Contents lists available at ScienceDirect Journal of Drug Delivery Science and Technology journal homepage: www.elsevier.com/locate/jddst Camptothecin loaded graphene oxide nanoparticle functionalized with polyethylene glycol and folic acid for anticancer drug delivery Ananya Deb a , Vimala R. b,* a School of Biosciences & Technology, VIT University, Vellore, 632-014, Tamil Nadu, India b Centre for Nanotechnology Research, VIT University, Vellore, 632-014, Tamil Nadu, India ARTICLE INFO Keywords: Graphene oxide Polyethylene glycol Folic acid Anticancer Camptothecin Drug delivery ABSTRACT Graphene oxide nanomaterials are widely used to achieve effective cancer treatment. In this study, a novel graphene oxide mediated drug delivery system was synthesized by combining anticancer drug camptothecin (CPT) to the large surface area of graphene oxide by π-π stacking. Initially graphene oxide was synthesized by hummer's method and to obtain a more precise drug delivery, the system was loaded onto polyethylene glycol (PEG) decorated with folic acid. The resultant conjugate was characterized by Fourier Transform Infrared spectroscopy (FTIR), X-Ray Diffraction (XRD) analysis, UV-visible Spectrophotometery, Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The graphene-oxide -polyethylene glycol-folic acid - camptothecin (GO-PEG-FA -CPT) drug delivery system showed a pH dependent drug release as observed by UV analysis. The anticancer activity of the synthesized drug delivery system was studied by MTT assay using MCF-7 breast cancer cell lines. The conjugate showed enhanced anticancer activity and thus could be used as a potential candidate for drug delivery. 1. Introduction Cancer is a life threatening disease which leads to abnormal growth of cells with the `potential to invade other parts of the body. The major cause of cancer related deaths in economically developed countries are due to the adoption of lifestyle which includes physical inactivity, smoking, drinking, and westernized diets [1]. In the year 2010, Na- tional Institute of Health estimated 1.5 million cases of cancer were diagnosed in the United States alone [2]. Thus development of re- markable diagnostic and therapeutic tools for cancer is crucial as the mortality rate due to cancer has remained relatively stagnant. The presently available chemotherapeutic drugs are low molecular weight agents with high pharmacokinetic volume of distribution both of which contributes to their cytotoxicity. To overcome the ease excretion of these low molecular weight drugs a higher concentration is ultimately required which consequently leads to higher toxicity and unwanted side effects like hair loss, bone marrow suppressions etc [3]. These drugs lack specificity and cause significant damage to noncancerous cells. In this scenario nanomaterials could be good allies to give more specific cancer treatment effectively reducing undesirable side effects and ac- curate diagnosis and successful therapy. A variety of nanomaterials both organic and inorganic are used for biomedical applications. The commonly available nanoparticles involved in drug delivery are liposome mediated, dendimers, carbon nanotubes, gold nanoparticles etc. The drug delivery appropriateness of a nanoparticle is largely de- termined by the in vitro and in vivo biocompatibility, physiological stability, ability to internalize therapeutic agents and cellular uptake [4]. Allotropes of carbon viz. Carbon nano tubes (CNT), multiwalled carbon nanotbes (MWCNT), nanohorns, nanodiamonds and a newly developed allotrope of carbon “graphene” has gained tremendous at- tention in the scientific community due to its brilliant features. Func- tionalized form of CNT, MWCNT and graphene oxide (GO) has also been reported to be used in ultrasonography studies due to their hy- perecogonic properties [5]. In a study carried out by Pescatori et al., four different forms of functionalized CNT was used to examine its in- teraction with the immune system on the basis of innate and adaptive immune response produced by the host [6]. Graphene has a wide number of biomedical applications due to its large surface area, elec- trostatic interactions, thermal and electrical conductivity and easy functionalization due to the presence of π-π interaction [7]. The above mentioned features make graphene and its derivatives (graphene oxide, reduced graphene oxide) a potent candidate for drug and gene delivery. In a recent study conducted by Russier et al., a newly discovered form of graphene named as “few-layer graphene” (FLG) was used for treat- ment of myelomonocytic leukemia. FLG was reported to have a specific action on the cancerous cells without any visible side effects and https://doi.org/10.1016/j.jddst.2017.10.025 Received 24 April 2017; Received in revised form 30 October 2017; Accepted 31 October 2017 * Corresponding author. E-mail address: vimararagu@gmail.com (R. Vimala). Journal of Drug Delivery Science and Technology 43 (2018) 333–342 1773-2247/ © 2017 Elsevier B.V. All rights reserved. MARK