文献：Characterization of RGD-modified liposomes for multimodal molecular imaging ofαvβ3 integrin-expressing pancreatic cancer

作者：Mitsuyoshi Yoshimoto, Takuya Hayakawa, Masayuki Yamaguchi, Sadaaki Kimura and Hirofumi Fujii

文献链接：https://jnm.snmjournals.org/content/57/supplement_2/1206.short

Methods Liposomes composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol and N-(carbonyl-methoxypolyethyleneglycol 2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG-DSPE) were prepared by thin film hydration method. RGD-modified liposomes were synthesized by coupling c(RGDfK)-SH with maleimide-mPEG-DSPE. The amount of RGD-modification was regulated by changing ratios of maleimide-mPEG-DSPE to total mPEG-DSPE (50%: SH-RGD-liposome, 5%: H-RGD-liposome, 2.5%: M-RGD-liposome, and 1%: L-RGD-liposome). As reference liposomes without targeting ability, RKG-liposome and unmodified liposome (NT-liposome) were prepared. The particle size was adjusted to 100 nm. Binding affinities of RGD-modified liposomes to αvβ3 integrin were assessed as IC50s for 125I-echistatine binding to PANC-1 human pancreatic cancer cells with expression of αvβ3 integrin. 111In-deferoxamine and Fe-deferoxamine were encapsulated into the liposomes for radionuclide and MR studies, respectively. Biodistribution and MR imaging were carried out in a PANC-1 xenograft model.

方法采用薄膜水合法制备由1,2-二硬脂酰基-sn-甘油-3-磷酸胆碱（DSPC）、胆固醇和N-（羰基甲氧基聚乙二醇2000）-1,2-二硬脂酰基-sn-甘油-3-磷乙醇胺（mPEG-DSPE）组成的脂质体。

通过将c（RGDfK）-SH与马来酰亚胺mPEG-DSPE偶联，合成了RGD修饰的脂质体。RGD修饰的量通过改变马来酰亚胺mPEG-DSPE与总mPEG-DSPE的比例来调节（50%：SH-RGD脂质体，5%：H-RGD脂质体，2.5%：M-RGD-脂质体，1%：L-RGD-脂质体）。

作为没有靶向能力的参考脂质体，制备了RKG脂质体和未修饰的脂质体（NT脂质体）。将粒径调节至100nm。 

111In-deferosamine和Fe-deferosaine分别包封在脂质体中用于放射性核素和MR研究。在PANC-1异种移植物模型中进行了生物分布和MR成像。

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