Rietscher René, Thum Carolin, Lehr Claus-Michael, Schneider Marc
Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Delivery (DDEL), Saarland University, Building A4.1, 66123, Saarbruecken, Germany,
Pharm Res. 2015 Jun;32(6):1859-63. doi: 10.1007/s11095-014-1612-z. Epub 2014 Dec 30.
The preparation of nano-sized carrier systems increasingly moved into focus of pharmaceutical research and industry in the past decades. Besides the drug load and properties of the selected polymer/lipid, the size of such particles is one of the most important parameters regarding their use as efficient drug delivery systems. However, the preparation of nanoparticles with different sizes in a controlled manner is challenging, especially in terms of reproducibility and scale-up possibility. To overcome these hurdles we developed a system relying on nanoprecipitation, which meets all these requirements of an operator independent, scalable and size-adjustable nanoparticle synthesis-the Semi-Automated Nanoprecipitation-System. This system enables the adaption of the particle size to specific needs based on the process parameters-injection rate, flow rate and polymer concentration-identified within this study. The basic set-up is composed of a syringe pump and a gear pump for a precise control of the flow and injection speed of the system. Furthermore, a home-made tube-straightener guarantees a curvature-free injection point. Thus it could be shown that the production of poly(lactide-co-glycolide) nanoparticles from 150 to 600 nm with a narrow size distribution in a controlled semi-automatic manner is possible.
在过去几十年中,纳米级载体系统的制备日益成为药物研究和产业的焦点。除了所选聚合物/脂质的载药量和性质外,此类颗粒的大小是其作为高效药物递送系统使用时最重要的参数之一。然而,以可控方式制备不同大小的纳米颗粒具有挑战性,尤其是在可重复性和放大生产可能性方面。为克服这些障碍,我们开发了一种基于纳米沉淀法的系统,即半自动纳米沉淀系统,它满足了纳米颗粒合成中对操作者独立、可扩展和尺寸可调的所有这些要求。该系统能够根据本研究确定的工艺参数——注射速率、流速和聚合物浓度,使颗粒大小适应特定需求。基本设置由一个注射泵和一个齿轮泵组成,用于精确控制系统的流速和注射速度。此外,一个自制的管道矫直器确保注射点无弯曲。因此,可以证明以可控的半自动方式生产尺寸在150至600纳米之间、尺寸分布狭窄的聚(丙交酯-共-乙交酯)纳米颗粒是可行的。