title: Cholic acid modified 2 kDa polyethylenimine as efficient transfection agent.
abstract: New lipopolymers were synthesized by conjugating cholic acid (ChA) to polyethylenimines (PEI; 2 and 25 kDa) and a polyallylamine (PAA; 15 kDa) via N-acylation to develop effective gene delivery systems. The extent of ChA substitution linearly varied with the feed ratio during synthesis, indicating good control over grafting ratio. While ChA did not affect binding to plasmid DNA (pDNA) for higher molecular weight (MW) polymers, ChA substitution to 2 kDa PEI significantly affected the pDNA binding. Toxicity of the 2 kDa PEI was unaffected by ChA substitution, but it was improved for the higher MW polymers. Using immortal 293T cells and primary cord blood-derived mesenchymal stem cells, low MW (2 kDa) PEI was shown to display much better transfection efficiency as a result of ChA substitution, unlike the higher MW polymers. We conclude that ChA could be a suitable substituent for non-toxic (low MW) PEIs in order to improve their transfection efficiency.
authors: Dept. of Chemical & Materials Engineering, University of Alberta, Edmonton, AB, Canada; Dept. of Pharmacy, The M.S. University of Baroda, Vadodara, Gujarat, India.
authors: Brahmanand
authors: B
authors: Dube
authors: Laura
authors: L
authors: Rose
authors: Krutika
authors: K
authors: Sawant
authors: Hasan
authors: H
authors: Uludag
mesh_terms: D019826:Cholic Acid / Q000494:pharmacology*; D004247:DNA / Q000235:genetics; D018014:Gene Transfer Techniques; D057809:HEK293 Cells; D006801:Humans; D008970:Molecular Weight; D010316:Particle Size; D010957:Plasmids / Q000235:genetics; D011073:Polyamines / Q000737:chemistry; D011094:Polyethyleneimine / Q000737:chemistry*; D014162:Transfection
chemical_list: D011073:Polyamines; C063994:polyallylamine; D011094:Polyethyleneimine; D004247:DNA; D019826:Cholic Acid
keywords: biomaterials; lipid-polymer conjugates; transfection