An Investigation of the Mechanism of Flux Across Polydimethylsiloxane Membranes by use of Quantitative Structure-Permeability Relationships

Cronin, Mark T.D.; Dearden, John C.; Gupta, Rachna; Moss, Gary P.

doi:10.1111/j.2042-7158.1998.tb06169.x

Cited by 41 publications

(31 citation statements)

References 29 publications

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“…Moss et al reported that silicone membrane permeability is essentially different from that of human skin. 19,20) The log K o/w of the model compounds showed wide lipophilicity range from 0.84 to 5.36. On the other hand, in the present study, significance correlations of permeation parameters between silicone membrane and human or animal skin in the lipophilicity range of 0.5≤log K o/w ≤3.5 of model compounds.…”

Section: Discussionmentioning

confidence: 99%

“…17,18) However, it also has been reported that silicone membrane permeability is essentially different from human skin permeability, 19,20) and it is unclear if silicone membranes were effective as an alternative to human or animal skin.…”

mentioning

confidence: 99%

“…16) Subsequently, studies using flux as a permeation parameter have also been conducted, and it was found that a silicone membrane could be used as a substitute for human or animal skin. 17,18) However, it also has been reported that silicone membrane permeability is essentially different from human skin permeability, 19,20) and it is unclear if silicone membranes were effective as an alternative to human or animal skin.…”

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confidence: 99%

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Evaluation of a Silicone Membrane as an Alternative to Human Skin for Determining Skin Permeation Parameters of Chemical Compounds

Uchida

Yakumaru

Nishioka

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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We evaluated the effectiveness of a silicone membrane as an alternative to human skin using the skin permeation parameters of chemical compounds. An in vitro permeation study using 15 model compounds was conducted, and permeation parameters comprising permeability coefficient (P), diffusion parameter (DL 2 ), and partition parameter (KL) were calculated from each permeation profile. Significant correlations were obtained in log P, log DL 2 , and log KL values between the silicone membrane and human skin. DL 2 values of model compounds, except flurbiprofen, in the silicone membrane were independent of the lipophilicity of the model compounds and were 100-fold higher than those in human skin. For antipyrine and caffeine, which are hydrophilic, KL values in the silicone membrane were 100-fold lower than those in human skin, and P values, calculated as the product of a DL 2 and KL, were similar. For lipophilic compounds, such as nbutyl paraben and flurbiprofen, KL values for silicone were similar to or 10-fold higher than those in human skin, and P values for silicone were 100-fold higher than those in human skin. Furthermore, for amphiphilic compounds with log K o/w values from 0.5 to 3.5, KL values in the silicone membrane were 10-fold lower than those in human skin, and P values for silicone were 10-fold higher than those in human skin. The silicone membrane was useful as a human skin alternative in an in vitro skin permeation study. However, depending on the lipophilicity of the model compounds, some parameters may be over-or underestimated.Key words silicone membrane; skin; membrane permeation; alternative membrane Skin forms an interface between the body and environment and functions as a firm barrier against undesirable elements. Many skin permeation studies of therapeutic drugs have been conducted to develop transdermal drug delivery systems (TDDSs) for the purpose of preventing the hepatic first-pass effect, which is observed for some oral dosage forms, and for controlling release over long periods of time.1-3) For the development and evaluation of TDDSs, in vitro skin permeation tests using excised human skin have been performed in the European Union (EU) and United States; however, in Japan, it is difficult to obtain human skin, so permeation studies using human skin are not performed as frequently. Therefore, animal skins, particularly those of hairless rat, mouse, and guinea pig, have been used for the evaluation of percutaneous absorption. Recently, however, sales of cosmetics in the EU, 4) for which animal experiments were performed during their development have been prohibited out of concern for animal welfare, and alternative membranes are now required to determine percutaneous absorption. In addition, permeation studies using animal or human skin are associated with several difficulties and limitations for assessing the effects of formulations components, because of the complex nature of this biological tissue and inter- and intra-individuality of skin.Artificial model membranes offer a simple and ...

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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confidence: 99%

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Evaluation of a Silicone Membrane as an Alternative to Human Skin for Determining Skin Permeation Parameters of Chemical Compounds

Uchida

Yakumaru

Nishioka

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Similar studies by AgatonovicKustrin et al and Cheng et al have published on use of ANNs in determining the quantitative structure-permeability relationship of penetration across skin or polydimethylsiloxane membranes as the model of skin permeation [123][124][125][126]. A set of over 200 compounds and their maximum steady state flux was collected from the literature [127,128]. In Agatonovic-Kustrin et al study, twelve of 42 molecular descriptors were selected for ANN modeling of maximum steady-state flux by the use of genetic algorithm, that include molecular shape and size, inter-molecular interactions, hydrogen-bonding capacity of drugs, and conformational stability [123].…”

Section: Prediction Permeability Of Skin and Blood Brain Barriermentioning

confidence: 99%

Artificial Neural Network in Drug Delivery and Pharmaceutical Research

Sutariya¹,

Groshev²,

Sadana³

et al. 2013

TOBIOIJ

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Artificial neural networks (ANNs) technology models the pattern recognition capabilities of the neural networks of the brain. Similarly to a single neuron in the brain, artificial neuron unit receives inputs from many external sources, processes them, and makes decisions. Interestingly, ANN simulates the biological nervous system and draws on analogues of adaptive biological neurons. ANNs do not require rigidly structured experimental designs and can map functions using historical or incomplete data, which makes them a powerful tool for simulation of various non-linear systems.ANNs have many applications in various fields, including engineering, psychology, medicinal chemistry and pharmaceutical research. Because of their capacity for making predictions, pattern recognition, and modeling, ANNs have been very useful in many aspects of pharmaceutical research including modeling of the brain neural network, analytical data analysis, drug modeling, protein structure and function, dosage optimization and manufacturing, pharmacokinetics and pharmacodynamics modeling, and in vitro in vivo correlations. This review discusses the applications of ANNs in drug delivery and pharmacological research.

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“…In recent years there has been increasing attention paid to the problem of predicting the rate at which a substance will pass through human skin [1][2][3][4][5][6]. Interest in this issue has been driven by the pharmaceutical industry, where it is important to be able to predict the rate at which a drug will pass through the skin and into the bloodstream.…”

Section: Introductionmentioning

confidence: 99%

Predicting drug absorption rates through human skin

Sun

Lam

Moss

et al. 2010

The 2010 International Joint Conference on Neural Networks (IJCNN)

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AbstractPredicting the rate at which a substance will pass through human skin and into the bloodstream is a problem of current interest. We use Gaussian Process modeling to train a set of predictors using every combination of six molecular features. We find that only three of the features are needed for our best predictor. This result could be useful in the further analysis of skin permeability.

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An Investigation of the Mechanism of Flux Across Polydimethylsiloxane Membranes by use of Quantitative Structure-Permeability Relationships

Cited by 41 publications

References 29 publications

Evaluation of a Silicone Membrane as an Alternative to Human Skin for Determining Skin Permeation Parameters of Chemical Compounds

Evaluation of a Silicone Membrane as an Alternative to Human Skin for Determining Skin Permeation Parameters of Chemical Compounds

Artificial Neural Network in Drug Delivery and Pharmaceutical Research

Predicting drug absorption rates through human skin

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