Topical emulsions containing ceramides: Effects on the skin barrier function and anti‐inflammatory properties

Carneiro, Rita Terezinha de Oliveira; Salgado, Ana; Raposo, Sara; Marto, Joana; Simões, Sandra; Urbano, Manuela; Ribeiro, Helena Margarida

doi:10.1002/ejlt.201000495

Cited by 19 publications

(17 citation statements)

References 22 publications

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“…SC CERs can be generated either by serine palmitoyl transferase catalyzed de novo synthesis, which converts palmitoyl-CoA and L -serine into CERs [35], or by β- glucocerebrosidase [36] and acid sphingomyelinase [37] catalyzed hydrolysis of glucosylceramides (GlcCERs) and sphingomyelin (SPM), respectively. Large quantities of GlcCER and SPM precursors are produced in the epidermis and delivered to SC extracellular lipid domains.…”

Section: Epidermal Cers and Glucosylceramidesmentioning

confidence: 99%

“…The level of epidermal CERs is, therefore, regulated by the balance between β-glucocerebrosidase, sphingomyelinase, and ceramidase (which metabolizes CERs into SBs and free FAs) [3]. The deficiency of β-glucocerebrosidase in the epidermis alters the distribution of CERs and GlcCERs and the epidermal permeability barrier [36,43]. The impact of epidermal sphingolipids on the SC structure as well as their role in skin disorders have been reviewed by different authors [27,44].…”

Section: Epidermal Cers and Glucosylceramidesmentioning

confidence: 99%

“…With the recent understanding of the pathophysiological processes of skin diseases, different topical formulations containing CERs, pseudo-CERs, or agents correcting the depleted CERs have been produced [153], in addition to skin moisturizers. Studies have shown that CER-dominant emollients [154,155,156,157,158], CER [36,159], and pseudo-CER containing topical products [160,161,162] have beneficial effects in the management of skin diseases related to perturbation of SC lipids. However, many of these cosmetic products have limited published data to document their cutaneous efficacy [153].…”

Section: Topical Delivery Of Phytocersmentioning

confidence: 99%

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Potential Applications of Phyto-Derived Ceramides in Improving Epidermal Barrier Function

Tessema

Gebre‐Mariam

Neubert

et al. 2017

Skin Pharmacol Physiol

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The outer most layer of the skin, the stratum corneum, consists of corneocytes which are coated by a cornified envelope and embedded in a lipid matrix of ordered lamellar structure. It is responsible for the skin barrier function. Ceramides (CERs) are the backbone of the intercellular lipid membranes. Skin diseases such as atopic dermatitis and psoriasis and aged skin are characterized by dysfunctional skin barrier and dryness which are associated with reduced levels of CERs. Previously, the effectiveness of supplementation of synthetic and animal-based CERs in replenishing the depleted natural skin CERs and restoring the skin barrier function have been investigated. Recently, however, the barrier function improving effect of plant-derived CERs has attracted much attention. Phyto-derived CERs (phytoCERs) are preferable due to their assumed higher safety as they are mostly isolated from dietary sources. The beneficial effects of phytoCER-based oral dietary supplements for skin hydration and skin barrier reinforcement have been indicated in several studies involving animal models as well as human subjects. Ingestible dietary supplements containing phytoCERs are also widely available on the market. Nonetheless, little effort has been made to investigate the potential cosmetic applications of topically administered phytoCERs. Therefore, summarizing the foregoing investigations and identifying the gap in the scientific data on plant-derived CERs intended for skin-health benefits are of paramount importance. In this review, an attempt is made to synthesize the information available in the literature regarding the effects of phytoCER-based oral dietary supplements on skin hydration and barrier function with the underlying mechanisms.

