林源活性成分纳米载体的安全性评价研究

Safety Evaluation on the Nanocarrier of the Active Ingredients from Forest

[目的]评价人血清白蛋白纳米颗粒载体以及林源活性成分纳米颗粒制剂的安全性。[方法]以人血清白蛋白制备纳米颗粒载体,包埋红豆杉属植物抗癌活性成分紫杉醇及其衍生物多西紫杉醇,开展细胞实验和动物实验。[结果]与紫杉醇和多西紫杉醇市售制剂的溶剂相比,纳米颗粒载体对MCF-7细胞和C57BL/6小鼠的毒性比较小;紫杉醇和多西紫杉醇的纳米颗粒制剂对BALB/C-nu/nu裸鼠的最大耐受剂量大于市售制剂Taxol~和Taxotere~(40、30 mg/kg)。[结论]紫杉醇和多西紫杉醇的纳米颗粒制剂有很大的市场前景,而蛋白纳米载体技术在林源活性成分的应用研究中具有重要的推广价值。

[Objective]To evaluate the safety of the human serum albumin nanoparticle carrier and active ingredients-loaded nanoparticle formulation.[Method]A human serum albumin nanoparticle was designed to deliver paclitaxel and docetaxel,the anticancer ingredients derived from the bark of the Pacific yew or Western yew tree(Taxus Linn.).In vitro experiments in human breast cancer MCF-7 cells and in vivo experiments in C57BL/6 mice and BALB/C-nu/nu nude mice were performed.[Result]The toxicity of human serum albumin nanoparticle carrier to the MCF-7 cells and C57BL/6 mice was much less than that of the solvents in the Taxol and Taxotere.The maximum tolerated dose of paclitaxel/docetaxel-loaded nanoparticle formulations was higher than that of Taxol and Taxotere(40,30 mg/kg)in BALB/C-nu/nu nude mice.[Conclusion]The paclitaxel/docetaxel-loaded nanoparticle formulation will possess good market prospect.The protein-based nanocarrier has important value for extension and application of active ingredients from forest.