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     

Efavirenz oral delivery via lipid nanocapsules: formulation,optimisation, and ex‐vivo gut permeation study

Present investigation aimed to prepare, optimise, and characterise lipid nanocapsules (LNCs) for improving the solubility and bioavailability of efavirenz (EFV). EFV‐loaded LNCs were prepared by the phase‐inversion temperature method and the influence of various formulation variables was assessed using Box–Behnken design. The prepared formulations were characterised for particle size, polydispersity index (PdI), zeta potential, encapsulation efficiency (EE), and release efficiency (RE). The biocompatibility of optimised formulation on Caco‐2 cells was determined using 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyltetrazolium bromide assay. Then, it was subjected to ex‐vivo permeation using rat intestine. EFV‐loaded LNCs were found to be spherical shape in the range of 20–100 nm with EE of 82–97%. The best results obtained from LNCs prepared by 17.5% labrafac and 10% solutol HS15 when the volume ratio of the diluting aqueous phase to the initial emulsion was 3.5. The mean particle size, zeta potential, PdI, EE, drug loading%, and RE during 144 h of optimised formulation were confirmed to 60.71 nm, −35.93 mV, 0.09, 92.60, 7.39 and 55.96%, respectively. Optimised LNCs increased the ex vivo intestinal permeation of EFV when compared with drug suspension. Thus, LNCs could be promising for improved oral delivery of EFV.Inspec keywords: biomedical materials, solubility, drugs, encapsulation, emulsions, nanoparticles, particle size, nanofabrication, suspensions, toxicology, nanomedicine, cellular biophysics, lipid bilayers, electrokinetic effects, drug delivery systems, molecular biophysicsOther keywords: ex‐vivo permeation, diluting aqueous phase, mean particle size, zeta potential, drug loading, optimised formulation, ex vivo intestinal permeation, improved oral delivery, efavirenz oral delivery, optimisation, ex‐vivo gut permeation study, solubility, bioavailability, phase‐inversion temperature method, formulation variables, Box–Behnken design, polydispersity index, encapsulation efficiency, Caco‐2 cells, lipid nanocapsules, 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyltetrazolium bromide assay, EFV‐loaded LNC, drug suspension, size 20.0 nm to 100.0 nm, time 144.0 hour, size 60.71 nm, voltage ‐35.93 mV     

Novel nanoplex‐mediated plant transformation approach

Here, a rapid and easy transformation by electroporation technique for gene transfer in plants using cell penetrating amino nanocomplex (nanoplex) has been demonstrated in Nicotiana. Nanoplex was prepared using cell penetrating amino acids (CPAs) such as poly‐L‐lysine (PLL) and Argenine (Arg), in combination with the gold nanoparticles (AuNPs). PLLs‐modified nanoplex with zeta potential of 34.2 ± 1.22 mV charge showed 63.3% efficiency for gene transformation in plant cells as compared to 60% when modified with Arg and the zeta potential was found to be 30.0 ± 0.83 mV; whereas, the transformation efficiency without nanoplex was found to be 6.6%. The findings indicate that the zeta potential of positively charged nanocomplex (AuNPs/CPAs/DNA/CPAs) increases the transformation efficiency because of their ability to protect the DNA from electroporation wave and endogenous enzyme damage. Transformation was confirmed by GUS assay and amplification of npt gene. This technique may open up new possibilities of gene transfer in plants, which will enable to produce large number of transgenic plants.Inspec keywords: biochemistry, electrokinetic effects, DNA, biomedical materials, nanomedicine, nanoparticles, gold, cellular biophysics, enzymes, genetics, molecular biophysics, genomicsOther keywords: nanoplex‐mediated plant transformation approach, electroporation technique, gene transfer, cell penetrating amino nanocomplex, cell penetrating amino acids, poly‐L‐lysine, Arg, gold nanoparticles, PLLs‐modified nanoplex, zeta potential, gene transformation, plant cells, transformation efficiency, positively charged nanocomplex, electroporation wave, npt gene, transgenic plants, AuNPs‐CPAs‐DNA‐CPAs, voltage 32.980000000000004 mV to 35.42 mV, voltage 29.169999999999998 mV to 30.830000000000002 mV, Au     

