Formulation and characterisation of a self‐nanoemulsifying drug delivery system of amphotericin B for the treatment of leishmaniasis

This study was aimed to develop a self‐nanoemulsifying drug delivery system (SNEDDS) for amphotericin B (AmB) potential use in leishmaniasis through topical and oral routes. Two formulations, formulation A and formulation B (FA and FB) of AmB loaded SNEDDS were developed by mixing their excipients through vortex and sonication. The SNEDDS formulation FA and FB displayed a mean droplet size of 27.70 ± 0.5 and 30.17 ± 0.7 nm and zeta potential −11.4 ± 3.25 and −13.6 ± 2.75 mV, respectively. The mucus permeation study showed that formulation FA and FB diffused 1.45 and 1.37%, respectively in up to 8 mm of mucus. The cell permeation across Caco‐2 cells monolayer was 10 and 11%, respectively. Viability of Caco‐2 cells was 89% for FA and 86.9% for FB. The anti‐leishmanial activities of FA in terms of IC₅₀ were 0.017 µg/ml against promastigotes and 0.025 µg/ml against amastigotes, while IC₅₀ values of FB were 0.031 and 0.056 µg/ml, respectively. FA and FB killed macrophage harboured Leishmania parasites in a dose‐dependent manner and a concentration of 0.1 µg/ml killed 100% of the parasites. These formulations have the potential to provide a promising tool for AmB use through oral and topical routes in leishmaniasis therapy.Inspec keywords: nanomedicine, drops, microorganisms, electrokinetic effects, cellular biophysics, drug delivery systems, monolayers, drugs, diseasesOther keywords: self‐nanoemulsifying drug delivery system, topical routes, oral routes, SNEDDS formulation, mucus permeation study, cell permeation, leishmaniasis treatment, amphotericin B, zeta potential, Caco‐2 cell monolayer, vortex, sonication, droplet size, Caco‐2 cell viability, antileishmanial activity, promastigotes, amastigotes, Leishmania parasites     

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     

Preparation of alginate oligosaccharide nanoliposomes and an analysis of their inhibitory effects on Caco‐2 cells

The conditions were optimised for preparing Alginate oligosaccharide (AOS) nanoliposomes, and Caco‐2 cell experiments were carried out to examine their antitumour effects. The optimal formulation of AOS nanoliposomes was as follows: a phosphatidylcholine‐to‐cholesterol ratio of 5.12, AOS concentration of 8.44 mg/mL, Tween 80 concentration of 1.11%, and organic phase to aqueous phase ratio of 5.25. Under the above conditions, the experimental encapsulation efficiency was 65.84%, and the AOS nanoliposomes exhibited a small particle size of 323 nm. After Caco‐2 cells were treated with AOS liposomes and AOS for 24 h, AOS nanoliposomes inhibited the growth of Caco‐2 cells to a greater extent than AOS at concentrations of 0.0625, 0.125, 0.25, 0.5 and 1 mg/mL (P  <  0.01). LDH leakage exhibited a concentration‐dependent increase following treatment with 0.5‐1 mg/mL AOS nanoliposomes, and the inhibitory effect of AOS nanoliposomes exhibited a more significant difference than AOS (P  <  0.01). Cells treated with 0.5 mg/mL and 1 mg/mL AOS nanoliposomes displayed a substantial and significant increase in activity compared with AOS (P  < 0.01). Based on these results, AOS nanoliposomes exerted a more significant effect on inhibiting Caco‐2 cell proliferation than AOS.Inspec keywords: evaporation, cellular biophysics, biomedical materials, biomembranes, nanomedicine, enzymes, biochemistry, drug delivery systems, particle size, response surface methodology, molecular biophysics, encapsulation, drugs, lipid bilayers, nanofabrication, materials preparation, polymers, nanostructured materialsOther keywords: reverse‐phase evaporation method, response surface methodology, alginate oligosaccharide nanoliposomes, mitochondrial function, AOS concentration, AOS liposomes, Caco‐2 cell proliferation, AOS nanoliposomes, methyl thiazolyl tetrazolium assay, cell counting kit‐8, lactate dehydrogenase, LDH assay, phosphatidylcholine‐to‐cholesterol ratio, size 323.0 nm, time 24.0 hour     

