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Folate – Galactose – targeted delivery of fluoresceine isothiocyanate as a drug model prepared by FOL-PEG-g-PEI-GAL conjugate as a novel carrier
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UPLOADED BY-ADMIN, S.GHIAMKAZEMI, M.HAJIABEDIN, A.AMANZADEH, T.AMINI, R.DINARVAND, M.AMINI, M.RAFIEE-TEHRANI
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| Abstract:
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Polyethylenimine (PEI) is a well-known cationic polymer that has gained recent attention as a transfection and transduction
agent. However; it is extremely cytotoxic in many cell lines because of its high surface charge (about +40 mV), nonbiodegradability
and non-biocompatibility. Other drawbacks of this polymer include, low duration of expression, nonspecific
cell uptake and instability in blood circulation. To enhance Polyethyleneimine biocompatibility, the graft pegylated
copolymer was synthesized. To target cancer liver cells, two targeting ligands folic acid and galactose (lactobionic acid)
were attached with graft Pegylated copolymer to increase specifically the entrance of this new targeted copolymer to cancer
liver cells, because the folic acid and lactobionic acid receptors are over expressed only on human hepatocyte carcinoma.
The composition of this new conjugated copolymer was characterized using 1H-NMR spectra. Its molecular weight and zeta
potential were compared to polyethyleneimine. To study the entrance of this targeted carrier to human hepatocyte carcinoma
(HepG2), fluoresceine isothiocyanate (FITC) as a model drug was conjugated to this novel carrier and the emission of green
fluorescent was determined from three cell lines (HEK293, KB and HepG2) and compared with fluoresceine isothiocyanate
alone. The conjugated copolymer showed no cytotoxicity and targeted cultured HepG2 cells more effectively than KB and
HEK 293 cell lines because of its two targeting moieties. In conclusion, the results indicate that the novel biocompatible
copolymer can be considered as a useful carrier for targeted drug delivery to liver cancer cells.
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Polyethylenimine, FOL-PEG-g-PEI-GAL, targeted drug delivery, fluoresceine isothiocyanate, pegylation,HEK293 and KB and HepG2 cell lines.
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