Glucosylated polyethylenimine as a tumor-targeting gene carrier

• Published in: Archives of pharmacal research Vol. 28; no. 11; pp. 1302 - 1310
• Main Authors: Park, In-Kyu, Cook, Seung-Eun, Kim, You-Kyoung, Kim, Hyun-Woo, Cho, Myung-Haing, Jeong, Hwan-Jeong, Kim, Eun-Mi, Nah, Jae-Woon, Bom, Hee-Seung, Cho, Chong-Su
• Format: Journal Article
• Language: English
• Published: Korea (South) 대한약학회 01.11.2005
• Subjects: Carbohydrate Sequence; Cell Line, Tumor; Cell Survival - drug effects; Drug Carriers - chemistry; Drug Delivery Systems; Gamma Cameras; Genes, Reporter; Genetic Therapy - methods; Glucose - chemistry; Humans; Image Processing, Computer-Assisted; Indicators and Reagents; Light; Luciferases - genetics; Molecular Sequence Data; Particle Size; Polyethyleneimine - chemistry; Scattering, Radiation; Technetium; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/BF02978216

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.