Positive regulation of biochemical parameters by tea polyphenol encapsulated solid lipid nanoparticles at in vitro and in vivo conditions

Tea polyphenols (TPPs) comprise preventive and therapeutic potentials against cancer, cardiovascular and neurological disorders. Chemical instability of TPP which leads to low bioavailability is the major constrain to its use as therapeutic agent. The authors prepared TPP encapsulated solid lipid nanoparticles (TPP‐SLNs) to increase its stability and bioefficacy. Comparison of Fourier transformed infrared spectra of unloaded SLN, free TPP and TPP‐SLN indicated encapsulation of TPP. Sustained release of TPP from TP‐SLN was observed. TPP‐SLN showed prolonged free radical scavenging activity compared with free TPP indicating protection of TPP. TPP‐SLN showed activation of Caspases‐9 and ‐3 cascades in breast cancer cell line (Michigan cancer foundation (MCF)‐7) at in vitro conditions. Biochemical parameters were altered in Ehrlich ascetic carcinoma (EAC) cell bearing mice compared with normal (uninduced) mice which were ameliorated significantly by oral feeding of TPP‐SLN. Oral administration (pre‐ and post‐treated) of TPP‐SLN in EAC bearing mice resulted in significant increase of plasma haemoglobin, glucose, superoxide dismutase and catalase when compared with EAC bearing control mice. Other biochemical parameters (cholesterol, bilirubin, triglyceride, urea, total protein, alanine aminotransferase, alkaline phosphatase and aspertate transaminase were significantly decreased on oral administration (pre‐ and post‐treated) of TPP‐SLN in EAC bearing mice.Inspec keywords: biochemistry, nanomedicine, nanoparticles, free radicals, cancer, enzymes, patient treatmentOther keywords: positive regulation, biochemical parameters, tea polyphenol encapsulated solid lipid nanoparticles, in vitro conditions, in vivo conditions, preventive potentials, therapeutic potentials, cardiovascular disorders, neurological disorders, catalase, superoxide dismutase, glucose, plasma haemoglobin, oral feeding, EAC cell, Ehrlich ascetic carcinoma, MCF‐7, breast cancer cell line, free radical scavenging activity, encapsulation, TPP‐SLN, free TPP, unloaded SLN, Fourier transformed infrared spectra, bioefficacy, therapeutic agent, low bioavailability, chemical instability     

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     

Chondroitin/doxorubicin nanoparticulate polyelectrolyte complex for targeted delivery to HepG2 cells

Chondroitin (Chn) sulphate composed of N‐acetyl galactoseamine units was chosen to target doxorubicin (DOX) to asialoglycoprotein receptors (ASGPRs) overexpressed in HepG2 cells of hepatocellular carcinoma (HCC). Two different ways of targeting the drug to the receptors were compared with each other; (i) by polyelectrolyte complex formation of DOX and Chn (DC), (ii) by loading the drug in gelatin nanoparticles (NPs) and then coating them by Chn. The characteristics of DC complexes were determined by Fourier transform infrared spectroscopy, differential scanning calorimetry and CHN analysis. The complexes and Chn coated NPs were characterised for their particles size, zeta potential, drug loading and release efficiency. The morphology of NPs was studied by transmission electron microscopy. The cytotoxicity of DC complex and Chn coated NPs were compared on HepG₂ cells by MTT assay. The results showed that the cytotoxicity of both Chn coated gelatin NPs and DC complexes were significantly increased in comparison with free DOX. However, the presence of Chn did not have significant effect on the cytotoxicity of DOX loaded NPs. It was concluded that polyelectrolyte complex of DC could successfully target the drug to the hepatic ASGPRs and may be a simple promising way for targeted drug delivery in HCC.Inspec keywords: drug delivery systems, drugs, polymer electrolytes, electrokinetic effects, nanoparticles, particle size, cellular biophysics, nanocomposites, nanofabrication, molecular biophysics, cancer, gelatin, coatings, Fourier transform infrared spectra, differential scanning calorimetry, filled polymers, transmission electron microscopy, toxicology, nanomedicine, biomedical materialsOther keywords: chondroitin‐doxorubicin nanoparticulate polyelectrolyte complex, HepG2 cells, N‐acetyl galactoseamine units, chondroitin sulphate, asialoglycoprotein receptors, hepatocellular carcinoma, drug targeted delivery, receptors, polyelectrolyte complex formation, gelatin nanoparticles, DC complexes, Fourier transform infrared spectroscopy, differential scanning calorimetry, CHN analysis, Chn coated NPs, particle size, zeta potential, drug loading, drug release efficiency, morphology, transmission electron microscopy, cytotoxicity, MTT assay, hepatic ASGPRs     

Controllable synthesis and characterisation of palladium (II) anticancer complex‐loaded colloidal gelatin nanoparticles as a novel sustained‐release delivery system in cancer therapy

