Percutaneous penetration studies for risk assessment

Sartorelli, Pietro; Andersen, Helle Raun; Angerer, Jürgen; Corish, J.; Drexler, Hans; Göen, Thomas; Griffin, Peter; Hotchkiss, Sharon A.M.; Larese, F; Montomoli, L; Perkins, John; Schmelz, Martin; Sandt, J. van de; Williams, Faith M.

doi:10.1016/s1382-6689(00)00035-1

Cited by 64 publications

(62 citation statements)

References 45 publications

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“…[39] However, a review has been presented to compare various skins 270 including human and animal skins. [40] In this study, the authors have concluded that mammal skin is a reasonable model to study transdermal delivery in humans.…”

Section: Resultsmentioning

confidence: 99%

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

Al-Qallaf

Das

Davidson

2009

Asia-Pacific J Chem Eng

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Drug administration through transdermal delivery is restricted by the top layer of skin, the stratum corneum. One possible solution to overcome the barrier function of the stratum corneum is to employ microneedle arrays. However, detailed theoretical models relating drug‐coated microneedles and their geometry to the drug concentration in the blood are limited. This article aims to address this issue by examining the blood concentration profiles for a model drug, insulin, that has been administered via coated microneedles. A mathematical model is introduced and applied to predict theoretical blood concentrations. Furthermore, the insulin concentration in blood is calculated for a range of different microneedle shapes and dimensions to identify the most effective geometry. The results indicate that the optimum microneedle geometry in terms of maximizing insulin concentration was a rocket‐shaped needle with a constant tip angle of 90°. Also, it has been found that the number of microneedles in an array is the most significant factor in determining maximum insulin concentration in the blood (Cb, max). Penetration depth of the microneedle, centre‐to‐centre spacing and microneedle thickness had a less significant effect on the maximum insulin concentration in the blood. It is envisaged that the current study will help in designing microneedles of optimum size and shape for transdermal drug delivery. Copyright © 2009 Curtin University of Technology and John Wiley & Sons, Ltd.

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Section: Resultsmentioning

confidence: 99%

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

Al-Qallaf

Das

Davidson

2009

Asia-Pacific J Chem Eng

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“…The extent and the structure of the misclassification will depend greatly on the relation between inhalation and dermal exposure estimates and the way the exposure estimates are used (continuous, categorical). Several investigations have studied the correlation between dermal and airborne exposure estimates and found correlation coefficients ranging from as low as 0.06 to as high as 0.99, with a median correlation coefficient of r=0.4 (37,43,57,86,94,107,109,110). As these statistics indicate, assuming that the optimal grouping strategy for inhalation and dermal exposure is the same is often not justified, because exposure sources and pathways for the two exposure routes may have distinct characteristics.…”

Section: Discussionmentioning

confidence: 99%

“…Compound-specific factors are inherent to the chemical under consideration and therefore are unlikely to lead to differences in percutaneous penetration between workers or groups of workers. On the other hand, concomitant exposures to ethanol and other short-chain alkanols, polyethylene glycols, acetone, and other solvents have been found to enhance the percutaneous penetration of several compounds (40,57) and could result in substantial differences in uptake between (groups of) workers.…”

Section: Uptakementioning

confidence: 99%

Dermal exposure assessment in occupational epidemiologic research

Vermeulen¹,

Stewart²,

Kromhout³

2002

Scand J Work Environ Health

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“…Forty-six XMEs, including thirteen cytochrome P450 (CYP) proteins were detected in the liver only. Xenobiotic metabolizing pathways in the skin, previously identified in liver, have been reviewed by Sartorelli et al 49 Phase I reactions are represented with oxidation (e.g., hydroxylation, epoxidation), reduction (e.g., azo reduction, nitroxide reduction), and hydrolysis (e.g., phosphate ester hydrolysis, epoxide hydrolation) pathways. Concerning phase II reactions, glucuronidation, sulfation, glutathione conjugation, acetylation, amino acid conjugation, and methylation pathways are reported.…”

Section: Skin Versus Livermentioning

confidence: 99%

“…Thus, skin metabolism should be considered as part of the percutaneous absorption process. 49 One element for future consideration about skin metabolism could be the presence of skin bacteria on the skin surface. Recently it has been shown that azo dyes or benzo[a]pyene can be transformed by skin bacteria.…”

Section: Inter-individual and Intra-individual Variationsmentioning

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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Percutaneous penetration studies for risk assessment

Cited by 64 publications

References 45 publications

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

Dermal exposure assessment in occupational epidemiologic research

Review of the Availability ofIn VitroandIn SilicoMethods for Assessing Dermal Bioavailability

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