配备自发气泡产生功能的活性微针贴片用于增强类风湿性关节炎治疗
Active microneedle patch equipped with spontaneous bubble generation for enhanced rheumatoid arthritis treatment.
作者信息
Liu Ting, Fu Jintao, Zheng Ziyang, Chen Minglong, Wang Wenhao, Wu Chuanbin, Quan Guilan, Pan Xin
机构信息
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
School of Pharmaceutical Sciences, Hainan University, Haikou 570200, China.
出版信息
Theranostics. 2025 Feb 24;15(8):3424-3438. doi: 10.7150/thno.103080. eCollection 2025.
The utilization of dissolving microneedles (MNs) facilitates the painless delivery of pharmaceuticals the transdermal route. However, conventional MNs rely on passive diffusion through the gradual dissolving of the matrix, which can impede the therapeutic efficacy of the delivered drugs. In this study, we present the development of a novel degradable active MNs platform. This platform employs sodium bicarbonate and citric acid loaded in a dissolving MNs patch as a built-in motor for deeper and faster intradermal payload delivery. The sodium bicarbonate microparticles and citric acid undergo a chemical reaction when in contact with tissue fluid, resulting in the rapid formation of explosive carbon dioxide bubbles. This provides the necessary force to break through dermal barriers and enhance payload delivery. The results demonstrated that the active MNs possessed excellent mechanical properties, rapid detachment characteristics, and superior drug release kinetics. Furthermore, the drug permeation behavior of active MNs exhibited enhanced permeation and distribution in skin-mimicking gel and porcine skin when compared to conventional passive MNs. experiments employing a rat model of rheumatoid arthritis showed that active MNs achieved superior therapeutic efficacy compared to passive MNs. This universal and effective autonomous dynamic microneedle delivery technology is straightforward to prepare and ultilize, and has the potential to improve the therapeutic efficacy of drugs, offering significant prospects for a diverse range of therapeutic applications.
溶解微针(MNs)的应用有助于通过透皮途径实现药物的无痛递送。然而,传统微针依赖于基质逐渐溶解的被动扩散,这可能会阻碍所递送药物的治疗效果。在本研究中,我们展示了一种新型可降解活性微针平台的开发。该平台采用负载在溶解微针贴片中的碳酸氢钠和柠檬酸作为内置马达,用于更深更快地进行皮内有效载荷递送。碳酸氢钠微粒和柠檬酸与组织液接触时会发生化学反应,迅速形成爆炸性二氧化碳气泡。这提供了突破皮肤屏障并增强有效载荷递送所需的力。结果表明,活性微针具有优异的机械性能、快速脱离特性和卓越的药物释放动力学。此外,与传统被动微针相比,活性微针在仿皮肤凝胶和猪皮中的药物渗透行为表现出增强的渗透和分布。使用类风湿性关节炎大鼠模型的实验表明,活性微针比被动微针具有更好的治疗效果。这种通用且有效的自主动态微针递送技术易于制备和使用,并且有可能提高药物的治疗效果,为各种治疗应用提供了广阔的前景。