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     

Biosynthesis of AgNPs using aqueous leaf extract of Ipomoea eriocarpa and their anti‐inflammatory effect on carrageenan‐induced paw edema in male Wistar rats

Silver nanoparticles (AgNPs) were synthesised from aqueous Ag nitrate through a simple, competent and eco‐friendly method using the leaf extract of Ipomoea eriocarpa as reducing as well as capping agent. Ultraviolet–visible absorption spectroscopy was used to confirm the formation of AgNPs which displayed the substantiation of surface plasmon bands at 425 nm. The NPs were also characterised using Fourier transformer infrared spectroscopy, X‐ray diffraction method, transmission electron microscope and zeta potential. The characterisation study confirmed the formation of AgNPs, their spherical shape and average diameter of 12.85 ± 8.65 nm. Zeta potential value of −20.5 mV suggested that the AgNPs are stable in the suspension. The aqueous extract and the AgNPs were further screened for in vivo anti‐inflammatory activity using carrageenan‐induced paw edema in male Wistar rats. The study demonstrated that the AgNPs (1 ml kg⁻¹) had a significant (p  < 0.05) anti‐edemic effect and inhibition was observed from the first hour (21.31 ± 1.34) until the sixth hour (52.67 ± 1.41), when the inhibitory effect was greatest and superior to the aqueous extract and the standard, diclofenac.Inspec keywords: silver, nanoparticles, nanofabrication, ultraviolet spectra, visible spectra, absorption coefficients, surface plasmons, Fourier transform infrared spectra, X‐ray diffraction, transmission electron microscopy, suspensions, drugs, nanomedicineOther keywords: biosynthesis, aqueous leaf extract, ipomoea eriocarpa, antiinflammatory effect, carrageenan‐induced paw edema, male Wistar rats, silver nanoparticles, aqueous nitrate, capping agent, ultraviolet‐visible absorption spectroscopy, surface plasmon band, Fourier transformer infrared spectroscopy, X‐ray diffraction, transmission electron microscopy, zeta potential, spherical shape, suspension, aqueous extract, in vivo antiinflammatory activity, antiedemic effect, inhibitory effect, diclofenac, wavelength 425 nm, size 12.85 nm to 8.65 nm, Ag     

Antibacterial,anti‐inflammatory and antioxidant effects of acetyl‐11‐α‐keto‐β‐boswellic acid mediated silver nanoparticles in experimental murine mastitis

Mastitis is an important economic disease causing production losses in dairy industry. Antibiotics are becoming ineffective in controlling mastitis due to the emergence of resistant strains requiring the development of novel therapeutic agents. In this study, the authors present the phytochemical synthesis of silver nanoparticles (AgNPs) with acetyl‐11‐α‐keto‐β‐boswellic acid and evaluation of their activity in Staphylococcus aureus induced murine mastitis. Boswellic acid mediated AgNP (BANS) were oval, polydispersed (99.8 nm) with an minimum inhibitory concentration of 0.033 µg ml⁻¹ against S. aureus, inhibitory concentration (IC₅₀) of 30.04 µg ml⁻¹ on mouse splenocytes and safe at an in vivo acute oral dose of 3.5 mg kg⁻¹ in mice. Mastitis was induced in lactating mice by inoculating S. aureus (log₁₀ 5.60 cfu) and treated 6 h post‐inoculation with BANS (0.12 mg kg⁻¹, intramammary and intraperitoneal), and cefepime (1 mg kg⁻¹, intraperitoneal). S. aureus inoculated mice showed increased bacterial load, neutrophil infiltration in mammary glands and elevated C‐reactive protein (CRP) in serum. Oxidative stress was also observed with elevated malondialdehyde level, superoxide dismutase (SOD) and catalase (CAT) activities. BANS treatment significantly (P  < 0.05) reduced bacterial load, CRP, SOD, CAT activities and neutrophil infiltration in affected mammary glands. BANS could be a potential therapeutic agent for managing bovine mastitis.Inspec keywords: nanomedicine, nanoparticles, silver, antibacterial activity, drugs, diseases, enzymesOther keywords: antibacterial effects, antiinflammatory effects, antioxidant effects, acetyl‐11‐α‐keto‐β‐boswellic acid, mediated silver nanoparticles, experimental murine mastitis, economic disease, dairy industry, resistant strains, phytochemical synthesis, Staphylococcus aureus, minimum inhibitory concentration, inoculating S. aureus, neutrophil infiltration, mammary glands, elevated C‐reactive protein, superoxide dismutase, catalase, bovine mastitis, Ag     

