Owen Matthew J, Celik Umit, Chaudhary Subash K, Yik Jasper H N, Patton John S, Kuo Mei-Chang, Haudenschild Dominik R, Liu Gang-Yu
Department of Chemistry, University of California, Davis, CA 95616, USA.
Tesio Pharmaceuticals, Inc., Davis, CA 95616, USA.
Micromachines (Basel). 2022 Aug 25;13(9):1382. doi: 10.3390/mi13091382.
A table-top microdevice was introduced in this work to produce ultrasmall particles for drug delivery via inhalation. The design and operation are similar to that of spray-drying equipment used in industry, but the device itself is much smaller and more portable in size, simpler to operate and more economical. More importantly, the device enables more accurate control over particle size. Using Flavopiridol, an anti-inflammation medication, formulations have been developed to produce inhalable particles for pulmonary delivery. A solution containing the desired components forms droplets by passing through an array of micro-apertures that vibrate via a piezo-electrical driver. High-purity nitrogen gas was introduced and flew through the designed path, which included the funnel collection and cyclone chamber, and finally was pumped away. The gas carried and dried the micronized liquid droplets along the pathway, leading to the precipitation of dry solid microparticles. The formation of the cyclone was essential to assure the sufficient travel path length of the liquid droplets to allow drying. Synthesis parameters were optimized to produce microparticles, whose morphology, size, physio-chemical properties, and release profiles met the criteria for inhalation. Bioactivity assays have revealed a high degree of anti-inflammation. The above-mentioned approach enabled the production of inhalable particles in research laboratories in general, using the simple table-top microdevice. The microparticles enable the inhalable delivery of anti-inflammation medicine to the lungs, thus providing treatment for diseases such as pulmonary fibrosis and COVID-19.
在这项工作中引入了一种桌面式微型设备,用于生产通过吸入进行药物递送的超小颗粒。其设计和操作与工业中使用的喷雾干燥设备类似,但该设备本身尺寸更小、更便于携带,操作更简单且更经济。更重要的是,该设备能够更精确地控制颗粒大小。使用抗炎药物黄酮哌酯,已开发出用于肺部递送的可吸入颗粒制剂。含有所需成分的溶液通过一系列由压电驱动器振动的微孔径形成液滴。引入高纯度氮气并使其通过设计路径,该路径包括漏斗收集器和旋风室,最后被抽走。气体沿着路径携带并干燥微粉化的液滴,导致干燥的固体微粒沉淀。旋风的形成对于确保液滴有足够的行进路径长度以实现干燥至关重要。优化合成参数以生产微粒,其形态、尺寸、物理化学性质和释放曲线符合吸入标准。生物活性测定显示出高度的抗炎性。上述方法总体上能够在研究实验室中使用简单的桌面式微型设备生产可吸入颗粒。这些微粒能够将抗炎药物吸入递送至肺部,从而为诸如肺纤维化和新冠肺炎等疾病提供治疗。