title: pH-responsive drug delivery of chitosan nanoparticles as Tamoxifen carriers for effective anti-tumor activity in breast cancer cells.
abstract: Tamoxifen (Tam) has a broad spectrum of anticancer activity, but is limited in clinical application. The aim of this study was to explore the smart pH-responsive drug delivery system (DDS) based on chitosan (CH) nanoparticles (NPs) for its potential in enabling more intelligent controlled release and enhancing chemotherapeutic efficiency of Tamoxifen. Tamoxifen was loaded onto CH-nanoparticles by forming complexes and Tamoxifen was released from the DDS much more rapidly at pH 4.0 and 6.0 than at pH 7.4, which is a desirable characteristic for tumor-targeted drug delivery. Tamoxifen-loaded CH nanoparticles induced remarkable improvement in anticancer activity, as demonstrated by MTT-assay, AO/EtBr and Hoechst nuclear staining. Furthermore, the possible signaling pathway was explored by RT-PCR. For instance, in human breast cancer MCF-7 cells, it was demonstrated that Tamoxifen-loaded CH nanoparticles increase intracellular concentration of Tamoxifen and enhance its anticancer efficiency by inducing apoptosis in a caspase-dependent manner, indicating that drug loaded nanoparticles could act as an efficient DDS importing Tamoxifen into target cancer cells.
authors.affiliation: Proteomics & Molecular Cell Physiology Laboratory, Department of Zoology, School of Life Sciences, Bharathiar University, Coimbatore 641046, TN, India.
authors.forename: R
authors.initials: R
authors.lastname: Vivek
authors.affiliation: Proteomics & Molecular Cell Physiology Laboratory, Department of Zoology, School of Life Sciences, Bharathiar University, Coimbatore 641046, TN, India.
authors.forename: V
authors.initials: V
authors.lastname: Nipun Babu
authors.affiliation: Proteomics & Molecular Cell Physiology Laboratory, Department of Zoology, School of Life Sciences, Bharathiar University, Coimbatore 641046, TN, India; Department of Virology, King Institute of Preventive Medicine & Research, Guindy, Chennai 600032, TN, India.
authors.forename: R
authors.initials: R
authors.lastname: Thangam
authors.affiliation: Department of Nano Science & Technology, Tamil Nadu Agricultural University, Coimbatore 641003, TN, India.
authors.forename: K S
authors.initials: KS
authors.lastname: Subramanian
authors.affiliation: Proteomics & Molecular Cell Physiology Laboratory, Department of Zoology, School of Life Sciences, Bharathiar University, Coimbatore 641046, TN, India. Electronic address: sk_protein@buc.edu.in.
authors.forename: S
authors.initials: S
authors.lastname: Kannan
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000473:pathology*; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004705:Endocytosis / Q000187:drug effects; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008027:Light; D061986:MCF-7 Cells; D008954:Models, Biological; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D012542:Scattering, Radiation; D055672:Static Electricity; D013629:Tamoxifen / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013629:Tamoxifen; D048271:Chitosan
keywords: Apoptosis; Drug delivery system; MCF-7 cells; Nanoparticles; Tamoxifen