DOI: 10.5061/dryad.k8j74
title: Data from: Niclosamide loaded biodegradable chitosan nanocargoes: an in vitro study for potential application in cancer therapy

description: Chitosan nanoparticles can advance the pharmacological and therapeutic
 properties of chemotherapeutic agents by controlling release rates and
 targeted delivery process, which eliminates the limitations of
 conventional anti-cancer therapies and they are also safe as well as
 cost-effective. The aim of present study is to explore the anti-tumour
 effect of niclosamide in lung and breast cancer cell lines using
 biocompatible and biodegradable carrier where nanoparticles loaded with
 hydrophobic drug (niclosamide) were synthesized, characterized and applied
 as a stable anti-cancer agent. Niclosamide loaded chitosan nanoparticles
 (Nic-Chi Np's) of size approximately 100–120 nm in diameter
 containing hydrophobic anti-cancer drug, i.e. niclosamide, were prepared.
 Physico-chemical characterization confirms that the prepared nanoparticles
 are spherical, monodispersed and stable in aqueous systems. The
 therapeutic efficacy of Nic-Chi Np's was evaluated against breast
 cancer cell line (MCF-7) and human lung cancer cell line (A549). MTT assay
 reveals the cell viability of the prepared Nic-Chi Np's against A549
 and MCF-7 cells and obtained an IC50 value of 8.75 µM and 7.5 µM,
 respectively. Acridine orange/ethidium bromide dual staining results
 verified the loss of the majority of the cells by apoptosis. Flow
 cytometer analysis quantified the generation of intracellular reactive
 oxygen species (ROS) and signified that exposure to a higher concentration
 (2 × IC50) of Nic-Chi Np's resulted in elevated ROS generation.
 Notably, Nic-Chi Np treatment showed more apoptosis and cell death in
 MCF-7 as compared to A549. Further, the remarkable induction of apoptosis
 by Nic-Chi Np's was confirmed by semi-quantitative reverse
 transcription polymerase chain reaction, scanning electron microscopy and
 cell-cycle analysis. Thus, Nic-Chi Np's may have a great potential
 even at low concentration for anti-cancer therapy and may replace or
 substitute more toxic anti-mitotic drugs in the near future.
description: Dynamic light scattering
 experimentFigure S1. Dynamic light
 scattering experiment showing size and size distribution of void chitosan
 nanoparticles (VCN).Figure
 _ESM1.tifZeta potential on the
 void chitosan nanoparticles (VCN).Figure S2. Zeta
 potential on the void chitosan nanoparticles (VCN).Figure
 _ESM2.tifEDAX spectrum and
 elemental compositionFig. S3 EDAX spectrum
 and elemental composition of Nic@Chi Np’sFigure
 _ESM3.tifFE-SEM image of Nic@Chi
 Np’s and colour coded SEM/EDX dot maps after incubation of Nic@Chi Np’s in
 cancer cells.Figure S4. FE-SEM image
 of Nic@Chi Np’s and colour coded SEM/EDX dot maps after incubation of
 Nic@Chi Np’s in cancer cells. (A) Overlay FE-SEM image depicting elemental
 distributions in Nic@Chi Np’s after internalization into cancer cells.
 (a-d): Individual elemental distribution (red for carbon, dark green for
 Oxygen, olive green for nitrogen and indigo for chlorine ). (B) Elemental
 Spectrum of Nic@Chi Np’s.Figure
 _ESM4.tifAFM image of niclosamide
 loaded chitosan nanoparticles.Figure S5. AFM image of
 niclosamide loaded chitosan nanoparticles.Figure
 _ESM5.tifFTIR spectra of (a)
 Nic@Chi Np’s, (b) Chitosan nanoparticles (void), (c) Niclosamide drug
 alone.Figure S6. FTIR spectra
 of (a) Nic@Chi Np’s, (b) Chitosan nanoparticles (void), (c) Niclosamide
 drug alone.Figure
 _ESM6.tifForward and reverse
 primer sequences for various apoptotic signaling genes.Table S1. Forward and
 reverse primer sequences for various apoptotic signaling
 genes.Table
 _ESM1.tif