HER‐2 aptamer‐targeted Ecoflex® nanoparticles loaded with docetaxel promote breast cancer cells apoptosis and anti‐metastatic effect

Breast cancer is a major cause of cancer mortality. Regarding the advantages of polymeric nanoparticles as drug delivery systems with targeting potential, in this study the antitumor mechanism of targeted docetaxel polymeric nanoparticles of Ecoflex^® was exploited. Since the overexpression of HER‐2 receptor in breast cancer cases is associated with poor prognosis and more aggressive disease, the proposed nanoparticles were conjugated to HER‐2 specific aptamer molecules. In vitro cytotoxicity was evaluated by MTT assay. Flow‐cytometry analysis was performed to evaluate the cellular uptake of nanoparticles loaded with a fluorescent probe. Anti‐migration effects of samples were studied. Annexin IV‐FITC and propidium iodide were implemented to investigate apoptosis induction and cell cycle analysis. Enhanced cytotoxicity compared with free docetaxel was explained considering improved cellular uptake of the nanoparticles and induced apoptosis in a larger portion of cells. Lower relative migration demonstrated enhanced anti‐migration effect of nanoparticles, and cell cycle was arrested in G2/M phase using both formulations so the anti‐microtubule mechanism of the drug was not altered. Therefore, this system could offer a potential substitute for the currently marketed docetaxel formulations, which may reduce adverse effects of the drug, while further in vivo and clinical investigations are required.Inspec keywords: cancer, molecular biophysics, drug delivery systems, fluorescence, biomedical materials, drugs, tumours, nanomedicine, proteins, toxicology, biochemistry, nanoparticles, diseases, cell motility, polymersOther keywords: antitumor mechanism, targeted docetaxel polymeric nanoparticles, HER‐2 specific aptamer molecules, MTT assay, flow‐cytometry analysis, annexin IV‐FITC, apoptosis induction, cell cycle, lower relative migration, cancer mortality, drug delivery systems, aggressive disease, in vitro cytotoxicity, cellular uptake, breast cancer cell apoptosis, antimetastatic effect, HER‐2 aptamer‐targeted Ecoflex nanoparticles, antimigration effect, antimicrotubule mechanism, HER‐2 receptor, fluorescent probe, propidium iodide     

Green synthesis of silver nanoparticles using Rubia tinctorum extract and evaluation the anti‐cancer properties in vitro

Cancer is one of the leading causes of human death. Nanotechnology could offer new and optimised anticancer agents in order to fight cancer. It was shown that metal nanoparticles, in particular silver nanoparticles (AgNPs) were effective in cancer therapy. In this study, AgNPs were synthesised using Rubia tinctorum L. extract (Ru‐AgNPs). Then, cytotoxicity effects of the Ru‐AgNPs against MDA‐MB‐231 carcinoma cell line and human dermal fibroblast as normal cell line were performed. Furthermore, anti‐apoptotic effects of Ru‐AgNPs on these cancer and normal cell lines were compared using acridine orange/propidium iodide staining, flow cytometry analysis and real‐time qPCR in apoptosis gene markers. Results of UV‐vis spectroscopy showed that Ru‐AgNPs have a peak at 430 nm, which indicated synthesis of AgNPs. Ru‐AgNPs had spherical shape and average size of 12 nm. Ru‐AgNPs have cytotoxicity on MDA‐MB‐231 cells and decrease cancerous cell viability (IC50 = 4 µg/ml/48 h). Ru‐AgNPs could induce apoptosis in MDA‐MB‐231 cells through upregulation of Bax and downregulation of Bcl‐2 gene expression. The results opened up new avenues to develop Rubia based metal complexes as an anticancer agent.Inspec keywords: cellular biophysics, genetics, cancer, toxicology, nanoparticles, nanofabrication, nanomedicine, silver, biomedical materials, ultraviolet spectra, visible spectraOther keywords: Ru‐AgNPs, MDA‐MB‐231 carcinoma cell line, normal cell line, cancerous cell viability, in vitro anticancer properties, green synthesis, silver nanoparticles, Rubia tinctorum L. extract, cytotoxicity effects, human dermal fibroblast HFF, antiapoptotic effects, acridine orange‐propidium iodide staining, flow cytometry analysis, real‐time qPCR, apoptosis gene markers, UV‐visible spectroscopy, spherical shape, Bcl‐2 gene expression, Ag     

