Predicting the Percutaneous Penetration of Cosmetic Ingredients*

Apr 1, 2010 | Contact Author | By: Sara Farahmand, PhD, University of Cincinnati College of Pharmacy; and Howard I. Maibach, MD, PhD, University of California School of Medicine
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Title: Predicting the Percutaneous Penetration of Cosmetic Ingredients*
percutaneous penetrationx absorptionx QSARx in vivox cosmetic ingredientsx
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Keywords: percutaneous penetration | absorption | QSAR | in vivo | cosmetic ingredients

Abstract: While previous algorithms for predicting the skin absorption of permeants was based on in vitro data, the present article proposes a quantitative structure-activity relationship (QSAR) model based on in vivo human data. Here, a set of human in vivo data is described that provides entry into predicting the penetration of cosmetic ingredients.

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S Farahmand and HI Maibach, A dermatological view—Predicting the percutaneous penetration of cosmetic ingredients, Cosm & Toil 125(4) 24-29 (Apr 2010)

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Until the early 1960s, theory suggested that cosmetic ingredients rarely penetrated the skin. However, many experts today suspect that penetration occurs with most ingredients. As consumers and health care professionals have become educated about safety, the percutaneous penetration of cosmetic and fragrance ingredients has gained interest. Therefore, the industry has sought means to estimate the penetration of chemical structures through human skin.

While previous algorithms for predicting the skin absorption of permeants was based on in vitro data, the present article proposes a quantitative structure-activity relationship (QSAR) model based on in vivo human data. Here, a set of human in vivo data is described that provides entry into predicting the penetration of cosmetic ingredients.

Assessing Delivery

Due to skin barrier properties, a chemical must exhibit specific physicochemical traits in order to be a candidate for passive transdermal delivery. For example, its molecules should be small (MW < 500) and have a low melting point (< 200°C). However, detailed analysis of the pharmacokinetics of transdermal drug delivery and its correlation with physicochemical characteristics of the delivered drugs is minimal. Predictive equations for skin permeability coefficients of chemicals are made based on in vitro static cell experiments using animal or human skin. Moreover, there is considerable interindividual variation in transdermal penetration and pharmacokinetics, which could be one reason for imprecision in predicting dermatopharmacokinetic parameters of transdermally delivered drugs based on their molecular properties.

Therefore, the dermatopharmacokinetic parameters of transdermal drugs are reviewed here. In addition, the interindividual variations in pharmacokinetic parameters such as maximal plasma concentration (Cmax) are assessed and the in vivo data and physicochemical characteristics of the drugs are correlated. For the present work, patches were chosen since they minimize variance by removing three forces that affect penetration: rub-off, exfoliation and wash.

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Figure 1. Interindividual variation of Cmax in different routes of administration of drugs

The CV of Cmax for nicotine after smoking and for fentanyl after intravenous infusion

Figure 2. Two-segmental linear correlation of Cmax and log Koct for eight drugs

When Cmax was plotted against log Koct, there is a two-segment linear correlation of Cmax and log Koct (r2 = 0.984, p < 0.05)

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