School of Engineering and Applied Sciences, Department of Physics, Harvard University, Cambridge, Massachusetts, USA.
Lab Chip. 2011 Jul 21;11(14):2362-8. doi: 10.1039/c1lc20298g. Epub 2011 May 26.
Early development drug formulation is exacerbated by increasingly poor bioavailability of potential candidates. Prevention of attrition due to formulation problems necessitates physicochemical analysis and formulation studies at a very early stage during development, where the availability of a new substance is limited to small quantities, thus impeding extensive experiments. Miniaturization of common formulation processes is a strategy to overcome those limitations. We present a versatile technique for fabricating drug nanoformulations using a microfluidic spray dryer. Nanoparticles are formed by evaporative precipitation of the drug-loaded spray in air at room temperature. Using danazol as a model drug, amorphous nanoparticles of 20-60 nm in diameter are prepared with a narrow size distribution. We design the device with a geometry that allows the injection of two separate solvent streams, thus enabling co-spray drying of two substances for the production of drug co-precipitates with tailor-made composition for optimization of therapeutic efficiency.
早期开发药物制剂的工作因候选药物的生物利用度越来越差而变得更加复杂。为了防止因制剂问题而导致药物淘汰，有必要在药物开发的早期阶段进行物理化学分析和制剂研究，而此时新物质的供应量有限，只能进行少量实验。常见制剂工艺的微型化是克服这些限制的一种策略。我们提出了一种使用微流喷射干燥器制备药物纳米制剂的通用技术。纳米颗粒是通过在室温下将载药喷雾在空气中蒸发沉淀形成的。我们使用丹那唑作为模型药物，制备了直径为 20-60nm、粒径分布较窄的无定形纳米颗粒。我们设计的装置具有允许注入两种单独溶剂流的几何形状，从而能够实现两种物质的共喷射干燥，从而生产出具有定制组成的药物共沉淀物，以优化治疗效果。
