触敏微针阵列贴片用于闭环经皮药物输送。
Touch-actuated microneedle array patch for closed-loop transdermal drug delivery.
机构信息
a Guangdong Provincial Key Laboratory of Sensor Technology and Biomedical Instrument, School of Biomedical Engineering , Sun Yat-Sen University , Guangzhou , PR China.
b Department of Mechanical and Biomedical Engineering , City University of Hong Kong , Hong Kong , PR China.
出版信息
Drug Deliv. 2018 Nov;25(1):1728-1739. doi: 10.1080/10717544.2018.1507060.
To date, only approximately 20 drugs synthesized with small molecules have been approved by the FDA for use in traditional transdermal patches (TTP) owing to the extremely low permeation rate of the skin barrier for macromolecular drugs. A novel touch-actuated microneedle array patch (TMAP) was developed for transdermal delivery of liquid macromolecular drugs. TMAP is a combination of a typical TTP and a solid microneedle array (MA). High doses of liquid drug formulations, especially heat-sensitive compounds can be easily filled and stored in the drug reservoir of TMAPs. TMAP can easily penetrate the skin and automatically retract from it to create microchannels through the stratum corneum (SC) layer using touch-actuated 'press and release' actions for passive permeation of liquid drugs. Comparison of subcutaneous injection, TTP, solid MA, and dissolvable MA, indicated that insulin-loaded TMAP exhibited the best hypoglycemic effect on type 1 diabetic rats. A 'closed-loop' permeation control was also provided for on-demand insulin delivery based on feedback of blood glucose levels (BGLs). Twenty IU-insulin-loaded TMAP maintained the type 1 diabetic rats in a normoglycemic state for approximately 11.63 h, the longest therapeutic duration among all previously reported results on microneedle-based transdermal patches. TMAP possesses excellent transdermal drug delivery capabilities.
迄今为止,由于皮肤对大分子药物的渗透性极低,仅有大约 20 种小分子合成药物被 FDA 批准用于传统透皮贴片(TTP)。一种新型的触敏微针贴片(TMAP)被开发用于透皮输送液体大分子药物。TMAP 是典型 TTP 和固体微针阵列(MA)的组合。高剂量的液体药物制剂,特别是热敏化合物,可以很容易地填充和储存在 TMAP 的药物储存库中。TMAP 可以很容易地穿透皮肤,并通过触敏的“按压和释放”动作自动从皮肤中缩回,在角质层(SC)层中创建微通道,以实现液体药物的被动渗透。与皮下注射、TTP、固体 MA 和可溶解 MA 的比较表明,载胰岛素的 TMAP 在 1 型糖尿病大鼠中表现出最佳的降血糖效果。还提供了基于血糖水平(BGL)反馈的按需胰岛素输送的“闭环”渗透控制。20IU 载胰岛素 TMAP 使 1 型糖尿病大鼠的血糖维持在正常水平约 11.63 小时,这是所有以前报道的基于微针的透皮贴片的最长治疗时间。TMAP 具有出色的透皮药物输送能力。