Kazsoki Adrienn, Palcsó Barnabás, Omer Safaa Mohammed, Kovacs Zoltan, Zelkó Romána
University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre utca 7-9, H-1092 Budapest, Hungary.
Department of Measurements and Process Control, Institute of Food Science and Technology, Hungarian University of Agriculture and Life Sciences, Somlói Street 14-16, H-1118 Budapest, Hungary.
Pharmaceutics. 2022 Jul 11;14(7):1442. doi: 10.3390/pharmaceutics14071442.
Several applications of nanofiber-based systems are based on their corresponding functionality-related properties, which often cannot be satisfied by a fiber web with a monolithic structure because of the various physicochemical properties and amounts of embedded compounds. Therefore, one of the main directions in the development of fiber systems is creating core-shell type complex fiber structures that can provide application-specific properties to the fiber matrix. The present study aimed to formulate levocetirizine-loaded core-shell type hydrophilic polymer-based fibrous systems. The core phase contained the antihistamine levocetirizine, while the permeation enhancer (Na-taurocholate), the local pH regulator (citric acid), and the cyclodextrin used as a taste masking agent were included in the shell phase of the fibrous formulation. Scanning electron microscopy images indicated that a randomly oriented homogeneous fibrous structure was obtained, while the Raman mapping and chemometric analysis confirmed the partially formed core-shell structure. A fast release rate of the antihistamine drug from the complex structural fibrous system was obtained (within 1 min complete dissolution can be observed) due to its increased surface area to volume ratio and its more favorable wettability properties, which consequently allows for more erosion. The masking properties against the unpleasant bitter taste of API of the formulated complex nanostructure were confirmed by the results of the electronic tongue. The formulated complex nanostructure enabled fast and complete release of the API, providing a potential enhancement in the rate and extent of absorption while masking the unpleasant taste of levocetirizine, which has a high impact on the patient adherence. All in all, the results show that the developed orally dissolving fibrous web formulation can be a potential alternative to the commercially available orally disintegrating tablets.
基于纳米纤维的系统的几种应用是基于其与功能相关的特性，由于各种物理化学性质和嵌入化合物的数量，具有整体结构的纤维网通常无法满足这些特性。因此，纤维系统开发的主要方向之一是创建核壳型复合纤维结构，这种结构可以为纤维基质提供特定应用的特性。本研究旨在制备负载左西替利嗪的核壳型亲水性聚合物基纤维系统。核相包含抗组胺药左西替利嗪，而渗透促进剂（牛磺胆酸钠）、局部pH调节剂（柠檬酸）和用作掩味剂的环糊精包含在纤维制剂的壳相中。扫描电子显微镜图像表明获得了随机取向的均匀纤维结构，而拉曼映射和化学计量分析证实了部分形成的核壳结构。由于其增加的表面积与体积比和更有利的润湿性，从而允许更多的侵蚀，抗组胺药物从复合结构纤维系统中获得了快速释放速率（在1分钟内可观察到完全溶解）。电子舌的结果证实了所制备的复合纳米结构对API不愉快苦味的掩味性能。所制备的复合纳米结构能够使API快速完全释放，在提高吸收速率和程度的同时，掩蔽左西替利嗪的不愉快味道，这对患者的依从性有很大影响。总而言之，结果表明所开发的口腔溶解纤维网制剂可能是市售口腔崩解片的潜在替代品。
