Luteinizing hormone‐releasing hormone targeted poly(methyl vinyl ether maleic acid) nanoparticles for doxorubicin delivery to MCF‐7 breast cancer cells

The purpose of this study was to design a targeted anti‐cancer drug delivery system for breast cancer. Therefore, doxorubicin (DOX) loaded poly(methyl vinyl ether maleic acid) nanoparticles (NPs) were prepared by ionic cross‐linking method using Zn²⁺ ions. To optimise the effect of DOX/polymer ratio, Zn/polymer ratio, and stirrer rate a full factorial design was used and their effects on particle size, zeta potential, loading efficiency (LE, %), and release efficiency in 72 h (RE₇₂, %) were studied. Targeted NPs were prepared by chemical coating of tiptorelin/polyallylamin conjugate on the surface of NPs by using 1‐ethyl‐3‐(3‐dimethylaminopropyl) carboiimid HCl as cross‐linking agent. Conjugation efficiency was measured by Bradford assay. Conjugated triptorelin and targeted NPs were studied by Fourier‐transform infrared spectroscopy (FTIR). The cytotoxicity of DOX loaded in targeted NPs and non‐targeted ones were studied on MCF‐7 cells which overexpress luteinizing hormone‐releasing hormone (LHRH) receptors and SKOV3 cells as negative LHRH receptors using Thiazolyl blue tetrazolium bromide assay. The best results obtained from NPs prepared by DOX/polymer ratio of 5%, Zn/polymer ratio of 50%, and stirrer rate of 960 rpm. FTIR spectrum confirmed successful conjugation of triptorelin to NPs. The conjugation efficiency was about 70%. The targeted NPs showed significantly less IC₅₀ for MCF‐7 cells compared to free DOX and non‐targeted NPs.Inspec keywords: nanoparticles, polymer blends, cancer, cellular biophysics, drug delivery systems, drugs, biomedical materials, zinc, positive ions, Fourier transform infrared spectra, nanomedicine, proteinsOther keywords: luteinizing hormone‐releasing hormone, poly(methyl vinyl ether maleic acid), doxorubicin delivery, MCF‐7 breast cancer cell, anticancer drug delivery system, doxorubicin‐loaded PVM‐MA nanoparticle, ionic cross‐linking method, zinc ion, doxorubicin‐polymer ratio effect, zinc‐polymer ratio effect, particle size, zeta potential, loading efficiency, release efficiency, chemical coating, tiptorelin‐polyallylamin conjugation, PVM‐MA nanoparticle surface, 1‐ethyl‐3‐(3‐dimethylaminopropyl) carboiimid HCl, cross‐linking agent, Bradford assay, Fourier transform infrared spectroscopy, cytotoxicity, LHRH receptor, SKOV3 cell, Thiazolyl blue tetrazolium bromide assay, conjugation efficiency, time 72 h, Zn²⁺      

Facile synthesis by a covalent binding reaction for pH‐responsive drug release of carboxylated chitosan coated hollow mesoporous silica nanoparticles

In this study, a promising drug nano‐carrier system consisting of mono‐dispersed and pH sensitive carboxylated chitosan‐hollow mesoporous silica nanoparticles (Ccs‐HMSNs) suitable for the treatment of malignant cells was synthesised and investigated. At neutral pH, the Ccs molecules are orderly aggregated state, which could effectively hinder the release of loaded drug molecules. However, in slightly acidic environment, Ccs chains are heavily and flexibly entangled in gel state, which would enhance the subsequent controlled release of the loaded drug. Using doxorubicin hydrochloride (DOX•HCl) as the drug model, their results demonstrated that the system had an excellent loading efficiency (64.74 μg/mg Ccs‐HMSNs) and exhibited a pH‐sensitive release behaviour. Furthermore, confocal laser scanning microscopy revealed that the Ccs‐HMSNs nanocomposite could effectively deliver and release DOX•HCl to the nucleus of HeLa cells, thereby inducing apoptosis. In addition, MTT assay also confirmed that DOX•HCl loaded Ccs‐HMSNs (DOX•HCl@Ccs‐HMSNs) exhibited a good anticancer effect on HeLa cells with a time‐dependent manner. Finally, haemolysis experiment showed Ccs‐HMSNs had no haemolytic activity at all the tested concentrations (5–320 μg/mL). Thus, this biocompatible and effective nano‐carrier system will have potential applications in controllable drug delivery and cancer therapy.Inspec keywords: drug delivery systems, mesoporous materials, silicon compounds, nanoparticles, nanocomposites, nanofabrication, drugs, nanomedicine, biomedical materials, pH, aggregation, gels, optical microscopy, cellular biophysics, cancer, filled polymersOther keywords: facile synthesis, covalent binding reaction, pH‐responsive drug release, carboxylated chitosan coated hollow mesoporous silica nanoparticles, drug nanocarrier system, monodispersed carboxylated chitosan‐hollow mesoporous silica nanoparticles, pH sensitive carboxylated chitosan‐hollow mesoporous silica nanoparticles, malignant cell treatment, neutral pH, orderly aggregated state, loaded drug molecules, acidic environment, gel state, doxorubicin hydrochloride, drug model, confocal laser scanning microscopy, nanocomposite, HeLa cells, apoptosis, MTT assay, anticancer effect, haemolysis experiment, biocompatible nanocarrier system, drug delivery, cancer therapy, SiO₂      

