Development of a Two-Dimensional Model for Predicting Transdermal Permeation with the Follicular Pathway: Demonstration with a Caffeine Study
| Autor: | Tao Chen, Panayiotis Kattou, Stephen Glavin, Guoping Lian, Ian Sorrell |
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| Rok vydání: | 2017 |
| Předmět: |
Skin Absorption
Biological Availability Pharmaceutical Science 02 engineering and technology Pharmacology Administration Cutaneous 030226 pharmacology & pharmacy Permeability in silico modelling 03 medical and health sciences chemistry.chemical_compound Drug Delivery Systems 0302 clinical medicine Dermis Caffeine Follicular phase medicine Humans Computer Simulation Pharmacology (medical) Transdermal Corneocyte Chemistry diffusion Organic Chemistry Permeation 021001 nanoscience & nanotechnology Hair follicle Lipids transdermal drug delivery Bioavailability Sebum Solutions Drug Liberation medicine.anatomical_structure pharmacokinetic model Molecular Medicine Epidermis bioavailability 0210 nano-technology Hair Follicle Hair Research Paper Biotechnology |
| Zdroj: | Pharmaceutical Research |
| ISSN: | 1573-904X 0724-8741 |
| DOI: | 10.1007/s11095-017-2209-0 |
| Popis: | Purpose The development of a new two-dimensional (2D) model to predict follicular permeation, with integration into a recently reported multi-scale model of transdermal permeation is presented. Methods The follicular pathway is modelled by diffusion in sebum. The mass transfer and partition properties of solutes in lipid, corneocytes, viable dermis, dermis and systemic circulation are calculated as reported previously [Pharm Res 33 (2016) 1602]. The mass transfer and partition properties in sebum are collected from existing literature. None of the model input parameters was fit to the clinical data with which the model prediction is compared. Results The integrated model has been applied to predict the published clinical data of transdermal permeation of caffeine. The relative importance of the follicular pathway is analysed. Good agreement of the model prediction with the clinical data has been obtained. The simulation confirms that for caffeine the follicular route is important; the maximum bioavailable concentration of caffeine in systemic circulation with open hair follicles is predicted to be 20% higher than that when hair follicles are blocked. Conclusions The follicular pathway contributes to not only short time fast penetration, but also the overall systemic bioavailability. With such in silico model, useful information can be obtained for caffeine disposition and localised delivery in lipid, corneocytes, viable dermis, dermis and the hair follicle. Such detailed information is difficult to obtain experimentally. |
| Databáze: | OpenAIRE |
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