Synthesis of surfactant‐modified ZIF‐8 with controllable microstructures and their drug loading and sustained release behaviour

Metal‐organic frameworks (MOFs) as drug carriers have many advantages than traditional drug carriers and have received extensive attention from researchers. However, how to regulate the microstructure of MOFs to improve the efficiency of drug delivery and sustained release behaviour is still a big problem for the clinical application. Herein, the authors synthesise surfactant‐modified ZIF‐8 nanoparticles with different microstructures by using different types of surfactants to modify ZIF‐8. The surfactant‐modified ZIF‐8 nanoparticles have the larger specific surface area and total micropore volumes than the original ZIF‐8, which enables doxorubicin (DOX) to be more effectively loaded on the drug carriers and achieve controlled drug sustained release. Excellent degradation performance of ZIF‐8 nanoparticles facilitates the metabolism of drug carriers. The formulation was evaluated for cytotoxicity, cellular uptake and intracellular location in the A549 human non‐small‐cell lung cancer cell line. ZIF‐8/DOX nano drugs exhibit higher cytotoxicity towards cells in comparison with free DOX, suggesting the potential application in nano drugs to cancer chemotherapy.Inspec keywords: nanomedicine, lung, nanofabrication, drug delivery systems, cellular biophysics, nanoparticles, cancer, toxicology, biomedical materials, drugs, organometallic compounds, surfactants, porosity, biodegradable materialsOther keywords: controlled drug sustained release, nanodrugs, controllable microstructures, drug loading, metal‐organic frameworks, traditional drug carriers, drug delivery, surfactant‐modified ZIF‐8 nanoparticles, specific surface area, micropore volumes, doxorubicin, degradation performance, metabolism, cytotoxicity, cellular uptake, intracellular location, A549 human nonsmall‐cell lung cancer cell line, cancer chemotherapy     

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     

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⁺      

Enhancement of in vitro antitumour activity of epirubicin in HER2+ breast cancer cells using immunoliposome formulation

Epirubicin (EPI) is one of the potent breast cancer (BC) chemotherapeutic agents, but its adverse effects limit its efficacy. Herein, EPI was selected to be loaded in liposomal carrier, which has been targeted by a monoclonal antibody, Herceptin. The preparation process of liposomes was a modified ethanol injection method followed by Herceptin conjugation. The in vitro cell toxicity and cellular uptake of optimum formulation against HER2+ and HER2− cancer cell lines were evaluated. The results showed that the drug loading (DL%) and encapsulation efficiency (EE%) of liposome preparation method yielded 30.62% ± 0.49% and 62.39% ± 8.75%, respectively. The average size of naked liposomes (EPI‐Lipo) and immunoliposomes (EPI‐Lipo‐mAb) was 234 ± 9.86 and 257.26 ± 6.25 nm, with a relatively monodisperse distribution, which was confirmed by SEM micrographs. The release kinetic followed Higuchi model for both naked and immunoliposomes. In vitro cytotoxicity study on three different BC cell lines including BT‐20, MDA‐MB‐453 and MCF‐7 demonstrated higher toxicity of EPI in the Herceptin conjugated form (EPI‐Lipo‐mAb) in comparison with the free EPI and EPI‐Lipo in HER2 overexpressing cell line. In addition, the cellular uptake study showed a higher uptake of immunoliposomes by MCF‐7 cells in comparison with naked liposomes. In conclusion, these data show that the targeted delivery of EPI to breast cancer cells can be achieved by EPI‐Lipo‐mAb in vitro, and this strategy could be used for breast cancer therapy with further studies.     

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     

Characterisation of sol–gel method synthesised MgZnFe2 O4 nanoparticles and its cytotoxic effects on breast cancer cell line,MDA MB‐231 in vitro

