title: Synthesis of folate- pegylated polyester nanoparticles encapsulating ixabepilone for targeting folate receptor overexpressing breast cancer cells.
abstract: The aim of this study was the preparation of novel polyester nanoparticles based on folic acid (FA)-functionalized poly(ethylene glycol)-poly(propylene succinate) (PEG-PPSu) copolymer and loaded with the new anticancer drug ixabepilone (IXA). These nanoparticles may serve as a more selective (targeted) treatment of breast cancer tumors overexpressing the folate receptor. The synthesized materials were characterized by (1)H-NMR, FTIR, XRD and DSC. The nanoparticles were prepared by a double emulsification and solvent evaporation method and characterized with regard to their morphology by scanning electron microscopy, drug loading with HPLC-UV and size by dynamic light scattering. An average size of 195 nm and satisfactory drug loading efficiency (3.5%) were observed. XRD data indicated that IXA was incorporated into nanoparticles in amorphous form. The nanoparticles exhibited sustained drug release properties in vitro. Based on in vitro cytotoxicity studies, the blank FA-PEG-PPSu nanoparticles were found to be non-toxic to the cells. Fluorescent nanoparticles were prepared by conjugating Rhodanine B to PEG-PPSu, and live cell, fluorescence, confocal microscopy was applied in order to demonstrate the ability of FA-PEG-PPSu nanoparticles to enter into human breast cancer cells expressing the folate receptor.
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, 54 124, Thessaloniki, Macedonia, Greece.
authors.forename: P
authors.initials: P
authors.lastname: Siafaka
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, 54 124, Thessaloniki, Macedonia, Greece.
authors.forename: M
authors.initials: M
authors.lastname: Betsiou
authors.affiliation: Department of Molecular Biology and Genetics, Democritus University of Thrace, Xanthi, Greece.
authors.forename: A
authors.initials: A
authors.lastname: Tsolou
authors.affiliation: Department of Molecular Biology and Genetics, Democritus University of Thrace, Xanthi, Greece.
authors.forename: E
authors.initials: E
authors.lastname: Angelou
authors.affiliation: Department of Molecular Biology and Genetics, Democritus University of Thrace, Xanthi, Greece.
authors.forename: B
authors.initials: B
authors.lastname: Agianian
authors.affiliation: Department of Molecular Biology and Genetics, Democritus University of Thrace, Xanthi, Greece.
authors.forename: M
authors.initials: M
authors.lastname: Koffa
authors.affiliation: Pharmathen S.A, Pharmaceutical Industry, Dervenakion Str6, 153 51, Attiki, Greece.
authors.forename: S
authors.initials: S
authors.lastname: Chaitidou
authors.affiliation: Pharmathen S.A, Pharmaceutical Industry, Dervenakion Str6, 153 51, Attiki, Greece.
authors.forename: E
authors.initials: E
authors.lastname: Karavas
authors.affiliation: Department of Pharmacy, University of Patras, 26500, Patras, Greece.
authors.forename: K
authors.initials: K
authors.lastname: Avgoustakis
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, 54 124, Thessaloniki, Macedonia, Greece. dbic@chem.auth.gr.
authors.forename: D
authors.initials: D
authors.lastname: Bikiaris
mesh_terms: D001943:Breast Neoplasms / Q000378:metabolism*; D045744:Cell Line, Tumor; D034261:Epothilones / Q000737:chemistry*; D005260:Female; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D053758:Nanoparticles; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D011956:Receptors, Cell Surface / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D034261:Epothilones; D011091:Polyesters; D011956:Receptors, Cell Surface; D011092:Polyethylene Glycols; D005492:Folic Acid; C430592:ixabepilone