热驱动自组装白蛋白纳米粒的制备及体外评价

发布时间：2018-01-22 04:44

本文关键词： 热驱动自组装白蛋白纳米粒紫杉醇制备形成机制胞内降解动力学　出处：《中国药科大学学报》2016年03期 　论文类型：期刊论文

【摘要】：探讨热驱动自组装白蛋白纳米粒的制备方法,并对其形成机制、细胞摄取、细胞摄取动力学与降解动力学等进行考察。通过测定巯基、氨基与羧基的浓度揭示白蛋白纳米粒的形成机制。采用CCK-8法检测纳米粒的细胞毒性,通过倒置荧光显微镜观察纳米粒的摄取行为,采用荧光共振能量转移(FRET)法测定白蛋白纳米粒在细胞内的摄取与降解动力学,并以紫杉醇为模型药物考察其对疏水性药物的包载能力。结果表明,热驱动自组装法制得的白蛋白纳米粒依靠分子间二硫键与酰胺键而稳定,安全无毒,易于被肿瘤细胞摄取并在胞内降解。载药实验结果显示,该纳米粒对紫杉醇有较高的包载。因此,热驱动自组装法绿色环保、操作简便,制得的白蛋白纳米粒可作为抗肿瘤药物传递的新平台。
[Abstract]:The preparation method of heat-driven self-assembled albumin nanoparticles was discussed, and the formation mechanism, cell uptake, cell uptake kinetics and degradation kinetics of albumin nanoparticles were investigated. The concentration of amino and carboxyl groups revealed the formation mechanism of albumin nanoparticles. CCK-8 assay was used to detect the cytotoxicity of nanoparticles and the uptake behavior of nanoparticles was observed by inverted fluorescence microscope. The uptake and degradation kinetics of albumin nanoparticles in cells were determined by fluorescence resonance energy transfer spectrometry. The encapsulation ability of paclitaxel to hydrophobic drugs was investigated using paclitaxel as a model drug. The albumin nanoparticles prepared by thermal driven self-assembly method are stable by intermolecular disulfide bond and amide bond, safe and non-toxic, easy to be ingested by tumor cells and degraded in cells. Therefore, the thermal driven self-assembly method is environmentally friendly and easy to operate. The albumin nanoparticles can be used as a new platform for the delivery of anti-tumor drugs.
【作者单位】：中国药科大学药剂学教研室;盐城卫生职业技术学院药学院;徐州医科大学药学院;
【基金】：国家自然科学基金资助项目(No.81402878) 江苏省普通高校研究生科研创新计划项目(No.CXZZ13_0327)~~
【分类号】：R943
【正文快照】： 白蛋白具有无毒、无免疫原性、生物相容性好以及生物可降解等优点,是目前临床上最理想的静脉输液载体材料。白蛋白结合型紫杉醇(Abraxane湟)为FDA批准上市的第1个纳米药物,广泛用于乳腺癌、非小细胞肺癌及转移性胰腺癌的治疗,它借助白蛋白的gp 60-窖蛋白-SPARC蛋白转运通路将

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