The Targeting Behavior of Folate-Nanohydrogel Evaluated by Near Infrared Imaging System in Tumor-Bearing Mouse Model
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- Zhang, J., Deng, D., Qian, Z. et al. Pharm Res (2010) 27: 46. doi:10.1007/s11095-009-0005-1
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To synthesize P[(Folate-Allylamine)-co-(N-isopropylacrylamine)- co-Acrylamide] (P(FoAAn-co-NIPA-AAm), folate-NHG) with appropriate diameter and lower critical solution temperature (LCST) for targeting to folate receptor (FR) expressing tumors.
Folate-NHG was synthesized by free-radical precipitation polymerization method reported in our previous work and other reports. LCST, diameter and morphology of folate-NHG were characterized by UV-vis spectrophotometer, laser particle size analyzer (LPSA) and transmission electron microscope (TEM), respectively. No.12 near infrared dye (NIRD-12) was entrapped into folate-NHG by hydrophobic association to trace the in vivo dynamic behavior of folate-NHG. This process was evaluated by a homemade near infrared (NIR) imaging system.
Spherical folate-NHG with diameter of about 50 nm and LCST of about 40°C was successfully synthesized. The photo stability of NIRD-12 was strengthened after being entrapped into folate-NHG, which enabled NIRD-12 to better trace the in vivo dynamic process of folate-NHG. Folate-NHG showed good targeting capability for all three folate receptor expressing tumor models (SMMC-7721, Bel-7402 and HeLa) with different sizes, and this accumulation could last for more than 96 h. D-folate-NHG, synthesized with double amount of FoAAn, showed better targeting effect for SMMC-7721 tumor model than that of folate-NHG.
Folate-NHG could actively accumulate in three models of folate receptor positive tumors with different sizes and keep retention for more than 96 h, which enables it to be used as a diagnostic reagent or anti-tumor drug carrier for tumor therapy.
KEY WORDSactive targetingfolate receptornanohydrogelNIR imagingtumor
special folate-NHG synthesized with as double amount of FoAAn as that of folate-NHG
folate binding protein
- folate-NHG or P(FoAAn-co-NIPA-co-AAm)
liquid chromatograph-mass spectrum
lower critical solution temperature
laser particle size analyzer
methyl thiazolyl tetrazolium
No.12 near infrared dye
region of interest
Roswell Park Memorial Institute
simulated body fluid
transmission electron microscope
((WAAm/WNIPA) × 100%)