Over the past few years, there have been several attempts to deliver anticancer drugs into the body. It has been shown that compared to other available carriers, colloidal gelatin nanoparticles (CGNPs) have distinct properties due to their exceptional physico‐chemical and biological characteristics. In this study, a novel water‐soluble palladium (II) anticancer complex was first synthesised, and then loaded into CGNPs. The CGNPs were synthesised through a two‐step desolvation method with an average particle size of 378 nm. After confirming the stability of the drug in the nanoparticles, the drug‐loaded CGNPs were tested for in vitro cytotoxicity against human breast cancer cells. The results showed that the average drug encapsulating efficiency and drug loading of CGNPs were 64 and 10 ± 2.1% (w/w), respectively. There was a slight shift to higher values of cumulative release, when the samples were tested in lower pH values. In addition, the in vitro cytotoxicity test indicated that the number of growing cells significantly decreased after 48 h in the presence of different concentrations of drug. The results also demonstrated that the released drug could bind to DNA by a static mechanism at low concentrations (0.57 µM) on the basis of hydrophobic and hydrogen binding interactions.Inspec keywords: cancer, drug delivery systems, drugs, palladium compounds, colloids, gelatin, nanoparticles, nanomedicine, biomedical materials, nanofabrication, nanocomposites, molecular biophysics, molecular configurations, pH, solubility, particle size, cellular biophysics, encapsulation, DNA, hydrophobicity, hydrogen bondsOther keywords: controllable synthesis, sustained‐release delivery system, cancer therapy, palladium (II) anticancer complex‐loaded colloidal gelatin nanoparticles, anticancer drug delivery, physicochemical characteristics, biological characteristics, therapeutic pathways, water‐soluble palladium (II) anticancer complex, two‐step desolvation method, particle size, drug stability, gelatin matrix, drug‐loaded CGNPs, in vitro cytotoxic activity, human breast cancer cells, average drug encapsulating efficiency, pH values, cell growth, drug concentrations, DNA, static mechanism, hydrophobic interaction, hydrogen binding interactions     

Nigella sativa oil entrapped polycaprolactone nanoparticles for leishmaniasis treatment

This study is the first to investigate the antileishmanial activities of Nigella sativa oil (NSO) entrapped poly‐ɛ ‐caprolactone (PCL) nanoparticles on Leishmania infantum promastigotes and amastigotes in vitro. NSO molecules with variable initial doses of 50, 100, 150, and 200 mg were successfully encapsulated into PCL nanoparticles identified as formulations NSO1, NSO2, NSO3, and NSO4, respectively. This process was characterised by scanning electron microscope, dynamic light scattering, Fourier transform infrared, encapsulation efficiency measurements, and release profile evaluations. The resulting synthetised nanoparticles had sizes ranging between 200 and 390 nm. PCL nanoparticles encapsulated 98% to 80% of initial doses of NSO and after incubation released approximately 85% of entrapped oil molecules after 288 h. All investigated formulations demonstrated strong antileishmanial effects on L. infantum promastigotes by inhibiting up to 90% of parasites after 192 h. The tested formulations decreased infection indexes of macrophages in a range between 2.4‐ and 4.1‐fold in contrast to control, thus indicating the strong anti‐amastigote activities of NSO encapsulated PCL nanoparticles. Furthermore, NSO‐loaded PCL nanoparticles showed immunomodulatory effects by increasing produced nitric oxide amounts within macrophages by 2–3.5‐fold in contrast to use of free oil. The obtained data showed significant antileishmanial effects of NSO encapsulated PCL nanoparticles on L. infantum promastigotes and amastigotes.Inspec keywords: antibacterial activity, drug delivery systems, nanofabrication, nitrogen compounds, nanomedicine, microorganisms, cellular biophysics, diseases, scanning electron microscopy, oils, polymers, biomedical materials, nanoparticles, encapsulation, Fourier transform infrared spectraOther keywords: encapsulation efficiency measurements, entrapped oil molecules, investigated formulations, NSO‐loaded PCL nanoparticles, Nigella sativa oil entrapped polycaprolactone nanoparticles, antileishmanial activities, poly‐ε‐caprolactone nanoparticles, scanning electron microscope, DLS, Fourier transform infrared, release profile evaluations, Leishmania infantum promastigotes, Leishmania infantum amastigotes, parasites, infection, infection indexes, macrophages, immunomodulatory effects, time 288.0 hour, time 192.0 hour, mass 50.0 mg, mass 100.0 mg, mass 150.0 mg, mass 200.0 mg, size 200.0 nm to 390.0 nm     

Fabrication of poly(D,L‐lactic acid) nanoparticles as delivery system for sustained release of L‐theanine

