基于mPEG-DSPE的RGD修饰脂质体的制备与表征
文献资料:Characterization of RGD-modified liposomes for multimodal molecular imaging ofαvβ3 integrin-expressing pancreatic cancer小说作品:Mitsuyoshi Yoshimoto, Takuya Hayakawa, Masayuki Yamaguchi, Sadaaki Kimura and Hirofumi Fujii论文外部链接://jnm.snmjournals.org/content/57/supplement_2/1206.shortMethods 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.



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