Dual-Mode Vasodilator M119 Delivery to Hair Follicle via Dissolving Microneedle for Advanced Alopecia Treatment

Abstract

Finasteride, the most widely used oral alopecia drug, shows several side effects such as hypoactive sexual dysfunction or depression, whereas the topical drug minoxidil demonstrates unsatisfactory efficacy. Thus, there is an increasing need for new alopecia drugs and alternative delivery systems for future alopecia treatment. Researchers have developed dissolving microneedle (DMN), a transdermal drug delivery system, which can be used with minimal invasion. However, DMN has limited application for the alopecia treatment owing to its unsuccessful implantation on the hairy scalp. Here, it is suggested that TOP-M119 (M119), a novel drug acting as a vasodilator in the scalp, and M119-loaded DMN with a specially designed shape can be used for the alopecia treatment. This M119-loaded DMN system is delivered using a newly designed applicator that supports patchless scalp implantation of DMN by microsized pillars designed to prevent accidental skin insertion. Enhanced hair follicle targeting drug delivery and superior alopecia treatment efficacy of specially designed shaped DMN and M119 has been demonstrated through in vitro and ex vivo studies. Moreover, M119-loaded DMN system shows enhanced in vivo efficacy in mouse skin and through expression markers related to hair growth, such as β-catenin, proliferating cell nuclear antigen, MECA 32, and versican.