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     

Biosynthesis of gold nanoparticles using fungus Trichoderma sp. WL‐Go and their catalysis in degradation of aromatic pollutants

An efficient green method of gold nanoparticles (AuNPs) biosynthesis was achieved by cell‐free extracts of fungus Trichoderma sp. WL‐Go. Based on UV–Vis spectra, AuNPs biosynthesised by cell‐free extracts with 90 mg/l protein exhibited a characteristic absorption band at 556 nm and was stable for 7 days. Transmission electron microscopy images revealed that the as‐synthesised AuNPs were spherical and pseudo‐spherical, and the average size was calculated to be 9.8 nm with a size range of 1–24 nm. The AuNPs illustrated their good catalytic activities for reduction of nitro‐aromatics (2‐nitrophenol, 3‐nitrophenol, 4‐nitrophenol, 2‐nitroaniline, 3‐nitroaniline) with catalytic rate constants of 7.4 × 10⁻³ s⁻¹, 10.3 × 10⁻³ s⁻¹, 4.9 × 10⁻³ s⁻¹, 5.8 × 10⁻³ s⁻¹, 15.0 × 10⁻³ s⁻¹, respectively. Meanwhile, the AuNPs also showed excellent catalytic performance in decolourisation of azo dyes with decolourisation efficiency from 82.2 to 97.5%. This study provided a green gentle method for AuNPs synthesis as well as exhibiting efficient catalytic capability for degradation of aromatic pollutants.Inspec keywords: catalysts, dyes, particle size, reduction (chemical), nanobiotechnology, nanofabrication, ultraviolet spectra, gold, transmission electron microscopy, nanoparticles, proteins, catalysis, visible spectra, pollution control, microorganismsOther keywords: nitro‐aromatics, catalytic rate constants, decolourisation efficiency, green gentle method, efficient green method, gold nanoparticles biosynthesis, cell‐free extracts, UV–Vis spectra, characteristic absorption band, transmission electron microscopy images, as‐synthesised AuNPs, catalytic performance, protein, catalytic activities, efficient catalytic capability, fungus Trichoderma sp. WL‐Go, aromatic pollutants degradation, 2‐nitrophenol, 3‐nitrophenol, 4‐nitrophenol, 2‐nitroaniline, 3‐nitroaniline, azo dye decolourisation, Au     

Synthesis,characterisation and anti‐tumour activity of biopolymer based platinum nanoparticles and 5‐fluorouracil loaded platinum nanoparticles