Treatment of tumour tissue with radio‐frequency hyperthermia (using antibody‐carrying nanoparticles)

Intelligent inorganic nanoparticles were designed and produced for use in imaging and annihilating tumour cells by radio‐frequency (RF) hyperthermia. Nanoparticles synthesised to provide RF hyperthermia must have magnetite properties. For this purpose, magnetite nanoparticles were first synthesised by the coprecipitation method (10–15 NM). These superparamagnetic nanoparticles were then covered with gold ions without losing their magnetic properties. In this step, gold ions are reduced around the magnetite nanoparticles. Surface modification of the gold‐coated magnetic nanoparticles was performed in the next step. A self‐assembled monolayer was created using cysteamine (2‐aminoethanethiol) molecules, which have two different end groups (SH and NH₂). These molecules react with the gold surface by SH groups. The NH₂ groups give a positive charge to the nanoparticles. After that, a monoclonal antibody (Monoclonal Anti‐N‐CAM Clone NCAM‐OB11) was immobilised by the 1‐ethyl‐3‐(3‐dimethylaminopropyl)carbodiimide/N‐hydroxysuccinimide method. Then, the antenna RF system (144.00015 MHz) was created for RF hyperthermia. The antibody‐nanoparticle binding rate and cytotoxicity tests were followed by in vitro and in vivo experiments. As the main result, antibody‐bound gold‐coated magnetic nanoparticles were successfully connected to tumour cells. After RF hyperthermia, the tumour size decreased owing to apoptosis and necrosis of tumour cells.     

Co‐condensation synthesis of well‐defined mesoporous silica nanoparticles: effect of surface chemical modification on plasmid DNA condensation and transfection

Chemically modified mesoporous silica nanoparticles (MSNs) are of interest due to their chemical and thermal stability with adjustable morphology and porosity; therefore, it was aimed to develop and compare the MCM‐41 MSNs functionalised with imidazole groups (MCM‐41‐Im) to unmodified (MCM‐41‐OH) and primary amine functionalised (MCM‐41‐NH₂) MSNs for experimental gene delivery. The results show efficient transfection of the complexes of the plasmid and either MCM‐41‐NH₂ or MCM‐41‐Im. Furthermore, following transfection of HeLa cells using MCM‐41‐Im, an enhanced GFP expression was achieved consistent with the noticeable DNase1 protection and endosomal escape properties of MCM‐41‐Im using carboxyfluorescein tracer.Inspec keywords: condensation, mesoporous materials, silicon compounds, nanoparticles, DNA, surface chemistry, porosity, gene therapy, cellular biophysics, biomedical materials, nanomedicine, nanofabrication, molecular biophysics, biochemistryOther keywords: co‐condensation synthesis, surface chemical modification, plasmid DNA condensation, plasmid DNA transfection, chemical modified mesoporous silica nanoparticles, chemical stability, thermal stability, adjustable morphology, porosity, MCM‐41 MSN functionalisation, imidazole groups, MCM‐41‐OH, primary amine functionalised MSN, gene delivery, HeLa cell transfection, GFP expression, DNase1 protection, endosomal escape properties, carboxyfluorescein tracer, SiO₂      

Gold nanoparticles decorated reduced graphene oxide nanolabel for voltammetric immunosensing

This study describes the development and testing of a simple and novel enzyme‐free nanolabel for the detection and signal amplification in a sandwich immunoassay. Gold nanoparticles decorated reduced graphene oxide (rGOAu) was used as the nanolabel for the quantitative detection of human immunoglobulin G (HIgG). The rGOAu nanolabel was synthesised by one pot chemical reduction of graphene oxide and chloroauric acid using sodium borohydride. The pseudo‐peroxidase behaviour of rGOAu makes the nanolabel unique from other existing labels. The immunosensing platform was fabricated using self‐assembled monolayers of 11‐mercaptoundecanoic acid (11‐MUDA) on a gold disc electrode. The covalent immobilisation of antibody was achieved through the bonding of the carboxyl group of 11‐MUDA and the amino group of the antibody using chemical linkers [1‐ethyl‐3‐(3‐dimethylaminopropyl)carbodiimide] and N ‐hydroxysuccinimide. The fabricated immunosensor exhibited a linear range that included HIgG concentrations of 62.5–500 ng ml⁻¹. The sensor was also used for the testing of HIgG in the blood sample.Inspec keywords: proteins, nanomedicine, reduction (chemical), chemical sensors, nanofabrication, electrochemical sensors, voltammetry (chemical analysis), gold, oxidation, self‐assembly, monolayers, molecular biophysics, biochemistry, biosensors, nanoparticles, nanosensors, blood, grapheneOther keywords: gold nanoparticles, voltammetric immunosensing, enzyme‐free nanolabel, signal amplification, sandwich immunoassay, human immunoglobulin G, rGOAu nanolabel, chloroauric acid, sodium borohydride, 11‐mercaptoundecanoic acid, 11‐MUDA, gold disc electrode, chemical linkers, 1‐ethyl‐3‐(3‐dimethylaminopropyl)carbodiimide], HIgG concentrations, reduced graphene oxide nanolabel, quantitative HIgG detection, one pot chemical reduction, covalent antibody immobilisation, carboxyl group bonding, pseudo‐peroxidase behaviour, self‐assembled monolayers, N‐hydroxysuccinimide, immunosensor, blood sample, Au‐CO     