L‐theanine is present in tea as a unique, free, non‐protein amino acid. Due to various beneficial effects on brain activity, it is widely used as a nutraceutical. After consumption, it is rapidly absorbed and metabolised followed by excretion through urine. Therefore, the authors developed an L‐theanine delivery system by encapsulating into polymeric nanoparticles to release it slowly and make it available for a longer period of time. Poly(D, L‐lactic acid) nanoparticle (PLANP) was fabricated by the double emulsion method and L‐theanine was encapsulated into it (PLANP‐T). Spherical nanoparticles with a hydrodynamic diameter of 247 and 278 nm and surface charge of −14.5 and −25.7 mV for PLANP and PLANP‐T, respectively, were fabricated. The Fourier transform infrared spectroscopic data indicated encapsulation of L‐theanine into PLANP. The PLANP showed high L‐theanine encapsulation capacity (71.65%) with a sustained release character. The maximum release (66.3%) of L‐theanine was recorded in pH 7.3 at 48 h. The release kinetics followed the Higuchi model and the release mechanism was determined as super case‐II transport (erosion). This slow release will make it available to the target tissue for a longer period of time (sustain release effect) and will also avoid immediate metabolism and clearance from the circulation.Inspec keywords: nanomedicine, pH, polymers, nanofabrication, emulsions, biomedical materials, drug delivery systems, nanoparticles, Fourier transform infrared spectraOther keywords: brain activity, L‐theanine delivery system, polymeric nanoparticles, double emulsion method, spherical nanoparticles, surface charge, L‐theanine encapsulation capacity, poly(D, L‐lactic acid) nanoparticles, nonprotein amino acid, urine, hydrodynamic diameter, Fourier transform infrared spectroscopy, time 48.0 hour, voltage ‐25.7 mV, voltage ‐14.5 mV, size 278.0 nm, size 247.0 nm, target tissue, Higuchi model, pH     

Enhanced efficacy of clindamycin hydrochloride encapsulated in PLA/PLGA based nanoparticle system for oral delivery

Clindamycin hydrochloride (CLH) is a clinically important oral antibiotic with wide spectrum of antimicrobial activity that includes gram‐positive aerobes (staphylococci, streptococci etc.), most anaerobic bacteria, Chlamydia and certain protozoa. The current study was focused to develop a stabilised clindamycin encapsulated poly lactic acid (PLA)/poly (D,L‐lactide‐co‐glycolide) (PLGA) nano‐formulation with better drug bioavailability at molecular level. Various nanoparticle (NPs) formulations of PLA and PLGA loaded with CLH were prepared by solvent evaporation method varying drug: polymer concentration (1:20, 1:10 and 1:5) and characterised (size, encapsulation efficiency, drug loading, scanning electron microscope, differential scanning calorimetry [DSC] and Fourier transform infrared [FTIR] studies). The ratio 1:10 was found to be optimal for a monodispersed and stable nano formulation for both the polymers. NP formulations demonstrated a significant controlled release profile extended up to 144 h (both CLH‐PLA and CLH‐PLGA). The thermal behaviour (DSC) studies confirmed the molecular dispersion of the drug within the system. The FTIR studies revealed the intactness as well as unaltered structure of drug. The CLH‐PLA NPs showed enhanced antimicrobial activity against two pathogenic bacteria Streptococcus faecalis and Bacillus cereus. The results notably suggest that encapsulation of CLH into PLA/PLGA significantly increases the bioavailability of the drug and due to this enhanced drug activity; it can be widely applied for number of therapies.Inspec keywords: drug delivery systems, biomedical materials, antibacterial activity, nanoparticles, nanomedicine, microorganisms, polymers, nanofabrication, differential scanning calorimetry, encapsulation, drugs, scanning electron microscopy, Fourier transform infrared spectraOther keywords: Streptococcus faecalis, Bacillus cereus, DSC, stable nanoformulation, monodispersed nanoformulation, pathogenic bacteria, FTIR spectra, molecular dispersion, thermal behaviour, controlled release profile, Fourier transform infrared spectra, differential scanning calorimetry, scanning electron microscopy, drug loading, encapsulation efficiency, polymer concentration, solvent evaporation method, molecular level, drug bioavailability, stabilised clindamycin encapsulated poly lactic acid‐poly (D,L‐lactide‐co‐glycolide) nanoformulation, protozoa, Chlamydia, anaerobic bacteria, gram‐positive aerobes, antimicrobial activity, oral antibiotics, oral delivery, PLA‐PLGA based nanoparticle system, clindamycin hydrochloride     

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     

Pectin‐decorated selenium nanoparticles as a nanocarrier of curcumin to achieve enhanced physicochemical and biological properties