A facile and green synthesis of platinum nanoparticles [gum kondagogu platinum nanoparticles (GKPtNP)] using biopolymer‐ gum kondagogu was developed. The formation of GKPtNP was confirmed by ultraviolet (UV)–visible spectroscopy, scanning electron microscopy–energy dispersive X‐ray spectroscopy, transmission electron microscopy, X‐ray diffraction, Zeta potential, Fourier transform infrared, inductively coupled plasma mass spectroscopy. The formed GKPtNP are well dispersed, homogeneous with a size of 2–4 ± 0.50 nm, having a negative zeta potential (−46.1 mV) indicating good stability. 5‐Fluorouracil (5FU) was loaded onto the synthesised GKPtNP, which leads to the development of a new combination of nanomedicine (5FU–GKPtNP). The in vitro drug release studies of 5FU–GKPtNP in pH 7.4 showed a sustained release profile over a period of 120 min. Agrobacterium tumefaciens induced in vitro potato tumour bioassay was employed for screening the anti‐tumour potentials of GKPtNP, 5FU, and 5FU–GKPtNP. The experimental results suggested a complete tumour inhibition by 5FU–GKPtNP at a lower concentration than the GKPtNP and 5FU. Furthermore, the mechanism of anti‐tumour activity was assessed by their interactions with DNA using agarose gel electrophoresis and UV‐spectroscopic analysis. The electrophoresis results revealed that the 5FU–GKPtNP totally diminishes DNA and the UV‐spectroscopic analysis showed a hyperchromic effect with red shift indicating intercalation type of binding with DNA. Over all, the present study revealed that the combined exposure of the nanoformulation resulted in the enhanced anti‐tumour effect. Inspec keywords: nanoparticles, transmission electron microscopy, biomedical materials, tumours, ultraviolet spectra, DNA, drugs, electrophoresis, polymers, platinum, pH, drug delivery systems, biochemistry, X‐ray chemical analysis, microorganisms, molecular biophysics, electrokinetic effects, X‐ray diffraction, scanning electron microscopy, cancer, nanofabrication, visible spectra, nanomedicine, Fourier transform infrared spectra, materials preparationOther keywords: 5FU–GKPtNP, 5‐fluorouracil loaded platinum nanoparticles, gum kondagogu platinum nanoparticles, antitumour activity, scanning electron microscopy‐energy dispersive X‐ray spectroscopy, biopolymer‐based platinum nanoparticles, biopolymer‐based platinum nanoparticles, ultraviolet‐visible spectroscopy, UV‐visible spectroscopy, transmission electron microscopy, X‐ray diffraction, zeta potential, Fourier transform infrared spectroscopy, inductively coupled plasma mass spectroscopy, nanomedicine, in vitro drug release studies, sustained release profile, Agrobacterium tumefaciens, in vitro potato tumour bioassay, tumour inhibition, tumour activity, agarose gel electrophoresis, UV‐spectroscopic analysis, DNA, time 120.0 min, Pt     

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      

Sustained delivery of olanzapine from sunflower oil‐based polyol‐urethane nanoparticles synthesised through a cyclic carbonate ring‐opening reaction

The forefront horizon of biomedical investigations in recent decades is parcelling‐up and delivery of drugs to achieve controlled/targeted release. In this regard, developing green‐based delivery systems for a spatiotemporal controlling therapeutic agent have drawn a lot of attention. A facile route based on cyclic carbonate ring‐opening reaction has been utilised to synthesise a bio‐based polyol‐containing urethane bond [polyol‐urethane (POU)] as a nanoparticulate drug delivery system of olanzapine in order to enhance its bioavailability. After characterisation, the nanoparticles were also estimated for in vitro release, toxicity, and pharmacokinetic studies. As olanzapine has shown poor bioavailability and permeability in the brain, the sustained release of olanzapine from the designed carriers could enhance pharmacokinetic effectiveness. POU in the aqueous solution formed micelles with a hydrophobic core and embedded olanzapine under the influence of its hydrophobic nature. Drug release from the nanoparticles (90 ± 0.43 nm in diameter) indicated a specific pattern with initial burst release, and then a sustained release behaviour (82 ± 3% after 168 h), by the Higuchi‐based release mechanism. Pharmacokinetics assessments of POU‐olanzapine nanoparticles were carried in male Wistar rats through intravenous administration. The obtained results paved a way to introduce the POU as an efficient platform to enhance the bioavailability of olanzapine in therapeutic methods.Inspec keywords: hydrophobicity, nanomedicine, nanofabrication, nanoparticles, drug delivery systems, biomedical materials, polymers, brainOther keywords: cyclic carbonate ring‐opening reaction, nanoparticulate drug delivery system, bioavailability, drug release, initial burst release, Higuchi‐based release mechanism, POU‐olanzapine nanoparticles, sunflower oil‐based polyol‐urethane nanoparticles, forefront horizon, biomedical investigations, green‐based delivery systems, spatiotemporal controlling therapeutic agent, bio‐based polyol‐containing urethane bond, polyol‐urethane, toxicity, pharmacokinetic studies, olanzapine, aqueous solution, micelles, hydrophobic core, Pharmacokinetics, male Wistar rats, brain     

