Abstract

PurposeThe aim of this work was to evaluate whether improved topical delivery of finasteride, focussed to the hair follicles of human scalp skin could be achieved with application of short durations of heat and use of specific chemical penetration enhancers.MethodsFranz cell experiments with human scalp skin were performed with a range of chemical penetration enhancers at 32°C and 45°C to simulate normal and heated conditions. Selected chemical penetration enhancers were taken forward for finite dose Franz cell studies which examined the effect of heat produced by a prototype external heating system that supplied either 20 or 30 min of additional heat over both a 24 h and a 1 h time period.ResultsShort durations of externally applied heat significantly increased finasteride penetration into human scalp skin after 24 h. Analysis of drug distribution in the skin after 1 h and 24 h indicated that both heat and chemical penetration enhancer selection influenced drug delivery to the hair follicles.ConclusionThe use of short durations of heat in combination with specific chemical penetration enhancers was able to increase the delivery of finasteride to human scalp skin and provide focussed drug delivery to the hair follicles.

Highlights

  • Finasteride is used systemically as an oral medication for the treatment of androgenetic alopecia (AGA) in men, which is commonly known as male pattern baldness

  • If effective concentrations of finasteride could be delivered by topical administration to the hair follicles, treatment could be provided, and the side effects associated with systemic delivery could potentially be minimised or prevented

  • The solvents selected included those from different categories of enhancer, e.g. alcohol and fatty acid ester and may work differently with heat and be able to demonstrate synergistic effects on finasteride transport into the skin when used as solvent mixtures [20]

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Summary

Introduction

Finasteride is used systemically as an oral medication for the treatment of androgenetic alopecia (AGA) in men, which is commonly known as male pattern baldness. In scalps with AGA, dihydrotestosterone causes progressive miniaturisation of the hair follicles and shortening of the different phases of the hair growth cycle producing hair loss [2,3] Finasteride reverses these processes, preventing further hair loss and induces hair regrowth. The high follicular surface area of human scalp skin and that the hair follicles are the drug target site suggests that such an approach would be feasible [10,11] Features such as the high follicular density of scalp skin are thought to increase drug absorption to a greater extent for hydrophilic drugs in comparison to lipophilic molecules such as finasteride making it difficult to predict how effective follicular delivery of finasteride from topical administration would be [12,13]. An understanding of the effects of this enhancement approach on clinically relevant, 112 Page 2 of 12

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