title: Folic acid conjugated Fe3O4magnetic nanoparticles for targeted delivery of doxorubicin.
abstract: The interfacial engineering of magnetic nanoparticles (MNPs) with specific functional groups or targeting ligands is important for their in vivo applications. We report here the preparation and characterization of bifunctional magnetic nanoparticles (BMNPs) which contain a carboxylic moiety for drug binding and an amine moiety for folate mediated drug targeting. BMNPs were prepared by introducing bioactive cysteine molecules onto the surface of undecenoic acid coated Fe3O4magnetic nanoparticles (UMNPs) via a thiol-ene click reaction and then, folic acid was conjugated with these BMNPs through an EDC-NHS coupling reaction. X-ray diffraction (XRD) and transmission electron microscopy (TEM) analysis indicate the formation of highly crystalline single-phase Fe3O4nanostructures. The changes in the interfacial characteristics of the nanoparticles and the presence of an organic coating are evident from Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), zeta-potential measurement, and thermogravimetric analysis (TGA). These nanocarriers have an average size of 10 nm, and have a pH dependent charge conversional feature and protein resistance characteristic in physiological medium. These nanoparticles also show high loading affinity for an anticancer drug, doxorubicin hydrochloride (DOX) and its pH dependent release. This is highly beneficial for cancer therapy as the relatively low pH in tumors will specifically stimulate the drug release at the site of interest. Furthermore, our fluorescence microscopy and flow cytometry studies confirmed the higher cellular internalization capability of these folic acid conjugated nanoparticles in cancer cells over-expressing folate receptors.
authors.affiliation: Chemistry Division, Bhabha Atomic Research Centre, Mumbai - 400085, India. kcbarick@barc.gov.in hassan@barc.gov.in and Homi Bhabha National Institute, Anushaktinagar, Mumbai - 400094, India.
authors.forename: Suman
authors.initials: S
authors.lastname: Rana
authors.affiliation: Homi Bhabha National Institute, Anushaktinagar, Mumbai - 400094, India and Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai - 400085, India.
authors.forename: Neena G
authors.initials: NG
authors.lastname: Shetake
authors.affiliation: Chemistry Division, Bhabha Atomic Research Centre, Mumbai - 400085, India. kcbarick@barc.gov.in hassan@barc.gov.in.
authors.forename: K C
authors.initials: KC
authors.lastname: Barick
authors.affiliation: Homi Bhabha National Institute, Anushaktinagar, Mumbai - 400094, India and Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai - 400085, India.
authors.forename: B N
authors.initials: BN
authors.lastname: Pandey
authors.affiliation: Homi Bhabha National Institute, Anushaktinagar, Mumbai - 400094, India and Technical Physics Division, Bhabha Atomic Research Centre, Mumbai - 400085, India.
authors.forename: H G
authors.initials: HG
authors.lastname: Salunke
authors.affiliation: Chemistry Division, Bhabha Atomic Research Centre, Mumbai - 400085, India. kcbarick@barc.gov.in hassan@barc.gov.in and Homi Bhabha National Institute, Anushaktinagar, Mumbai - 400094, India.
authors.forename: P A
authors.initials: PA
authors.lastname: Hassan
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D003545:Cysteine / Q000737:chemistry; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004705:Endocytosis; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007624:KB Cells; D058185:Magnetite Nanoparticles / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D017550:Spectroscopy, Fourier Transform Infrared; D013818:Thermogravimetry; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D058185:Magnetite Nanoparticles; D004317:Doxorubicin; D005492:Folic Acid; D003545:Cysteine