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Synergistic delivery of 5-fluorouracil and curcumin using human serum albumin-coated iron oxide nanoparticles by folic acid targeting

机译:叶酸靶向使用人血清白蛋白包被的氧化铁纳米颗粒协同递送5-氟尿嘧啶和姜黄素

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摘要

Human serum albumin is the most abundant protein in plasma with the ability to bind to a variety of drug molecules. Magnetic nanoparticles are being extensively used in drug delivery due to its intrinsic magnetic properties. In this work, we have synthesized human serum albumin-coated citrate-functionalized iron oxide nanoparticles by CDI coupling. Furthermore, folic acid was decorated on human serum albumin by EDC and NHS coupling to confer targetability. Two cytotoxic drugs 5-fluorouracil (5FU) and curcumin were co-delivered. Wherein, the former is an anticancer agent and latter is a drug resistance depressor of former. The nanoparticles showed good aqueous dispersibility with a zeta potential of − 49.1 mV and magnetic core size in the range of 10–15 nm, thus exhibiting good magnetic property with magnetic saturation of 33.59 emu/g. Controlled drug release behavior was noticed in both drugs with faster release profile of 5FU. Nanoparticles also showed good cytotoxicity with lower IC50 values in the presence of magnetic field. The contrasting difference was noticed in folic acid-decorated and non-decorated composites, similarly in the presence of magnetic field where cell uptake was enhanced.
机译:人血清白蛋白是血浆中最丰富的蛋白质,具有与多种药物分子结合的能力。磁性纳米粒子因其固有的磁性而被广泛用于药物输送。在这项工作中,我们已经通过CDI偶联合成了人血清白蛋白包被的柠檬酸盐官能化的氧化铁纳米颗粒。此外,通过EDC和NHS偶联将叶酸修饰在人血清白蛋白上,以赋予靶向性。共递送两种细胞毒性药物5-氟尿嘧啶(5FU)和姜黄素。其中,前者是抗癌药,后者是前者的抗药性抑制剂。纳米粒子表现出良好的水分散性,ζ电位为−49.1 mV,磁芯尺寸在10-15 nm范围内,因此表现出良好的磁性,磁饱和度为33.59 emu / g。在两种具有5FU较快释放曲线的药物中都注意到了受控的药物释放行为。纳米颗粒还显示出良好的细胞毒性,在磁场存在下具有较低的IC50值。在装饰有叶酸和未装饰叶酸的复合物中观察到相反的差异,类似地,在存在磁场的情况下,细胞摄取得到了增强。

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