In this study, nanocrystalline magnesium zinc ferrite nanoparticles were successfully prepared by a simple sol–gel method using copper nitrate and ferric nitrate as raw materials. The calcined samples were characterised by differential thermal analysis/thermogravimetric analysis, Fourier transform infrared spectroscopy and X‐ray diffraction. Transmission electron microscopy revealed that the average particle size of the calcined sample was in a range of 17–41 nm with an average of 29 nm and has spherical size. A cytotoxicity test was performed on human breast cancer cells (MDA MB‐231) and (MCF‐7) at various concentrations starting from (0 µg/ml) to (800 µg/ml). The sample possessed a mild toxic effect toward MDA MB‐231 and MCF‐7 after being examined with MTT (3‐[4, 5‐dimethylthiazol‐2‐yl]‐2, 5 diphenyltetrazolium bromide) assay for up to 72 h of incubation. Higher reduction of cells viability was observed as the concentration of sample was increased in MDA MB‐231 cell line than in MCF‐7. Therefore, further cytotoxicity tests were performed on MDA MB‐231 cell line.Inspec keywords: sol‐gel processing, nanoparticles, nanofabrication, magnesium compounds, zinc compounds, toxicology, biological organs, cancer, cellular biophysics, nanomedicine, calcination, differential thermal analysis, Fourier transform infrared spectra, X‐ray diffraction, transmission electron microscopy, particle size, organic compoundsOther keywords: sol‐gel method, cytotoxic effects, breast cancer cell line, MDA MB‐231 in vitro, nanocrystalline magnesium zinc ferrite nanoparticles, copper nitrate, ferric nitrate, raw materials, calcined samples, differential thermal analysis, thermogravimetric analysis, Fourier transform infrared spectroscopy, X‐ray diffraction, transmission electron microscopy, average particle size, cytotoxicity testing, human breast cancer cells, mild toxic effect, 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5 diphenyltetrazolium bromide) assay, cell viability, MCF‐7, MDA MB‐231 cell line, size 17 nm to 41 nm     

CdO nanoparticles,c‐MWCNT nanoparticles and CdO nanoparticles/c‐MWCNT nanocomposite fibres: in vitro assessment of anti‐proliferative and apoptotic studies in HeLa cancer cell line

A simple ultrasonic assisted chemical technique was used to synthesise cadmium oxide (CdO) nanoparticles (NPs) and CdO NPs/c‐Multiwalled carbon nanotube (c‐MWCNT) nanocomposite fibres.To confirm the physio‐chemico properties and to analyse surface morphology of the obtained nanomaterials X‐Ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR) and field emission scanning electron microscopy (FESEM) were performed. To evaluate the anti‐cancer property of CdO NPs, c‐MWCNT NPs and CdO NPs/c‐MWCNT nanocomposite fibres, an anti‐proliferative assay test (Methylthiazolyl diphenyl‐ tetrazolium bromide ‐ MTT assay) were performed on HeLa cells which further estimated IC50 value (Least concentration of sample in which nearly 50% of cells remain alive) under in‐vitro conditions. On comparison, CdONPs/c‐MWCNT based system was found to be superior by achieving 52.3% cell viability with its minimal IC50 value of 31.2 μg/ml. Lastly, the CdO NPs based system was taken up for an apoptotic study using DNA fragmentation assay for estimating its ability to cleave the DNA of the HeLa cells into internucleosomal fragments using the agarose gel electrophoresis method. In conclusion, based on our observations, CdO NPs/c‐MWCNT hybrid based system can be further used for the development of efficient drug delivery and therapeutic systems.Inspec keywords: drug delivery systems, electrophoresis, oxidation, toxicology, DNA, nanoparticles, drugs, field emission electron microscopy, scanning electron microscopy, nanofabrication, surface morphology, cancer, X‐ray diffraction, nanomedicine, cellular biophysics, filled polymers, biomedical materials, molecular biophysics, biochemistry, Fourier transform infrared spectra, multi‐wall carbon nanotubesOther keywords: c‐MWCNT nanoparticles, apoptotic study, HeLa cancer cell line, cadmium oxide nanoparticles, c‐MWCNT NPs, anti‐proliferative assay test [methyl thiazolyl diphenyl‐tetrazolium bromide assay], human epithelioid cervix carcinoma cells, live cells, CdO NP‐based system, IC50 concentration, HeLa cell line, cell deaths, CdO‐C     

Lobelia trigona Roxb ‐based nanomedicine with enhanced biological applications: in vitro and in vivo approach

