Department of Mechanical Engineering, University College London, London, UK.
J R Soc Interface. 2010 Apr 6;7(45):667-75. doi: 10.1098/rsif.2009.0348. Epub 2009 Oct 14.
The objective of this work was to produce drug-loaded nanometre- and micrometre-scale particles using a single-step process that provides control over particle size and size distribution. Co-axial electrohydrodynamic processing was used, at ambient temperature and pressure, with poly(lactic-co-glycolic acid) as the polymeric coating material and oestradiol as the encapsulated drug. The particle diameter was varied from less than 120 nm to a few micrometres, by simple methodical adjustments in the processing parameters (polymer concentration and applied voltage). In vitro studies were performed to determine the drug release profile from the particles during unassisted and ultrasound-stimulated degradation in simulated body fluid. An encapsulation efficiency of approximately 70% was achieved and release of the drug was sustained for a period of over 20 days. Exposing the particles to ultrasound (22.5 kHz) increased the rate of release by approximately 8 per cent. This processing method offers several advantages over conventional emulsification techniques for the preparation of drug-loaded particles. Most significantly, process efficiency and the drug's functionality are preserved, as complex multistep processing involving harsh solvents, other additives and elevated temperatures or pressures are avoided. Production rates of 10(12) particles min(-1) can be achieved with a single pair of co-axial needles and the process is amenable to being scaled up by using multiple sets.
本工作的目的是使用单步工艺制备载药的纳米级和微米级颗粒,从而控制颗粒大小和粒径分布。在环境温度和压力下,使用聚(乳酸-共-乙醇酸)作为聚合涂层材料和雌二醇作为包裹药物,采用同轴电动力学处理。通过简单地调整工艺参数(聚合物浓度和施加电压),可以将粒径从小于 120nm 变化到几微米。通过在模拟体液中进行未辅助和超声刺激降解的体外研究,确定了药物从颗粒中的释放曲线。实现了约 70%的包封效率,药物释放持续了 20 多天。将颗粒暴露于超声(22.5kHz)可使释放率增加约 8%。与传统的乳化技术相比,这种处理方法在制备载药颗粒方面具有多项优势。最重要的是,由于避免了涉及苛刻溶剂、其他添加剂以及高温或高压的复杂多步处理,因此保留了工艺效率和药物的功能。使用单个同轴针可实现 10(12)个/分钟的颗粒生产速率,并且可以通过使用多组来进行放大。