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Prolonged Delivery of Ciprofloxacin and Diclofenac Sodium from a Polymeric Fibre Device for the Treatment of Peridontal Disease

机译:从用于治疗牙周疾病的聚合物纤维装置中延长环丙沙星和双氯芬酸钠的输送

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摘要

In vitro analysis of drug release and antimicrobial activity of the coblended crosslinked polymeric fibre device (PFD) were investigated. The fibre loaded with ciprofloxacin and diclofenac sodium was comprised of alginate and glycerol crosslinked with barium cations. The pH dependent drug release was evident with ciprofloxacin and diclofenac sodium diffusing from the fibre at pH 4.0 compared to pH 6.8, where the fibre swelled and eroded resulting in zero-order drug release. Agar diffusion studies followed by minimum inhibitory assays were conducted to determine the antimicrobial activity of the device against Escherichia coli, Enterococcus faecalis, and Streptococcus mutans. The antimicrobial activity of the PFD was confirmed in both test assays against all test pathogens. The MIC ranges at pH 4.0 for E. coli, E. faecalis, and S. mutans were 0.5–0.8, 0.4–1.1, and 0.7–2.1 μg/mL, respectively. At pH 6.8, similar efficacies (0.3–0.5 μg/mL for E. coli and E. faecalis and 0.6–1.0 μg/mL for S. mutans) were observed. The effect of varying the plasticizer and crosslinking ion concentration on drug release profile of the fibers was further elucidated and conceptualized using molecular mechanics energy relationships (MMER) and by exploring the spatial disposition of geometrically minimized molecular conformations.
机译:研究了共混交联聚合物纤维装置(PFD)的药物释放和抗菌活性的体外分析。载有环丙沙星和双氯芬酸钠的纤维由与钡阳离子交联的藻酸盐和甘油组成。环丙沙星和双氯芬酸钠从pH值6.8的纤维中扩散出来,与pH 6.8相比,pH依赖性药物的释放是明显的,在该处纤维膨胀并腐蚀,导致药物的零级释放。进行琼脂扩散研究,然后进行最小抑制试验,以确定该装置对大肠杆菌,粪肠球菌和变形链球菌的抗菌活性。在两种测试方法中都证实了PFD对所有测试病原体的抗菌活性。在pH 4.0下,大肠杆菌,粪肠球菌和变形链球菌的MIC范围分别为0.5–0.8、0.4–1.1和0.7–2.1μg / mL。在pH 6.8时,观察到相似的功效(大肠杆菌和粪肠球菌为0.3-0.5μg/ mL,变形链球菌为0.6-1.0μg/ mL)。使用分子力学能量关系(MMER)并通过探索几何最小化分子构象的空间布置,进一步阐明和概念化了改变增塑剂和交联离子浓度对纤维的药物释放曲线的影响。

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