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Sustained Release of Linezolid from Prepared Hydrogels with Polyvinyl Alcohol and Aliphatic Dicarboxylic Acids of Variable Chain Lengths
Pharmaceutics ( IF 4.9 ) Pub Date : 2020-10-17 , DOI: 10.3390/pharmaceutics12100982
Gustavo Carreño , Adolfo Marican , Sekar Vijayakumar , Oscar Valdés , Gustavo Cabrera-Barjas , Johanna Castaño , Esteban F. Durán-Lara

A series of hydrogels with a specific release profile of linezolid was successfully synthesized. The hydrogels were synthesized by cross-linking polyvinyl alcohol (PVA) and aliphatic dicarboxylic acids, which include succinic acid (SA), glutaric acid (GA), and adipic acid (AA). The three crosslinked hydrogels were prepared by esterification and characterized by equilibrium swelling ratio, infrared spectroscopy, thermogravimetric analysis, mechanical properties, and scanning electron microscopy. The release kinetics studies of the linezolid from prepared hydrogels were investigated by cumulative drug release and quantified by chromatographic techniques. Mathematical models were carried out to understand the behavior of the linezolid release. These data revealed that the sustained release of linezolid depends on the aliphatic dicarboxylic acid chain length, their polarity, as well as the hydrogel crosslinking degree and mechanical properties. The in vitro antibacterial assay of hydrogel formulations was assessed in an Enterococcus faecium bacterial strain, showing a significant activity over time. The antibacterial results were consistent with cumulative release assays. Thus, these results demonstrated that the aliphatic dicarboxylic acids used as crosslinkers in the PVA hydrogels were a determining factor in the antibiotic release profile.

中文翻译:

聚乙烯醇和链长可变的脂肪族二羧酸从制备的水凝胶中持续释放利奈唑胺

成功合成了一系列具有利奈唑胺特定释放特性的水凝胶。通过交联聚乙烯醇(PVA)和脂肪族二羧酸(包括琥珀酸(SA),戊二酸(GA)和己二酸(AA))来合成水凝胶。通过酯化制备三种交联的水凝胶,并通过平衡溶胀率,红外光谱,热重分析,机械性能和扫描电子显微镜进行表征。通过累积药物释放研究了利奈唑胺从制备的水凝胶中的释放动力学,并通过色谱技术对其进行了定量。进行数学模型以了解利奈唑胺释放的行为。这些数据表明,利奈唑胺的持续释放取决于脂族二羧酸的链长,极性,水凝胶的交联度和机械性能。水凝胶制剂的体外抗菌测定在粪肠球菌菌株,随时间推移表现出明显的活性。抗菌结果与累积释放试验一致。因此,这些结果证明,在PVA水凝胶中用作交联剂的脂族二羧酸是抗生素释放曲线的决定因素。
更新日期:2020-10-17
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