Abstract

In dissolving microneedle (DMN)-mediated therapy, complete and rapid delivery of DMNs is critical for the desired efficacy. Traditional patch-based DMN delivery, however, may fail due to incomplete delivery from insufficient skin insertion or rapid separation of microneedles due to their strong bond to the backing film. Here, we introduce the Troy microneedle, which was created by cyclic contact and drying on the pillar (CCDP), and which enabled simultaneous complete and rapid delivery of DMN. This CCDP process could be flexibly repeated to achieve a specific desired drug dose in a DMN. We evaluated DMN separation using agarose gel, and the Troy microneedle achieved more complete and rapid separation than other, more deeply dipped DMN, primarily because of the Troy’s minimal junction between the DMN and pillar. When Troy microneedles were applied to pig cadaver skin, it took only 15 s for over 90% of encapsulated rhodamine B to be delivered, compared to 2 h with application of a traditional DMN patch. In vivo skin penetration studies demonstrated rapid DMN-separation of Troy microneedles still in solid form before dissolution. The Troy microneedle overcomes critical issues associated with the low penetration efficiency of flat patch-based DMN and provides an innovative route for DMN-mediated therapy, combining patient convenience with the desire drug efficacy.

Highlights

  • A dissolving microneedle (DMN) is a micro-sized needle made of biodegradable polymer that encapsulates pharmaceuticals within a matrix and releases the drugs after skin insertion via dissolving of the polymeric compound [1, 2]

  • We introduce the Troy microneedle, which was created by cyclic contact and drying on the pillar (CCDP), and which enabled simultaneous complete and rapid delivery of DMN

  • When Troy microneedles were applied to pig cadaver skin, it took only 15 s for over 90% of encapsulated rhodamine B to be delivered, compared to 2 h with application of a traditional DMN patch

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Summary

Introduction

A dissolving microneedle (DMN) is a micro-sized needle made of biodegradable polymer that encapsulates pharmaceuticals within a matrix and releases the drugs after skin insertion via dissolving of the polymeric compound [1, 2]. DMN has received attention as an innovative transdermal drug delivery system due to minimum pain on delivery, biocompatibility and patient convenience [3, 4]. In spite of these advantages, some challenges for the complete delivery of encapsulated pharmaceuticals remain because of incomplete insertion of the DMNs. Usually, DMNs are fabricated on a sticky flat patch that facilitates their insertion into the skin and keeps them on the skin surface until they are completely dissolved. Due to the viscoelastic properties of skin, DMNs on a flat patch often do not completely penetrate the skin, PLOS ONE | DOI:10.1371/journal.pone.0136513 August 26, 2015

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