NGR多肽修饰雷公藤甲素脂质体的制备及对人脐静脉内皮细胞抑制作用的初步研究

Preparation of Triptolide Liposomes Modified by NGR Polypeptide and Its Inhibitory Effect on Human Umbilical Vein Endothelial Cells

目的:制备精氨酸-甘氨酸-天冬酰胺(Asn-Gly-Arg,NGR)多肽修饰的雷公藤甲素脂质体(NGR-TP-LPs),初步研究其对人脐静脉内皮细胞(HUVEC)细胞的抑制作用。方法:选用薄膜分散法制备NGR-TP-LPs,采用CCK-8法考察NGR-TP-LPs对HUVEC的抑制作用。结果:NGR-TP-LPs的平均粒径为330.0 nm,多分散系数为0.266,Zeta电位为+8.45 mV,包封率为65.10%。雷公藤甲素(TP)、雷公藤甲素脂质体(TP-LPs)、NGR-TP-LPs的平均半抑制浓度(IC50)分别为18.19,23.27,11.02nmol·ml^-1。结论:采用薄膜分散法制得的NGR-TP-LPs粒径分布均匀,符合制剂学要求。NGR修饰的雷公藤甲素脂质体对HUVEC抑制作用明显增强。

Objective:To prepared triptolide liposomes modified by Asn-Gly-Arg(NGR)peptide(NGR-TP-LPs)and discusse its inhibitory effects on human umbilical vein endothelial cells(HUVEC).Methods:NGR-TP-LPs were prepared by a thin film dispersion method and the inhibition of NGR-TP-LPs on HUVEC was studied by CCK-8 assay.Results:The average size of liposomes was330.0 nm,the polydispersity index was 0.266 and the zeta potential was+8.45 mV.The average half maximal inhibitory concentration(IC50)of TP,TP-LPs and NGR-TP-LPs on HUVEC cells was 18.19,23.27 and 11.02 nmol·ml^-1,respectively.Conclusion:The size distribution of NGR-TP-LPs prepared by the film dispersion method is uniform,which meets the requirements of pharmaceutics.The inhibitory effect of triptolide liposomes modified by NGR peptide on HUVEC is significantly enhanced.