title: Arginine-conjugated polypropylenimine dendrimer as a non-toxic and efficient gene delivery carrier.
abstract: We synthesized arginine-conjugated polypropylenimine dendrimer G2 (DAB-8), PPI2-R for gene delivery systems. Synthesized PPI2-R could retard plasmid DNA at a weight ratio of 4 completely and PPI2-R polyplexes showed a fluorescence of less than 10% over a charge ratio of 2 by PicoGreen reagent assay, suggesting its good DNA condensing ability. The size of PPI2-R polyplex was measured to about 200nm at a charge ratio of 150. PPI2-R displayed 80-90% cell viability at even a 150microg/mL concentration. Transfection efficiency of PPI2-R was found to be high comparable to that of PEI25kD and to be 8-214 times higher than that of unmodified PPI2 on HeLa and 293 cells. Moreover, PPI2-R showed 4 times higher transfection efficiency than PEI25kD, treating with 10microg pDNA because of its low cytotoxicity on HeLa cells. Finally, PPI2-R showed a transfection efficiency 2-3 times higher than PEI25kD on HUVECs, showing its potency as a gene delivery carrier for primary cells. These results demonstrate that arginine-conjugation of PPI2 is successful in developing a low toxic and highly transfection efficient gene delivery carrier.
authors.affiliation: School of Chemistry & Molecular Engineering, Seoul National University, San 56-1, Shillim-dong, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors.forename: Tae-Il
authors.initials: TI
authors.lastname: Kim
authors.forename: Jung-Un
authors.initials: JU
authors.lastname: Baek
authors.forename: Cheng
authors.initials: C
authors.lastname: Zhe Bai
authors.forename: Jong-Sang
authors.initials: JS
authors.lastname: Park
mesh_terms: D001120:Arginine / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival; D004247:DNA / Q000737:chemistry; D050091:Dendrimers; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods*; D004730:Endothelium, Vascular / Q000378:metabolism; D018014:Gene Transfer Techniques; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D009930:Organic Chemicals / Q000494:pharmacology; D011073:Polyamines / Q000737:chemistry*; D014162:Transfection
chemical_list: D050091:Dendrimers; D004337:Drug Carriers; D009930:Organic Chemicals; C104700:PAMAM Starburst; C099476:PicoGreen; D011073:Polyamines; D004247:DNA; D001120:Arginine