转铁蛋白与RGD共修饰PLGA纳米粒的制备及其对黑色素瘤的靶向性研究  

Preparation of transferrin and RGD co-modified PLGA nanoparticles and its targeting to melanoma

作　　者：李宗祥[1] 孙平[1] 

机构地区：[1]华中农业大学医院,湖北武汉430070

出　　处：《中国生化药物杂志》2014年第4期19-21,共3页Chinese Journal of Biochemical Pharmaceutics

基　　金：国家自然科学基金(81171365)

摘　　要：目的构建转铁蛋白(transferrin,TF)与RGD(精氨酸-甘氨酸-天冬氨酸,Arg-Gly-Asp)共修饰PLGA(聚乳酸羟基乙酸,poly(lactic-co-dycolic acid)纳米粒(TF/RGD-NPs),研究其黑色素瘤靶向性。方法采用乳化法制备TF和RGD共修饰纳米粒(TF/RGD-NPs),考察其形态、粒径、电位等理化性质。通过细胞摄取实验和黑色素瘤肿瘤球穿透实验考察TF/RGD-NPs与黑色素瘤B16细胞的亲和力和肿瘤组织穿透能力。结果制备的TF/RGD-NPs粒径为(113.4±12.5)nm,电位为(4.53±2.15)mV。体外细胞摄取实验表明B16细胞对TF/RGD-NPs的摄取效率分别是TF-NPs和RGD-NPs的2.7倍和2.9倍,差异均具有统计学意义(P<0.01)。细胞摄取实验和肿瘤球摄取实验结果表明TF/RGD-NPs具有良好的黑色素瘤细胞亲和力。结论转铁蛋白与RGD共修饰纳米粒具有良好的黑色素瘤靶向性,是一种潜在的黑色素瘤靶向给药系统。Objective To prepare transferrin and Arg-Gly-Asp polypeptide co-modified nanoparticles(TF/RGD-NPs)and evaluate its targeting efficiency to melanoma.Methods The co-modified nanoparticles were prepared by emulsion method and its appearance,particle size and Zeta potential were evaluated.The cellular uptake experiment and melanoma tumor spheroids penetration test were used to evaluate the affinity and ability to penetrate tumor tissues of TF/RGD-NPs to melanoma B16 cells. Results The particle diameter of co-modified nanoparticles was(113.4 ±12.5)nm and the Zeta potential was(4.53 ±2.15)mV.In vitro uptake test demonstrated that the efficacy of cellular uptaken TF/RGD-NPs by B16 cells were 2.7 times and 2.9 times to TF-NPs and RGD-NPs,respectively,the differences were all significant(P<0.05 ).Tumor spheroid penetration test results showed that TF/RGD-NPs has good affinity to melanoma cells.Conclusion TF/RGD-NPs can target to melanoma B16 cell efficiency in vitro,it may be serve as a potential drug delivery system for targeting melanoma.

关 键 词：转铁蛋白 RGD PLGA纳米粒 黑色素瘤 药物靶向 

分 类 号：R739.5[医药卫生—肿瘤]