Built‐In Active Microneedle Patch with Enhanced Autonomous Drug Delivery

Abstract

The use of microneedles has facilitated the painless localized delivery of drugs across the skin. However, their efficacy has been limited by slow diffusion of molecules and often requires external triggers. Herein, an autonomous and degradable, active microneedle delivery platform is introduced, employing magnesium microparticles loaded within the microneedle patch, as the built-in engine for deeper and faster intradermal payload delivery. The magnesium particles react with the interstitial fluid, leading to an explosive-like rapid production of H2 bubbles, providing thenecessary force to breach dermal barriers and enhance payload delivery. The release kinetics of active microneedles is evaluated in vitro by measuring the amount of IgG antibody (as a model drug) that passed through phantom tissue and a pigskin barrier. In vivo experiments using a B16F10 mouse melanoma model demonstrate that the active delivery of anti-CTLA-4 (a checkpoint inhibitor drug) results in greatly enhanced immune response. and significantly longer survival. Moreover, spatially resolved zones of active and passive microneedles allow a combinatorial rapid burst response along with slow, sustained release, respectively. Such versatile and effective autonomous dynamic microneedle delivery technology offers considerable promise for a wide range of therapeutic applications, toward a greatly enhanced outcome, convenience, and cost.

Biodegradable β‐Cyclodextrin Conjugated Gelatin Methacryloyl Microneedle for Delivery of Water‐Insoluble Drug

“…Both fast release and sustained release profiles can be adopted in transdermal drug delivery. For example, cancer immunotherapy delivered by MN patch may benefit from the fast release, [ 43 ] while prolonged release is preferred delivery of antibiotics. [ 44 ] Therefore, the GelMA‐ β ‐CD MN‐based platform can be further optimized for different applications.…”

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

“…To address this challenge, researchers designed a variety of external stimuli methods to promote percutaneous drug absorption. These external triggers include iontophoresis, ultrasonic introduction, electroporation, and thermal perforation (Jabbari et al, 2015;Ita, 2016;Lopez-Ramirez et al, 2020). However, these methods can cause pain, and patients cannot administer the compounds by themselves.…”

Rapidly Separable Micropillar Integrated Dissolving Microneedles

“…On the other hand, depending on the chemical structures and concentrations of backbone matrices used in the fabrication of DMNs, the dissolution time varies from minutes to hours, leading to inconvenience, irritation, and allergic reactions in some patients [ 15 ]. Therefore, various innovative systems, including double-layered and tip-loaded DMNs, arrow-head DMNs, physical and chemical application enhancers, and DMN applicators, have been developed to overcome the current patch-based DMN limitations [ 16 , 17 , 18 , 19 , 20 , 21 , 22 ]. However, double layer and tip-loaded DMNs are limited by low loading capacity and complexities that limit their use as an optimal platform for DMNs [ 23 , 24 , 25 , 26 ].…”