Trastuzumab‐conjugated nanoparticles composed of poly(butylene adipate‐co ‐butylene terephthalate) prepared by electrospraying technique for targeted delivery of docetaxel

Human epidermal growth factor receptor 2 (HER‐2) is overexpressed in 20–30% of human breast cancers, associated with poor prognosis and tumour aggression. The aim of this study was the production of trastuzumab‐targeted Ecoflex nanoparticles (NPs) loaded with docetaxel and in vitro evaluation of their cytotoxicity and cellular uptake. The NPs were manufactured by electrospraying and characterised regarding size, zeta potential, drug loading, and release behaviour. Then their cytotoxicity was evaluated by MTT assay against an HER‐2‐positive cell line, BT‐474, and an HER‐2‐negative cell line, MDA‐MB‐468. The cellular uptake was studied by flow cytometry and fluorescent microscope. The particle size of NPs was in an appropriate range, with relatively high drug entrapment and acceptable release efficiency. The results showed no cytotoxicity for the polymer, but the significant increment of cytotoxicity was observed by treatment with docetaxel‐loaded NPs in both HER‐2‐positive and HER‐2‐negative cell lines, in comparison with the free drug. The trastuzumab‐targeted NPs also significantly enhanced cytotoxicity against BT‐474 cells, compared with non‐targeted NPs.Inspec keywords: cancer, proteins, biomedical materials, nanofabrication, drug delivery systems, cellular biophysics, biological organs, nanomedicine, toxicology, tumours, nanoparticles, biomedical optical imaging, fluorescence, particle sizeOther keywords: human breast cancers, tumour aggression, trastuzumab‐targeted Ecoflex nanoparticles, cellular uptake, zeta potential drug loading, HER‐2‐positive cell line, HER‐2‐negative cell line, MDA‐MB‐468, particle size, trastuzumab‐conjugated nanoparticles, electrospraying technique, human epidermal growth factor receptor, cytotoxicity, nontargeted nanoparticles, butylene adipate‐co‐butylene terephthalate, trastuzumab‐targeted NP, docetaxel‐loaded NP     

Actinobacterial‐mediated synthesis of silver nanoparticles and their activity against pathogenic bacteria

In this study, silver nanoparticles (AgNPs) were biosynthesised by using acidophilic actinobacterial SH11 strain isolated from pine forest soil. Isolate SH11 was identified based on 16S rRNA gene sequence to Streptomyces kasugaensis M338‐M1^T and S. celluloflavus NRRL B‐2493^T (99.8% similarity, both). Biosynthesised AgNPs were analysed by UV–visible spectroscopy, which revealed specific peak at λ  = 420 nm. Transmission electron microscopy analyses showed polydispersed, spherical nanoparticles with a mean size of 13.2 nm, while Fourier transform infrared spectroscopy confirmed the presence of proteins as the capping agents over the surface of AgNPs. The zeta potential was found to be −16.6 mV, which indicated stability of AgNPs. The antibacterial activity of AgNPs from SH11 strain against gram‐positive (Staphylococcus aureus and Bacillus subtilis) and gram‐negative (Escherichia coli) bacteria was estimated using disc diffusion, minimum inhibitory concentration and live/dead analyses. The AgNPs showed the maximum antimicrobial activity against E. coli, followed by B. subtilis and S. aureus. Further, the synergistic effect of AgNPs in combination with commercial antibiotics (kanamycin, ampicillin, tetracycline) was also evaluated against bacterial isolates. The antimicrobial efficacy of antibiotics was found to be enhanced in the presence of AgNPs.Inspec keywords: antibacterial activity, silver, nanoparticles, electrokinetic effects, Fourier transform infrared spectra, microorganisms, nanofabricationOther keywords: actinobacterial mediated synthesis, silver nanoparticles, pathogenic bacteria, biosynthesis, acidophilic actinobacterial SH11 strain, pine forest soil, 16S rRNA gene sequence, Streptomyces kasugaensis M338‐M1T, S. celluloflavus NRRL B‐2493T, UV–visible spectroscopy, transmission electron microscopy, Fourier transform infrared spectroscopy, zeta potential, gram positive bacteria, Staphylococcus aureus, Bacillus subtilis, gram negative bacteria, Escherichia coli, disc diffusion, wavelength 420 nm, Ag     