Poly(glycerol sebacate) nanoparticles for ocular delivery of sunitinib: physicochemical,cytotoxic and allergic studies

Poly(glycerol sebacate) (PGS) is a new biodegradable polymer with good biocompatibility used in many fields of biomedicine and drug delivery. Sunitinib‐loaded PGS/gelatine nanoparticles were prepared by the de‐solvation method for retinal delivery and treatment of diabetic retinopathy. The nanoparticles were characterised by Fourier‐transform infrared and differential scanning calorimetry. The effects of different formulation variables including drug‐to‐carrier ratio, gelatine‐to‐PGS ratio, and glycerine‐to‐sebacate ratio were assessed on the encapsulation efficiency (EE%), particle size, release efficiency (RE), and zeta potential of the nanoparticles. The in vitro cytotoxicity of PGS/gelatine nanoparticles was studied on L929 cells. Draize test on rabbit eyes was also done to investigate the possible allergic reactions caused by the polymer. Glycerine/sebacic acid was the most effective parameter on the EE and RE. Gelatine‐to‐PGS ratio had the most considerable effect on the particle size while the RE was more affected by the glycerine/sebacic acid ratio. The optimised formulation (S₁ G_0.7 D_21.2) exhibited a particle size of 282 nm, 34.6% EE, zeta potential of −8.9 mV, and RE% of about 27.3% for drug over 228 h. The 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay indicated PGS/gelatine nanoparticles were not cytotoxic and sunitinib‐loaded nanoparticles were not toxic at concentrations <36 nM.Inspec keywords: polymers, differential scanning calorimetry, toxicology, drug delivery systems, solvation, eye, encapsulation, particle size, drugs, biodegradable materials, nanofabrication, nanomedicine, nanoparticles, gelatin, Fourier transform infrared spectraOther keywords: gelatine‐to‐PGS ratio, glycerine‐to‐sebacate ratio, particle size, zeta potential, sunitinib‐loaded nanoparticles, biodegradable polymer, retinal delivery, differential scanning calorimetry, drug‐to‐carrier ratio, allergic reactions, physicochemistry, cytotoxicity, poly(glycerol sebacate) nanoparticles, sunitinib ocular delivery, drug delivery, sunitinib‐loaded PGS‐gelatine nanoparticles, Fourier‐transform, in vitro cytotoxicity, biocompatibility, Draize test, rabbit eyes, 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay     

Preparation and in vitro evaluation of novel cross‐linked chondroitin sulphate nanoparticles by aluminium ions for encapsulation of green tea flavonoids

Chondroitin sulphate is a sulphated glycosaminoglycan biopolymer composed over 100 individual sugars. Chondroitin sulphate nanoparticles (NPs) loaded with catechin were prepared by an ionic gelation method using AlCl₃ and optimised for polymer and cross‐linking agent concentration, curing time and stirring speed. Zeta potential, particle size, loading efficiency, and release efficiency over 24 h (RE₂₄ %) were evaluated. The surface morphology of NPs was investigated by scanning electron microscopy and their thermal behaviour by differential scanning calorimetric. Antioxidant effect of NPs was determined by chelating activity of iron ions. The cell viability of mesenchymal stem cells was determined by 3‐[4, 5‐dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay and the calcification of osteoblasts was studied by Alizarin red staining. The optimised NPs showed particle size of 176 nm, zeta potential of −20.8 mV, loading efficiency of 93.3% and RE₂₄ % of 80.6%. The chatechin loaded chondroitin sulphate NPs showed 70‐fold more antioxidant activity, 3‐fold proliferation effect and higher calcium precipitation in osteoblasts than free catechin.Inspec keywords: nanoparticles, encapsulation, biomedical materials, particle size, nanofabrication, nanomedicine, electrokinetic effects, cellular biophysics, polymer blends, molecular biophysics, molecular configurations, biochemistry, curing, surface morphology, scanning electron microscopy, differential scanning calorimetry, dyes, precipitationOther keywords: in vitro evaluation, cross‐linked chondroitin sulphate nanoparticles, aluminium ions, nanoparticles, green tea flavonoids, sulphated glycosaminoglycan biopolymer, sugars, catechin, ionic gelation method, cross‐linking agent concentration, curing time, size 176 nm, time 24 h, calcium precipitation, 3‐fold proliferation effect, antioxidant activity, chatechin loaded chondroitin sulphate NPs, Alizarin red staining, osteoblasts, calcification, 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyl tetrazolium bromide assay, mesenchymal stem cells, cell viability, chelating activity, differential scanning calorimetry, thermal behaviour, scanning electron microscopy, surface morphology, release efficiency, loading efficiency, particle size, zeta potential, stirring speed     

