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Chondroitin/doxorubicin nanoparticulate polyelectrolyte complex for targeted delivery to HepG2 cells
Authors:Jaleh Varshosaz  Hojjat Sadeghi aliabadi  Fereshte Asheghali
Affiliation:1. Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan Iran ; 2. Department of Biotechnology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan Iran
Abstract:Chondroitin (Chn) sulphate composed of N‐acetyl galactoseamine units was chosen to target doxorubicin (DOX) to asialoglycoprotein receptors (ASGPRs) overexpressed in HepG2 cells of hepatocellular carcinoma (HCC). Two different ways of targeting the drug to the receptors were compared with each other; (i) by polyelectrolyte complex formation of DOX and Chn (DC), (ii) by loading the drug in gelatin nanoparticles (NPs) and then coating them by Chn. The characteristics of DC complexes were determined by Fourier transform infrared spectroscopy, differential scanning calorimetry and CHN analysis. The complexes and Chn coated NPs were characterised for their particles size, zeta potential, drug loading and release efficiency. The morphology of NPs was studied by transmission electron microscopy. The cytotoxicity of DC complex and Chn coated NPs were compared on HepG2 cells by MTT assay. The results showed that the cytotoxicity of both Chn coated gelatin NPs and DC complexes were significantly increased in comparison with free DOX. However, the presence of Chn did not have significant effect on the cytotoxicity of DOX loaded NPs. It was concluded that polyelectrolyte complex of DC could successfully target the drug to the hepatic ASGPRs and may be a simple promising way for targeted drug delivery in HCC.Inspec keywords: drug delivery systems, drugs, polymer electrolytes, electrokinetic effects, nanoparticles, particle size, cellular biophysics, nanocomposites, nanofabrication, molecular biophysics, cancer, gelatin, coatings, Fourier transform infrared spectra, differential scanning calorimetry, filled polymers, transmission electron microscopy, toxicology, nanomedicine, biomedical materialsOther keywords: chondroitin‐doxorubicin nanoparticulate polyelectrolyte complex, HepG2 cells, N‐acetyl galactoseamine units, chondroitin sulphate, asialoglycoprotein receptors, hepatocellular carcinoma, drug targeted delivery, receptors, polyelectrolyte complex formation, gelatin nanoparticles, DC complexes, Fourier transform infrared spectroscopy, differential scanning calorimetry, CHN analysis, Chn coated NPs, particle size, zeta potential, drug loading, drug release efficiency, morphology, transmission electron microscopy, cytotoxicity, MTT assay, hepatic ASGPRs
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