Directly Compressed Tablets: A Novel Drug-Containing Reservoir Combined with Hydrogel-Forming Microneedle Arrays for Transdermal Drug Delivery

Emma McAlister, Bridie Dutton, Lalitkumar K. Vora, Li Zhao, Anastasia Ripolin, Dk Siti Zawanah Binti Pg Hj Zahari, Helen L. Quinn, Ismaiel A. Tekko, Aaron J. Courtenay, Stephen A. Kelly, Aoife M. Rodgers, Lilach Steiner, Galit Levin, Etgar Levy-Nissenbaum, Nava Shterman, Helen O. McCarthy, Ryan F. Donnelly

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

Abstract

Microneedle (MN) patches consist of a hydrogel-forming MN array and a drug-containing reservoir. Drug-containing reservoirs documented in the literature include polymeric films and lyophilized wafers. While effective, both reservoir formulations are aqueous based, and so degradation can occur during formulation and drying for drugs inherently unstable in aqueous media. The preparation and characterization of novel, nonaqueous-based, directly compressed tablets (DCTs) for use in combination with hydrogel-forming MN arrays are described for the first time. In this work, a range of drug molecules are investigated. Precipitation of amoxicillin (AMX) and primaquine (PQ) in conventional hydrogel-forming MN arrays leads to use of poly(vinyl alcohol)-based MN arrays. Following in vitro permeation studies, in vivo pharmacokinetic studies are conducted in rats with MN patches containing AMX, levodopa/carbidopa (LD/CD), and levofloxacin (LVX). Therapeutically relevant concentrations of AMX (≥2 µg mL −1), LD (≥0.5 µg mL −1), and LVX (≥0.2 µg mL −1) are successfully achieved at 1, 2, and 1 h, respectively. Thus, the use of DCTs offers promise to expand the range of drug molecules that can be delivered transdermally using MN patches.

Original languageEnglish
Article number2001256
Pages (from-to)2001256 (1-19)
Number of pages19
JournalAdvanced Healthcare Materials
Volume10
Issue number3
Early online date14 Dec 2020
DOIs
Publication statusPublished - 3 Feb 2021

Keywords

  • directly compressed tablets
  • drug-containing reservoirs
  • hydrogel-forming microneedle arrays
  • in vivo pharmacokinetic studies
  • transdermal drug delivery

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