This is the first study to report the green synthesis of Lobelia trigona Roxb‐ mediated silver nanoparticles (LTAgNPs). The optical and structural properties of the synthesised LTAgNPs were analysed using ultraviolet–visible spectroscopy, scanning electron microscopy, Fourier transform infrared, dynamic light scattering and energy dispersive X‐ray. LTAgNps were evaluated for their anti‐bacterial and anti‐fungal properties against 18 pathogens and exhibited significant inhibition against all the strains tested. LTAgNPs had potential scavenging effects on the DPPH, ^• OH, O₂ ^•− free radical scavenging assays and reducing power assay. LTAgNps possess strong anti‐cancer activity against five human cancer cell lines (A549, MCF‐7, MDA‐MB‐231, HeLa and KB) in a dose‐dependent manner. The antiproliferative, anti‐inflammatory and genotoxicity effects of LTAgNPs were further confirmed by the lactate dehydrogenase release assay, nitric oxide inhibitory assay and comet assay. Furthermore, the incision, excision and burn wound‐healing activity of formulated LTAgNPs ointment was assessed in rats. All the wounds had significant healing in groups treated with LTAgNPs ointment compared to the groups treated with the commonly prescribed ointment (Silverex^TM). This study shows and suggests that the previously unreported LTAgNPs could be used as a nanomedicine with significant biological applications.Inspec keywords: molecular biophysics, biomedical materials, scanning electron microscopy, biochemistry, cancer, microorganisms, silver, cellular biophysics, nanofabrication, wounds, nanomedicine, ultraviolet spectra, toxicology, antibacterial activity, light scattering, nanoparticles, enzymes, visible spectra, Fourier transform infrared spectraOther keywords: Lobelia trigona Roxb‐based nanomedicine, biological applications, Lobelia trigona Roxb‐mediated silver nanoparticles, optical properties, structural properties, ultraviolet‐visible spectroscopy, dynamic light scattering, antibacterial properties, antifungal properties, scavenging effects, free radical scavenging, power assay, anticancer activity, antiinflammatory effects, genotoxicity effects, lactate dehydrogenase release assay, nitric oxide inhibitory assay, excision, burn wound‐healing activity, formulated LTAgNPs ointment, in vivo approach, in vitro approach, scanning electron microscopy, Fourier transform infrared spectroscopy, energy dispersive X‐ray analysis, pathogens, strains, A549 human cancer cell lines, MCF‐7 human cancer cell lines, MDA‐MB‐231 human cancer cell lines, HeLa human cancer cell lines, antiproliferative effects, comet assay, Ag     

Bio‐green synthesis ZnO‐NPs in Brassica napus pollen extract: biosynthesis,antioxidant, cytotoxicity and pro‐apoptotic properties

The bio‐green methods of synthesis nanoparticles (NPs) have advantages over chemo‐physical procedures due to cost‐effective and ecofriendly products. The goal of current investigation is biosynthesis of zinc oxide NPs (ZnO‐NPs) and evaluation of their biological assessment. Water extract of Brassica napus pollen [rapeseed (RP)] prepared and used for the synthesis of ZnO‐NPs and synthesised ZnO‐NP characterised using ultraviolet–visible, X‐ray diffraction, Fourier‐transform infrared spectroscopy, field emission scanning electron microscope and transmission electron microscope. Antioxidant properties of ZnO‐NPs, cytotoxic and pro‐apoptotic potentials of NPs were also evaluated. The results showed that ZnO‐NPs have a hexagonal shape with 26 nm size. ZnO‐NPs synthesised in RP (RP/ZnO‐NPs) exhibited the good antioxidant potential compared with the butylated hydroxyanisole as a positive control. These NPs showed the cytotoxic effects against breast cancer cells (M.D. Anderson‐Metastasis Breast cancer (MDA‐MB)) with IC₅₀ about 1, 6 and 6 μg/ml after 24, 48 and 72 h of exposure, respectively. RP/ZnO‐NPs were found effective in increasing the expression of catalase enzyme, the enzyme involved in antioxidants properties of the cells. Bio‐green synthesised RP/ZnO‐NPs showed antioxidant and cytotoxic properties. The results of the present study support the advantages of using the bio‐green procedure for the synthesis of NPs as an antioxidant and as anti‐cancer agents.Inspec keywords: II‐VI semiconductors, wide band gap semiconductors, ultraviolet spectra, toxicology, X‐ray diffraction, biochemistry, zinc compounds, nanomedicine, enzymes, biomedical materials, particle size, antibacterial activity, transmission electron microscopy, molecular biophysics, visible spectra, nanofabrication, cellular biophysics, nanoparticles, cancer, field emission scanning electron microscopy, Fourier transform infrared spectra, semiconductor growthOther keywords: bio‐green synthesis ZnO‐NPs, zinc oxide NPs, synthesised ZnO‐NP, field emission scanning electron microscope, transmission electron microscope, antioxidant properties, bio‐green synthesised RP‐ZnO‐NPs, Fourier‐transform infrared spectroscopy, X‐ray diffraction, breast cancer cells MDA‐MB, pro‐apoptotic potentials, cytotoxic effects, catalase enzyme, bio‐green procedure, time 48.0 hour, time 72.0 hour, size 26.0 nm, time 24.0 hour, ZnO     

