Biology of percutaneous penetration

Blickenstaff, Nicholas; Coman, Garrett; Blattner, Collin M.; Andersen, Rikke Sand; Maibach, Howard I.

doi:10.1515/reveh-2014-0052

Cited by 22 publications

(11 citation statements)

References 91 publications

(88 reference statements)

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“…The stratum corneum also impedes the skin penetration of topical drugs. [46][47][48] A good topical delivery system can enhance the skin penetration of drugs and active ingredients. Paudel et al 49 revealed that the output value of topical and transdermal drug delivery systems will reach 32 billion in the US market in 2015, including polymeric nanoparticles, solid lipid nanoparticles, liposomes, and nanoemulsions.…”

Section: Discussionmentioning

confidence: 99%

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

Lin

Lee²,

Tsai

et al. 2016

IJN

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Exposure to particulate matter (PM), a major form of air pollution, can induce oxidative stress and inflammation and may lead to many diseases in various organ systems including the skin. Eupafolin, a flavonoid compound derived from Phyla nodiflora , has been previously shown to exhibit various pharmacological activities, including antioxidant and anti-inflammatory effects. Unfortunately, eupafolin is characterized by poor water solubility and skin penetration, which limits its clinical applications. To address these issues, we successfully synthesized a eupafolin nanoparticle delivery system (ENDS). Our findings showed that ENDS could overcome the physicochemical drawbacks of raw eupafolin with respect to water solubility and skin penetration, through reduction of particle size and formation of an amorphous state with hydrogen bonding. Moreover, ENDS was superior to raw eupafolin in attenuating PM-induced oxidative stress and inflammation in HaCaT keratinocytes, by mediating the antioxidant pathway (decreased reactive oxygen species production and nicotinamide adenine dinucleotide phosphate oxidase activity) and anti-inflammation pathway (decreased cyclooxygenase-2 expression and prostaglandin E2 production through downregulation of mitogen-activated protein kinase and nuclear factor-κB signaling). In summary, ENDS shows better antioxidant and anti-inflammatory activities than raw eupafolin through improvement of water solubility and skin penetration. Therefore, ENDS may potentially be used as a medicinal drug and/or cosmeceutical product to prevent PM-induced skin inflammation.

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Section: Discussionmentioning

confidence: 99%

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

Lin

Lee²,

Tsai

et al. 2016

IJN

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“…Many products contain additional chemicals like surfactants and solvents to stabilize the formulation. These can alter the barrier properties of the stratum corneum by increasing the lipid bilayer's fluidity resulting in an enhancement of skin permeability [39]. In general, solutions showed the lowest prediction factors.…”

Section: Additional Factors Influencing Absorptionmentioning

confidence: 99%

In silico prediction of dermal absorption of pesticides – an evaluation of selected models against results from in vitro testing

Eleftheriadou

Luette

Kneuer

2019

SAR and QSAR in Environmental Research

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Current guidance for the estimation of dermal absorption (DA) of pesticides recommends the use of default values, read-across of information between formulations and in vitro testing. While QSARs exist to estimate percutaneous absorption, their use is currently not encouraged. Therefore, the potential of publicly available models for DA estimation was investigated based on data from 564 human in vitro DA experiments on pesticides. The classic Potts Guy model, the correction of Cleek Bunge for highly lipophilic chemicals, the mechanistic model of Mitragotri, and the COSMOS model were used to estimate the permeability coefficient k p. Different approaches were explored to calculate the percentage of external dose absorbed. IH SkinPerm was examined as stand-alone model. The models generally failed to accurately predict experimental values. For 30-40% of the predictions, there was overestimation by one order of magnitude. Three models underpredicted >10% of the cases, the remaining models <5%. DA of hydrophilic substances was typically underpredicted. Overprediction was more prominent for solid preparations and suspensions. The molecular weight, irritation potential and skin thickness did not correlate with the models' predictivity. Of the models investigated, IH SkinPerm performed best with 38% of the predictions within one order of magnitude and 2% underpredicted cases.

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“…This route is the most common. 19 Hydrophilic compounds are thought to pass mainly via the transcellular route (crossing into and out of the corneocytes) or ''polar pathway.'' For many compounds, the lipophilic stratum corneum represents the primary or rate-limiting barrier.…”

Section: Skin Penetrationmentioning

confidence: 99%

Review of the Availability ofIn VitroandIn SilicoMethods for Assessing Dermal Bioavailability

DumontCoralie

PrietoPilar

AsturiolDavid

et al. 2015

Applied In Vitro Toxicology

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The exposure of the skin to consumer products, drugs, and environmental chemicals can result in their penetrating the skin barrier and entering systemic circulation, potentially resulting in adverse effects in the skin and other organs. The assessment of dermal penetration and bioavailability (including penetration, metabolism, and entry into the systemic circulation) is therefore an important consideration in the risk assessment of chemicals. The skin is a heterogeneous organ with a multilayer structure. Based on its architecture and physiology, substances can penetrate through three major ways but can also be blocked in the different skin layers and in the skin appendages, which act as reservoir. In addition to that, as the skin is a metabolically competent organ, substances can undergo metabolism. After a brief description of the skin architecture, this review will focus on the skin penetration mechanisms and skin metabolic capacities. The skin absorption has traditionally been tested in vivo on animals. However, with the new legislation (i.e., Registration, Evaluation, Authorisation, and Restriction of Chemicals Regulation or Cosmetics Regulation), alternatives to animal testing have to be implemented. In a second part, this review will provide a description of the main in vitro and in silico or computational models available to study skin absorption and skin metabolism (i.e., ex vivo skin models, artificial membrane barriers, primary cells and cell lines, Quantitative Structure-Activity Relationship [QSAR], simulators for the prediction of skin metabolism).

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Biology of percutaneous penetration

Cited by 22 publications

References 91 publications

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

In silico prediction of dermal absorption of pesticides – an evaluation of selected models against results from in vitro testing

Review of the Availability ofIn VitroandIn SilicoMethods for Assessing Dermal Bioavailability

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