含 Poloxamer 407 和海藻酸钠的凝胶作为阴道给药载体

Kakwokpo Clémence N’GUESSAN-GNAMAN, Awa Nakognon TUO-KOUASSI, Sandrine AKA-ANY-GRAH, Rosine Désirée CHOUGOUO KENGNE-NKUITCHOU, Apo Laurette Anin, A. Lia, Alain N’GUESSAN, Ismael Dally
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摘要

研究海藻酸钠和聚氧乙烯聚酰胺 407 的目的是设计一种水凝胶给药系统,作为配制阴道药物的平台。海藻酸钠是一种天然阴离子粘附性聚合物,而 poloxamer 407 则是一种对温度敏感的聚合物。对一种商用海藻酸盐进行了表征。然后,制备了海藻酸钠溶液(0.5-2 % w/w)、聚二酰胺 407 溶液(16-21.5 % w/w)及其混合物。对它们的流变特性和阴道模拟液的影响进行了评估。这种商用海藻酸盐的甘露聚糖酸盐与谷胱甘肽的比率为 1.24,重量平均分子量为 300 000 ± 2% g.mol-1,多分散指数为 1.8 ± 3%。藻酸盐溶液具有粘性,不适合阴道给药。Poloxamer 溶液及其与海藻酸盐的混合物具有温度敏感性、剪切稀化性、非各向同性,并具有适合阴道给药的弹性行为。它们不易被阴道液稀释,可延长阴道的停留时间。关键词制剂、poloxamer 407、流变学、海藻酸钠、温度敏感性、阴道液、粘弹性能。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Gels Containing Poloxamer 407 and Sodium Alginate as Vehicles for Vaginal Administration
Sodium alginate and poloxamer 407 were both studied in order to design a hydrogel-based delivery system as a platform for the formulation of vaginal medecines. Sodium alginate is a natural anionic mucoadhesive polymer while poloxamer 407 is a temperature-sensitive polymer. A commercial alginate was characterized. Then, its solutions (0.5-2 % w/w), poloxamer 407 solutions (16-21.5 % w/w) and their mixtures were prepared. Their rheological properties and the influence of vaginal simulated fluid were assessed. This commercial alginate had a mannuronate-to-guluronate ratio of 1.24, a weight-average molecular weight of 300 000 ± 2% g.mol-1, a polydispersity index of 1.8 ± 3%. Alginate solutions displayed a viscous behavior not suitable for a vaginal administration. Poloxamer solutions and their mixtures with alginate were temperature-sensitive, shear-thinning, non-thixotropic and had an elastic behavior suitable for a vaginal administration. Their resistance to dilution with vaginal fluid could prolonge vaginal residence. Keywords: Formulation, poloxamer 407, rheology, sodium alginate, temperature–sensitive, vaginal fluid, viscoelastic properties.
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