Sipos Bence, Mayer Levente, Budai-Szűcs Mária, Katona Gábor, Ambrus Rita, Csóka Ildikó
Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Street 6, H-6720 Szeged, Hungary.
Pharmaceutics. 2025 Apr 18;17(4):533. doi: 10.3390/pharmaceutics17040533.
: The combination of nanomedicine with nasal administration is of paramount importance in current research and development. Polymeric micelles coated with hyaluronic acid may be a suitable solution to enhance drug release and permeation whilst properly adhering to the nasal mucosa, increasing residence time. : Solid state characterization included morphology and laser diffraction-based size analysis and X-ray powder diffraction. The characterization of dispersed polymeric micelles in aqueous media was performed based on dynamic light scattering and determining the solubility enhancement related factors such as encapsulation efficiency and thermodynamic solubility. In vitro nasal drug release and permeability studies were also conducted to characterize the different hyaluronic acid-modified polymeric micelles. Quantitative measurements were carried out via liquid chromatography. : Concentration dependence on hyaluronic acid was found during all measurements, with one formulation candidate overcoming the others. With a high yield above 80%, monodispersed particles were formulated with an approximately 4 µm particle size in uniform distribution and spherical morphology. The small micelle size (107.3 nm) in uniform manner led to a high encapsulation efficiency above 80% and released the drug amount above 70% in 15 min. High drug permeation was also achieved compared with the initial active substance by itself. : A value-added polymeric micelle formulation was developed with rapid drug release and permeation kinetics alongside its high mucoadhesion.
纳米医学与鼻腔给药相结合在当前的研发中至关重要。涂有透明质酸的聚合物胶束可能是一种合适的解决方案，既能增强药物释放和渗透，又能很好地粘附于鼻黏膜，延长停留时间。固态表征包括形态学、基于激光衍射的粒度分析和X射线粉末衍射。基于动态光散射并确定与溶解度增强相关的因素（如包封效率和热力学溶解度）对水性介质中分散的聚合物胶束进行表征。还进行了体外鼻腔药物释放和渗透性研究，以表征不同的透明质酸修饰的聚合物胶束。通过液相色谱进行定量测量。在所有测量过程中均发现浓度对透明质酸有依赖性，有一种候选制剂优于其他制剂。以高于80%的高产率制备了单分散颗粒，粒径约为4 µm，分布均匀，呈球形形态。均匀的小胶束尺寸（107.3 nm）导致包封效率高于80%，并在15分钟内释放药物量超过70%。与初始活性物质本身相比，还实现了高药物渗透性。开发了一种增值聚合物胶束制剂，具有快速的药物释放和渗透动力学以及高粘膜粘附性。