In this study, the authors developed pectin‐stabilised selenium nanoparticles (pectin‐SeNPs) for curcumin (Cur) encapsulation and evaluated their physicochemical properties and biological activities. Results showed that pectin‐SeNPs and Cur‐loaded pectin‐SeNPs (pectin‐SeNPs@Cur) exhibited monodisperse and homogeneous spherical structures in aqueous solutions with mean particle sizes of ∼61 and ∼119 nm, respectively. Cur was successfully encapsulated into pectin‐SeNPs through hydrogen bonding interactions with an encapsulation efficiency of ∼60.6%, a loading content of ∼7.4%, and a pH‐dependent and controlled drug release in vitro. After encapsulation was completed, pectin‐SeNPs@Cur showed enhanced water solubility (∼500‐fold), dispersibility, and storage stability compared with those of free Cur. Moreover, pectin‐SeNPs@Cur possessed significant free radical scavenging ability and antioxidant capacity in vitro, which were stronger than those of pectin‐SeNPs. Antitumour activity assay in vitro demonstrated that pectin‐SeNPs@Cur could inhibit the growth of HepG2 cells in a concentration‐dependent manner, and the nanocarrier pectin‐SeNPs exhibited a low cytotoxic activity against HepG2 cells. Therefore, the results suggested that pectin‐SeNPs could function as effective nanovectors for the enhancement of the water solubility, stability, and in vitro bioactivities of hydrophobic Cur.Inspec keywords: hydrogen bonds, selenium, nanoparticles, solubility, drug delivery systems, toxicology, hydrophobicity, free radicals, particle size, nanofabrication, cancer, nanomedicine, drugs, biomedical materials, encapsulation, cellular biophysics, pH, organic compoundsOther keywords: pectin‐decorated selenium nanoparticles, pectin‐stabilised selenium nanoparticles, curcumin encapsulation, Cur‐loaded pectin‐SeNPs, nanocarrier pectin‐SeNPs, physicochemical properties, biological properties, homogeneous spherical structures, monodisperse spherical structures, aqueous solutions, particle size, hydrogen bonding interactions, encapsulation efficiency, loading content, pH‐dependent drug release, in vitro controlled drug release, water solubility, free radical scavenging ability, in vitro antioxidant capacity, in vitro antitumour activity assay, HepG2 cells, cytotoxic activity, in vitro bioactivity, hydrophobic curcumin, Se     

Influence of PVP/PEG impregnated CuO NPs on physiological and biochemical characteristics of Trigonella foenum‐graecum L

Incorporation of nanoparticles into a number of manufacturing products raised the concern of environmental release via deliberate or accidental routes. Here, experiments were performed to examine the effect of copper oxide nanoparticles (CuO NPs), and polyvinyl pyrrolidone (PVP) and polyethylene glycol (PEG) impregnated CuO NPs on seed germination and growth of Trigonella foenum‐graecum L. as well as on callus induction through tissue culture technique. Seed germination frequency, length, and weight parameters did not inhibit at higher extent by application of NPs; however, copper acetate, PVP, and PEG significantly decreased the values of all parameters. In all the cases, negative effects were observed concentration‐dependent. PVP and PEG impregnated CuO were found less toxic for calli fresh and dry weight induced from leaf and stem explants. The 2, 2‐diphenyl‐1‐picrylhydrazyl reagent‐free radical scavenging activity, total antioxidative potential, and total reducing power potential along with total flavonoid and phenolic contents are found elevated in root when compared with shoot. Furthermore, impregnation of PVP and PEG on CuO NPs increases the oxidative response. The results conclude that impregnation of organic molecules on nanoparticles does not reduce the toxicity though can be exploited for enhanced production of secondary metabolites for medicinal purposes.Inspec keywords: botany, copper compounds, nanoparticles, toxicology, polymers, biochemistry, nanomedicine, biological tissues, free radical reactionsOther keywords: PVP‐PEG, physiological characteristics, biochemical characteristics, Trigonella foenum‐graecum L, copper oxide nanoparticles, polyvinyl pyrrolidone, polyethylene glycol, callus induction, tissue culture technique, seed germination frequency, weight parameters, copper acetate, leaf explants, stem explants, 2,2‐diphenyl‐1‐picrylhydrazyl reagent‐free radical scavenging activity, antioxidative potential, reducing power potential, flavonoid, phenolic contents, root, shoot, oxidative response, organic molecules, toxicity, secondary metabolites, CuO     

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     

Silver nanoparticles biologically synthesised using tea leaf extracts and their use for extension of fruit shelf life