Facile synthesis of mesoporous alumina using hexadecyltrimethylammonium bromide (HTAB) as template: simplified sol‐gel approach

Herein the authors present the synthesis of surface functionalised mesoporous alumina (MeAl) for textural characterisation by a simplified sol–gel method obtained by using hexadecyltrimethylammonium bromide as a template. Etoricoxib (ETOX) was used as a model drug for the study. Alumina supported mesoporous material containing drug was characterised using instrumental technique namely Brunauer–Emmett–Teller surface area, Fourier transform‐infrared, differential scanning calorimetry, transmission electron microscopy, X‐ray diffraction, and field emission scanning electron microscopy. Diffusion study using a dialysis bag method used to check the release pattern of ETOX‐loaded‐MeAl. Results of characterisation study revealed the successful surface functionalisation of the drug on nanocomposite. The IC₅₀ value obtained from cell viability study demonstrated the non‐toxic behaviour of synthesised drug‐loaded mesoporous alumina up to the tested concentration range. The present work has demonstrated that synthesised MeAl showed excellent stability with an expanded surface area suitable for carrier material for drug delivery system.Inspec keywords: Fourier transform spectra, adsorption, biomedical materials, silicon compounds, drug delivery systems, X‐ray diffraction, alumina, differential scanning calorimetry, nanocomposites, field emission electron microscopy, nanofabrication, nanomedicine, mesoporous materials, transmission electron microscopy, sol‐gel processing, scanning electron microscopyOther keywords: ETOX‐loaded‐MeAl, successful surface functionalisation, synthesised drug‐loaded mesoporous alumina, synthesised MeAl, expanded surface area, drug delivery system, hexadecyltrimethylammonium bromide, sol‐gel approach, surface functionalised mesoporous alumina, simplified sol–gel method, mesoporous material containing drug, Brunauer–Emmett–Teller surface area, Fourier transform‐infrared, differential scanning calorimetry, transmission electron microscopy, X‐ray diffraction, field emission scanning electron microscopy, dialysis bag method     

Synthesis and characterisation of iron oxide nanoparticles conjugated with epidermal growth factor receptor (EGFR) monoclonal antibody as MRI contrast agent for cancer detection

The aim of this study is to synthesise superparamagnetic iron oxide nanoparticles conjugated with anti‐epidermal growth factor receptor monoclonal antibody (ANTI‐EGFR‐SPION) and investigate its physicochemical characterisation and biocompatibility as a targeted magnetic resonance imaging (MRI) contrast agent for the EGFR‐specific detection in EGFR expressing tumour cells. These particles employed biocompatible polymers, poly(D,L‐lactide‐co‐glycolide) (PLGA) and polyethylene glycol aldehyde (PEG‐aldehyde), to increase the half‐life of particles in circulation and reduce their side effects. The Fe₃ O₄ ‐loaded PLGA‐PEG‐aldehyde nanoparticles were prepared by a modified water‐in‐oil‐in‐water double emulsion method. The EGFR antibody was conjugated to the surface of SPIONs using the aldehyde‐amine reaction. Synthesised conjugates (nanoprobes) were characterised using Fourier transform infrared spectrophotometry, dynamic light scattering, transmission electron microscopy images, and vibrating‐sample magnetometery, and the results showed that the conjugation was successful. The mean diameter of nanoprobes was about 25 nm. These nanoprobes exhibited excellent water‐solubility, stability, and biocompatibility. Meanwhile, MR susceptibility test proved that synthesised nanoprobes can be managed for negative contrast enhancement. The results of this study suggested the potential use of these nanoprobes for non‐invasive molecular MRI in EGFR detection in the future.Inspec keywords: solubility, nanomedicine, cancer, spectrophotometry, emulsions, biomedical MRI, nanomagnetics, nanofabrication, tumours, nanoparticles, magnetic particles, molecular biophysics, light scattering, proteins, cellular biophysics, Fourier transform spectra, superparamagnetism, polymers, transmission electron microscopy, iron compoundsOther keywords: physicochemical characterisation, superparamagnetic iron oxide nanoparticles, novel targeting cancer detection, anti‐epidermal growth factor receptor monoclonal antibody, ANTI‐EGFR‐SPION, biocompatibility, targeted magnetic resonance imaging contrast agent, EGFR‐specific detection, EGFR expressing tumour cells, biocompatible polymers, PLGA‐PEG‐aldehyde nanoparticles, modified water‐in‐oil‐in‐water double emulsion method, EGFR antibody, aldehyde‐amine reaction, synthesised conjugates were characterised using Fourier, transmission electron microscopy images, synthesised nanoprobes, EGFR detection, size 25.0 nm, Fe₃ O₄      

Enhanced stability of L‐asparaginase by its bioconjugation to poly(styrene‐co‐maleic acid) and Ecoflex nanoparticles

