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用于替诺福韦控释的基于黄原胶的粘膜粘附性三层阴道膜中的优化水合动力学

Optimized hydration dynamics in mucoadhesive xanthan-based trilayer vaginal films for the controlled release of tenofovir.

作者信息

Martín-Illana Araceli, Chinarro Eva, Cazorla-Luna Raul, Notario-Perez Fernando, Veiga-Ochoa M D, Rubio Juan, Tamayo Aitana

机构信息

Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Universidad Complutense de Madrid, Plaza Ramón y Cajal s.n, 28007 Madrid, Spain.

Institute of Ceramics and Glass, CSIC, Kelsen 5, 28049 Madrid, Spain.

出版信息

Carbohydr Polym. 2022 Feb 15;278:118958. doi: 10.1016/j.carbpol.2021.118958. Epub 2021 Dec 2.

Abstract

Karaya gum, pectin and xanthan gum have been tested as candidates for manufacturing mucoadhesive trilayer films containing ethylcellulose and chitosan for the vaginal administration of the antiviral Tenofovir (TFV). The swelling profile correlated with the amount of mobile dipoles determined by impedance spectroscopy allows the determination of the hydration dynamics of these films. The fast water penetration has been demonstrated to favor the formation of polyelectrolyte complexes (PEC) via hydrogen or ionic bonds which would favor a controlled release. The incorporation of an inorganic drug release regulator induces the weakness of the polymeric chains thus enhancing the ionic mobility via the formation of low molecular weight PECs in films manufactured with karaya gum. Due to the different mechanical properties of the individual components, pectin-based films failed for a potential pharmaceutical formulation. However, mucoadhesive trilayer films produced with xanthan gum have demonstrated a moderate swelling, improved wettability and a controlled release of TFV.

摘要

卡拉亚胶、果胶和黄原胶已被作为制造含乙基纤维素和壳聚糖的黏膜黏附三层膜的候选材料进行测试,该三层膜用于抗病毒药物替诺福韦(TFV)的阴道给药。通过阻抗谱测定的与移动偶极子数量相关的溶胀曲线,能够确定这些膜的水化动力学。快速的水渗透已被证明有利于通过氢键或离子键形成聚电解质复合物(PEC),这将有利于控释。加入无机药物释放调节剂会导致聚合物链的弱化,从而通过在以卡拉亚胶制造的膜中形成低分子量PEC来增强离子迁移率。由于各组分的机械性能不同,基于果胶的膜未能成为潜在的药物制剂。然而,用黄原胶生产的黏膜黏附三层膜已表现出适度的溶胀、改善的润湿性以及TFV的控释。

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