The biosynthesis of nanoparticles (NPs) from plant extracts is important in nanotechnology because the employed methods are environmentally friendly and cost‐effective. In this study, silver NPs (AgNPs) were synthesised using Chinese tea (Oolong tea) extract. The effects of the relative content of the employed silver nitrate, the reaction temperature, the incubation time, and the tea‐to‐water ratio on the formation of the AgNPs were examined. The synthesised AgNPs were also analysed by UV–vis spectroscopy, dynamic light scattering, transmission electron microscopy, X‐ray diffraction, Fourier transform infrared spectroscopy, and thermo‐gravimetric analysis. The NPs were observed to be highly crystalline, approximately spherical, and 10–50 nm in diameter. They were also tested for their use in preserving the postharvest quality of cherry tomatoes, with good results obtained. The tea AgNP treatment was specifically found to reduce the weight loss of the tomatoes, as well as changes in their total soluble solids, vitamin C, and titratable acid contents. The findings of this study indicate that postharvest tea AgNP treatment affords a clean, safe, high‐quality, and environmentally friendly method for extending the shelf life of fruits.Inspec keywords: silver, nanoparticles, nanofabrication, ultraviolet spectra, visible spectra, light scattering, transmission electron microscopy, X‐ray diffraction, Fourier transform infrared spectra, thermal analysisOther keywords: silver nanoparticles, tea leaf extracts, fruit shelf life, Chinese tea extract, Oolong tea, silver nitrate, reaction temperature, incubation time, tea‐water ratio, UV‐vis spectroscopy, dynamic light scattering, transmission electron microscopy, X‐ray diffraction, Fourier transform infrared spectroscopy, thermo‐gravimetric analysis, cherry tomatoes, Ag     

Development of nanoformulation of picroliv isolated from Picrorrhiza kurroa

Picroliv, a mixture of picroside I and kutkoside isolated from rhizome of Picrorrhiza kurroa has been reported for many pharmaceutical properties such as hepatoprotective, anticholestatic, antioxidant and immune‐modulating activity. However, picroliv possessed lesser efficacy due to its poor aqueous solubility and lesser bioavailability. To find solution, picroliv was loaded into biodegradable poly lactic acid nanoparticles (PLA NPs) using solvent evaporation method. The picroliv‐loaded PLA NPs were characterised by UV–vis spectroscopy, atomic force microscopy, transmission electron microscopy, Fourier transform infrared and Zeta sizer. The size of picroliv‐loaded PLA NPs was 182 ± 20 nm. Zeta potential of picroliv‐loaded PLA NPs was −23.5 mV, indicated their good stability. In vitro picroliv release from picroliv‐loaded PLA NPs showed an initial burst release followed by slow and sustained release. The efficacy of picroliv‐loaded PLA NPs was assessed against KB cell lines. Blank PLA NPs showed no cytotoxicity on KB cells. The picroliv‐loaded PLA NPs showed more cytotoxic activity on KB cells as compared to the pure drug. Hence, the developed picroliv nanoformulation would find potential application in pharma‐sector.Inspec keywords: drugs, nanomedicine, nanofabrication, biodegradable materials, nanoparticles, biomedical materials, evaporation, ultraviolet spectra, visible spectra, atomic force microscopy, transmission electron microscopy, Fourier transform infrared spectra, electrokinetic effects, drug delivery systems, cellular biophysics, toxicologyOther keywords: nanoformulation development, Picrorrhiza kurroa, picroside I‐kutkoside mixture, rhizome, pharmaceutical properties, hepatoprotective activity, anticholestatic activity, antioxidant activity, immune‐modulating activity, aqueous solubility, bioavailability, biodegradable poly lactic acid nanoparticles, solvent evaporation method, picroliv‐loaded PLA NPs, UV‐visible spectroscopy, atomic force microscopy, transmission electron microscopy, Fourier transform infrared spectra, zeta‐sizer, in vitro picroliv release, KB cell lines, initial burst release, cytotoxic activity, picroliv nanoformulation, pharma‐sector     

Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

The present study aimed to develop a surface‐modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE‐40‐S) to improve the oral bioavailability of poorly water‐soluble Biopharmaceutics Classification System class‐II drug like tamoxifen (TMX). Also aimed to screen the most influential factors affecting the particle size (PS) using Taguchi (L₁₂ (2¹¹)) orthogonal array design (TgL₁₂ OA). Then, to optimize the TMX loaded POE‐40‐S (P) surface‐modified NLCs (TMX‐loaded‐PEG‐40‐S coated NLC (PNLCs) or PNLCs) by central composite design (CCD) using a four‐factor, five‐level model. The most influential factors affecting the PS was screened and optimized. The in‐vitro study showed that increased drug‐loading (DL) and encapsulation efficiency (EE), decreased PS and charge, sustained drug release for the prolonged period of the time with good stability and suppressed protein adsorption. The Ex‐vivo study showed that decreased mucous binding with five‐fold enhanced permeability of PNLC formulation after surface modification with POE‐40‐S. The in‐vitro cytotoxicity study showed that the blank carrier is biocompatible and cytotoxicity of the formulation was dependent on the concentration of the drug. Finally, it can be concluded that the surface‐modified PNLCs formulation was an effective, biocompatible, stable formulation in the enhancement of dissolution rate, solubility, stability with reduced mucus adhesion and increased permeability thereby which indicates its enhanced oral bioavailability.Inspec keywords: nanoparticles, cellular biophysics, solubility, drug delivery systems, toxicology, adsorption, adhesion, dissolving, biomedical materials, encapsulation, polymers, proteins, nanomedicine, permeability, particle size, electrokinetic effectsOther keywords: water‐soluble BCS class‐II, TgL₁₂ OA, TMX‐loaded POE‐40‐S surface‐modified NLC, surface‐modified PNLC formulation, lipid‐based NLC system, oral bioavailability, stable formulation, biocompatible formulation, blank carrier, in vitro cytotoxicity, surface modification, PNLC formulation, drug release, central composite design, orthogonal array design, encapsulation efficiency, steric stabilisation effect, particle size, dissolution rate, polyoxyethylene stearate, surface‐modified biocompatible carrier system, systemic toxicity, water‐soluble drug, tamoxifen‐loaded surface‐modified nanostructured lipid carrier     