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     

In‐vitro and in‐vivo evaluation of chitosan‐based thermosensitive gel containing lorazepam NLCs for the treatment of status epilepticus

The objective of this study was to develop an in‐situ gel containing lorazepam (LZM) loaded nanostructured lipid carriers (NLCs) for direct nose‐to‐brain delivery in order to increase drug therapeutic efficacy in the treatment of epilepsy. Accordingly, LZM loaded NLCs were formulated using emulsification solvent diffusion and evaporation method; then the effects of the formulation variables on different physicochemical characteristics of NLCs were investigated. Thermosensitive in‐situ gels containing LZM‐NLCs were prepared using a combination of chitosan and β‐glycerol phosphate (β‐GP). The anticonvulsant efficacy of LZM‐NLCs‐Gel was then examined using the pentylenetetrazole (PTZ) model. The optimised NLCs were spherical, showing the particle size of 71.70 ± 5.16 nm and the zeta potential of −20.06 ± 2.70 mV. The pH and gelation time for the chitosan solution with 15% (w/v) β‐GP were determined to be 7.12 ± 0.03 and 5.33 ± 0.58 min, respectively. The in‐vivo findings showed that compared with the control group and the group that received LZM‐Gel, the occurrence of PTZ‐induced seizures in the rats was significantly reduced by LZM‐NLCs‐Gel after intranasal administration. These results, therefore, suggested that the LZM‐NLCs‐Gel system could have potential applications for brain targeting through nasal route and might increase LZM therapeutic efficacy in the treatment of epilepsy.Inspec keywords: biomedical materials, nanomedicine, cellular biophysics, electrokinetic effects, drug delivery systems, nanoparticles, brain, pH, drugs, particle size, nanofabrication, medical disorders, polymer gelsOther keywords: evaporation method, β‐glycerol phosphate, β‐GP, optimised NLCs, received LZM‐Gel, LZM therapeutic efficacy, chitosan‐based thermosensitive gel, lorazepam NLCs, nose‐to‐brain delivery, drug therapeutic efficacy, emulsification solvent diffusion, in‐vivo evaluation, in‐vitro evaluation, LZM‐NLC‐gel system, status epilepticus treatment, lorazepam loaded nanostructured lipid carriers, epilepsy treatment, physicochemical characteristics, thermosensitive in‐situ gel, anticonvulsant efficacy, pentylenetetrazole model, particle size, zeta potential, pH, gelation time, chitosan solution, PTZ‐induced seizures, intranasal administration     

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⁺      

Biomimetic production,characterisation, in vitro cytotoxic and anticancer assessment of aqueous extract‐mediated AgNPs of Teucrium stocksianum Boiss

Owing to the numerous biological applications, cost effectiveness and low cytotoxicity of the biomimetic nanoparticles (NPs), the authors optimised the production of silver NPs (AgNPs) using aqueous extract of Teucrium stocksianum Boiss. The NPs were characterised by ultraviolet‐visible (UV‐vis) spectroscopy, X‐ray diffraction (XRD), scanning electron microscopy (SEM), dynamic light scattering (DLS) and Fourier transform‐infrared spectroscopy (FTIR). The UV‐vis spectroscopy revealed a surface plasmon resonance (410‐440 nm) at an incubation temperature of 90°C when 1 mM Ag nitrate combined to 5 mg/ml extract concentration in the ratio of 1:10. DLS results show an average zeta size of ∼44.61 nm and zeta potential of −15.3 mV. SEM and XRD confirmed the high crystallinity and cubical symmetry with an average size below 100 nm. FTIR measurement shows the presence of various functional groups, responsible for the capping and reduction of Ag metal. The 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide cell viability assay shows that AgNPs are less cytotoxic to J774 and L929 cells as compared with enhanced anticancer activity with low IC50 concentrations (68.24 µg/ml) against Michigan Cancer Foundation‐7 (MCF‐7) cells. The ethidium bromide/acridine orange assay shows that the AgNPs kill the cell by apoptosis. Overall, the results show that AgNPs possesses potent anticancer activities.Inspec keywords: cellular biophysics, cancer, nanobiotechnology, nanomedicine, ultraviolet spectra, X‐ray diffraction, scanning electron microscopes, light scattering, patient treatmentOther keywords: anticancer assessment, in vitro cytotoxic assessment, aqueous extract‐mediated AgNPs, Teucrium stocksianum Boiss, nanoparticles, biological applications, biosynthesis, silver NPs, X‐ray diffraction, scanning electron microscopy, dynamic light scattering, Fourier transform‐infrared spectroscopy, UV‐vis spectroscopy, surface plasmon resonance, extract concentration, zeta potential, high crystallinity, FTIR measurement, amide molecules, viability assay, enhanced anticancer activity, potent anticancer activities     

