鼻内途径,在规避胃肠道降解和肝脏首过消除的情况下,确保药物的适当生物利用度,一直是药物输送的热门选择。在鼻腔剂型中,粘膜粘附固体插入物已被证明抵抗粘膜纤毛清除并提供延长的鼻停留时间。因此,这项研究的目的是制备和表征基于k-角叉菜胶(k-CA)和壳聚糖(CS)的聚电解质复合物(PECs)的鼻插入物,以提高琥珀酸舒马曲坦治疗偏头痛的疗效。K-CA/CSPEC以不同的摩尔比开发,在琥珀酸舒马曲坦的存在下,在小插入物中进行冻干,最后研究了吸水能力,粘膜粘附潜力,和药物释放概况。用傅里叶变换红外光谱(FTIR)肯定了两种聚合物之间PEC的构成。根据结果,结果表明,聚阴离子/聚阳离子摩尔比在调节插入物的特性中起着至关重要的作用,在所有的配方中,包含摩尔比为(4:1)的k-CA/CSPEC的一种,(k-CA/CS(4:1)),表现出最高的吸水能力和粘膜粘附潜力,并提供了更可控的琥珀酸舒马曲坦释放。这项研究说明了基于k-CA/CSPEC的冻干插入物的潜力,特别是k-CA/CS(4:1),通过鼻给药途径有效递送琥珀酸舒马曲坦,并提出了终止偏头痛发作的潜在治疗方法。
Intranasal route, ensuring suitable bioavailability of medicines under circumvention of the gastrointestinal degradation and hepatic first-pass elimination, has been a popular choice for drug delivery. Among nasal dosage forms, mucoadhesive solid inserts have been shown to resist mucociliary clearance and provide a prolonged nasal residence time. Hence, the purpose of this study was the preparation and characterization of nasal inserts composing of polyelectrolyte complexes (PECs) based on k-carrageenan (k-CA) and chitosan (CS) to boost therapeutic efficacy of sumatriptan succinate in the treatment of migraine headache. k-CA/CS PECs were developed in different molar ratios, subjected to lyophilization in small inserts in the presence of sumatriptan succinate, and finally investigated for water uptake ability, mucoadhesive potential, and drug release profile. The formation of PEC between the two polymers was affirmed by Fourier transform infrared spectroscopy (FTIR). Based on the results, it was revealed that the polyanion/polycation molar ratio plays a critical role in modulating the characteristics of the inserts, and among all the formulations, the one comprising k-CA/CS PEC with molar ratio of (4:1), (k-CA/CS (4:1)), demonstrated the highest water uptake ability and mucoadhesive potential and provided a more controlled release of sumatriptan succinate. This study illustrates the potential of the lyophilized inserts based on the k-CA/CS PECs, especially k-CA/CS (4:1), for efficient delivery of sumatriptan succinate via the nasal route of administration and suggests a potential therapeutic approach for the termination of migraine attacks.