Party Petra, Klement Márk László, Szabó-Révész Piroska, Ambrus Rita
Interdisciplinary Excellence Centre, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Street 6, 6720 Szeged, Hungary.
Pharmaceutics. 2023 Feb 6;15(2):545. doi: 10.3390/pharmaceutics15020545.
A fatal hereditary condition, cystic fibrosis (CF) causes severe lung problems. Ibuprofen (IBU), a non-steroidal anti-inflammatory drug, slows the progression of disease without causing significant side effects. Considering the poor water-solubility of the drug, IBU nanoparticles are beneficial for local pulmonary administration. We aimed to formulate a carrier-free dry powder inhaler containing nanosized IBU. We combined high-performance ultra-sonication and nano spray-drying. IBU was dissolved in ethyl acetate; after that, it was sonicated into a polyvinyl alcohol solution, where it precipitated as nanoparticles. Mannitol and leucine were added when producing dry particles using nano-spray drying. The following investigations were implemented: dynamic light scattering, laser diffraction, surface tension measurement, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, Fourier-transform infrared spectroscopy, in vitro dissolution test, and in vitro aerodynamic assessment (Andersen Cascade Impactor). The particle diameter of the IBU was in the nano range. The spray-dried particles showed a spherical morphology. The drug release was rapid in artificial lung media. The products represented large fine particle fractions and proper aerodynamic diameters. We successfully created an inhalable powder, containing nano-sized IBU. Along with the exceptional aerodynamic performance, the ideal particle size, shape, and drug-release profile might offer a ground-breaking local therapy for CF.
囊性纤维化（CF）是一种致命的遗传性疾病，会导致严重的肺部问题。布洛芬（IBU）是一种非甾体抗炎药，可减缓疾病进展且无明显副作用。考虑到该药物水溶性差，IBU纳米颗粒有利于局部肺部给药。我们旨在制备一种含纳米级IBU的无载体干粉吸入器。我们结合了高性能超声处理和纳米喷雾干燥技术。将IBU溶解于乙酸乙酯中；之后，将其超声处理至聚乙烯醇溶液中，在其中沉淀形成纳米颗粒。在使用纳米喷雾干燥制备干燥颗粒时加入甘露醇和亮氨酸。进行了以下研究：动态光散射、激光衍射、表面张力测量、扫描电子显微镜、X射线粉末衍射、差示扫描量热法、傅里叶变换红外光谱、体外溶出试验和体外空气动力学评估（安德森撞击器）。IBU的粒径处于纳米范围。喷雾干燥颗粒呈球形形态。在人工肺介质中药物释放迅速。产品表现出较大的细颗粒分数和合适的空气动力学直径。我们成功制备了一种含纳米级IBU的可吸入粉末。连同出色的空气动力学性能，理想的粒径、形状和药物释放曲线可能为CF提供一种开创性的局部治疗方法。
