Skin Efficacy and Biophysical Assessment of Glycerol-Containing Hydrocolloid Patches

Paepe, Kristien De; Wibaux, Anne; Ward, Carol; Rogiers, Vera

doi:10.1159/000235553

Cited by 8 publications

(8 citation statements)

References 55 publications

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“…The penetration is therefore increased compared to the nanosuspension without additives. The penetration enhancement is concentration dependent, because the increase of the concentration of glycerol, i.e., from 2% to 5%, increased the skin moisturizing properties [ 44 ].…”

Section: Resultsmentioning

confidence: 99%

Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Pelikh

Keck

2020

Nanomaterials

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Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.

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Section: Resultsmentioning

confidence: 99%

Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Pelikh

Keck

2020

Nanomaterials

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“…They all increased skin hydration to the same extent. This was expected as 5% (w/w) of glycerol - well known for its stratum corneum humectancy - was added to the basic W/O formula in which the different silicones were incorporated [7,29,47,48]. …”

Section: Resultsmentioning

confidence: 99%

Silicones as Nonocclusive Topical Agents

Paepe

Sieg²,

Meur³

et al. 2014

Skin Pharmacol Physiol

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Background/Aims: Silicone excipients are commonly used ingredients because of their emollient and skin-conditioning effects, and their ability to form uniform, water-resistant, yet permeable films. Based on comparisons with organic materials and conflicting knowledge from silicones used in scar treatment, the misconception still exists that silicone topical excipients are occlusive substances that may block the passive loss of water through the upper skin layers. Therefore, 3 types of common silicone excipients and 3 water-in-(oil-plus-silicone) or W/(O + Si) creams, containing 10% (w/w) of the respective silicones, were investigated as a function of time and compared to petrolatum. Methods: Transepidermal water loss (TEWL) and skin hydration measurements were carried out after a single topical application on forearm skin of 26 healthy young female volunteers. Results: Both petrolatum and silicones significantly decreased TEWL 15 min after application, but the measurements for the silicones were not significantly different from the untreated control values. The tested silicones did not moisturize the skin. Petrolatum formed an occlusive layer, creating an increase in skin hydration for more than 4 h. The results measured for the W/(O + Si) creams indicated that they moisturized the skin, without any effect on TEWL. Conclusion: A clear difference was shown between the skin occlusive properties of petrolatum and the water vapor permeability of the common silicone excipient materials.

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“…Clinical studies have demonstrated that topical moisturizer alone improves psoriasis . Previous studies have shown that both Cer and glycerol, ingredients in our moisturizer, increase SC hydration in normal and diseased skin . In addition, the activation of PPARγ by LA upregulates aquaporin 3 expression , which in turn increases skin hydration .…”

Section: Discussionmentioning

confidence: 96%

Topical application of a linoleic acid-ceramide containing moisturizer exhibit therapeutic and preventive benefits for psoriasis vulgaris: a randomized controlled trial

Liu

Chen

et al. 2015

Dermatologic Therapy

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Psoriasis is a chronic skin inflammatory disorder with frequent relapse. Ceramides and their key enzymes are deficient in the lesions, resulting in impaired epidermal permeability barrier, which correlates with disease severity. We evaluated the efficacy of linoleic acid-ceramide moisturizer (LA-Cer) as an adjunctive and preventive therapy for psoriasis vulgaris. 106 patients were randomized into two groups. The control group (C1 ) received Mometasone Furoate 0.1% Cream (MF) while the treatment group (T1 ) was given 0.1% MF in combination with LA-Cer moisturizer. Psoriasis Area and Severity Index (PASI), pruritus, capacitance (CAP), and transepidermal water loss (TEWL) of normal skin and lesion were evaluated at Week 0, 2, 4, 8. Subsequently, T1 patients were randomized for another 1 year. LA-Cer-group (T2 ) maintained the use of moisturizer while control group (C2 ) discontinued. CAPs, TEWLs, PASI were assessed after 1 year. Primary endpoints (PASI-50 at Week 8) revealed superiority of LA-Cer-MF versus MF, less relapse, and rebound in LA-Cer-group than control (C2 ) at Year 1. There were time-by-therapy interaction effect on CAPs, lesional TEWL, and PASI. LA-Cer-MF induced higher CAP, an earlier reduction of lesional TEWL and PASI than control (C1 ). CAPs, lesional TEWL, and PASI remained stable in LA-Cer-group. CAPs, lesional TEWL, and PASI were comparable to the baseline levels in control group (C2 ). Topical LA-Cer moisturizer can alleviate psoriasis, and could be a valuable approach for the treatment and prevention of psoriasis.

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Skin Efficacy and Biophysical Assessment of Glycerol-Containing Hydrocolloid Patches

Cited by 8 publications

References 55 publications

Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Silicones as Nonocclusive Topical Agents

Topical application of a linoleic acid-ceramide containing moisturizer exhibit therapeutic and preventive benefits for psoriasis vulgaris: a randomized controlled trial

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