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基于聚电解质复合物的比凝胶作为阴道给药系统。

Bigels based on polyelectrolyte complexes as vaginal drug delivery systems.

作者信息

Cazorla-Luna Raúl, Notario-Pérez Fernando, Martín-Illana Araceli, Ruiz-Caro Roberto, Rubio Juan, Tamayo Aitana, Veiga María Dolores

机构信息

Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n 28040, Madrid, Spain.

Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n 28040, Madrid, Spain; Instituto Universitario de Farmacia Industrial, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n 28040, Madrid, Spain.

出版信息

Int J Pharm. 2025 Jan 25;669:125065. doi: 10.1016/j.ijpharm.2024.125065. Epub 2024 Dec 8.

DOI:10.1016/j.ijpharm.2024.125065
PMID:39657868
Abstract

Bigels in which the cationic polymer -chitosan- is combined with an anionic polymer -karaya gum, pectin or xanthan gum- were prepared. These polymers, thanks to the attraction of their charged surface groups, are liable to form a polyelectrolyte complex that would modify the characteristics of the bigel. The obtained bigels were subsequently freeze-dried and tested to study their behavior against different conditions occurring in the vaginal environment. Swelling and drug release profiles have been evaluated in a medium that simulates the ordinary vaginal conditions and simulating the conditions after ejaculation. Thanks to the formation of polyelectrolyte complexes, the bigel is able to provide a pH-independent sustained drug release. However, when one of the polymers predominates, the release of the active ingredient turns out to be pH-dependent -which can also be beneficial in some therapeutic applications-. It has been proved that the inclusion of a higher percentage of chitosan in the bigel improves its mechanical properties, while the mucoadhesivity of the system can be improved by increasing the anionic polymer. The versatility of these systems in modulating their physicochemical properties, provides a substantial advantage over the formulations currently available on the market for vaginal drug delivery.

摘要

制备了阳离子聚合物壳聚糖与阴离子聚合物刺梧桐树胶、果胶或黄原胶结合的双凝胶。由于其带电荷的表面基团相互吸引,这些聚合物易于形成聚电解质复合物,从而改变双凝胶的特性。随后对所得双凝胶进行冷冻干燥并进行测试,以研究它们在阴道环境中不同条件下的行为。在模拟正常阴道条件和射精后条件的介质中评估了溶胀和药物释放曲线。由于聚电解质复合物的形成,双凝胶能够实现与pH无关的持续药物释放。然而,当其中一种聚合物占主导时,活性成分的释放就会依赖于pH值——这在某些治疗应用中也可能是有益的。已经证明,在双凝胶中加入更高比例的壳聚糖可改善其机械性能,而通过增加阴离子聚合物可提高该系统的粘膜粘附性。这些系统在调节其物理化学性质方面的多功能性,相对于目前市场上用于阴道给药的制剂具有显著优势。

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