Ultrarapid-Acting Microneedles for Immediate Delivery of Biotherapeutics.

Subcutaneous injection is a common administration route for rapid and efficient delivery of biotherapeutics. However, syringe-based injections usually require professional assistance and are associated with pain and potential risks of infections, thus leading to undesired patient compliance and poor life quality. Herein, we present an ultrarapid-acting microneedle (URA-MN) patch for immediate transdermal delivery of therapeutics in a minimally invasive manner. Effervescent agents are incorporated into the tip of URA-MN for rapid generation of CO bubbles upon insertion into the skin, immediately powering the biotherapeutics release within a few minutes. The release kinetics of diverse agents including liraglutide, insulin, and heparin from the URA-MN were evaluated in three different mouse models, and the rapid release of biotherapeutics and potent therapeutic effects were achieved with only 5-minute administration. Noteworthily, attributed to the short application duration and negligible residuals of MN matrix remaining in the skin, the URA-MN patch showed desirable biocompatibility after 6-week administration. This article is protected by copyright. All rights reserved.