Acute lymphoblastic leukemia (ALL) is the white blood cell cancer in children. L‐asparaginase (L‐ASNase) is one of the first drugs used in ALL treatment. Anti‐tumor activity of L‐ASNase is not specific and indicates limited stability in different biological environments, in addition to its quick clearance from blood. The purpose of the present study was to achieve a new L‐ASNase polymer bioconjugate to improve pharmacokinetic, increase half‐life and stability of the enzyme. The conjugations were achieved by the cross‐linking agent of 1‐ethyl‐3‐(3‐ dimethylaminopropyl) carbodiimide (EDC) which activates the carboxylic acid groups of polymeric nanoparticles to create amide bond. EDC conjugated the L‐ASNase to two biodegradable polymers including; Ecoflex^® and poly (styrene‐co‐maleic acid) (PSMA) nanoparticles. To achieve optimal L‐ASNase nanoparticles the amounts of each polymer and the crosslinker were optimized and the nanoparticles were characterized according to their particle size, zeta potential and percent of conjugation of the enzyme. The results showed that conjugated enzyme had more stability against pH changes and proteolysis. It had lower Km value (indicating more affinity to the substrate) and greater half‐life in plasma and phosphate buffered saline, in comparison to native enzyme. Generally, the conjugated enzyme to PSMA nanoparticles showed greater results than Ecoflex^® nanoparticles.Inspec keywords: enzymes, polymer blends, nanomedicine, biomedical materials, blood, nanoparticles, cancer, molecular biophysics, molecular configurations, biochemistry, conducting polymers, electrokinetic effects, particle size, bonds (chemical), biodegradable materials, pHOther keywords: enhanced stability, L‐asparaginase, bioconjugation, poly(styrene‐co‐maleic acid), Ecoflex nanoparticles, acute lymphoblastic leukaemia, white blood cell cancer, children, drugs, ALL treatment, antitumour activity, biological environments, L‐ASNase polymer bioconjugate, pharmacokinetic, enzyme, crosslinking agent, amide bond, 1‐ethyl‐3‐(3‐dimethylaminopropyl) carbodiimide, carboxylic acid groups, polymeric nanoparticles, EDC conjugation, biodegradable polymers, PSMA nanoparticles, optimal L‐ASNase nanoparticles, particle size, zeta potential, pH changes, proteolysis, native enzyme, conjugated enzyme     

Sialic acid‐conjugated PLGA nanoparticles enhance the protective effect of lycopene in chemotherapeutic drug‐induced kidney injury

Lycopene (LYC) is known to protect cells from oxidative damage caused by free radicals in human tissues. In the present study, the authors designed a LYC‐loaded sialic acid (SA)‐conjugated poly(D,L‐lactide‐co‐glycolide) (PLGA) nanoparticle (LYC‐NP) to enhance the therapeutic efficacy of LYC in acute kidney injury. The characteristics of the LYC‐NPs were defined according to particle size, morphology, and in vitro drug release. The LYC‐NPs exhibited a controlled release of LYC over 48 h. Confocal laser scanning microscopy clearly highlighted the targeting potential of SA. Enhanced green fluorescence was observed for the LYC‐NPs in H₂ O₂ ‐treated human umbilical vein endothelial cells, indicating enhanced internalisation of NPs. The LYC‐NPs showed significantly greater cell viability than H₂ O₂ ‐treated cells. In addition, the LYC‐NPs remarkably reduced proinflammatory cytokine levels, attributable mainly to the increased cellular internalisation of the SA‐based carrier delivery system. Furthermore, protein levels of caspase‐3 and ‐9 were significantly down‐regulated after treatment with the LYC‐NPs. Overall, they have demonstrated that SA‐conjugated PLGA‐NPs containing LYC could be used to treat kidney injury.Inspec keywords: fluorescence, biomedical materials, biological tissues, cellular biophysics, drugs, proteins, molecular biophysics, injuries, drug delivery systems, kidney, nanomedicine, biochemistry, optical microscopy, nanoparticles, nanofabrication, cancer, toxicology, blood vessels, particle sizeOther keywords: sialic acid‐conjugated PLGA nanoparticles, chemotherapeutic drug‐induced kidney injury, LYC‐NP, LYC‐loaded sialic acid‐conjugated poly(D,L‐lactide‐co‐glycolide) nanoparticle, SA‐conjugated PLGA‐NP, protective effect, lycopene, human tissues, particle size, in vitro drug release, confocal laser scanning microscopy, green fluorescence, human umbilical vein endothelial cells, cell viability, proinflammatory cytokine levels, cellular internalisation, SA‐based carrier delivery system, time 48.0 hour     

Facile synthesis of multi‐walled carbon nanotube via folic acid grafted nanoparticle for precise delivery of doxorubicin

The motive of work was to develop a multi‐walled carbon nanoplatform through facile method for transportation of potential anticancer drug doxorubicin (DOX). Folic acid (FA)‐ethylene diamine (EDA) anchored and acid functionalised MWCNTs were covalently grafted with DOX via π–π stacking interaction. The resultant composite was corroborated by ¹ H NMR, FTIR, XRD, EDX, SEM, and DSC study. The drug entrapment efficiency of FA‐conjugated MWCNT was found high and stability study revealed its suitability in biological system. FA‐EDA‐MWCNTs‐DOX conjugate demonstrated a significant in vitro anticancer activity on human breast cancer MCF‐7 cells. MTT study revealed the lesser cytotoxicity of folate‐conjugated MWCNTs. The obtained results demonstrated the targeting specificity of FA‐conjugate via overexpressed folate receptor deemed greater scientific value to overcome multidrug protection during cancer therapy. The proposed strategy is a gentle contribution towards development of biocompatible targeted drug delivery and offers potential to address the current challenges in cancer therapy.Inspec keywords: toxicology, nanoparticles, biomedical materials, scanning electron microscopy, drug delivery systems, nanofabrication, nanomedicine, nanocomposites, cellular biophysics, cancer, drugs, multi‐wall carbon nanotubes, Fourier transform infrared spectra, X‐ray chemical analysis, differential scanning calorimetry, proton magnetic resonance, organic compoundsOther keywords: facile synthesis, multiwalled carbon nanotube, precise delivery, multiwalled carbon nanoplatform, drug entrapment efficiency, FA‐conjugated MWCNT, stability study, biological system, human breast cancer MCF‐7 cells, MTT study, folate‐conjugated MWCNTs, overexpressed folate receptor, cancer therapy, biocompatible targeted drug delivery, anticancer drug doxorubicin, π‐π stacking interaction, composite material, ¹ H NMR, in vitro anticancer activity, folic acid grafted nanoparticle, folic acid‐ethylene diamine, acid functionalised MWCNT, FTIR spectra, XRD, EDX, SEM, FA‐EDA‐MWCNT‐DOX conjugate, cytotoxicity, DSC, C     