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Section: Epidermal Cers and Glucosylceramidesmentioning

confidence: 99%

Section: Epidermal Cers and Glucosylceramidesmentioning

confidence: 99%

Section: Topical Delivery Of Phytocersmentioning

confidence: 99%

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Potential Applications of Phyto-Derived Ceramides in Improving Epidermal Barrier Function

Tessema

Gebre‐Mariam

Neubert

et al. 2017

Skin Pharmacol Physiol

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“…The amount of corticosteroids recovered from the skin surface after penetration is usually high (about 60–95% of the dose applied) and forms a surface reservoir 13 14. The ability to develop a reservoir is highly dependent on the vehicle.…”

Section: Discussionmentioning

confidence: 99%

Betamethasone dipropionate compounding for cutaneous T-cell lymphoma management

Trindade¹,

Gelpi

Salgado³

et al. 2016

Eur J Hosp Pharm

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BackgroundPrimary cutaneous lymphomas (extranodular non-Hodgkin lymphomas) are rare (incidence 1:100 000). Mycosis fungoides is the most common cutaneous T-cell lymphoma (CTCL) subtype. Treatment options are based on the diagnosis and the stage of the disease. Skin-directed therapies are useful for the initial stages and include topical treatments such as corticosteroids. Betamethasone dipropionate (BD) is a synthetic glucocorticoid with high anti-inflammatory activity, potency and immunosuppressant effects. It is used for topical treatment of CTCL within the following dosage 0.025–0.1% (w/w). In the Portuguese market only one topical cream contains BD at 0.05% (w/w).ObjectivesTo develop a new and stable emulsion containing 0.1% of BD.MethodsTo accomplish this aim, development, stability, in vitro release and clinical studies of a new topical water-in-oil emulsion containing BD 0.1% w/w were assessed for the topical treatment of CTCL.ResultsThe three batches prepared were physically, chemically and microbiologically stable over a period of 90 days. 40% of BD was released over 6 hours and evaluation of skin lesions showed a favourable clinical effect (less itching, less infiltration, fewer patches and a reduced area of plaque).ConclusionsThe clinical results show the effective cutaneous improvement of skin barrier conditions during the study.

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“…Emollients are often used in the treatment of atopic dermatitis and other inflammatory dermatitis with the aim of improving skin hydration and mitigating xerosis. Given their resemblance to the lipids in the SC, beneficial effect of skin lipid supplementation both in composition and in the structuring of topical formulations for skin repair was already described (Coderch et al, 2002;Carneiro et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

et al. 2014

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Over the years, research has focused on strategies to increase benefit/risk ratio of corticoids. However, vehicles intended for topical glucocorticoids delivery with an improved benefit/risk ratio are still on demand. The aim of this work was the in vitro and in vivo characterization of cold processed oil-in-water (o/w) emulsions intended for mometasone furoate (MF) delivery to induce drug targeting to upper skin strata, decreasing adverse effects. Two o/w emulsions, containing 0.1% of MF, were developed differing in the glycol used (2-methyl-2,4-pentanediol -PT and ethoxydiglycol -TC emulsions). In vitro permeation studies revealed that these emulsions are suitable vehicles for the delivery of MF containing ingredients which are responsible for a drastically increased on the permeability coefficients of MF from a theoretical value of 1.18 Â 10 À4 cm/h to 5.20 Â 10 À4 AE 2.05 Â 10 À4 cm/h and 6.30 Â 10 À4 AE 2.94 Â 10 À4 cm/h, for PT and TC, respectively. The tape stripping results showed that the amount of drug that reached the viable skin layers was very low (1.99 %) and the amount that remained in the stratum corneum (SC) was 10.61%. The in vivo studies showed that the developed formulations decreased the edema and erythema in mice skin in more that 90%, assuring, at least, the same anti-inflammatory effect compared with the commercial cream. PT placebo demonstrated to contribute to restore the skin barrier by increasing the amount of lipids within the human skin.

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Topical emulsions containing ceramides: Effects on the skin barrier function and anti‐inflammatory properties

Cited by 19 publications

References 22 publications

Potential Applications of Phyto-Derived Ceramides in Improving Epidermal Barrier Function

Potential Applications of Phyto-Derived Ceramides in Improving Epidermal Barrier Function

Betamethasone dipropionate compounding for cutaneous T-cell lymphoma management

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

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