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Preparation and evaluation of human serum albumin-methotrexate nanoparticles as a potential drug delivery system for cancer.

机译:人血清白蛋白-甲氨蝶呤纳米颗粒的制备和评估,作为癌症的潜在药物递送系统。

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Nanoparticles of human serum albumin (HSA) represent a promising strategy for drug delivery to tumor cells. The conjugation of methotrexate to HSA takes advantage of reducing its systemic toxicity and increases its therapeutic benefits. In our study, we developed a new and simple method to producing albumin-methotrexate nanoparticles .Albumin-methotrexate conjugate prepared by a carbodiimide reaction were crosslinked with l-ethyl-3-(diaminopropyl)carbodiimde HC1 (EDC) to form nanoparticles. Particle size and size distribution of nanoparticles were determined by laser light scattering and TEM. The nanoparticles size were between 90-150 nm. The release of free methotrexate was estimated both in aqueous buffer solution and after incubation in serum. Only 5 and 9 percent of methotrexate were released at aqueous buffer solution and after incubation in serum respectively. Cytotoxicity of nanoparticles was investigated by MTT test. MTX-albumin-NPs have more cytotoxic effect on T47D cells than MTX (in equivalent MTX concentration).
机译:人血清白蛋白(HSA)的纳米颗粒代表了一种有前途的将药物递送至肿瘤细胞的策略。甲氨蝶呤与HSA的共轭具有减少其全身毒性和增加治疗益处的优势。在我们的研究中,我们开发了一种新的简单方法来生产白蛋白-甲氨蝶呤纳米颗粒。将通过碳二亚胺反应制备的白蛋白-甲氨蝶呤共轭物与1-乙基-3-(二氨基丙基)碳二亚胺HCl(EDC)交联形成纳米颗粒。通过激光散射和TEM确定纳米颗粒的粒度和粒度分布。纳米颗粒的尺寸在90-150nm之间。在缓冲水溶液中和在血清中孵育后,估计了游离甲氨蝶呤的释放。分别在缓冲水溶液和血清中孵育后,仅释放5%和9%的甲氨蝶呤。通过MTT试验研究了纳米颗粒的细胞毒性。 MTX-白蛋白-NP对T47D细胞的杀伤作用比MTX(相当于MTX浓度)更大。

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