In vivo study of anti‐epidermal growth factor receptor antibody‐based iron oxide nanoparticles (anti‐EGFR‐SPIONs) as a novel MR imaging contrast agent for lung cancer (LLC1) cells detection

Superparamagnetic iron oxide nanoparticles (SPIONs) conjugated with anti‐epidermal growth factor receptor monoclonal antibody (anti‐EGFR‐SPIONs) were characterised, and its cytotoxicity effects, ex vivo and in vivo studies on Lewis lung carcinoma (LLC1) cells in C57BL/6 mice were investigated. The broadband at 679.96 cm⁻¹ relates to Fe–O, which verified the formation of the anti‐EGFR‐Mab with SPIONs was obtained by the FTIR. The TEM images showed spherical shape 20 and 80 nm‐sized for nanoparticles and the anti‐EGFR‐SPIONs, respectively. Results of cell viability at 24 h after incubation with different concentrations of nanoprobe showed it has only a 20% reduction in cell viabilities. The synthesised nanoprobe administered by systemic injection into C57BL/6 mice showed good Fe tumour uptake and satisfied image signal intensity under ex vivo and in vivo conditions. A higher concentration of nanoprobe was achieved compared to non‐specific and control, indicating selective delivery of nanoprobe to the tumour. It is concluded that the anti‐EGFR‐SPIONs was found to be as an MR imaging contrast nanoagent for lung cancer (LLC1) cells detection.Inspec keywords: toxicology, biomedical MRI, lung, magnetic particles, biomedical materials, nanofabrication, nanomagnetics, transmission electron microscopy, nanomedicine, superparamagnetism, nanoparticles, iron compounds, proteins, cellular biophysics, molecular biophysics, cancer, tumours, Fourier transform infrared spectraOther keywords: MR imaging contrast agent, LLC1, superparamagnetic iron oxide nanoparticles, Lewis lung carcinoma cells, ex vivo conditions, cell viability, antiepidermal growth factor receptor antibody‐based iron oxide nanoparticles, antiEGFR‐SPION, lung cancer cell detection, antiepidermal growth factor receptor monoclonal antibody, cytotoxicity effects, C57BL‐6 mice, antiEGFR‐Mab, FTIR spectra, TEM, spherical shape, incubation, nanoprobe concentrations, systemic injection, Fe tumour uptake, image signal intensity, in vivo conditions, time 24.0 hour, Fe₃ O₄      

Honokiol–camptothecin loaded graphene oxide nanoparticle towards combinatorial anti‐cancer drug delivery

Honokiol (HK) is a natural product isolated from the bark, cones, seeds and leaves of plants belonging to the genus Magnolia. It possesses anti‐cancer activity which can efficiently impede the growth and bring about apoptosis of a diversity of cancer cells. The major concerns of using HK are its poor solubility and lack of targeted drug delivery. In this study, a combinatorial drug is prepared by combining HK and camptothecin (CPT). Both CPT and HK belong to the Magnolian genus and induce apoptosis by cell cycle arrest at the S‐phase and G1 phase, respectively. The combinatorial drug thus synthesised was loaded onto a chitosan functionalised graphene oxide nanoparticles, predecorated with folic acid for site‐specific drug delivery. The CPT drug‐loaded nanocarrier was characterised by X‐ray diffractometer, scanning electron microscope, transmission electron microscope, UV–vis spectroscopy and fluorescence spectroscopy, atomic force microscopy. The antioxidant properties, haemolytic activity and anti‐inflammatory activities were analysed. The cellular toxicity was analysed by 3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐Diphenyltetrazolium Bromide (MTT assay) and Sulforhodamine B (SRB) assay against breast cancer (MCF‐7) cell lines.Inspec keywords: nanofabrication, cancer, nanoparticles, atomic force microscopy, graphene, scanning electron microscopy, cellular biophysics, toxicology, transmission electron microscopy, drug delivery systems, nanomedicine, tumours, solubilityOther keywords: targeted drug delivery, combinatorial drug, Magnolian genus, apoptosis, cell cycle, chitosan functionalised graphene oxide nanoparticles, site‐specific drug delivery, CPT drug‐loaded nanocarrier, transmission electron microscope, fluorescence spectroscopy, haemolytic activity, antiinflammatory activities, breast cancer cell lines, honokiol–camptothecin loaded graphene oxide nanoparticle, combinatorial anti‐cancer drug delivery, natural product, genus Magnolia, anticancer activity, cancer cells     