Folate encapsulation in PEG‐diamine grafted mesoporous Fe3 O4 nanoparticles for hyperthermia and in vitro assessment

Effective and targeted delivery of the antitumour drugs towards the specific cancer spot is the major motive of drug delivery. In this direction, suitably functionalised magnetic iron oxide nanoparticles (NPs) have been utilised as a theranostic agent for imaging, hyperthermia and drug delivery applications. Herein, the authors reported the preparation of multifunctional polyethyleneglycol‐diamine functionalised mesoporous superparamagnetic iron oxide NPs (SPION) prepared by a facile solvothermal method for biomedical applications. To endow targeting ability towards tumour site, folic acid (FA) is attached to the amine groups which are present on the NPs surface by 1‐ethyl‐3‐(3‐dimethylaminopropyl) carbodiimide hydrochloride/N‐hydroxysuccinimide chemistry. FA attached SPION shows good colloidal stability and possesses high drug‐loading efficiency of ∼ 96% owing to its mesoporous nature and the electrostatic attachment of daunosamine (NH₃ ⁺) group of doxorubicin (DOX) towards the negative surface charge of carboxyl and hydroxyl group. The NPs possess superior magnetic properties in result endowed with high hyperthermic ability under alternating magnetic field reaching the hyperthermic temperature of 43°C within 223 s at NP''s concentration of 1 mg/ml. The functionalised NPs possess non‐appreciable toxicity in breast cancer cells (MCF‐7) which is triggered under DOX‐loaded SPION.Inspec keywords: nanoparticles, nanocomposites, mesoporous materials, colloids, biochemistry, nanomagnetics, molecular biophysics, tumours, superparamagnetism, drugs, toxicology, biomedical materials, nanofabrication, hyperthermia, cancer, magnetic particles, cellular biophysics, nanomedicine, iron compounds, drug delivery systems, filled polymers, biological organs, liquid phase depositionOther keywords: NP surface, colloidal stability, drug‐loading efficiency, hydroxyl group, magnetic properties, high hyperthermic ability, magnetic field, DOX‐loaded SPION, folate encapsulation, targeted delivery, antitumour drugs, specific cancer spot, magnetic iron oxide nanoparticles, theranostic agent, drug delivery applications, multifunctional polyethyleneglycol‐diamine, facile solvothermal method, biomedical applications, tumour site, amine groups, mesoporous superparamagnetic nanoparticles, PEG‐diamine grafted mesoporous nanoparticles, 1‐ethyl‐3‐(3‐dimethylaminopropyl) carbodiimide hydrochloride‐N‐hydroxysuccinimide chemistry, daunosamine group, carboxyl group, breast cancer cells, temperature 43.0 degC, Fe₃ O₄      

Investigation of chitosan‐g‐PEG grafted nanoparticles as a half‐life enhancer carrier for tissue plasminogen activator delivery

Tissue plasminogen activator (tPA) a thrombolytic agent is commonly used for digesting the blood clot. tPA half‐life is low (4–6 min) and its administration needs a prolonged continuous infusion. Improving tPA half‐life could reduce enzyme dosage and enhance patient compliance. Nano‐carries could be used as delivery systems for the protection of enzymes physically, enhancing half‐life and increasing the stability of them. In this study, chitosan (CS) and polyethylene glycol (PEG) were used for the preparation of CS‐g‐PEG/tPA nanoparticles (NPs) via the ion gelation method. Particles’ size and loading capacity were optimised by central composite design. Then, NPs cytotoxicity, release profile, enzyme activity and in vivo half‐life and coagulation time were investigated. The results showed that NPs does not have significant cytotoxicity. Release study revealed that a burst effect happened in the first 5 min and resulted in releasing 30% of tPA. Loading tPA in NPs could decrease 25% of its activity but the half‐life of it increases in comparison to free tPA in vivo. Also, blood coagulation time has significantly affected (p ‐value = 0.041) by encapsulated tPA in comparison to free tPA. So, CS‐g‐PEG/tPA could increase enzyme half‐life during the time and could be used as a non‐toxic candidate delivery system for tPA.Inspec keywords: drug delivery systems, nanofabrication, drugs, nanomedicine, coagulation, biomedical materials, cellular biophysics, enzymes, biochemistry, toxicology, molecular biophysics, biological tissues, blood, nanoparticles, polymersOther keywords: chitosan‐g‐PEG grafted nanoparticles, half‐life enhancer carrier, tissue plasminogen activator delivery, tPA half‐life, prolonged continuous infusion, enzyme dosage, polyethylene glycol, cytotoxicity, enzyme activity, encapsulated tPA, enzyme half‐life, blood coagulation, time 5.0 min     

