Department of Nanomedicine, Houston Methodist Research Institute, Houston, TX, USA; University of Chinese Academy of Science (UCAS), Beijing, China.
Department of Nanomedicine, Houston Methodist Research Institute, Houston, TX, USA.
Nanomedicine. 2021 Oct;37:102417. doi: 10.1016/j.nano.2021.102417. Epub 2021 Jun 22.
Hypertension is a chronic condition that requires lifelong therapeutic management. Strict adherence to drug administration timing improves efficacy, while poor adherence leads to safety concerns. In light of these challenges, we present a nanofluidic technology that enables long-acting drug delivery with tunable timing of drug administration using buried gate electrodes in nanochannels. We developed a poly(ethylene glycol) methyl ether-block-poly(ε-caprolactone) (PEG-PCL)-based micellar formulation of amlodipine besylate, a calcium channel blocker for hypertension treatment. The electrostatically charged PEG-PCL micellar formulation enhanced drug solubility and rendered amlodipine responsive to electrostatic release gating in nanochannels for sustained release at clinically relevant therapeutic dose. Using a low-power (<3 VDC) gating potential, we demonstrated tunable release of amlodipine-loaded micelles. Additionally, we showed that the released drug maintained biological activity via calcium ion blockade in vitro. This study represents a proof of concept for the potential applicability of our strategy for chronotherapeutic management of hypertension.
高血压是一种需要终身治疗管理的慢性疾病。严格遵循药物给药时间可以提高疗效,而不良的依从性则会引发安全性问题。有鉴于此,我们提出了一种基于纳流控技术的长效药物输送系统,该系统使用纳米通道中的埋置栅电极,可实现给药时间的可调控制。我们开发了一种基于聚乙二醇甲基醚-聚己内酯(PEG-PCL)的苯磺酸氨氯地平(amlodipine besylate)胶束制剂,苯磺酸氨氯地平是一种用于治疗高血压的钙通道阻滞剂。带电荷的 PEG-PCL 胶束制剂提高了药物的溶解度,并使氨氯地平对纳米通道中的静电释放门控产生响应,从而以临床相关的治疗剂量进行持续释放。通过使用低功率(<3VDC)门控电位,我们证明了载药胶束的可调节释放。此外,我们还表明,释放的药物通过体外阻断钙离子来保持生物活性。这项研究为我们的策略在高血压的时间治疗管理中的潜在应用提供了概念验证。