title: Uptake of etoposide in CT-26 cells of colorectal cancer using folate targeted dextran stearate polymeric micelles.
abstract: Targeted drug delivery using folate receptors is one of the most interesting chemotherapeutic research areas over the past few years. A novel folate targeted copolymer was synthesized using dextran stearate coupled to folic acid. FT-IR and NMR spectroscopy were used to confirm successful conjugation. Micelles prepared using this copolymer were characterized for their particle size, zeta potential, critical micelle concentration (CMC), drug loading capacity, and release efficiency. Cytotoxicity and cellular uptake of the micelles were estimated using CT-26 colorectal carcinoma cell line. FT-IR and NMR spectroscopy confirmed production of folate grafted dextran stearate copolymer. Low CMC value indicates that the copolymers are suitable for preparation of stable micelles useful in parenteral dosage forms. Particle size and zeta potential of the targeted nanoparticles were 105.5 ± 2.0 nm and -21.2 mV, respectively. IC50 of etoposide loaded in folate grafted dextran stearate enhanced about 20-fold compared to the pure drug (0.49 ± 0.11 μg/mL versus 9.41 ± 0.52 μg/mL). It seems that etoposide loaded in micelles of folate grafted dextran stearate copolymer is promising in reducing drug resistance of colorectal cancer by boosting etoposide cellular uptake.
authors.affiliation: Department of Pharmaceutics, Novel Drug Delivery Systems Research Center, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81745-359, Iran.
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81746-73461, Iran.
authors.forename: Farshid
authors.initials: F
authors.lastname: Hassanzadeh
authors.affiliation: Department of Biotechnology, Isfahan Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81746-73461, Iran.
authors.forename: Hojjat
authors.initials: H
authors.lastname: Sadeghi-Aliabadi
authors.affiliation: Department of Pharmaceutics, Novel Drug Delivery Systems Research Center, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81745-359, Iran.
authors.forename: Farzin
authors.initials: F
authors.lastname: Firozian
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D015179:Colorectal Neoplasms / Q000378:metabolism*; D003911:Dextrans / Q000737:chemistry*; D005047:Etoposide / Q000494:pharmacology*; D005453:Fluorescence; D005492:Folic Acid / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D011108:Polymers / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D013228:Stearates / Q000737:chemistry*
chemical_list: D003911:Dextrans; D008823:Micelles; D011108:Polymers; D013228:Stearates; D005047:Etoposide; D005492:Folic Acid