Key Laboratory of Advanced Drug Delivery Systems of Zhejiang Province, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Department of Burns and Wound Care Center, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, 310009, China.
Adv Mater. 2023 Nov;35(45):e2304582. doi: 10.1002/adma.202304582. Epub 2023 Oct 11.
Subcutaneous (SC) 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, this work presents 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 (LRT), insulin, and heparin from the URA-MN patches are evaluated in three different mouse models, and the rapid release of biotherapeutics and potent therapeutic effects are achieved with only 5 min administration. Noteworthily, attributed to the short application duration and negligible residuals of MN matrix remaining in the skin, the URA-MN patch shows desirable biocompatibility after six-week administration.
皮下（SC）注射是一种常见的管理途径，用于快速有效地输送生物治疗药物。然而，基于注射器的注射通常需要专业人员的帮助，并且会引起疼痛和潜在的感染风险，从而导致患者的依从性不理想和生活质量下降。在此，本工作提出了一种超快速作用的微针（URA-MN）贴片，以微创的方式立即经皮输送治疗药物。泡腾剂被掺入 URA-MN 的尖端，在插入皮肤时迅速产生 CO 气泡，在几分钟内立即为生物治疗药物的释放提供动力。在三种不同的小鼠模型中评估了包括利拉鲁肽（LRT）、胰岛素和肝素在内的多种药物从 URA-MN 贴片的释放动力学，并且仅通过 5 分钟的给药就实现了生物治疗药物的快速释放和有效的治疗效果。值得注意的是，由于 MN 基质在皮肤中的应用时间短且残留量可忽略不计，URA-MN 贴片在六周的给药后表现出良好的生物相容性。
