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Synthesis, characterization and biological activity of cefazolin sodium dendrimer complexes
Journal of the Taiwan Institute of Chemical Engineers ( IF 5.7 ) Pub Date : 2020-11-10 , DOI: 10.1016/j.jtice.2020.10.033
Valikala Viswanath , Kannappan Santhakumar

The potent bacterial infections serve as the primary cause of mortality due to the absence of novel antibacterial therapy. The present investigation synthesized citric acid dendrimers through the divergent method that serves as a suitable platform in fulfilling the prerequisites of drug delivery. The cytotoxicity studies revealed 5.4 ± 0.3% of cell viability at 0.5 μg/ml and 35±0.3% at 300 μg/ml after 36 h. The IC50 values on Human Alveolar Epithelial (HAE) cells for unmodified dendrimers were 1.36±0.06 mg ml−1while for PEG CZ G5 dendrimers were 35.19±0.15 mg/mlwith 9 ± 0.18% hemolysis. The significant differences were due to the variations in drug content and PEG shield density at the terminal surface. The Reactive Oxygen Species (ROS) uptake and dichlorofluorescein intensity for PEG CZ G2 dendrimers was 24.15 ± 1.24% and 42.3 ± 0.12%whichincreased significantly with the degree of pegylation and revealed 72.5 ± 1.03% and 79.2 ± 0.24%for PEG CZ G5 dendrimers. The increased ROS concentrations altered the mitochondrial functioning and served as a proof for antibacterial effect. Drug release pattern when heuristically fitted into various kinetic models specified zero-order release with non-fickian diffusion. Antibacterial investigations and pharmacokinetic studies revealed that the synthesized generations were quite effective against various bacterial pathogens with optimized concentrations.



中文翻译:

头孢唑林钠树枝状聚合物配合物的合成,表征和生物学活性

由于缺乏新型抗菌疗法,强力细菌感染是导致死亡的主要原因。本研究通过发散法合成柠檬酸树枝状聚合物,该散发方法可作为满足药物递送先决条件的合适平台。细胞毒性研究显示,在36 h后,0.5μg/ ml时细胞活力为5.4±0.3%,300μg/ ml时为35±0.3%。未经修饰的树状聚合物对人肺泡上皮(HAE)细胞的IC 50值为1.36±0.06 mg ml -1PEG CZ G5树枝状聚合物为35.19±0.15 mg / ml,溶血率为9±0.18%。显着差异是由于末端表面药物含量和PEG屏蔽密度的变化所致。PEG CZ G2树枝状聚合物的活性氧(ROS)吸收和二氯荧光素强度分别为24.15±1.24%和42.3±0.12%,随着聚乙二醇化程度的增加而显着增加,而PEG CZ G5树枝状聚合物的活性氧种类(ROS)吸收为72.5±1.03%和79.2±0.24%。ROS浓度的增加改变了线粒体的功能,并证明了其抗菌作用。试探性地拟合到各种动力学模型中时,药物释放模式指定了零阶释放和非菲克扩散。

更新日期:2020-12-08
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