Synthesis,characterisation and potential biomedical applications of magnetic core–shell structures: carbon‐, dextran‐, SiO2 ‐ and ZnO‐coated Fe3 O4 nanoparticles

Due to the strong effect of nanoparticles'' size and surface properties on cellular uptake and bio‐distribution, the selection of coating material for magnetic core–shell nanoparticles (CSNPs) is very important. In this study, the effects of four different biocompatible coating materials on the physical properties of Fe₃ O₄ (magnetite) nanoparticles (NPs) for different biomedical applications are investigated and compared. In this regard, magnetite NPs are prepared by a simple co‐precipitation method. Then, CSNPs including Fe₃ O₄ as a core and carbon, dextran, ZnO (zincite) and SiO₂ (silica) as different shells are synthesised using simple one‐ or two‐step methods. A comprehensive study is carried out on the prepared samples using X‐ray diffraction, vibrating sample magnetometry, transmission electron microscopy and Fourier transform infrared spectroscopy analyses. According to the authors'' findings, it is suggested that carbon‐ and dextran‐coated magnetite NPs with high M _s have great potential in the application of magnetic resonance imaging contrast agents. Moreover, silica‐coated magnetite NPs with high coercivity are potentially suitable candidates for hyperthermia and ZnO‐coated Fe₃ O₄ is potentially suitable for photothermal therapy.Inspec keywords: iron compounds, carbon, silicon compounds, zinc compounds, nanomedicine, biomedical materials, nanofabrication, nanoparticles, magnetic particles, coatings, X‐ray diffraction, magnetometry, transmission electron microscopy, Fourier transform spectra, infrared spectra, biomedical MRI, hyperthermia, radiation therapyOther keywords: biomedical applications, magnetic core‐shell nanoparticles, CSNP, cellular uptake, biodistribution, coating material, biocompatible coating materials, co‐precipitation, dextran, zincite, silica, X‐ray diffraction, vibrating sample magnetometry, transmission electron microscopy, Fourier transform infrared spectroscopy, magnetic resonance imaging contrast agents, hyperthermia, photothermal therapy, SiO₂ ‐Fe₃ O₄ , ZnO‐Fe₃ O₄      

Synthesis of biotin‐targeted chitosan/poly (methyl vinyl ether‐alt ‐maleic acid) copolymeric micelles for delivery of doxorubicin

Biotinylated chitosan/poly(methyl vinyl ether‐alt ‐maleic acid) (PMVEMA) copolymer was synthesised by an amide reaction in two steps. Structural characterisation was performed using ¹ HNMR and Fourier transform infra‐red (FTIR) spectra. Critical micelle concentration (CMC) of the copolymer was determined by pyrene as a fluorescent probe. Doxorubicin (DOX) was loaded in the micelles by the direct dissolution method. The effects of different variables including type of copolymer, copolymer concentration, stirring rate and stirring time were studied on the physicochemical properties of the micelles including: particle size, zeta potential, release efficiency and loading efficiency of nanoparticles using an irregular factorial design. The in vitro cytotoxicity of DOX‐loaded biotin‐targeted micelles was studied in HepG2 cells which over express biotin receptors by 3, 5‐[dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay. The successful synthesis of the biotinylated copolymer of chitosan/PMVEMA was confirmed by FTIR and ¹ HNMR. The optimised micelles showed the CMC of 33 μg/ml, particle size of 247 ± 2 nm, zeta potential of +9.46 mV, polydispersity index of 0.22, drug‐loading efficiency of 71% and release efficiency of 84.5 ± 1.6%. The synthesised copolymer was not cytotoxic. The cytotoxicity of DOX‐loaded in targeted micelles on HepG2 cell line was about 2.2‐fold compared with free drug.Inspec keywords: biomedical materials, cellular biophysics, dissolving, drug delivery systems, drugs, electrokinetic effects, fluorescence, Fourier transform infrared spectra, particle size, polymer blends, spectrochemical analysis, toxicologyOther keywords: ¹ HNMR spectra, biotin‐targeted chitosan‐poly (methyl vinyl ether‐alt‐maleic acid) copolymeric micelles, doxorubicin delivery, amide reaction, structural characterisation, Fourier transform infrared spectra, pyrene, fluorescent probe, direct dissolution method, physicochemical properties, particle size, zeta potential, nanoparticles, irregular factorial design, in vitro cytotoxicity, DOX‐loaded biotin‐targeted micelles, 3, 5‐[dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay, polydispersity index, drug‐loading efficiency, HepG2 cell line, voltage 9.46 mV     

Catalytic hydrolysis of cellobiose using different acid‐functionalised Fe3 O4 magnetic nanoparticles

