CAJ | 학술논문

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-glycolic 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。
목적：구건전철단백（transferrin，TF）여RGD（정안산-감안산-천동안산，Arg-Gly-Asp）공수식PLGA（취유산간기을산， poly（lactic-co-glycolic acid）납미립（TF/RGD-NPs），연구기흑색소류파향성。방법채용유화법제비TF화RGD공수식납미립（TF/RGD-NPs），고찰기형태、립경、전위등이화성질。통과세포섭취실험화흑색소류종류구천투실험고찰TF/RGD-NPs여흑색소류B16세포적친화력화종류조직천투능력。결과제비적TF/RGD-NPs립경위（113.4±12.5）nm，전위위（4.53±2.15）mV。체외세포섭취실험표명B16세포대TF/RGD-NPs적섭취효솔분별시TF-NPs화RGD-NPs적2.7배화2.9배，차이균구유통계학의의（P＜0.01）。세포섭취실험화종류구섭취실험결과표명TF/RGD-NPs구유량호적흑색소류세포친화력。결론전철단백여RGD공수식납미립구유량호적흑색소류파향성，시일충잠재적흑색소류파향급약계통。
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.