Apoptotic efficacy and antiproliferative potential of silver nanoparticles synthesised from aqueous extract of sumac (Rhus coriaria L.)

Currently, nanotechnology and nanoparticles (NPs) are recognised due to their extensive applications in medicine and the treatment of certain diseases, including cancer. Silver NPs (AgNPs) synthesised by environmentally friendly method exhibit a high medical potential. This study was conducted to determine the cytotoxic and apoptotic effects of AgNPs synthesised from sumac (Anacardiaceae family) fruit aqueous extract (AgSu/NPs) on human breast cancer cells (MCF‐7). The anti‐proliferative effect of AgSu/NPs was determined by MTT assay. The apoptotic properties of AgSu/NPs were assessed by morphological analysis and acridine orange/propidium iodide (AO/PI) and DAPI staining. The mechanism of apoptosis induction in treated cells was investigated using molecular analysis. Overall results of morphological examination and cytotoxic assay revealed that AgSu/NPs exert a concentration‐dependent inhibitory effect on the viability of MCF‐7 cells (IC50 of ∼10 µmol/48 h). AO/PI staining confirmed the occurrence of apoptosis in cells treated with AgSu/NPs. In addition, molecular analysis demonstrated that the apoptosis in MCF‐7 cells exposed to AgSu/NPs was induced via up‐regulation of Bax and down‐regulation of Bcl‐2. These findings suggested the potential use of AgSu/NP as cytotoxic and pro‐apoptotic efficacy and its possible application in modern medicine for treating certain disorders, such as cancer.Inspec keywords: nanoparticles, silver, nanomedicine, biomedical materials, toxicology, cancer, molecular biophysics, proteins, biochemistry, cellular biophysics, nanofabricationOther keywords: Ag, Bcl‐2 down‐regulation, Bax up‐regulation, MCF‐7 cell viability, concentration‐dependent inhibitory effect, cytotoxic assay, molecular analysis, DAPI staining, acridine orange‐propidium iodide staining, morphological analysis, MTT assay, human breast cancer cells, sumac fruit aqueous extract, Anacardiaceae family, cytotoxic effects, drug delivery function, diseases, Rhus coriaria L, silver nanoparticles, antiproliferative potential, apoptotic efficacy     

Formulation and characterisation of poly(lactic‐co‐glycolic acid) encapsulated clove oil nanoparticles for dental applications

