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One-step electrohydrodynamic production of drug-loaded micro- and nanoparticles.

机译:一步一步的电动流体动力学生产载药的微粒和纳米颗粒。

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摘要

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.
机译:这项工作的目的是使用一步控制颗粒大小和尺寸分布的单步法生产载药的纳米和微米级颗粒。在环境温度和压力下使用同轴电流体动力学方法,其中聚乳酸-乙醇酸作为聚合物涂层材料,雌二醇作为包封药物。通过对加工参数(聚合物浓度和施加电压)进行简单的方法调整,可以将粒径从小于120 nm更改为几微米。进行了体外研究,以确定在模拟体液中无助的和超声刺激的降解过程中,颗粒中的药物释放曲线。达到约70%的包封效率,药物释放持续20天以上。将颗粒暴露于超声(22.5 kHz)可使释放速率提高约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​​多个优势。最重要的是,由于避免了涉及刺激性溶剂,其他添加剂以及升高的温度或压力的复杂的多步加工过程,因此保留了工艺效率和药物功能。一对同轴针可以实现10(12)个粒子min(-1)的生产率,并且该过程可以通过使用多组来扩大规模。

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