Abstract
Hesperidin is a flavonoid glycoside with proven therapeutic activities for various diseases, including cancer. However, its poor solubility and bioavailability render it only slightly absorbed, requiring a delivery system to reach its therapeutic target. Hesperidin loaded on gold nanoparticles (Hsp-AuNPs) was prepared by a chemical synthesis method. Various characterization techniques such as UV-VIS spectroscopy, FTIR, XRD, FESEM, TEM and EDX, Zeta potential analysis, particle size analysis, were used to confirm the synthesis of Hsp-AuNPs. The cytotoxic effect of Hsp-AuNPs on human breast cancer cell line (MDA-MB-231) was assessed using MTT and crystal violet assays. The results revealed significant decrease in proliferation and inhibition of growth of the treated cells when compared with human normal breast epithelial cell line (HBL-100). Determination of apoptosis by fluorescence microscope was also performed using acridine orange-propidium iodide dual staining assay. The in vivo study was designed to evaluate the toxicity of Hsp-AuNPs in mice. The levels of hepatic and kidney functionality markers were assessed. No significant statistical differences were found for the tested indicators. Histological images of liver, spleen, lung and kidney showed no apparent damages and histopathological abnormalities after treatment with Hsp-AuNPs. Hsp-AuNPs ameliorated the functional activity of macrophages against Ehrlich ascites tumor cells-bearing mice. The production of the pro-inflammatory cytokines was also assessed in bone marrow–derived macrophage cells treated with Hsp-AuNPs. The results obviously demonstrated that Hsp-AuNPs treatment significantly inhibited the secretion of IL-1β, IL-6 and TNF.
Highlights
Hesperidin is a flavonoid glycoside with proven therapeutic activities for various diseases, including cancer
In our previous study we introduced a new method to enhance the drug’s efficiency, solubility, biocompatibility and cytotoxic effects on human breast MCF-7 cancer cells by synthesizing hesperidin encapsulated PLGA nanoparticles
Our findings suggest that hesperidin can be employed in the treatment of cancer, since it showed higher cytotoxic effects to tumor cells when it was conjugated to AuNPs
Summary
Hesperidin is a flavonoid glycoside with proven therapeutic activities for various diseases, including cancer. The unique characteristics of gold nanoparticle (AuNPs), along with their multiple surface functionalities, enhanced their broad applications in the field of bionanotechnology, as drug-delivery systems since NPs are biocompatible and possess a surface are that is sufficiently high to load more elevated concentration of the delivered drug or even several drugs on one particle[10] Through their role as drug carriers, gold NPs reportedly achieved superior results over the traditional cancer treatment, with continuously growing research on the best methods for their development and applications[11]. In our previous study we introduced a new method to enhance the drug’s efficiency, solubility, biocompatibility and cytotoxic effects on human breast MCF-7 cancer cells by synthesizing hesperidin encapsulated PLGA nanoparticles Such models need to deliver the drug to the targeted tissue using a highly active system, which can be based on a variety of biomaterials including the biodegradable nanoparticles. The cytotoxic potentials against human triple –negative breast cancer cell line MDA-MB-231 were determined
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