This study investigated synthesis and characterisation of Nano‐PLGA (poly(lactic‐co‐glycolic acid))/CO (clove‐oil) nanoparticles. The delivery of drug‐loaded nanoparticles to demineralised dentin substrates and their morphological association with a two‐step etch‐and‐rinse adhesive system was studied. The effect of Nano‐PLGA/CO pretreatment on micro‐tensile bond strength of resin‐dentin bonding was scrutinised. This study employed CO‐containing PLGA nanoparticles as a delivery vehicle for sustainable drug release inside dentinal‐tubules for potential dental applications. Emulsion evaporation resulted in uniformly distributed negatively‐charged Nano‐PLGA/Blank and Nano‐PLGA/CO nanoparticles. Scanning electron microscopy/ transmission electron microscopy revealed even spherical nanoparticles with smooth texture. High CO‐loading and encapsulation were achieved. Moreover, controlled CO‐release was evidenced after 15 days, in‐vitro and ex‐vivo. Nanoparticles exhibited low initial toxicity towards human mesenchymal stem cells with excellent antibacterial properties. Nanoparticles penetration inside dentinal‐tubules indicated a close correlation with resin‐tags. Nano‐PLGA/CO pretreatment indicated reduction in short‐term bond strength of resin‐dentin specimens. Nano‐PLGA/CO as model drug‐loaded nanoparticles showed excellent metric and antibacterial properties, low toxicity and sustained CO release. However, the loading of nanoparticles with CO up to ∼10 mg (Nano‐PLGA/CO:10) did not adversely affect short‐term bond strength values. This drug‐delivery strategy could be further expanded to deliver other pulp‐sedative agents and medications with other dental relevance.Inspec keywords: nanoparticles, dentistry, encapsulation, filled polymers, nanofabrication, nanocomposites, nanomedicine, biomedical materials, drug delivery systems, adhesives, tensile strength, biomechanics, resins, proteins, molecular biophysics, biochemistry, emulsions, evaporation, scanning electron microscopy, transmission electron microscopy, texture, cellular biophysics, antibacterial activity, bonds (chemical)Other keywords: poly(lactic‐co‐glycolic acid) encapsulated clove oil nanoparticles, dental applications, drug‐loaded nanoparticle delivery, demineralised dentin substrates, morphological association, two‐step etch‐and‐rinse adhesive system, simulated pulpal pressure, nanoPLGA‐CO pretreatment, microtensile bond strength, resin‐dentin bonded specimens, CO‐containing PLGA nanoparticles, delivery vehicle, sustainable drug release, dentinal‐tubules, potential dental applications, emulsion evaporation, uniformly‐distributed negatively‐charged nanoPLGA‐blank, scanning electron microscopy‐transmission electron microscopy, spherical nanoparticles, smooth texture, high CO‐loading, controlled CO‐release, human mesenchymal stem cells, antibacterial properties, antibiofilm properties, deep nanoparticle penetration, resin‐tags, short‐term bond strength, resin‐dentin specimens, metric properties, antibacterial properties, sustained CO release, pulp‐sedative agents, time 15 d     

Design and fabrication of drug‐eluting polymeric thin films for applications in ophthalmology

To study the development, characterisation, and drug release of one‐ and two‐layered thin films based on organic polymers [poly(D,L‐lactide‐co ‐glycolide) lactide:glycolide (65:35), poly(D,L‐lactide‐co ‐glycolide) lactide:glycolide (75:25), and polycaprolactone] and dexamethasone. To examine their applicability for intraocular lenses (IOLs) and function in intraocular drug delivery systems. Four series of thin films, single and double‐layer, were prepared by the spin‐coating method on a silicon substrate. The films were studied using atomic force microscopy and spectroscopic ellipsometry. The release rate of dexamethasone was studied for a period of ten weeks. Series A and C demonstrated the formation of large dexamethasone aggregates. The monolayer films of series C and D formed pores, in agreement with previous findings. The spectroscopic ellipsometry study demonstrated that the samples were transparent. The drug release study demonstrated that dexamethasone was released during the first 6 weeks at a desirable rate. The films exhibited properties suitable for use in intraocular drug delivery systems. The single‐layer thin films demonstrated a sufficient encapsulation of dexamethasone and appropriate release of the therapeutic substance. Further studies are necessary to investigate the possibility of developing the films directly on the surface of the IOL.Inspec keywords: eye, ellipsometry, spin coating, biomedical materials, polymer films, encapsulation, atomic force microscopy, drug delivery systems, aggregation, drugs, monolayers, ophthalmic lenses, polymer blendsOther keywords: IOL, intraocular drug delivery systems, spin‐coating method, atomic force microscopy, dexamethasone aggregates, monolayer films, organic polymers, spectroscopic ellipsometry, drug release, drug‐eluting polymeric thin films, ophthalmology, one‐layered thin films, two‐layered thin films, poly(D,L‐lactide‐co‐glycolide), polycaprolactone, intraocular lenses, dexamethasone release rate, dexamethasone encapsulation, time 6.0 week, Si     

Preparation and characterisation of atorvastatin and curcumin‐loaded chitosan nanoformulations for oral delivery in atherosclerosis

Atorvastatin known to be a potential inhibitor of HMG‐CoA reductase involved in the synthesis of cholesterol. It is touted as miracle drug due to its profound effect in decreasing the low‐density lipoproteins in blood. Unfortunately, the high dosage used poses side‐effects relatively in comparison to other statins. On the other hand, curcumin has a diverse therapeutic potential in health and disease. However, the poor aqueous solubility and low bioavailability hinders the therapeutic potential of it when administrated orally. Therefore, it was thought to minimise the frequency of atorvastatin doses to avoid the possibility of drug resistance and also to overcome the limitations of curcumin for desirable therapeutic effects by using nanocarriers in drug delivery. In this investigation, synergistic effect of atorvastatin and curcumin nanocarriers was encapsulated by chitosan polymer. The chitosan nanocarriers prepared by ionic gelation method were characterised for their particle size, zeta potential, and other parameters. The drug‐loaded nanocarriers exhibited good encapsulation efficiency (74.25%) and showed a slow and sustained release of atorvastatin and curcumin 60.36 and 61.44%, respectively, in a span of 48 h. The drug‐loaded nanocarriers found to be haemocompatible and qualified for drug delivery in atherosclerosis.Inspec keywords: nanomedicine, drug delivery systems, diseases, cardiovascular system, enzymes, nanofabricationOther keywords: atorvastatin chitosan nanoformulation, curcumin‐loaded chitosan nanoformulation, oral delivery, atherosclerosis, potential inhibitor, HMG‐CoA reductase, cholesterol synthesis, miracle drug, low‐density lipoproteins, blood, diverse therapeutic potential, poor aqueous solubility, low bioavailability, drug resistance, nanocarriers, ionic gelation method, particle size, zeta potential, encapsulation efficiency     

