Effects of Sebum on Drug Transport across the Human Stratum Corneum in vivo

Tsai, Jui-Chen; Lu, Cheng-Chan; Lin, Ming-Chung; Guo, Jiun‐Wen; Sheu, Hamm Ming

doi:10.1159/000336245

Cited by 13 publications

(10 citation statements)

References 39 publications

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“…These data are suggestive that the combination of artificial sebum and aqueous vehicles containing ZnPT increases the permeability of the skin under these experimental conditions. Similar results were obtained by Tsai et al [50] who measured a 2- to 3-fold increase in the transverse diffusion coefficients for 4-cyanophenol and cimetidine applied to sebum-supplemented skin compared to untreated skin in vivo. In that study, the authors noted that sebum treatment increased the SC permeability and altered barrier function by disordering structures of the intercellular lipid bilayers.…”

Section: Discussion/conclusionsupporting

confidence: 89%

Formulation and Artificial Sebum Effects on the Percutaneous Absorption of Zinc Pyrithione through Excised Human Skin

Rush

Nash

Smith

et al. 2019

Skin Pharmacol Physiol

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Background: Zinc pyrithione (ZnPT) is deposited on the skin as a fine particulate and must reach microorganisms localized in the stratum corneum and hair follicles in molecular form to exert its broad-spectrum antimicrobial/antifungal activity. Dissolution of ZnPT particles followed by molecular speciation results in the organic portion, i.e. pyrithione, being more susceptible to skin penetration than the inorganic component, i.e. zinc, or the chelate itself, i.e. ZnPT. Objectives: To further test the hypothesis that ZnPT skin penetration is rate-limited by dissolution and molecular speciation, the effect of different formulations and artificial sebum on the in vitro percutaneous absorption of radiolabel associated with Zn[¹⁴C]PT was investigated. Method: In vitro penetration of [¹⁴C]PT into and through excised human skin was measured following application of Zn[¹⁴C]PT prepared as suspensions in distinct vehicles including water-based carboxymethylcellulose (CMC), diluted body wash comprised of surfactants, and castor oil, in the presence and absence of artificial sebum. Results: The steady-state flux and cumulative absorption of Zn[¹⁴C]PT increased 4- to 5-fold when deposited from a body wash or castor oil compared to a water-based CMC suspension. Tritiated water flux measured before and after treatment showed that neither the surfactant vehicle nor castor oil significantly altered barrier function versus water alone. An artificial sebum layer on the skin potentiated Zn[¹⁴C]PT and ³H₂O absorption when dosed from both aqueous formulations, but not from castor oil. Conclusion: These data are consistent with the hypothesis that ZnPT percutaneous absorption, as measured by [¹⁴C]PT kinetics, is controlled by particle dissolution and molecular speciation.

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Section: Discussion/conclusionsupporting

confidence: 89%

Formulation and Artificial Sebum Effects on the Percutaneous Absorption of Zinc Pyrithione through Excised Human Skin

Rush

Nash

Smith

et al. 2019

Skin Pharmacol Physiol

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“…These findings suggest that not only the anti-inflammatory agent (MF) itself but also the formulation will play an important role in the treatment of skin disorders like atopic dermatitis. It was demonstrated that the amount of sebum affects the permeability of skin to molecules and the presence of sebum on the forehead or forearm increased the diffusion of both hydrophilic and lipophylic molecules through the human skin (Tsai et al, 2012). The increase of the amount of lipids in the SC can, thus, explain the formulation effect on the enhancement of MF permeation across the human epidermis.…”

Section: Discussionmentioning

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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“…Human sebum extract used in this study consisted of approximately 36.4% free fatty acids, 15.5% triglycerides, 22% wax esters, 20.6% squalene, and 5.5% cholesterol/cholesterol esters, as previously reported [10]. Following sebum applications, redness began to appear on the dorsal skin of hairless mice on day 1 (i.e., S1D, 24 h after the 1st sebum application), and then minor scales appeared on day 2 (S2D, i.e., 24 h after the 2nd sebum application, data not shown).…”

Section: Application Of Human Sebum Induced Scales Erythema Perturbmentioning

confidence: 98%

“…Six healthy male volunteers (>20 y/o) were included in the study. The skin surface lipids were obtained by pouring 400 mL of 95% ethanol through the scalp [10][11][12]. The solution was then filtered through a quantitative filter paper to remove particles, followed by rotary evaporation to remove solvent.…”

Section: Collection Of Human Sebum Extractmentioning

confidence: 99%

“…consumed the saturated fatty acids released from the triglycerides, and left behind the unsaturated fatty acids which caused inflammation and irritation [2,4,5]. In the previous work, we have demonstrated in humans in vivo, sebum supplement to the forearm increased the stratum corneum (SC) permeability of hydrophilic molecules for more than threefold, while removal of sebum from the forehead reduced slightly, but significantly (À22%) the SC permeability of these molecules [10], attributable to the altered barrier function of SC due to the disordering structures of the intercellular lipid molecules. In addition, applying palmitoleic acid or triolein to the hairless mouse skin increased transepidermal water loss and decreased skin hydration (data not shown).…”

mentioning

confidence: 98%

See 1 more Smart Citation

Human sebum extract induces barrier disruption and cytokine expression in murine epidermis

Guo

Lin

et al. 2015

Journal of Dermatological Science

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Effects of Sebum on Drug Transport across the Human Stratum Corneum in vivo

Cited by 13 publications

References 39 publications

Formulation and Artificial Sebum Effects on the Percutaneous Absorption of Zinc Pyrithione through Excised Human Skin

Formulation and Artificial Sebum Effects on the Percutaneous Absorption of Zinc Pyrithione through Excised Human Skin

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

Human sebum extract induces barrier disruption and cytokine expression in murine epidermis

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