Lachowicz Dorota, Kaczyńska Agnieszka, Bodzon-Kulakowska Anna, Karewicz Anna, Wirecka Roma, Szuwarzyński Michał, Zapotoczny Szczepan
Academic Centre for Materials and Nanotechnology, AGH University of Science and Technology, al. A. Mickiewicza 30, 30-059 Krakow, Poland.
Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland.
Int J Mol Sci. 2020 Dec 18;21(24):9664. doi: 10.3390/ijms21249664.
Low water solubility frequently compromises the therapeutic efficacy of drugs and other biologically active molecules. Here, we report on coacervate polysaccharide nanoparticles (CPNs) that can transport and release a model hydrophobic drug, piroxicam, to the cells in response to changes in temperature. The proposed, temperature-responsive drug delivery system is based on ionic derivatives of natural polysaccharides-curdlan and hydroxypropyl cellulose. Curdlan was modified with trimethylammonium groups, while the anionic derivative of hydroxypropyl cellulose was obtained by the introduction of styrenesulfonate groups. Thermally responsive nanoparticles of spherical shape and average hydrodynamic diameter in the range of 250-300 nm were spontaneously formed in water from the obtained ionic polysaccharides as a result of the coacervation process. Their morphology was visualized using SEM and AFM. The size and the surface charge of the obtained objects could be tailored by adjusting the polycation/polyanion ratio. Piroxicam (PIX) was effectively entrapped inside the nanoparticles. The release profile of the drug from the CPNs-PIX was found to be temperature-dependent in the range relevant for biomedical applications.
低水溶性常常会影响药物和其他生物活性分子的治疗效果。在此，我们报道了凝聚层多糖纳米颗粒（CPNs），它能够响应温度变化，将模型疏水性药物吡罗昔康转运并释放到细胞中。所提出的温度响应型药物递送系统基于天然多糖（可得然胶和羟丙基纤维素）的离子衍生物。可得然胶用三甲基铵基团进行了修饰，而羟丙基纤维素的阴离子衍生物则通过引入苯乙烯磺酸盐基团获得。通过凝聚过程，由所得到的离子多糖在水中自发形成了平均流体动力学直径在250 - 300 nm范围内的球形热响应纳米颗粒。使用扫描电子显微镜（SEM）和原子力显微镜（AFM）对其形态进行了可视化观察。通过调整聚阳离子/聚阴离子比例，可以对所得到物体的尺寸和表面电荷进行调整。吡罗昔康（PIX）被有效地包裹在纳米颗粒内部。发现药物从CPNs - PIX中的释放曲线在生物医学应用相关的温度范围内是温度依赖性的。
