Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, China.
Hunan Zaochen Nanorobot Co., Ltd, Liuyang, China.
Drug Deliv. 2021 Dec;28(1):692-699. doi: 10.1080/10717544.2021.1905739.
To overcome the shortcoming of conventional transarterial chemoembolization (cTACE) like high systemic release, a novel droplet-based flow-focusing microfluidic device was fabricated and the biocompatible poly(lactic-co-glycolic acid) (PLGA) magnetic drug-eluting beads transarterial chemoembolization (TACE) microspheres with tunable size and shell thickness were prepared via this device. Paclitaxel, as a model active, was loaded through O/O/W emulsion method with high efficiency. The size and the shell thickness vary when adjusting the flow velocity and/or solution concentration, which caters for different clinical requirements to have different drug loading and release behavior. Under the designed experimental conditions, the average diameter of the microspheres is 60 ± 2 μm and the drug loading efficiency has reached 6%. The drug release behavior of the microspheres shows the combination of delayed release and smoothly sustained release profiles and the release kinetics differ within different shell thickness. The microspheres also own the potential of magnetic resonance imaging (MRI) visuality because of the loaded magnetic nanoparticles. The microsphere preparation method and device we proposed are simple, feasible, and effective, which have a good application prospect.
为了克服传统经动脉化疗栓塞（cTACE）的缺点，如全身释放率高，我们制备了一种新型基于液滴的流聚焦微流控装置，并通过该装置制备了具有可调节粒径和壳厚的生物相容性聚乳酸-羟基乙酸共聚物（PLGA）载药磁栓塞（TACE）微球。紫杉醇作为一种模型药物，通过 O/O/W 乳液法高效负载。通过调整流速和/或溶液浓度，可以改变微球的粒径和壳厚，以适应不同的临床需求，具有不同的载药和释放行为。在设计的实验条件下，微球的平均直径为 60±2μm，载药效率达到 6%。微球的药物释放行为表现出迟释和平稳持续释放的组合，不同壳厚的释放动力学不同。由于加载了磁性纳米颗粒，微球还具有磁共振成像（MRI）可视化的潜力。我们提出的微球制备方法和装置简单、可行、有效，具有良好的应用前景。
