Preparation and characterization of folate-poly(ethylene glycol)-grafted-trimethylchitosan for intracellular transport of protein through folate receptor-mediated endocytosis.
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.
Zheng
Yu
Y
Sichuan University, Chengdu, China.
Song
Xiangrong
X
Darby
Michael
M
Liang
Yufeng
Y
He
Ling
L
Cai
Zheng
Z
Chen
Qiuhong
Q
Bi
Yueqi
Y
Yang
Xiaojuan
X
Xu
Jiapeng
J
Li
Yuanbo
Y
Sun
Yiyi
Y
Lee
Robert J
RJ
Hou
Shixiang
S
D002352:Carrier Proteins / Q000378:metabolism*; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004705:Endocytosis; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D015151:Immunoblotting; D008856:Microscopy, Fluorescence; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D021381:Protein Transport; D011956:Receptors, Cell Surface / Q000378:metabolism*
D002352:Carrier Proteins; D058973:Folate Receptors, GPI-Anchored; D011108:Polymers; D011956:Receptors, Cell Surface; D011092:Polyethylene Glycols; D048271:Chitosan; D005492:Folic Acid