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Int J Biol Macromol. 2021 Dec 30;199:150-161. doi: 10.1016/j.ijbiomac.2021.12.070. Epub 2021 Dec 30.

Folate functionalized chitosan nanoparticles as targeted delivery systems for improved anticancer efficiency of cytarabine in MCF-7 human breast cancer cell lines.

International journal of biological macromolecules

Deepa Geethakumari, Anoop Bhaskaran Sathyabhama, Krishnapriya Raji Sathyan, Dhaneesha Mohandas, Jisha V Somasekharan, Sajeevan Thavarool Puthiyedathu

Affiliations

  1. National Centre for Aquatic Animal Health, Cochin University of Science and Technology, Fine Arts Avenue, Kochi 682 016, Kerala, India.
  2. Research and Post Graduate Department of Chemistry, MES Keveeyam College, Valanchery 676552, Kerala, India.
  3. National Centre for Aquatic Animal Health, Cochin University of Science and Technology, Fine Arts Avenue, Kochi 682 016, Kerala, India. Electronic address: [email protected].

PMID: 34973988 DOI: 10.1016/j.ijbiomac.2021.12.070

Abstract

Anticancer drug cytarabine, has been widely used for treating haematological malignancies while it has minimal activity against solid tumours, which demands continuous infusion leading to high dose cytarabine toxicity. In this study, folate conjugated chitosan nanoparticles (FCCNP) were used for targeted delivery of cytarabine in breast adenocarcinoma cell lines by making use of the overexpressed folate receptors on the surface of MCF-7. Folate was conjugated to chitosan using carbodiimide. FCCNPs show spherical morphology with a size of<50 nm. Zeta potential of + 45.2 mV and PDI of 0.98 from DLS measurement confirms a stable monodisperse nanoformulation. Cytotoxicity was studied in folate receptor positive, MCF-7 and folate receptor negative, A-549 cell lines. Increased cellular uptake of the drug incorporated nanoparticles was confirmed in MCF-7 cells with fluorophore, squaraine 650 compared to A-549 cells. The relative fold of expression of genes involved in apoptosis such as bax, cyt c and cas 9 were upregulated. The present in vitro study confirms improved cytotoxicity of cytarabine folate conjugated chitosan nanoparticles in MCF-7 cells.

Copyright © 2021 Elsevier B.V. All rights reserved.

Keywords: A-549 cells; Chitosan; Cytarabine; Folate receptors; MCF-7 cells

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