Structural and physicochemical properties of Rheum emodi mediated Mg(OH)2 nanoparticles and their antibacterial and cytotoxic potential

In the present investigation, Rheum emodi roots extract mediated magnesium hydroxide nanoparticles [Mg(OH)₂ NPs] through the bio‐inspired experimental technique were synthesised. Mg(OH)₂ NPs were characterised by using various characterisation techniques such as field emission scanning electron microscopy, transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and ultraviolet–visible spectroscopy. The formation of Mg(OH)₂ NPs was confirmed by X‐ray diffraction. The structural analysis confirmed the hexagonal crystal symmetry of Mg(OH)₂ NPs with space group P‐3m1 and space group no. 164 using the Rietveld refinement technique. TEM micrographs illustrated the nano‐size formation of Mg(OH)₂ NPs of spherical shape and size ∼14.86 nm. With the aid of FTIR data, plant metabolites such as anthraquinones have been identified as a stabilising and reducing agent for the synthesis of biogenic Mg(OH)₂ NPs. The synthesised Mg(OH)₂ NPs showed antimicrobial and cytotoxic potential against Gram‐negative and Gram‐positive bacteria such as Escherichia coli (ATCC 25922) and Staphylococcus aureus (ATCC 25923) and MDA‐MB‐231 human breast cancer cell lines.Inspec keywords: antibacterial activity, microorganisms, visible spectra, cancer, X‐ray diffraction, cellular biophysics, nanomedicine, ultraviolet spectra, nanoparticles, transmission electron microscopy, nanofabrication, field emission scanning electron microscopy, Fourier transform infrared spectra, particle size, magnesium compounds, space groups, toxicologyOther keywords: physicochemical properties, structural properties, Rheum emodi root extract mediated magnesium hydroxide nanoparticles, bio‐inspired experimental technique, field emission scanning electron microscopy, transmission electron microscopy, TEM, Fourier transform infrared spectroscopy, FTIR spectroscopy, ultraviolet‐visible spectroscopy, X‐ray diffraction, hexagonal crystal symmetry, space group P‐3m1, space group no. 164, Rietveld refinement technique, nanosize formation, plant metabolites, spherical shape, antibacterial potential, cytotoxic potential, reducing agent, anthraquinones, stabilising agent, Gram‐positive bacteria, Gram‐negative bacteria, Escherichia coli, Staphylococcus aureus, MDA‐MB‐231 human breast cancer cell lines, Mg(OH)₂      

Atorvastatin lipid nanocapsules and gold nanoparticles embedded in injectable thermo‐gelling hydrogel scaffold containing adipose tissue extracellular matrix for myocardial tissue regeneration

