of corneocytes explaining its mild activity on retentional lesions. Thus, RAL and glycolic acid combined in the same product (Diacnéal^®) have complementary activities which can be of interest for acne patients. The aim of this study was to evaluate the tolerance of Diacnéal used by 1,709 acne patients in combination with their usual acne products except retinoids. Results: This study demonstrated a very good tolerance of Diacnéal when used with other acne treatments for 90 days. Complaints about side-effects were rare. Moreover, the significant decrease in both inflammatory and retentional lesions between day 0 and day 90 indicates that Diacnéal could amplify the efficiency of other anti-acne products used at the same time by the patients. The subjective evaluation of the preparation’s efficacy by investigators and patients was strongly favourable. Conclusion: These data show that a combination of RAL 0.1% and glycolic acid 6% may be used in association with other topical anti-acne treatments (benzoyl peroxide and topical antibiotics) with an excellent tolerance.

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Comedolytic Effect of Topical Retinaldehyde in the Rhino Mouse Model

Cited by 24 publications

References 3 publications

Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

RALGA (Diacnéal<sup>®</sup>), a Retinaldehyde and Glycolic Acid Association and Postinflammatory Hyperpigmentation in Acne – A Review

Topical Retinaldehyde with Glycolic Acid: Study of Tolerance and Acceptability in Association with Anti-Acne Treatments in 1,709 Patients

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