首页> 美国卫生研究院文献>Iranian Journal of Pharmaceutical Research : IJPR >Freeze-Dried K-Carrageenan/Chitosan Polyelectrolyte Complex-Based Insert: A Novel Intranasal Delivery System for Sumatriptan Succinate
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Freeze-Dried K-Carrageenan/Chitosan Polyelectrolyte Complex-Based Insert: A Novel Intranasal Delivery System for Sumatriptan Succinate

机译:冷冻干燥的K-卡拉胶/壳聚糖聚电解质复合物基插入物:舒马曲坦琥珀酸酯的新型鼻内给药系统

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摘要

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.
机译:鼻内途径在避免胃肠道降解和肝首过清除的情况下确保合适的药物生物利用度,已成为药物输送的普遍选择。在鼻剂中,粘膜粘附性固体插入物已显示出抗粘膜纤毛清除作用并提供延长的鼻腔停留时间。因此,本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(PEC)的鼻插入物,以增强琥珀酸舒马普坦治疗偏头痛的疗效。 。 k-CA / CS PECs以不同的摩尔比开发,在舒马曲坦琥珀酸酯存在下在小插入物中进行冻干,最后研究了其吸水能力,粘膜粘附潜能和药物释放曲线。傅立叶变换红外光谱(FTIR)证实了两种聚合物之间PEC的形成。根据结果​​,发现聚阴离子/聚阳离子摩尔比在调节嵌件特性方面起着关键作用,在所有配方中,包括摩尔比为(4:1)的k-CA / CS PEC )(k-CA / CS(4:1))表现出最高的吸水能力和粘膜粘附潜能,并提供了舒马曲坦琥珀酸酯的受控释放。这项研究说明了通过k-CA / CS PEC,特别是k-CA / CS(4:1)的冻干插入物可通过鼻内给药途径有效递送舒马普坦琥珀酸酯,并提出了一种潜在的治疗方法终止偏头痛发作。

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