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Improvement of the Biological Activity of a New Cobalt(III) Complex through Loading into a Nanocarrier, and the Characterization Thereof

机译:通过加载到纳米载体中的新钴(III)复合物的生物学活性,并进行表征

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In an effort to use a polymer carrier for the maintenance of biological activity of metal complexes; in this report, a novel cobalt(III) complex, trans-[Co(en)2(mtzt)2]NO3 (1) was prepared (en=ethylenediamine and Hmtzt=1-methyl-1-H-1,2,3,4-tetra- zol-5-thiol) and fully characterized. A biocompatible di-block polymer, containing poly lactic-co-glycolic acid and poly ethylene glycol (PLGA-PEG), was employed as the nanocarrier of complex 1 to achieve more efficacy and controlled drug release. Results illustrated that the successful loading of the cobalt complex on the PLGA-PEG polymer as well as pH dependent drug release with approximately 17%, 58% and 74% release within 168 hours at pH=7.4, 5.8 and 4.8 respectively. Antibacterial properties of complex 1 and corresponding nano- carrier have been determined against gram-negative (Escher- ichia coli) and gram-positive (Staphylococcus aureus) bacteria where the loading of the complex on nanocarrier enhances its antibacterial activity. Their anticancer activity was also eval- uated over human ovarian carcinoma cells and compared with cisplatin.
机译:为了使用聚合物载体来维持金属复合物的生物活性;在本报告中,制备了一种新颖的钴(III)复合物,trans- [co(en)2(mtzt)2] No3(1) 3,4-Tetra-Zol-5-硫醇),并充分表征。含有多乳酸 - 乙醇酸和聚乙二醇(PLGA-PEG)的生物相容性二块聚合物被用作复合物1的纳米载体,以实现更有效的药物和受控药物释放。结果表明,在PLGA-PEG聚合物以及pH依赖性药物释放上,成功的负载在168小时内释放了约17%,58%和74%,分别在pH = 7.4、5.8和4.8。已经确定了复合物1和相应的纳米载体的抗菌特性,已针对革兰氏阴性(Escher- iChia coli)和革兰氏阳性(金黄色葡萄球菌)细菌确定,其中纳米载体上络合物的载荷增强其抗体活性。它们的抗癌活性也对人卵巢癌细胞进行了评估,并与顺铂进行了比较。

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