Development and in vitro evaluation of oxytetracycline‐loaded PMMA nanoparticles for oral delivery against anaplasmosis

Poly‐methyl methacrylate (PMMA) polymer with remarkable properties and merits are being preferred in various biomedical applications due to its biocompatibility, non‐toxicity and cost effectiveness. In this investigation, oxytetracycline‐loaded PMMA nanoparticles were prepared using nano‐precipitation method for the treatment of anaplasmosis. The prepared nanoparticles were characterised using dynamic light scattering (DLS), atomic force microscopy (AFM), differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy. The mean average diameter of the nanoparticles ranged between 190–240 nm and zeta potential was found to be −19 mV. The drug loading capacity and entrapment efficiency of nanoparticles was found varied between 33.7–62.2% and 40.5–60.0%. The in vitro drug release profile exhibited a biphasic phenomenon indicating controlled drug release. The uptake of coumarin‐6(C‐6)‐loaded PMMA nanoparticles in Plasmodium falciparum (Pf 3D7) culture model was studied. The preferential uptake of C‐6‐loaded nanoparticles by the Plasmodium infected erythrocytes in comparison with the uninfected erythrocytes was observed under fluorescence microscopy. These findings suggest that oxytetracycline‐loaded PMMA nanoparticles were found to be an effective oral delivery vehicle and an alternative pharmaceutical formulation in anaplasmosis treatment, too.Inspec keywords: nanoparticles, nanomedicine, conducting polymers, microorganisms, cellular biophysics, toxicology, drug delivery systems, light scattering, atomic force microscopy, differential scanning calorimetry, Fourier transform infrared spectra, bloodOther keywords: in vitro evaluation, oxytetracycline‐loaded PMMA nanoparticles, anaplasmosis, polymethyl methacrylate polymer, biocompatibility, toxicity, oxytetracycline‐nanoparticles, nanoprecipitation method, dynamic light scattering, atomic force microscopy, AFM, differential scanning calorimetry, DSC, Fourier transform infrared spectroscopy, FTIR spectroscopy, zeta potential, drug loading capacity, entrapment efficiency, in vitro drug release profile, biphasic phenomenon, coumarin‐6(C‐6)‐loaded PMMA nanoparticles, plasmodium falciparum culture model, preferential uptake, plasmodium infected erythrocytes, fluorescence microscopy, oral delivery vehicle, anaplasmosis treatment, size 190 nm to 240 nm     

