Department of Chemical Engineering, Monash University, Melbourne, VIC 3800, Australia; Department of Immunology and Pathology, Monash University, Melbourne, VIC 3004, Australia.
Central Clinical School, Monash University, Clayton, Victoria 3800, Australia; Department of Pharmacology, Monash University, Clayton, Victoria 3800, Australia.
Int J Pharm. 2019 Oct 30;570:118654. doi: 10.1016/j.ijpharm.2019.118654. Epub 2019 Aug 30.
The use of nanoparticles for pulmonary delivery poses challenges such as the presence of anatomical barriers and the loss of bioactive components. Excipients are often used to facilitate delivery. Excipients suitable for nanoparticle delivery are still being explored. Herein we introduce for the first time, spray-dried glycine microparticle-based excipients loaded with nanoparticles of the size range known to be taken up by alveolar macrophages. Using a microfluidic jet spray dryer, we produced glycine microparticles-based excipients which are spherical, uniform, cenospheric (hollow at core), and "coral-like" with average diameter of 60 ± 10 μm, 29 ± 0.8% porosity, and showed their effective loading with glycine coated iron oxide superparamagnetic nanoparticles (GSPIONs). Our loading protocol with nanoparticles further increased microsphere porosity and improved aerodynamic performance unlike the dense, solid commercial excipient, Lactohale200™. This demonstrates a feasible approach for delivery of such nanoparticles in the lung.
用于肺部递药的纳米颗粒存在挑战，如解剖学屏障的存在和生物活性成分的损失。赋形剂通常用于促进递送。适合纳米颗粒递送的赋形剂仍在探索中。本文首次介绍了喷雾干燥法制备的基于甘氨酸微颗粒的赋形剂，其负载有已知被肺泡巨噬细胞摄取的纳米颗粒。使用微流喷射喷雾干燥器，我们制备了甘氨酸微颗粒基赋形剂，其为球形、均匀、空心（核中空）和“珊瑚样”，平均直径为 60±10μm，孔隙率为 29±0.8%，并显示出有效负载甘氨酸包覆的超顺磁性氧化铁纳米颗粒（GSPIONs）。与致密、实心的商业赋形剂 Lactohale200™不同，我们的纳米颗粒载药方案进一步增加了微球的孔隙率并改善了空气动力学性能。这表明在肺部递药方面是一种可行的方法。
