Development of a Two-Dimensional Model for Predicting Transdermal Permeation with the Follicular Pathway: Demonstration with a Caffeine Study

June 2017 in “ Pharmaceutical research ”

Panayiotis Kattou, Guoping Lian, Stephen Glavin, Ian Sorrell, Tao Chen

transdermal permeation follicular pathway caffeine systemic bioavailability hair follicles plasma concentrations dermal exposure diffusion coefficient sebum in silico screening

Studysummary This study presented a new two-dimensional model that successfully predicts transdermal permeation of caffeine, highlighting the significant role of the follicular pathway in increasing systemic bioavailability.

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In 2017, researchers developed a two-dimensional model to predict transdermal permeation through the skin, specifically focusing on the follicular pathway. The model was tested using caffeine and found that the follicular route significantly contributes to systemic bioavailability, predicting a 20% higher maximum concentration of caffeine in the bloodstream when hair follicles are open versus when they are blocked. The study, which involved six healthy volunteers, demonstrated that the model could accurately predict plasma concentrations of caffeine and emphasized the importance of the follicular pathway in the bioavailability of substances after dermal exposure. The model's sensitivity analysis indicated that changes in the diffusion coefficient of caffeine in sebum could significantly affect penetration rates. The study aimed to improve in silico screening for pharmaceuticals and reduce reliance on animal models, although further validation with more compounds was necessary. The research was supported by the UK Biotechnology and Biological Sciences Research Council and Unilever Research Colworth, UK.

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Research cited in this study

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research Contribution of the Hair Follicular Pathway to Total Skin Permeation of Topically Applied and Exposed Chemicals

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research Kinetics and Equilibrium of Solute Diffusion into Human Hair

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This study found that the uptake of molecules by hair is influenced by both hydrophobic and ionic charge interactions, with binding affinity decreasing as pH approaches the solute's dissociation constant.

Hair Follicles Contribute Significantly to Penetration Through Human Skin Only Shortly After Application as a Solvent Deposited Solid in Humans

research Hair Follicles Contribute Significantly to Penetration Through Human Skin Only Shortly After Application as a Solvent Deposited Solid in Humans

94 citations , May 2011 in “BJCP. British journal of clinical pharmacology/British journal of clinical pharmacology”

This study found that hair follicles contribute significantly to caffeine absorption shortly after topical application, with a faster absorption rate compared to the stratum corneum.

research Follicular Transport Route: Research Progress and Future Perspectives

211 citations , February 2009 in “European journal of pharmaceutics and biopharmaceutics”

This review summarizes recent advancements in follicular targeting for drug delivery via hair follicles and calls for pilot studies in humans to explore potential clinical applications.

research Comparison of Artificial Sebum with Human and Hamster Sebum Samples

49 citations , September 2008 in “International journal of pharmaceutics”

This study suggests that artificial sebum L may serve as an effective substitute for human sebum in drug transport studies, due to its similar physicochemical properties.

research The Role of Hair Follicles in the Percutaneous Absorption of Caffeine

182 citations , December 2007 in “BJCP. British journal of clinical pharmacology/British journal of clinical pharmacology”

This study demonstrated that hair follicles significantly expedite the absorption of caffeine through the skin compared to interfollicular pathways.

research Investigation of Drug Partition Property in Artificial Sebum

33 citations , June 2007 in “International Journal of Pharmaceutics”

This study found that the sebum partition coefficient (K(sebum)) for some drugs differs from the stratum corneum partition coefficient (K(sc)), indicating its importance for targeted drug delivery into hair and sebaceous follicles.

research Diffusion Properties of Model Compounds in Artificial Sebum

29 citations , May 2007 in “International journal of pharmaceutics”

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research Follicular Penetration of Topically Applied Caffeine via a Shampoo Formulation

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research Biology of the Hair Follicle: The Basics

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research Transfollicular Drug Delivery: Is It a Reality?

141 citations , November 2005 in “International journal of pharmaceutics”

This review examines the role of hair follicles and sebaceous glands in percutaneous drug delivery but does not report new clinical results; it calls for further exploration of follicle-targeting therapies.

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463 citations , September 2004 in “Clinics in dermatology”

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