This study aimed to prepare, optimise, and characterise the novel hybrid hydrogel scaffold containing atorvastatin lipid nanocapsules (LNCs) and gold nanoparticles (NPs) to improve cardiomyoblasts proliferation and regeneration of myocardium. A thermo‐responsive aminated guaran (AGG) hydrogel was prepared to encompass extracellular matrix (ECM) fetched from human adipose tissue. Emulsion phase‐inversion technique was used to obtain LNCs. Biocompatibility, tensile strength, conductivity, and proliferation of human myocardial cells of the optimised formulation were studied. The LNCs have a spherical shape, and the optimised formulation showed a mean particle size of 18.79 nm, the zeta potential of − 11.4 mV, drug loading of 99.99%, and release efficiency percent over 72 h was 18.73%. The injectable thermo‐sensitive hydrogel prepared using 1 w/v% of AGG, 35 w/w% of ECM, ∼0.5 mg/ml of gold NPs and atorvastatin loaded LNCs showed the best physical characteristics. The hybrid scaffold loaded with atorvastatin and gold NPs improved the proliferation of cardiomyoblasts more than sevenfold with enhanced cell attachment to the scaffold. The tensile strength and the conductivity of the scaffold were 300 kPa and 0.14 S/m, respectively. Injectable hybrid adipose tissue prepared by ECM and AGG hydrogel loaded with atorvastatin and gold NPs showed promising physical characteristics for myocardial tissue engineering.Inspec keywords: biological tissues, nanoparticles, tensile strength, electrokinetic effects, particle size, nanomedicine, emulsions, biomedical materials, cellular biophysics, nanofabrication, drugs, drug delivery systems, molecular biophysics, tissue engineering, hydrogels, goldOther keywords: Au, cardiomyoblast, hybrid hydrogel scaffold, myocardial tissue engineering, AGG hydrogel, injectable hybrid adipose tissue, atorvastatin loaded LNCs, gold NPs, thermo‐sensitive hydrogel, drug loading, human myocardial cells, tensile strength, emulsion phase‐inversion technique, human adipose tissue, ECM, thermo‐responsive aminated guaran hydrogel, cardiomyoblasts proliferation, atorvastatin lipid nanocapsules, myocardial tissue regeneration, adipose tissue extracellular matrix, thermo‐gelling hydrogel scaffold, gold nanoparticles     

Cytotoxicity of biologically synthesised bismuth nanoparticles against HT‐29 cell line

This study was purposed to examine the cytotoxicity and functions of biologically synthesised bismuth nanoparticles (Bi NPs) produced by Delftia sp. SFG on human colon adenocarcinoma cell line of HT‐29. The structural properties of Bi NPs were investigated using transmission electron microscopy, energy dispersive X‐ray, and X‐ray diffraction techniques. The cytotoxic effects of Bi NPs were analysed using flow cytometry cell apoptosis while western blot analyses were applied to analyse the cleaved caspase‐3 expression. Oxidative stress (OS) damage was determined using the measurement of the glutathione (GSH) and malondialdehyde (MDA) levels and antioxidant activity of superoxide dismutase (SOD) and catalase (CAT) levels. The half maximal inhibitory concentration (IC₅₀) value of Bi NPs was measured to be 28.7 ± 1.4 µg/ml on HT‐29 cell line. The viability of HT‐29 represented a concentration‐dependent pattern (5–80 µg/ml). The mode of Bi NPs induced apoptosis was found to be mainly related to late apoptosis or necrosis at IC₅₀ concentration, without the effect on caspase‐3 activities. Furthermore, Bi NPs reduced the GSH and increased the MDA levels and decreased the SOD and CAT activities. Taken together, biogenic Bi NPs induced cytotoxicity on HT‐29 cell line through the activation of late apoptosis independent of caspase pathway and may enhance the OS biomarkers.Inspec keywords: bismuth, nanoparticles, cellular biophysics, toxicology, nanomedicine, cancer, transmission electron microscopy, X‐ray chemical analysis, X‐ray diffraction, enzymes, biochemistryOther keywords: cytotoxicity, biologically synthesised bismuth nanoparticles, HT‐29 cell line, Delftia sp. SFG, human colon adenocarcinoma cell line, structural properties, transmission electron microscopy, energy dispersive X‐ray techniques, X‐ray diffraction, cytotoxic effects, flow cytometry cell apoptosis, western blot analyses, cleaved caspase‐3 expression, oxidative stress damage, glutathione, malondialdehyde, antioxidant activity, superoxide dismutase, catalase level, half maximal inhibitory concentration, cell viability, concentration‐dependent pattern, apoptosis, MDA levels, caspase pathway, Bi     

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,physicochemical characterisation and biological activity of anandamide/ɛ‐polycaprolactone nanoparticles obtained by electrospraying

Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this study, the authors’ work aimed to highlight the use of electrospraying techniques for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavourable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. The authors characterised physicochemically and evaluated in vitro biological activity of anandamide/ɛ‐polycaprolactone nanoparticles (Nps‐AEA/PCL) obtained by electrospraying in epithelial cells of the human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps‐AEA/PCL. They obtained particles from 100 to 900 nm of diameter with a predominance of 200–400 nm. Their zeta potential was −20 ± 1.86 mV. They demonstrated the stable encapsulation of AEA in Nps‐AEA/PCL, as well as its dose‐dependent capacity to induce the expression of iNOS and NO levels and to decrease the Na⁺ /K⁺ ATPase activity in HK2 cells. Obtaining Nps‐AEA/PCL by electrospraying would represent a promising methodology for a novel AEA pharmaceutical formulation development with optimal physicochemical properties, physical stability and biological activity on HK2 cells.Inspec keywords: cellular biophysics, molecular biophysics, nanoparticles, nanofabrication, biochemistry, encapsulation, drugs, neurophysiology, electrokinetic effects, enzymes, biomedical materials, nanomedicine, polymers, sprayingOther keywords: electrospraying techniques, pharmacological effects, pharmacokinetic properties, in vitro biological activity, biological effect, HK2 cells, optimal physicochemical properties, polymeric nanoparticles, AEA pharmaceutical formulation development, anandamide‐ε‐polycaprolactone nanoparticles, drug encapsulation, nanocarriers, endocannabinoid, central nervous system, epithelial cells, human proximal tubule, zeta potential, stable encapsulation, dose‐dependent capacity, Na⁺ ‐K⁺ ATPase activity, physical stability, size 100.0 nm to 900.0 nm, NO, Na⁺ ‐K⁺      

Surface‐functionalised hybrid nanoparticles for targeted treatment of cancer

Cancer is a leading cause of death worldwide. Despite the great advancement in understanding the pharmacology and biology of cancer, it still signifies one of the most serious human‐health related problems. The current treatments for cancer may include surgery, radiotherapy, and chemotherapy, but these procedures have several limitations. Current studies have shown that nanoparticles (NPs) can be used as a novel strategy for cancer treatment. Developing nanosystems that allow lower doses of therapeutic agents, as well as their selective release in tumour cells, may resolve the challenges of targeted cancer therapy. In this review, the authors discuss the role of the size, shape, and surface modifications of NPs in cancer treatment. They also address the challenges associated with cancer therapies based on NPs. The overall purpose of this review is to summarise the recent developments in designing different hybrid NPs with promising therapeutic properties for different types of cancer.Inspec keywords: tumours, reviews, patient treatment, nanomedicine, surgery, radiation therapy, cellular biophysics, nanobiotechnology, nanoparticles, cancerOther keywords: current treatments, cancer treatment, targeted cancer therapy, cancer therapies, surface‐functionalised hybrid nanoparticles, targeted treatment, serious human‐health related problems     

Polyethylenimine‐modified curcumin‐loaded mesoporus silica nanoparticle (MCM‐41) induces cell death in MCF‐7 cell line

Breast cancer accounts for the first highest mortality rate in India and second in world. Though current treatment strategies are effectively killing cancer cells, they also end in causing severe side effects and drug resistance. Curcumin is a nutraceutical with multipotent activity but its insolubility in water limits its therapeutic potential as an anti‐cancer drug. The hydrophilicity of curcumin could be increased by nanoformulation or changing its functional groups. In this study, curcumin is loaded on mesoporous silica nanoparticle and its anti‐cancer activity is elucidated with MCF‐7 cell death. Structural characteristics of Mobil Composition of Matter ‐ 41(MCM‐41) as determined by high‐resolution transmission electron microscopy (HR‐TEM) shows that MCM‐41 size ranges from 100 to 200 nm diameters with pore size 2–10 nm for drug adsorption. The authors found 80–90% of curcumin is loaded on MCM‐41 and curcumin is released efficiently at pH 3.0. The 50 µM curcumin‐loaded MCM‐41 induced 50% mortality of MCF‐7 cells. Altogether, their results suggested that increased curcumin loading and sustained release from MCM‐41 effectively decreased cell survival of MCF‐7 cells in vitro.Inspec keywords: cancer, cellular biophysics, nanoparticles, nanomedicine, biomedical materials, polymers, mesoporous materials, transmission electron microscopy, drugs, adsorptionOther keywords: polyethylenimine‐modified curcumin‐loaded mesoporus silica nanoparticle, MCF‐7 cell line, breast cancer, cancer cells, drug resistance, multipotent activity, therapeutic potential, anticancer drug, mesoporous silica nanoparticle, MCF‐7 cell death, high‐resolution transmission electron microscopy, drug adsorption, curcumin‐loaded MCM‐41, nutraceutical curcumin, size 2 nm to 10 nm, size 100 nm to 200 nm