抗肿瘤多肽M1-21的剂型优化

Desolution Optimization of Anti-tumor Peptide M1-21

通过去溶剂化方法,将单体抗肿瘤多肽M1-21纳米化,形成50 nm左右大小的多肽纳米颗粒(Nano-M1-21).运用动态光色散技术(DLS)和低压透射电镜(TEM)对Nano-M1-21进行表征,并进行体外37℃条件下颗粒稳定性测试.运用乳腺癌MDA-MB-231、MCF-7和4T1细胞验证Nano-M1-21的抗肿瘤效果,结果表明Nano-M1-21更容易被细胞摄取;相比单体多肽,达到抑制肿瘤细胞的浓度更低.运用小鼠乳腺癌4T1细胞活体肿瘤移植模型,发现Nano-M1-21展示出良好的抑瘤效果.总之,单体肽M1-21经纳米剂型优化后,有利于改善细胞的摄取,显示出更好的抑瘤效果.

The anti-tumor peptide M1-21 monomer was used to create nanoparticles(Nano-M1-21,about 50nm)by the desolution method. The characteristics of Nano-M1-21 were determined by the dynamic optical dispersion(DLS)and the low pressure transmission electron microscopy(TEM). The stability of Nano-M1-21 particles was measured in vitro at 37 degrees centigrade. To verify the anti-tumor effects of Nano-M1-21,we used breast cancer MDA-MB-231,MCF-7 and 4T1 cells to show that Nano-M1-21 was easily absorbed by the cells and its tumor inhibitory concentration was lower than that of monomer peptide. With a mouse breast cancer 4T1 cell-grafting tumor model,we found that Nano-M1-21 showed a good suppressive effect on the tumors. In conclusion,compared to the monomer peptide M1-21,the optimized Nano-M1-21 nanoparticles provide benefits to improve the cellular uptake and anti-tumor effects.