Ring inserts as a useful strategy to prepare tip-loaded microneedles for long-acting drug delivery with application in HIV pre-exposure prophylaxis

Alejandro J. Paredes, Andi Dian Permana, Fabiana Volpe-Zanutto, Muhammad Nur Amir, Lalitkumar K. Vora, Ismaiel A. Tekko, Nima Akhavein, Andrew D. Weber, Eneko Larrañeta, Ryan F. Donnelly*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)
44 Downloads (Pure)

Abstract

The role of microneedle array patches (MAPs) and, in particular, dissolving MAPs in transdermal drug delivery has increased exponentially over the last decade. MAPs are able to form drug depots in the viable skin from where poorly soluble drugs dissolve in a long-acting fashion, showing promise in the management of multiple diseases. The manufacture of these systems can present some challenges, including the presence of bubbles in the baseplates and consequent lack of uniformity in microneedle formation and drug content. Here, we present a simple method based on ring inserts to produce tip-loaded MAPs using the antiretroviral drug cabotegravir sodium (CAB). The obtained MAPs presented a high uniformity in terms of microneedle formation, and a suitable insertion capability, as per the mechanical characterisation performed. An optimisation based on design of experiments revealed that centrifugation parameters had a significant impact on the skin deposition of the MAPs in excised neonatal porcine skin using Franz cells, with values ranging from 62.24 ± 47.13 µg to 174.13 ± 41.10 µg of CAB. Pharmacokinetic studies carried out in rats evidenced the capacity of the MAPs to maintain therapeutic plasma levels of CAB for 14 days, with Tmax values reached between 5 and 8 days.
Original languageEnglish
Article number111416
Number of pages11
JournalMaterials & Design
Volume224
Early online date24 Nov 2022
DOIs
Publication statusPublished - Dec 2022

Keywords

  • Cabotegravir sodium
  • Dissolving microneedles
  • Human immunodeficiency virus
  • Long-acting
  • Pre-exposure prophylaxis
  • Ring inserts

ASJC Scopus subject areas

  • General Materials Science
  • Mechanics of Materials
  • Mechanical Engineering

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