Antimicrobial potential and in vitro cytotoxicity study of polyvinyl pyrollidone‐stabilised silver nanoparticles synthesised from Lysinibacillus boronitolerans

The main emphasis herein is on the eco‐friendly synthesis and assessment of the antimicrobial potential of silver nanoparticles (AgNPs) and a cytotoxicity study. Silver nanoparticles were synthesised by an extracellular method using bacterial supernatant. Biosynthesised silver nanoparticles were characterised by UV‐vis spectroscopy, transmission electron microscopy (TEM), Fourier transform infrared spectroscopy, dynamic light scattering, and zeta potential analysis. The synthesised silver nanoparticles exhibited a characteristic peak at 420 nm. TEM analysis depicted the spherical shape and approximately 20 nm size of nanoparticles. Silver nanoparticles carry a charge of −33.75 mV, which confirms their stability. Biogenic polyvinyl pyrrolidone‐coated AgNPs exhibited significant antimicrobial effects against all opportunistic pathogens (Gram‐positive and Gram‐negative bacteria, and fungi). Silver nanoparticles equally affect the growth of both Gram‐positive and Gram‐negative bacteria, with a maximum inhibition zone observed at 22 mm and a minimum at 13 mm against Pseudomonas aeruginosa and Fusarium graminearum, respectively. The minimum inhibitory concentration (MIC) of AgNPs against P. aeruginosa and Staphylococcus aureus was recorded at between 15 and 20 μg/ml. Synthesised nanoparticles exhibited a significant synergistic effect in combination with conventional antibiotics. Cytotoxicity estimates using C2C12 skeletal muscle cell line via 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) test and lactate dehydrogenase assay were directly related to the concentration of AgNPs and length of exposure. On the basis of the MTT test, the IC50 of AgNPs for the C2C12 cell line was approximately 5.45 μg/ml concentration after 4 h exposure.     

Polyacrylamide–punicic acid conjugate‐based micelles for flutamide delivery in PC3 cells of prostate cancer: synthesis,characterisation and cytotoxicity studies