FSE–Ag complex NS: preparation and evaluation of antibacterial activity

Silver (Ag) complexes of drugs and their nanosystems have great potential as antibacterials. Recently, an Ag complex of furosemide (Ag–FSE) has shown to be a promising antimicrobial. However, poor solubility of Ag–FSE could hamper its introduction into clinics. Therefore, the authors developed a nanosuspension of Ag–FSE (Ag–FSE_NS) for its solubility and antibacterial activity enhancement. The aim of this study was to introduce a novel nanoantibiotic with enhanced antibacterial efficacy. Ag–FSE_NS was prepared by precipitation–ultrasonication technique. Size, polydispersity index (PI) and zeta potential (ZP) of prepared Ag–FSE_NS were measured by dynamic light scattering, whereas surface morphology was determined using scanning electron microscopy (SEM). In vitro antibacterial activity was evaluated against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa using broth microdilution method. Size, PI and ZP of optimised Ag–FSE_NS1 were 191.2 ± 19.34 nm, 0.465 ± 0.059 and −55.7 ± 8.18 mV, respectively. SEM revealed that Ag–FSE_NS1 particles were rod or needle‐like with smooth surfaces. Saturation solubility of Ag–FSE in NS increased eight‐fold than pure Ag–FSE. Ag–FSE_NS1 exhibited two‐fold and eight‐fold enhancements in activity against E. coli and S. aureus, respectively. The results obtained showed that developed Ag–FSE_NS1 holds a promise as a topical antibacterial.Inspec keywords: nanomedicine, nanofabrication, light scattering, surface morphology, silver, particle size, solubility, suspensions, scanning electron microscopy, electrokinetic effects, drugs, biomedical materials, antibacterial activity, microorganisms, nanoparticles, drug delivery systems, transmission electron microscopyOther keywords: saturation solubility, topical antibacterial, size 171.86 nm to 210.54 nm, voltage ‐47.52 mV to ‐63.88 mV, Ag, broth microdilution method, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, SEM, scanning electron microscopy, surface morphology, dynamic light scattering, particle size, polydispersity index, precipitation–ultrasonication technique, nanoantibiotic, nanosuspension, furosemide, nanosystems, drugs, Ag–FSE_NS preparation, in vitro antibacterial activity, pure Ag–FSE, Ag–FSE_NS1 particles, optimised Ag–FSE_NS1, zeta potential, enhanced antibacterial efficacy, antibacterials     

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     

Factorial design analysis and optimisation of chitosan‐based nanogels as controlled release system for gentamicin

The aim of this study was preparation and optimisation of a controlled‐release delivery system to decrease the dose‐dependent side effects of gentamicin. Hydrogel nanoparticles composed of a polycationic polymer (chitosan) and an inorganic polyanion (sodium tripolyphosphate) were fabricated in the presence of gentamicin. An experimental design was drawn upon to determine the optimum condition of nanoparticle preparation. Various features of the nanoparticles including drug loading parameters, particle size distribution, zeta potential and in vitro drug release profile were evaluated. Ultimately, the antimicrobial activity of the gentamicin‐loaded nanoparticles was analysed by determination of the minimum inhibitory concentration (MIC) and the potency test. As a result, the nanocarriers with an average size of about 250 nm (unloaded) and 493 nm (gentamicin‐loaded) were obtained with unimodal distribution and a notable polydispersity index (≤0.3). The drug loading efficiency was between 28 and 32%. The gradual and sustained releases (∼90%) of gentamicin were achieved in 24 h. The MIC and potency test showed no significant decrease in the antibacterial activity of gentamicin‐loaded nanoparticles. The outcomes demonstrated that the optimised chitosan nanogels prepared in this study can be considered as a suitable carrier for a controlled release system.Inspec keywords: hydrogels, nanoparticles, drug delivery systems, particle size, electrokinetic effects, antibacterial activity, nanomedicineOther keywords: factorial design analysis, chitosan‐based nanogels, gentamicin, controlled‐release delivery system, hydrogel nanoparticles, polycationic polymer, inorganic polyanion, sodium tripolyphosphate, particle size distribution, drug loading parameters, zeta potential, in vitro drug release profile, antimicrobial activity, minimum inhibitory concentration, polydispersity index, drug loading efficiency, antibacterial activity     

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 and characterisation of PEG modified chitosan nanocapsules loaded with thymoquinone

