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Preparation and characterization of folate-poly(ethylene glycol)-grafted-trimethylchitosan for intracellular transport of protein through folate receptor-mediated endocytosis

Zheng, Yu, Song, Xiangrong, Darby, Michael, Liang, Yufeng, He, Ling, Cai, Zheng, Chen, Qiuhong, Bi, Yueqi, Yang, Xiaojuan, Xu, Jiapeng, Li, Yuanbo, Sun, Yiyi, Lee, Robert J., Hou, Shixiang
Journal of biotechnology 2010 v.145 no.1 pp. 47-53
biopharmaceuticals, biotechnology, bovine serum albumin, composite polymers, electrolytes, endocytosis, ethylene glycol, fluorescein, folic acid, neoplasm cells
To develop a receptor-mediated intracellular delivery system that can transport therapeutic proteins to specific tumor cells, folate-poly(ethylene glycol)-grafted-trimethylchitosan (folate-PEG-g-TMC) was synthesized. Nano-scaled spherical polyelectrolyte complexes between the folate-PEG-g-TMC and fluorescein isothiocyanate conjugated bovine serum albumin (FITC-BSA) were prepared under suitable weight ratio of copolymer to FITC-BSA by ionic interaction between the positively charged copolymers and the negatively charged FITC-BSA. Intracellular uptake of FITC-BSA was specifically enhanced in SKOV3 cells (folate receptor over-expressing cell line) through folate receptor-mediated endocytosis compared with A549 cells (folate receptor deficient cell line). Folate-PEG-g-TMC shows promise for intracellular transport of negatively charged therapeutic proteins into folate receptor over-expressing tumor cells.