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Polyelectrolyte Matrices in the Modulation of Intermolecular Electrostatic Interactions for Amorphous Solid Dispersions: A Comprehensive Review
Pharmaceutics ( IF 4.9 ) Pub Date : 2021-09-14 , DOI: 10.3390/pharmaceutics13091467
Anastasia Tsiaxerli 1 , Anna Karagianni 1 , Andreas Ouranidis 1, 2 , Kyriakos Kachrimanis 1
Affiliation  

Polyelectrolyte polymers have been widely used in the pharmaceutical field as excipients to facilitate various drug delivery systems. Polyelectrolytes have been used to modulate the electrostatic environment and enhance favorable interactions between the drug and the polymer in amorphous solid dispersions (ASDs) prepared mainly by hot-melt extrusion. Polyelectrolytes have been used alone, or in combination with nonionic polymers as interpolyelectrolyte complexes, or after the addition of small molecular additives. They were found to enhance physical stability by favoring stabilizing intermolecular interactions, as well as to exert an antiplasticizing effect. Moreover, they not only enhance drug dissolution, but they have also been used for maintaining supersaturation, especially in the case of weakly basic drugs that tend to precipitate in the intestine. Additional uses include controlled and/or targeted drug release with enhanced physical stability and ease of preparation via novel continuous processes. Polyelectrolyte matrices, used along with scalable manufacturing methods in accordance with green chemistry principles, emerge as an attractive viable alternative for the preparation of ASDs with improved physical stability and biopharmaceutic performance.

中文翻译:

无定形固体分散体分子间静电相互作用调制中的聚电解质基质:综合综述

聚电解质聚合物已广泛用于制药领域作为赋形剂以促进各种药物递送系统。聚电解质已被用于调节静电环境并增强药物与主要通过热熔挤出制备的无定形固体分散体 (ASD) 中的聚合物之间的有利相互作用。聚电解质已单独使用,或与非离子聚合物组合用作聚电解质间复合物,或在添加小分子添加剂后使用。发现它们通过有利于稳定分子间相互作用以及发挥抗塑化作用来增强物理稳定性。此外,它们不仅可以增强药物溶出度,还可以用于维持过饱和度,尤其是弱碱性药物容易在肠内沉淀的情况下。其他用途包括控制和/或靶向药物释放,具有增强的物理稳定性和易于通过新型连续工艺制备。聚电解质基质与符合绿色化学原理的可扩展制造方法一起使用,成为制备具有改善的物理稳定性和生物制药性能的 ASD 的有吸引力的可行替代方案。
更新日期:2021-09-14
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