Thymoquinone (TQ), a major bioactive compound of Nigella sativa seeds has several therapeutic properties. The main drawback in bringing TQ to therapeutic application is that it has poor stability and bioavailability. Hence a suitable carrier is essential for TQ delivery. Recent studies indicate biodegradable polymers are potentially good carriers of bioactive compounds. In this study, polyethylene glycol (PEG) modified chitosan (Cs) nanocapsules were developed as a carrier for TQ. Aqueous soluble low molecular weight Cs and PEG was selected among different biodegradable polymers based on their biocompatibility and efficacy as a carrier. Optimisation of synthesis of nanocapsules was done based on particle size, PDI, encapsulation efficiency and process yield. A positive zeta potential value of +48 mV, indicating good stability was observed. Scanning electron microscope and atomic‐force microscopy analysis revealed spherical shaped and smooth surfaced nanocapsules with size between 100 to 300 nm. The molecular dispersion of the TQ in Cs PEG nanocapsules was studied using X‐ray powder diffraction. The Fourier transform infrared spectrum of optimised nanocapsule exhibited functional groups of both polymer and drug, confirming the presence of Cs, PEG and TQ. In vitro drug release studies showed that PEG modified Cs nanocapsules loaded with TQ had a slow and sustained release.Inspec keywords: nanomedicine, drug delivery systems, polymers, scanning electron microscopy, electrokinetic effects, atomic force microscopy, X‐ray diffraction, Fourier transform infrared spectraOther keywords: PEG modified chitosan nanocapsules, thymoquinone, bioactive compound, Nigella sativa seeds, bioavailability, polyethylene glycol, molecular weight, zeta potential, scanning electron microscope, atomic force microscopy, molecular dispersion, X‐ray powder diffraction, Fourier transform infrared spectrum     

Method for enhancing bioavailability of myricetin based on self‐assembly of casein–myricetin nanomicelles

In order to expand the application in the medical field and enhance pharmacological effects, casein–myricetin nanomicelles were prepared by the self‐assembly method and characterised by ultraviolet–visible spectroscopy and Fourier transform infrared spectroscopy. The parameters in self‐assembly were optimised according to the factors of particle size, encapsulation yield, and drug loading. The result showed a pH of 5.5, a casein concentration of 2 mg/ml, a mass ratio of casein to myricetin of 8:1, ultrasonic power of 300 W, ultrasonic time of 5 min and ethanol volume of 7 ml were the optimal conditions. The situ cycle intestinal perfusion methods indicated that casein–myricetin nanomicelles can be more easily absorbed by small intestine than myricetin standard sample. Therefore, casein micelles are effective for improving the water solubility of myricetin.Inspec keywords: encapsulation, nanoparticles, nanomedicine, drugs, nanofabrication, biomedical materials, solubility, molecular biophysics, ultraviolet spectra, drug delivery systems, particle size, pH, visible spectra, colloids, self‐assembly, Fourier transform infrared spectraOther keywords: casein–myricetin nanomicelles, self‐assembly method, ultraviolet–visible spectroscopy, casein concentration, myricetin standard sample, casein micelles, medical field, pharmacological effects, Fourier transform infrared spectroscopy, particle size, pH, ultrasonic power, ethanol volume, water solubility, power 300.0 W, time 5.0 min     

Rapid synthesis of silver nanoparticles by Pseudomonas stutzeri isolated from textile soil under optimised conditions and evaluation of their antimicrobial and cytotoxicity properties

Present study utilised textile soil isolated bacterium Pseudomonas stutzeri to synthesise extracellular silver nanoparticles (AgNPs) under optimised conditions. The synthesised AgNPs were characterised using ultraviolet‐visible spectroscopy, Fourier transform infrared spectroscopy (FTIR) and transmission electron microscopy (TEM). Optimisation showed AgNPs synthesis within 8 h using 2mM Ag nitrate at pH9, temperature 80°C and maximum absorbance toward 400 nm. TEM analysis revealed spherical shape AgNPs and reduction in size upto 8 nm was observed under optimised conditions. FTIR spectra confirmed presence of proteins bound to AgNPs act as reducing agent. AgNPs showed strong antibacterial activity against multi‐drug resistant (MDR) Escherichia coli and Klebsiella pneumoniae as demonstrated by disc diffusion and colony forming unit assays. Zone of inhibition increased with increasing concentration of AgNPs with maximum of 19 mm against E. coli and 17 mm against K. pneumoniae at concentration of 2 μg/disc. Furthermore, AgNPs did not show any cytotoxic effects on human epithelial cells as demonstrated by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide assay even at 2 μg/ml concentration of AgNPs. The results of the present study suggest that AgNPs can be synthesised rapidly under optimised conditions and show strong antimicrobial property against MDR pathogens without having toxicity effect on human epithelial cells.Inspec keywords: ultraviolet spectra, proteins, transmission electron microscopy, infrared spectra, Fourier transform spectra, visible spectra, microorganisms, toxicology, cellular biophysics, biomedical materials, antibacterial activity, nanomedicine, nanofabrication, nanoparticles, silverOther keywords: 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide assay, human epithelial cells, cytotoxic effects, K. pneumoniae, colony forming unit counting assays, disc diffusion, Klebsiella pneumoniae, Escherichia coli, multidrug resistant, stabilising agent, reducing agent, proteins, parametric optimisation, TEM, transmission electron microscopy, FTIR spectra, Fourier transform infrared spectroscopy, ultraviolet‐visible spectroscopy, bacterium, cytotoxicity properties, antimicrobial properties, textile soil, Pseudomonas stutzeri, silver nanoparticle synthesis     