Synthesis and characterisation of liposomal doxorubicin with loaded gold nanoparticles

Developing nanostructures for cancer treatment is growing significantly. Liposomal doxorubicin is a drug that is used in the clinic and represents a lot of benefits over doxorubicin. The development of multifunctional liposomes with different cancer treatment capability enables broader applications of doxorubicin chemotherapy. Many efforts were carried to prepare more effective liposomal formulation through loading gold nanoparticles (GNPs) in the formulation. Here, GNPs with an average size of 6 nm were loaded in liposomal formulation alongside doxorubicin. The hydrodynamic diameter of final formulation was 177.3 ± 33.9 nm that in comparison with liposomes without GNPs (112.5 ± 10.3 nm), GNPs‐loaded liposomes showed the bigger hydrodynamic diameter. GNPs‐loaded liposomes are slightly positively charged (4.4 ± 1.1 mV), while liposomes without loading the GNPs were negatively charged (−18.5 ± 1.6 mV). Doxorubicin was loaded in this formulation through active loading technique. Doxorubicin loading efficiency in gold‐loaded liposomes is slightly lesser than liposomes without GNPs, but still considerably high in comparison to passive loading techniques.Inspec keywords: nanofabrication, drugs, nanomedicine, gold, cancer, lipid bilayers, drug delivery systems, nanoparticles, crystal growth from solutionOther keywords: liposomal doxorubicin, multifunctional liposomes, doxorubicin chemotherapy, active loading technique, doxorubicin loading efficiency, gold‐loaded liposomes, passive loading techniques, gold nanoparticles, cancer treatment, liposomal formulation, GNP‐loaded liposomes, hydrodynamic diameter     

Green synthesis of silver nanoparticles using bovine skin gelatin and its antibacterial effect on clinical bacterial isolates

Nanoparticles are being increasingly used in day‐to‐day life. Therefore, concerns have been raised regarding their interactions with the surrounding environment. This study focused on a simple green method for synthesizing silver nanoparticles (Ag‐NPs) in an autoclave at 15 psi (103 kPa) and 121°C. An aqueous solution of AgNO₃ as a precursor of Ag‐NPs and gelatin (type B) reducing and/or stabilizing (capping) agent were used. The effect of various AgNO₃ concentrations of certain gelatin concentration and various gelatin concentrations at constant AgNO₃ concentration, and autoclaving time, was studied. UV‐Vis spectra ascribed that the presence of localized surface plasmon resonance (SPR) of the synthesized Ag‐NPs. TEM images and the selected area of electron diffraction confirmed, the formation of Ag‐NPs with a diameter of approximately 5 ±0.35 nm. Furthermore, FT‐IR revealed that a gelatin polymer matrix stabilized the synthesized Ag‐NPs. The Well diffusion assay was used to test the effect of Ag‐NPs on six clinical bacterial isolates, where Gram positive bacteria were more susceptible to Ag‐NPs than Gram negative bacteria. Therefore, Ag‐NPs capped by gelatin have remarkable potential effect as an antibacterial agent, and they not only have various medical applications but can also be used in biological, pharmaceutical and industrial fields.Inspec keywords: silver, nanoparticles, nanomedicine, antibacterial activity, microorganisms, nanofabrication, skin, gelatin, ultraviolet spectra, visible spectra, surface plasmon resonance, transmission electron microscopy, electron diffraction, Fourier transform infrared spectra, polymers, biomedical materialsOther keywords: green synthesis, silver nanoparticles, bovine skin gelatin, antibacterial effect, clinical bacterial isolates, autoclave, reducing agent, stabilising agent, ultraviolet‐visible spectra, localised surface plasmon resonance, transmissions electron microscope images, electron diffraction, Fourier transform infrared spectroscopy, gelatin polymer matrix, well diffusion assay, gram negative bacteria, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, gram positive bacteria, Bacillus megaterium, Streptococcus pyogenes, Staphylococcus aureus, temperature 121 degC, Ag