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首页> 外文期刊>Journal of land use science >Hampered binding to blood serum albumin and antimicrobial activity of ibuprofen immobilised on magnetic nanoparticles Fe3O4
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Hampered binding to blood serum albumin and antimicrobial activity of ibuprofen immobilised on magnetic nanoparticles Fe3O4

机译:被阻碍与磁性纳米颗粒Fe3O4固定在磁性纳米颗粒上的布洛芬的血清白蛋白和抗菌活性的结合

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摘要

Drug distribution in an organism depends largely on the binding degree of drugs with blood serum proteins like albumin. Only free fraction of the drug can induce a therapeutic effect. A different affinity of particular drugs to proteins is also one of the reasons of the occurrence of drug interactions. It was decided to investigate if the immobilisation of some model drugs on magnetic nanoparticles Fe3O4 (MNPs)' would influence their activity and protect from binding to albumin. It was proposed to attach the drugs such as ibuprofen (IB), acetylsalicylic acid and naproxen to the MNPs coated with (3-aminopropyl)triethoxysilane' by electrostatic interaction since carboxyl groups of the drugs can form ionic bonds with amino groups of the silane. The characterisation of morphology of the obtained nanostructures was also carried out. The drug release studies showed very slow diffusion of the drugs from the MNPs surface. It has been demonstrated that IB immobilised on MNPs exhibits high antimicrobial activity even in its low concentration and in the presence of albumin - in contrast to the unattached form of the drug.
机译:生物体中的药物分布在很大程度上取决于血清血清蛋白质如白蛋白的药物的结合度。只有自由分数的药物可以诱导治疗效果。特定药物对蛋白质的不同亲和力也是药物相互作用发生的原因之一。决定研究一些模型药物在磁性纳米颗粒Fe3O4(MNP)'上的固定,影响它们的活性并保护与白蛋白结合。提出将这些药物如布洛芬(IB),乙酰胱氨酸和萘普生用静电相互作用涂覆有(3-氨基丙基)三乙氧基硅烷'的MNP,因为药物的羧基可以形成与硅烷的氨基的离子键。还进行了所得纳米结构的形态学的表征。药物释放研究表明,来自MNPS表面的药物非常缓慢扩散。已经证明,即使在其低浓度和白蛋白存在下,也表明IB在MNP上表现出高抗微生物活性 - 与药物的未附加的形式相比,白蛋白存在于白蛋白。

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