Merck

A microneedle platform for buccal macromolecule delivery.

Science advances (2021-02-02)
Ester Caffarel-Salvador, Soyoung Kim, Vance Soares, Ryan Yu Tian, Sarah R Stern, Daniel Minahan, Raissa Yona, Xiaoya Lu, Fauziah R Zakaria, Joy Collins, Jacob Wainer, Jessica Wong, Rebecca McManus, Siddartha Tamang, Shane McDonnell, Keiko Ishida, Alison Hayward, Xiewen Liu, František Hubálek, Johannes Fels, Andreas Vegge, Morten Revsgaard Frederiksen, Ulrik Rahbek, Tadayuki Yoshitake, James Fujimoto, Niclas Roxhed, Robert Langer, Giovanni Traverso
ABSTRACT

Alternative means for drug delivery are needed to facilitate drug adherence and administration. Microneedles (MNs) have been previously investigated transdermally for drug delivery. To date, drug loading into MNs has been limited by drug solubility in the polymeric blend. We designed a highly drug-loaded MN patch to deliver macromolecules and applied it to the buccal area, which allows for faster delivery than the skin. We successfully delivered 1-mg payloads of human insulin and human growth hormone to the buccal cavity of swine within 30 s. In addition, we conducted a trial in 100 healthy volunteers to assess potential discomfort associated with MNs when applied in the oral cavity, identifying the hard palate as the preferred application site. We envisage that MN patches applied on buccal surfaces could increase medication adherence and facilitate the painless delivery of biologics and other drugs to many, especially for the pediatric and elderly populations.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Sulforhodamine 101
Sigma-Aldrich
Human GH ELISA Kit, for serum, plasma, cell culture supernatant and urine
Sigma-Aldrich
Trichloro(1H,1H,2H,2H-perfluorooctyl)silane, 97%
Sigma-Aldrich
Poly(dimethylsiloxane), viscosity 1.0 cSt (25 °C)