Polymeric microarray patches for enhanced transdermal delivery of the poorly soluble drug olanzapine

Peter E. McKenna, Marco T. A. Abbate, Lalit K. Vora, Akmal H. Sabri, Ke Peng, Fabiana Volpe-Zanutto, Ismaiel A. Tekko, Andi Dian Permana, Cian Maguire, David Dineen, Mary-Carmel Kearney, Eneko Larrañeta, Alejandro J. Paredes, Ryan F. Donnelly*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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Transdermal drug delivery is an alternative route of administration that offers avoidance of the associated drawbacks of orally and parenterally administered hydrophobics. However, owing to the extremely specific set of physicochemical characteristics required for passive transdermal drug permeation, the development of marketed transdermal products containing poorly soluble drugs has been severely limited. Microarray patches (MAPs) are a type of transdermal patch that differ from the traditional patch design due to the presence of tiny, micron-sized needles that permit enhanced drug permeation on their application surface. To date, MAPs have predominantly been used to deliver hydrophilic compounds. However, this work challenges this trend and focuses on the use of MAPs, in combination with commonly utilized solubility-enhancing techniques, to deliver the hydrophobic drug olanzapine (OLP) across the skin. Specifically, cyclodextrin (CD) complexation and particle size reduction were employed in tandem with hydrogel-forming and dissolving MAPs, respectively. In vivo experimentation using a female Sprague-Dawley rat model confirmed the successful delivery of OLP from hydrogel-forming MAPs (Cmax = 611.13 ± 153.34 ng/mL, Tmax = 2 h) and dissolving MAPs (Cmax = 690.56 ± 161.33 ng/mL, Tmax = 2 h) in a manner similar to that of oral therapy in terms of the rate and extent of drug absorption, as well as overall drug exposure and bioavailability. This work is the first reported use of polymeric MAPs in combination with the solubility-enhancing techniques of CD complexation and particle size reduction to successfully deliver the poorly soluble drug OLP via the transdermal route. Accordingly, this paper provides significant evidence to support an expansion of the library of molecules amenable to MAP-mediated drug delivery to include those that exhibit poor aqueous solubility.

Original languageEnglish
Pages (from-to)31300-31319
Number of pages20
JournalACS Applied Materials and Interfaces
Issue number26
Early online date22 Jun 2023
Publication statusPublished - 05 Jul 2023


  • Antipsychotic
  • Cyclodextrin
  • Microneedle
  • Nanocrystal
  • Polymeric
  • Solubility
  • Transdermal


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