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具有可调释药动力学和双快速深部/持续释放能力的组合式微针贴片。

Combinatorial microneedle patch with tunable release kinetics and dual fast-deep/sustained release capabilities.

作者信息

Lopez-Ramirez Miguel Angel, Kupor Daniel, Marchiori Leonardo, Soto Fernando, Rueda Ricardo, Reynoso Maria, Narra Lakshmi Rekha, Chakravarthy Krishnan, Wang Joseph

机构信息

Department of Nanoengineering, University of California, San Diego, La Jolla, California 92093, USA.

Department of Anesthesiology and Pain Medicine, University of California, San Diego, Health Sciences, La Jolla, California 92093, USA.

出版信息

J Mater Chem B. 2021 Mar 11;9(9):2189-2199. doi: 10.1039/d1tb00141h.

DOI:10.1039/d1tb00141h
PMID:33651048
Abstract

Transdermal microneedle (MN) drug delivery patches, comprising water-soluble polymers, have played an essential role in diverse biomedical applications, but with limited development towards fast deep release or sustained delivery applications. The effectiveness of such MN delivery patches strongly depends on the materials from which they are constructed. Herein, we present a dual-action combinatorial programmable MN patch, comprising of fast and sustained-release MN zones, with tunable release kinetics towards delivering a wide range of therapeutics over different timeframes in single application. We demonstrate the fine tuning of MN materials; the patches can be tailored to deliver a first payload faster and deeper within minutes, while simultaneously delivering a second payload over long times ranging from weeks to months. The active and rapid burst release relies on embedding biodegradable Mg microparticle 'engines' in dissolvable MNs while the sustained release is attributed to biocompatible polymers that allow prolonged release in a controllable tunable manner. In addition, the patches are characterized and optimized for their design, materials and mechanical properties. These studies indicate that such programmable dual-action versatile MN platform is expected to improve therapeutic efficacy and patient compliance, achieving powerful benefits by single patch application at low manufacturing cost.

摘要

包含水溶性聚合物的透皮微针(MN)给药贴片在各种生物医学应用中发挥了重要作用,但在快速深度释放或持续给药应用方面的发展有限。此类MN给药贴片的有效性在很大程度上取决于其构建材料。在此,我们展示了一种双作用组合可编程MN贴片,它由快速释放和持续释放的MN区域组成,具有可调节的释放动力学,能够在单次应用中在不同时间范围内递送多种治疗药物。我们展示了MN材料的精细调节;这些贴片可以进行定制,以便在几分钟内更快、更深地递送第一种有效载荷,同时在从数周数月的长时间内递送第二种有效载荷。快速且活跃的爆发式释放依赖于将可生物降解的镁微粒“引擎”嵌入可溶解的MN中,而持续释放则归因于生物相容性聚合物,其能够以可控的可调节方式实现延长释放。此外,对这些贴片的设计、材料和机械性能进行了表征和优化。这些研究表明,这种可编程双作用多功能MN平台有望提高治疗效果和患者依从性,通过以低制造成本单次应用贴片实现显著益处。

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