嵌入 Poloxamer 407 原位凝胶的 TPGS 和 Soluplus 聚合胶束用于鼻内给药的比较研究

IF 5 3区 化学 Q1 POLYMER SCIENCE Gels Pub Date : 2024-08-09 DOI:10.3390/gels10080521
Bence Sipos, Frézia Földes, M. Budai-Szűcs, Gábor Katona, Ildikó Csóka
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引用次数: 0

摘要

本研究旨在强调选择合适的共聚物或共聚物混合组合对于设计高附加值鼻腔剂型的重要性。上呼吸道相关感染(如鼻炎)的局部治疗至关重要,因此需要先进的局部治疗方案。地塞米松被封装在三种不同的聚合物胶束配方中:Soluplus 或纯 TPGS 以及它们的混合组合。动态光散射测量结果表明,胶束粒径小于 100 纳米,呈单分散分布,封装效率高达 80% 以上,水溶性至少提高了 7 倍。抗菌剂妥布霉素被共同配制到原位胶凝体系中,该体系根据凝胶化时间和凝胶化温度进行了优化。溶胶-凝胶转变发生在 32-35 °C 之间,最佳温度低于鼻腔温度,且能在 5 分钟内快速完成,这是针对粘液纤毛清除的合适策略标准。体外药物释放和渗透性研究证实,封装的地塞米松具有快速的动力学特性,亲水性药物妥布霉素也能持续释放。
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Comparative Study of TPGS and Soluplus Polymeric Micelles Embedded in Poloxamer 407 In Situ Gels for Intranasal Administration
This study aims to highlight the importance of choosing the appropriate co-polymer or co-polymer mixed combinations in order to design value-added nasal dosage forms. Local therapy of upper respiratory tract-related infections, such as nasal rhinosinusitis is of paramount importance, thus advanced local therapeutic options are required. Dexamethasone was encapsulated into three different polymeric micelle formulations: Soluplus or TPGS-only and their mixed combinations. Dynamic light scattering measurements proved that the particles have a micelle size less than 100 nm in monodisperse distribution, with high encapsulation efficiency above 80% and an at least 7-fold water solubility increase. Tobramycin, as an antimicrobial agent, was co-formulated into the in situ gelling systems which were optimized based on gelation time and gelation temperature. The sol–gel transition takes place between 32–35 °C, which is optimally below the temperature of the nasal cavity in a quick manner below 5 min, a suitable strategic criterion against the mucociliary clearance. In vitro drug release and permeability studies confirmed a rapid kinetics in the case of the encapsulated dexamethasone accompanied with a sustained release of tobramycin, as the hydrophilic drug.
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来源期刊
Gels
Gels POLYMER SCIENCE-
CiteScore
4.70
自引率
19.60%
发文量
707
审稿时长
11 weeks
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