Microclimate next to the skin: influence on percutaneous absorption of caffeine (<i>ex‐vivo</i> study)

Lboutounne, Youssef; Silva, J.; Pazart, Lionel; Bérard, Michel; Muret, Patrice; Humbert, P.

doi:10.1111/srt.12118

Cited by 8 publications

(4 citation statements)

References 19 publications

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“…10 The data obtained in this study were used to develop a plasma/dermis population pharmacokinetic model. The geometric mean C max increased to a slightly lesser extent, 5.0-to 7.4-fold.…”

Section: Discussionmentioning

confidence: 99%

“…Occlusion has been shown to increase percutaneous penetration of caffeine ex vivo because of the increase in relative humidity in the occluded condition combined with less evaporation of ethanol from skin surface compared with the open condition. 10 The data obtained in this study were used to develop a plasma/dermis population pharmacokinetic model. 11 The model predicted a free dermis concentration 1.6fold the human IC 50 , suggesting a different formulation with a higher flux would be needed for efficacy in clinical trials.…”

Section: Discussionmentioning

confidence: 99%

“…The geometric mean C max increased to a slightly lesser extent, 5.0‐ to 7.4‐fold. Occlusion has been shown to increase percutaneous penetration of caffeine ex vivo because of the increase in relative humidity in the occluded condition combined with less evaporation of ethanol from skin surface compared with the open condition …”

Section: Discussionmentioning

confidence: 99%

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A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions

Brigandi

Zhu

Murnane

et al. 2019

Clinical Pharm in Drug Dev

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Stearoyl‐coenzyme A desaturase 1 (SCD‐1) in sebaceous glands is a key enzyme in the synthesis of monounsaturated fatty acids essential for acne development. GSK1940029 gel, a novel SCD‐1 inhibitor, is being developed as a potential treatment for acne. To assess the irritation potential, pharmacokinetics (PK), and safety of topical GSK1940029 to the skin of healthy adults, two interdependent studies were conducted in parallel. Study 1 (n = 54) investigated the irritation potential of GSK1940029 (0.3% and 1%, occluded application) to allow for its application to larger surface areas in study 2 (n = 39), which investigated the safety, tolerability, and PK of GSK1940029 after single and repeat doses as occluded and nonoccluded applications. GSK1940029 was not a primary or cumulative irritant after 2 and 21 days of dosing in study 1. In study 2, single and repeat applications of GSK1940029 (0.1% to 1%) doses were well tolerated with little or no influence on AUC and C max under occluded or unoccluded conditions. Systemic exposure increased proportionally with surface area and was higher in occluded conditions. Design of these interdependent studies allowed for the assessment of the irritation potential for topical GSK1940029 in parallel with the investigation of PK and safety profiles.

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“…10 The data obtained in this study were used to develop a plasma/dermis population pharmacokinetic model. The geometric mean C max increased to a slightly lesser extent, 5.0-to 7.4-fold.…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions

Brigandi

Zhu

Murnane

et al. 2019

Clinical Pharm in Drug Dev

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“…Record the room temperature used, and keep it constant during studies to mitigate the risk of variations due to changes in temperature. The skin surface temperature can be altered by the environmental temperature and can affect the cutaneous permeation of drugs applied to the skin, as demonstrated in several reports (Ashrafi et al, 2020;Chang & Riviere, 1991;Iikura et al, 2019;Lboutounne et al, 2014).…”

Section: Preparation Of Membranes For In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Stepwise Protocols for Preparation and Use of Porcine Ear Skin for in Vitro Skin Permeation Studies Using Franz Diffusion Cells

et al. 2022

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The skin, the largest organ of the body, is an attractive route of topical and systemic drug administration. During the development of topical formulations, in vitro skin permeation studies using biological membranes mounted in Franz diffusion cells are a useful tool to assess the permeation of substances through the skin, and are recommended by the Organization for Economic Cooperation and Development (OECD). Among the types of biological membranes used in such studies, porcine ear skin has been identified as the most promising, due to its similarities to human skin and its greater accessibility as compared to human skin. To standardize techniques for the preparation and use of porcine ear skin as biological membrane, here we present systematic procedures for the selection of porcine ears, their cleaning, the removal of skin from cartilage, its transformation into membranes, and its use for the in vitro assessment of the permeation of drugs from topical formulations. © 2022 Wiley Periodicals LLC. Basic Protocol 1: Obtaining porcine ear membranes Basic Protocol 2: Preparation of membranes from porcine ear skin and use of membranes for in vitro skin permeation studies

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Skin Absorption in Man In Vivo

Lboutounne

Muret²

2015

Agache’s Measuring the Skin

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Microclimate next to the skin: influence on percutaneous absorption of caffeine (ex‐vivo study)

Abstract: Our results highlight a preponderant role of microclimate above the skin on percutaneous absorption of caffeine. The device used in this study will be a useful tool to investigate ex vivo, the influence of microclimate on percutaneous absorption.

Cited by 8 publications

References 19 publications

A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions

A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions

Stepwise Protocols for Preparation and Use of Porcine Ear Skin for in Vitro Skin Permeation Studies Using Franz Diffusion Cells

Skin Absorption in Man In Vivo

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