Glucosylated polyethylenimine as a tumor-targeting gene carrier.
Glucosylated polyethylenimine (GPEI) was synthesized as a tumor-targeting gene carrier through facilitative glucose metabolism by tumor glucose transporter. Particle sizes of GPEI/DNA complex increased in proportion to glucose content of GPEI, whereas surface charge of the complex was not dependent on glucosylation, partially due to inefficient shielding of the short hydrophilic group introduced. GPEI with higher glucosylation (36 mol-%) had no cytotoxic effect on cells even at polymer concentrations higher than 200 microg/mL. Compared to unglucosylated PEI, glucosylation induced less than one-order decrease of transfection efficiency. Transfection of GPEI/DNA complex into tumor cells possibly occurred through specific interaction between glucose-related cell receptors and glucose moiety of GPEI. Gamma imaging technique revealed GPEI/DNA complex was distributed in liver, spleen, and tumors.
Park
In-Kyu
IK
School of Agricultural Biotechnology, Seoul National University, Seoul 151-742, Korea.
Cook
Seung-Eun
SE
Kim
You-Kyoung
YK
Kim
Hyun-Woo
HW
Cho
Myung-Haing
MH
Jeong
Hwan-Jeong
HJ
Kim
Eun-Mi
EM
Nah
Jae-Woon
JW
Bom
Hee-Seung
HS
Cho
Chong-Su
CS
D002240:Carbohydrate Sequence; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D015902:Gamma Cameras; D017930:Genes, Reporter; D015316:Genetic Therapy / Q000379:methods*; D005947:Glucose / Q000737:chemistry; D006801:Humans; D007091:Image Processing, Computer-Assisted; D007202:Indicators and Reagents; D008027:Light; D008156:Luciferases / Q000235:genetics; D008969:Molecular Sequence Data; D010316:Particle Size; D011094:Polyethyleneimine / Q000737:chemistry*; D012542:Scattering, Radiation; D013667:Technetium
D004337:Drug Carriers; D007202:Indicators and Reagents; D013667:Technetium; D011094:Polyethyleneimine; D008156:Luciferases; D005947:Glucose