白蛋白结合型紫杉醇的研究进展

Research progress on nanoparticle albumin-bound paclitaxel

纳米颗粒白蛋白结合型紫杉醇是一种全新剂型紫杉醇类药物,它不需要合成的溶剂作为载体,不需要皮质类固醇或抗组胺药物等预处理,静脉滴注时间短(30min)。白蛋白结合型紫杉醇利用了白蛋白的自然生物特性,通过gp-60介导的内皮细胞跨膜转运和一种与白蛋白结合的蛋白SPARC(一种酸性的富含半胱氨酸的分泌蛋白)的相互作用而增加肿瘤组织对紫杉醇的摄取和蓄积,临床前模型研究证实白蛋白结合型紫杉醇与溶剂型紫杉醇相比,抗肿瘤活性明显增强。以此为基础,近年国内外进行了一系列白蛋白结合型紫杉醇应用于各种恶性肿瘤化疗的临床研究,并且取得了令人鼓舞的结果。

Nanoparticle albumin-bound paclitaxel is a novel formulation of paclitaxel that does not require the synthetic solvent carrier used with other taxanes.It is given as a 30 min intravenous infusion without corticosteroid or antihistamine premedication.It exploits the natural properties of albumin to increase uptake and accumulation of paclitaxel in the tumor through gp60-mediated endothelial transcytosis,and interaction with the albumin-binding protein SPARC（secreted protein,acidic and rich in cysteine）.Preclinical models have shown that nab-paclitaxel has greater antitumor activity than solvent-based paclitaxel and that lead to the clinical testing of nab-paclitaxel in chemotherapy on the patients with malignant tumors.Some results are made us inspiring.