The present study demonstrated the preparation of three different acid‐functionalised magnetic nanoparticles (MNPs) and evaluation for their catalytic efficacy in hydrolysis of cellobiose. Initially, iron oxide (Fe₃ O₄)MNPs were synthesised, which further modified by applying silica coating (Fe₃ O₄ ‐MNPs@Si) and functionalised with alkylsulfonic acid (Fe₃ O₄ ‐MNPs@Si@AS), butylcarboxylic acid (Fe₃ O₄ ‐MNPs@Si@BCOOH) and sulphonic acid (Fe₃ O₄ ‐MNPs@Si@SO₃ H) groups. The Fourier transform infrared analysis confirmed the presence of above‐mentioned acid functional groups on MNPs. Similarly, X‐ray diffraction pattern and energy dispersive X‐ray spectroscopy analysis confirmed the crystalline nature and elemental composition of MNPs, respectively. TEM micrographs showed the synthesis of spherical and polydispersed nanoparticles having diameter size in the range of 20–80 nm. Cellobiose hydrolysis was used as a model reaction to evaluate the catalytic efficacy of acid‐functionalised nanoparticles. A maximum 74.8% cellobiose conversion was reported in case of Fe₃ O₄ ‐MNPs@Si@SO₃ H in first cycle of hydrolysis. Moreover, thus used acid‐functionalised MNPs were magnetically separated and reused. In second cycle of hydrolysis, Fe₃ O₄ ‐MNPs@Si@SO₃ H showed 49.8% cellobiose conversion followed by Fe₃ O₄ ‐MNPs@Si@AS (45%) and Fe₃ O₄ ‐MNPs@Si@BCOOH (18.3%). However, similar pattern was reported in case of third cycle of hydrolysis. The proposed approach is considered as rapid and convenient. Moreover, reuse of acid‐functionalised MNPs makes the process economically viable.Inspec keywords: scanning electron microscopy, catalysis, magnetic separation, magnetic particles, silicon compounds, iron compounds, nanomagnetics, coatings, X‐ray chemical analysis, nanoparticles, X‐ray diffraction, nanofabrication, Fourier transform infrared spectra, organic compounds, nanocompositesOther keywords: catalytic efficacy, alkylsulfonic acid, butylcarboxylic acid, energy dispersive X‐ray spectroscopy analysis, spherical polydispersed nanoparticles, cellobiose hydrolysis, acid‐functionalised MNPs, acid functional groups, cellobiose conversion, acid‐functionalised magnetic nanoparticle, silica coating, sulphonic acid, Fourier transform infrared analysis, SEM micrograph, X‐ray diffraction pattern, size 20.0 nm to 80.0 nm, Fe₃ O₄ , Si, SiO₂      

Fluorescein isothiocyanate‐dyed mesoporous silica nanoparticles for tracking antioxidant delivery

This study investigated the cellular uptake of fluorescein isothiocyanate‐labelled mesoporous silica nanoparticles (FITC‐MSNs), amine‐functionalised FITC‐MSNs (AP‐FITC‐MSNs) and their gallic acid (GA)‐loaded counterparts. Mesoporous silica nanoparticles were labelled with fluorescein isothiocyanate, functionalised by 3‐aminopropyltriethoxysilane (APTES) (AP‐FITC‐MSNs) and then loaded by GA. All nanoparticles were characterised by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy, and X‐ray diffraction. The cytotoxicity of different concentrations of dyed nanoparticles was investigated using (3‐(4,5‐trihydroxybenzoic acid, dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) assay and flow cytometry. TEM images showed that the average particle sizes of FITC‐MSNs and AP‐FITC‐MSNs were about 100 and 110 nm, respectively. These nanoparticles were internalised by Caco‐2 cells, accumulated and dispersed into the cytoplasm, nucleus, and subcellular organelles. Nanoparticles containing GA clearly decreased the viability of cells. FITC‐MSNs showed no toxicity on Caco‐2 cells at concentrations of ≤50 µg/ml. Functionalisation of FITC‐MSNs using APTES decreased toxicity effects on the cells. It was found that FITC‐MSNs can be applied at low concentrations as a marker in the cells. In addition, AP‐FITC‐MSNs showed better biocompatibility with Caco‐2 cells than FITC‐MSNs, because of their positive surface charges.Inspec keywords: mesoporous materials, porosity, nanoparticles, dyes, silicon compounds, nanocomposites, nanofabrication, nanomedicine, cellular biophysics, molecular biophysics, biochemistry, transmission electron microscopy, Fourier transform infrared spectra, X‐ray diffraction, toxicology, particle size, biomedical materials, surface charging, cancerOther keywords: fluorescein isothiocyanate‐dyed mesoporous silica nanoparticles, antioxidant delivery tracking, cellular uptake, amine‐functionalised FITC‐MSNs, gallic acid‐loaded counterparts, 3‐aminopropyltriethoxysilane, transmission electron microscopy, TEM, Fourier transform infrared spectroscopy, X‐ray diffraction, cytotoxicity, dyed nanoparticles, (3‐(4,5‐trihydroxybenzoic acid‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) assay, flow cytometry, particle sizes, AP‐FITC‐MSNs, Caco‐2 cells, cytoplasm, subcellular organelles, cell viability, biocompatibility, positive surface charges, SiO₂      

Synthesis of porous GdF3 :Er3+, Yb3+ –COOH core–shell structured bi‐functional nanoparticles for drug delivery

