The use of heat and chemical penetration enhancers to increase the follicular delivery of erythromycin to the skin

F. Caserta,W.J. McAuley,M.B. Brown

doi:10.1016/j.ejps.2019.02.030

F. Caserta, W.J. McAuley + Show 1 more

Open Access

https://doi.org/10.1016/j.ejps.2019.02.030

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Abstract

The effect of heat on the follicular absorption of drugs into the skin has not previously been investigated. In comparison to drug delivery across the continuous stratum corneum (SC), follicular absorption is known to be relatively rapid and therefore the use of short durations of heat may be particularly useful for enhancing drug delivery to the hair follicles, as well as being practical for patients to use. In this study erythromycin has been used as a model drug and the combined use of heat and chemical penetration enhancers was found to be able to synergistically increase the penetration of erythromycin into human skin via the follicular route. Moreover durations of heat application as short as 10 min in combination with particular enhancer systems were found to be sufficient to significantly increase erythromycin delivery to the skin. Overall the data indicate that the use of heat with chemical penetration enhancers offers a potentially valuable strategy for delivering drugs via the follicular route.

Highlights

Delivering drugs into the hair follicles and their associated pilosebaceous units is highly desirable, including for example in the treatment of conditions such as acne and alopecia
The focus of this study was to examine whether heat in combination with chemical penetration enhancers could improve delivery of erythromycin to the skin and in particular via the follicular pathway
Technologies that can generate short durations of heat and can be contained within flexible packages are commercially available and other suitable phase change materials have been proposed for heating applications in topical drug delivery [19]

Summary

Introduction

Delivering drugs into the hair follicles and their associated pilosebaceous units is highly desirable, including for example in the treatment of conditions such as acne and alopecia. A number of chemical penetration enhancers have been shown to interact with sebum raising the possibility of using these two penetration enhancement strategies, heat and chemical penetration enhancers together, to significantly increase follicular drug delivery [8]. To test this hypothesis erythromycin, a topical antibiotic used in acne treatment was selected for use in this study as a model drug along with a range of chemical penetration enhancers to investigate whether skin absorption and in particular follicular drug transport could be improved using a combined approach with heat

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Results

Conclusion