Co‐encapsulating CoFe2 O4 and MTX for hyperthermia

Magnetic manotheranostics can be a fascinating charm to diagnose a tumour with MRI, and treatment through hyperthermia. This study aims to synthesise and characterise magnetically responsive polymer colloids (MRPCs). Healthy tissue damage done by chemotherapy session could be minimised by MRPCs. For the colloidal formulation of MRPCs, the oil in water emulsion technique was employed with the aid of sonication and stirring. The organic phase of emulsion contained methotrexate (MTX) drug, Eudragit E100 and CoFe₂ O₄ (synthesised by co‐precipitation) in ethanol, and the aqueous phase contained tween 80 in deionised water. The emulsion was optimised by studying/adjusting two different parameters, i.e. the concentration of constituents and sonication cycles. Multiple formulations were produced at sonication amplitude of 60% at 20 kHz, followed by centrifugation and lyophilisation. Characterisation of MRPCs was done for morphology, size measurement (23–25 nm), surface charge (∼15.12), coercivity (∼1549.6 G), magnetisation (2.6 emu) and retentivity (1.34 emu). Drug release in simulating physiological environment (pH = 7.4), was observed for up to 48 h, and, to determine the best release kinetic mechanism results were compared with kinetic models. Magnetic hyperthermia studies showed that MRPCs achieved an acceptable temperature of 42°C, for hyperthermia treatments in cancer patients.Inspec keywords: biomedical materials, colloids, cancer, encapsulation, pH, polymers, hyperthermia, drugs, drug delivery systems, precipitation (physical chemistry), emulsions, tumours, materials preparation, coercive forceOther keywords: magnetic manotheranostics, magnetically responsive polymer colloids, healthy tissue damage, chemotherapy session, colloidal formulation, organic phase, aqueous phase, deionised water, sonication cycles, multiple formulations, sonication amplitude, size measurement, hyperthermia treatments, coencapsulation, MTX, oil‐in‐water emulsion technique, methotrexate drug, magnetic hyperthermia, tumour diagnosis, MRI, Eudragit E100, coprecipitation, ethanol, centrifugation, lyophilisation, surface charge, coercivity, magnetisation, retentivity, drug release, simulating physiological environment, pH, release kinetic mechanism, cancer patients, size 23.0 nm to 25.0 nm, frequency 20.0 kHz, CoFe₂ O₄      

Biosynthesis and characterisation of solid lipid nanoparticles and investigation of toxicity against breast cancer cell line

Solid lipid nanoparticles (SLNs) comprise non‐toxic surface‐active lipidic agents combined with appropriate ratios of drugs or essential oils. The goal of this research was to investigate the effects of the SLN synthesised using essential oils of Foeniculum vulgare on the MCF‐7 breast cancer cell line. SLNs were prepared by homogenisation and ultrasound techniques and characterised by dynamic light scattering (DLS), zeta potential assessment, and transmission electron microscopy (TEM). 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide assay (MTT assay), flow‐cytometry, and Acridine‐Orange assay were employed for assessing the biological activities of the SLNs. The average particle size was 55.43 nm and the net surface charge was −29.54 ± 11.67 mV. TEM showed that the mean particle size was 33.55 nm and the synthesised SLNs had a uniform round morphology. The MTT assay showed that the prepared SLNs had high toxicity against MCF‐7 cells and low toxicity against normal HUVECs cells. Flow‐cytometry revealed a noteworthy rise in the subG1 peak of the cell cycle in the cancer cells treated with SLNs compared to the controls, indicating apoptosis in cancer cells. The results also showed discolouration in SLNs‐treated cells, which further confirmed the induction of apoptosis and the toxicity of the SLNs against MCF‐7 cells.