The aim of the present study was to synthesize a novel biopolymeric micelle based on punicic acid (PA) and polyacrylamide (PAM) for carrying chemotherapeutic drugs used in prostate cancer treatment. A polymer composite micelle was prepared by chemical conjugation between PAM and PA. The micelles were prepared by self‐assembly via film casting followed by ultrasonication method. The successful production of PAMPA copolymeric micelles was confirmed using FTIR, 1H‐NMR, and TEM. Then, flutamide was loaded in the designed nanomicelles and they were characterized. The cell cytotoxicity of the micelles was studied on PC3 cells of prostate cancer. The prepared nanomicelles showed the particle size of 88 nm, PDI of 0.246, zeta potential of −9 mV, drug loading efficiency of 94.5%, drug release of 85.6% until 10 hours in pH 7.4 and CMC of 74.13 μg/ml. The cell viability in blank nanocarriers was about 70% in PC3 cells at concentration of 25 μM. More significant cytotoxic effects were seen for flutamide loaded micelles at this concentration compared to the free drug. The results suggest that the PAMPA co‐polymeric nanomicelles can be utilized as an effective carrier to enhance the cytotoxic effects of flutamide in prostate cancer.Inspec keywords: nanoparticles, cellular biophysics, drugs, biomedical materials, drug delivery systems, colloids, hydrophilicity, pH, transmission electron microscopy, particle size, cancer, casting, toxicology, electrokinetic effects, polymer blends, proton magnetic resonance, nanomedicine, self‐assembly, nanofabrication, Fourier transform infrared spectraOther keywords: PC3 cells, chemotherapeutic drugs, prostate cancer treatment, polymer composite micelle, chemical conjugation, proton nuclear magnetic resonance, cell cytotoxicity, prepared nanomicelles, drug loading efficiency, drug release, critical micelle concentration, cell viability, cytotoxic effects, flutamideloaded micelles, flutamide delivery, polyacrylamide‐punicic acid conjugate‐based micelles, PAMPA copolymeric nanomicelles, biopolymeric micelle, PAM‐punicic acid copolymer copolymeric micelles, hydrophilic shell, self‐assembly, film casting, ultrasonication method, Fourier transform infrared spectra, transmission electron microscopy, particle size, polydisperity index, zeta potential, pH, blank nanocarriers, time 10.0 hour     

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⁺      

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     

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⁺      

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,radiolabelling, and biological assessment of folic acid‐conjugated G‐3 99m Tc‐dendrimer as the breast cancer molecular imaging agent

Hence, in this study, the authors aimed to develop a dendrimer‐based imaging agent comprised of poly(ethylene glycol) (PEG)‐citrate, technetium‐99 m (^99m Tc), and folic acid. The dendrimer‐G3 was synthesised and conjugated with folic acid, which confirmed by Fourier transform infrared, proton nuclear magnetic resonance, dynamic light scattering, and transition electron microscopy. 2,3‐bis‐(2‐methoxy‐4‐nitro‐5‐sulfophenyl)‐2H‐Tetrazolium‐5‐Carboxanilide cytotoxicity assay kit was used to measure the cellular toxicity of dendrimer. Imaging and biodistribution studies were conducted on the mice bearing tumour. The results showed that the fabricated dendrimer‐G3 has a size of 90 ± 3 nm, which was increased to 100 ± 4 nm following the conjugation with folic acid. The radiostablity investigation showed that the fabricated dendrimers were stable in the human serum at various times. Toxicity assessment confirmed no cellular toxicity against HEK‐293 cells at 0.25, 0.5, 1, 2, 4, and 8 mg/μl concentrations. The in vivo studies demonstrated that the synthesised dendrimers were able to provide a bright SPECT image applicable for tumour detection. In conclusion, the authors’ study documented the positive aspects of PEG‐citrate dendrimer conjugated with folic acid as the SPECT contrast agent for breast cancer detection.Inspec keywords: toxicology, single photon emission computed tomography, technetium, cancer, bone, polymers, biochemistry, tumours, electrospinning, biomedical materials, light scattering, cellular biophysics, Fourier transform infrared spectra, proton magnetic resonance, transmission electron microscopy, biological organsOther keywords: biodistribution, toxicity assessment, cellular toxicity, bright SPECT image, PEG‐citrate dendrimer, breast cancer molecular imaging agent, proton nuclear magnetic resonance, dendrimer‐based imaging agent, folic acid‐conjugated G‐^399m Tc‐dendrimer, dendrimer‐G3, poly(ethylene glycol)‐citrate, Fourier transform infrared spectra, dynamic light scattering, transition electron microscopy, 2,3‐bis‐(2‐methoxy‐4‐nitro‐5‐sulfophenyl)‐2H‐tetrazolium‐5‐carboxanilide cytotoxicity assay, human serum, tumour detection