The authors synthesised porous GdF₃ :Er³⁺, Yb³⁺ –COOH core–shell structured bi‐functional nanoparticles through a one‐step hydrothermal route during which ethylene diamine tetraacetic acid) was bound to the surface of the nanoparticles. It has high up‐conversion emission intensity for monitoring the drug release process and magnetisation saturation value (10.2 emu/g) for drug targeting under foreign magnetic fields. Moreover, porous GdF₃ :Er³⁺, Yb³⁺ as drug carriers with a high drug‐loading efficiency. cis‐Dichlorodiammineplatinum(II) (cisplatin, CDDP)‐loaded GdF₃ :Er³⁺, Yb³⁺ nanoparticles (GdF₃ :Er³⁺, Yb³⁺ –CDDP) were characterised by the Fourier transform infrared spectra, and CDDP was loaded in the form of electrostatic interaction and hydrogen bonds. Compared with CDDP alone, GdF₃ :Er³⁺, Yb³⁺ –CDDP nanoparticles increase concentration of CDDP in the target site and enhance its anticancer efficiency. Therefore, the as‐prepared GdF₃ :Er³⁺, Yb³⁺ –COOH nanoparticles allow simultaneous targeted drug delivery and monitoring as promising anti‐cancer theranostic agents.Inspec keywords: gadolinium compounds, erbium, ytterbium, organic compounds, nanoporous materials, core‐shell nanostructures, drug delivery systems, Fourier transform infrared spectra, electrostatics, hydrogen bonds, magnetisation, nanofabrication, nanomedicine, spectrochemical analysisOther keywords: porous core–shell structured bifunctional nanoparticles, drug delivery, one‐step hydrothermal route, ethylene diamine tetraacetic acid, magnetisation saturation value, up‐conversion emission intensity, cis‐Dichlorodiammineplatinum(II), Fourier transform infrared spectra, electrostatic interaction, hydrogen bonds, anticancer theranostic agents     

Production of a new platform based on fumed and mesoporous silica nanoparticles for enhanced solubility and oral bioavailability of raloxifene HCl

The purpose of the present study was to compare mesoporous and fumed silica nanoparticles (NPs) to enhance the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RH). Mesoporous silica NPs (MSNs) and fumed silica NPs were used by freeze‐drying or spray‐drying methods. MSNs were obtained with different ratios of cetyltrimethylammonium bromide. Saturation solubility of the NPs was compared with the pure drug. The optimised formulation was characterised by scanning electron microscopy (SEM), X‐ray diffraction (XRD) and differential scanning calorimetry. The pharmacokinetic studies were done by oral administration of a single dose of 15 mg/kg of pure drug or fumed silica NPs of RH in Wistar rats. MSNs enhanced the solubility of RH from 19.88 ± 0.12 to 76.5 μg/ml. Freeze‐dried fumed silica increased the solubility of the drug more than MSNs (140.17 ± 0.45 μg/ml). However, the spray‐dried fumed silica caused about 26‐fold enhancement in its solubility (525.7 ± 93.5 μg/ml). Increasing the ratio of silica NPs enhanced the drug solubility. The results of XRD and SEM analyses displayed RH were in the amorphous state in the NPs. Oral bioavailability of NPs showed 3.5‐fold increase compared to the pure drug. The RH loaded fumed silica NPs prepared by spray‐drying technique could more enhance the solubility and oral bioavailability of RH.Inspec keywords: differential scanning calorimetry, mesoporous materials, freezing, nanofabrication, drug delivery systems, silicon compounds, drying, drugs, solubility, spraying, X‐ray diffraction, biomedical materials, scanning electron microscopy, nanoparticles, biochemistry, amorphous state, nanomedicineOther keywords: freeze‐dried fumed silica, spray‐dried, drug solubility, spray‐drying technique, fumed silica nanoparticles, mesoporous silica nanoparticles, aqueous solubility, mesoporous silica NPs, freeze‐drying, saturation solubility, differential scanning calorimetry, oral administration, fumed silica NPs     

HSA loaded with CoFe2 O4 /MNPs as a high‐efficiency carrier for epirubicin anticancer drug delivery

Drug delivery is one of the most important challenges in the domain of health. Non‐toxic and biocompatible carriers are provided by human serum albumin nano‐capsule (HSA/NC) for drug delivery applications. In this study, HSA, with high loadings of drug‐modified cobalt ferrite (CoFe₂ O₄) magnetic nanoparticle (CoFe₂ O₄ /MNPs) was fabricated for epirubicin anticancer drug delivery. In the initial step, CoFe₂ O₄ /MNPs was synthesised via co‐precipitation technique and characterised by X‐ray powder diffraction, vibrating sample magnetometry, energy dispersive X‐ray analysis, scanning electron microscopy and map analysis. Furthermore, CoFe₂ O₄ /MNPs and epirubicin were loaded into HSA/NC and utilised as a novel system against breast cancer cell line (MCF‐7). IC₅₀ for free epirubicin, unloaded CoFe₂ O₄ /MNPs/HSA/NC, CoFe₂ O₄ /MNPs and epirubicin‐loaded CoFe₂ O₄ /MNPs/HSA/NC were 7.7, 2400, 840 and 430 μg/ml, respectively. The results obtained revealed high cytotoxicity effect of epirubicin‐loaded CoFe₂ O₄ /MNPs on breast cancer cell line.Inspec keywords: drug delivery systems, biomedical materials, nanoparticles, cobalt compounds, ferrites, nanomedicine, proteins, molecular biophysics, drugs, magnetic particles, nanomagnetics, nanofabrication, precipitation (physical chemistry), X‐ray diffraction, X‐ray chemical analysis, scanning electron microscopy, cancer, cellular biophysics, toxicology, magnetic hysteresisOther keywords: HSA, high‐efficiency carrier, epirubicin anticancer drug delivery, human serum albumin nanocapsule, drug‐modified cobalt ferrite magnetic nanoparticle, coprecipitation technique, X‐ray powder diffraction, vibrating sample magnetometry, energy dispersive X‐ray analysis, scanning electron microscopy, map analysis, breast cancer cell line, cytotoxicity effect, CoFe₂ O₄