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     

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

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

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⁺      

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

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

Preparation,structural characterisation and release study of novel hybrid microspheres entrapping nanoselenium,produced by green synthesis

The main goal of this study was to synthesise and characterise different formulations based on alginate and alginate/chitosan microspheres containing nanoselenium (nano‐Se) for controlled delivery applications. Nanosize elemental selenium was produced by using probiotic yogurt bacteria (Lactobacillus casei) in a fermentation procedure. The structural and morphological characterisation of the microspheres was performed by Fourier transform infrared (FTIR), X‐ray diffraction (XRD) and scanning electron microscopy (SEM) analysis. FTIR and XRD pattern indicated that was an effective cross‐linking of selenium nanoparticles within the polymeric matrix in both cases. The SEM images reveal that selenium nanoparticles are mainly exposed on the surface of alginate, in contrast to porous structure of alginate/chitosan/nano‐Se, interconnected in a regular network. This architecture type has a considerable importance in the delivery process, as demonstrated by differential pulse voltammetry. Selenium release from both matrices is pH sensitive. Moreover, chitosan blended with alginate minimise the release of encapsulated selenium, in simulated gastric fluid, and prolong the duration of release in intestinal fluid. The overall effect is the enhancement of total percentage release concomitant with the longer duration of action. The authors’ formulation based on alginate/chitosan is a convenient matrix to be used for selenium delivery in duodenum, caecum and colon.Inspec keywords: organic‐inorganic hybrid materials, nanocomposites, blending, filled polymers, nanoparticles, nanofabrication, nanomedicine, biomedical materials, drug delivery systems, microorganisms, biological organs, selenium, polymer blends, fermentation, scanning electron microscopy, X‐ray diffraction, Fourier transform infrared spectra, surface morphology, nanoporous materials, porosity, pH, voltammetry (chemical analysis), encapsulationOther keywords: structural characterisation, hybrid microspheres entrapping nanoselenium, green synthesis, alginate‐chitosan microspheres, controlled delivery applications, nanosize elemental selenium, probiotic yogurt bacteria, Lactobacillus casei, fermentation, scanning electron microscopy, morphological characterisation, SEM, Fourier transform infrared spectra, FTIR, XRD, X‐ray diffraction, selenium nanoparticles, polymeric matrix, porous structure, differential pulse voltammetry, pH, blending, encapsulated selenium, simulated gastric fluid, intestinal fluid, total percentage release concomitant, duodenum, caecum, colon, Se     

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

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

Biosynthesis and characterisation of nano‐silica as potential system for carrying streptomycin at nano‐scale drug delivery

A growing trend within nanomedicine has been the fabrication of self‐delivering supramolecular nanomedicines containing a high and fixed drug content ensuring eco‐friendly conditions. This study reports on green synthesis of silica nanoparticles (Si‐NPs) using Azadirachta indica leaves extract as an effective chelating agent. X‐ray diffraction analysis and Fourier transform‐infra‐red spectroscopic examination were studied. Scanning electron microscopy analysis revealed that the average size of particles formed via plant extract as reducing agent without any surfactant is in the range of 100–170 nm while addition of cetyltrimethyl ammonium bromide were more uniform with 200 nm in size. Streptomycin as model drug was successfully loaded to green synthesised Si‐NPs, sustain release of the drug from this conjugate unit were examined. Prolong release pattern of the adsorbed drug ensure that Si‐NPs have great potential in nano‐drug delivery keeping the environment preferably biocompatible, future cytotoxic studies in this connection is helpful in achieving safe mode for nano‐drug delivery.Inspec keywords: silicon compounds, nanofabrication, nanomedicine, drug delivery systems, nanoparticles, X‐ray diffraction, Fourier transform infrared spectra, scanning electron microscopyOther keywords: nanosilica, streptomycin, nanoscale drug delivery, nanomedicine, silica nanoparticles, Azadirachta indica leaves extract, X‐ray diffraction analysis, Fourier transform‐infrared spectroscopy, scanning electron microscopy, cetyltrimethyl ammonium bromide, SiO₂      

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     

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     

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     

Alkaline treatment effect on the properties of in‐situ synthesised ZnO nanoparticles on cotton fabric

In this study, an in‐situ approach was used to synthesise zinc oxide nanoparticles on the surface of cotton fabric. The effect of alkaline pre‐ and after‐treatment and Zn²⁺ concentration was studied on the morphological, structural, thermal, photocatalytic, and antibacterial properties of loaded cotton fabrics. Scanning electron microscopy, energy dispersive X‐ray spectroscopy, X‐ray diffractometer, thermogravimetric analysis, and attenuated total reflection Fourier transform infrared spectrometer were used to characterise the properties of loaded cotton fabrics. Alkaline after‐treatment of cotton fabric presented more dispersed zinc oxide nanoparticles, and an increase in Zn²⁺ concentration led to form agglomerated nanoparticles on the surface of cotton fibres. The loaded cotton fabrics with zinc oxide nanoparticles presented an inhibition zone against Staphylococcus aureus and Escherichia coli. In addition, the stain of methylene blue on the surface of loaded samples was degraded after irradiated under visible light.Inspec keywords: nanofabrication, zinc compounds, II‐VI semiconductors, nanoparticles, nanomedicine, antibacterial activity, catalysis, photochemistry, cotton fabrics, scanning electron microscopy, X‐ray chemical analysis, X‐ray diffraction, thermal analysis, attenuated total reflection, Fourier transform infrared spectroscopy, microorganisms, materials preparationOther keywords: alkaline treatment effect, in‐situ synthesised ZnO nanoparticles, alkaline pretreatment, alkaline after‐treatment, Zn²⁺ concentration, morphological property, structural property, thermal property, photocatalytic property, antibacterial property, loaded cotton fabrics, scanning electron microscopy, energy dispersive X‐ray spectroscopy, X‐ray diffractometer, thermogravimetric analysis, attenuated total reflection Fourier transform infrared spectrometer, agglomerated nanoparticles, zinc oxide nanoparticles, inhibition zone, Staphylococcus aureus, Escherichia coli, methylene blue, visible light, ZnO     

Synthesis and characterisation of PEG modified chitosan nanocapsules loaded with thymoquinone

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

DOC‐LS,a new liposome for dermal delivery,and its endocytosis by HaCaT and CCC‐ESF‐1 cells

The main objective of this work was to investigate the uptake channels of skin cells through which coumarin 6, transported by deoxycholate‐mediated liposomes (DOC‐LS), was internalised; this was also compared against the action of conventional LS. Coumarin 6‐loaded DOC‐LS and LS were characterised for size distribution, zeta potential, and shape, and analysed in vitro in human epidermal immortal keratinocyte (HaCaT) (epidermal) and human embryonic skin fibroblast (CCC‐ESF‐1) (dermal) cell lines. Various endocytosis inhibitors were incubated with cells treated with the nanocarriers. Flow cytometry results indicated that HaCaT and CCC‐ESF‐1 cells internalise the tested preparations through pinocytotic vesicles, macropinocytosis, clathrin‐mediated endocytic pathways, and via lysosomes, which consume a considerable amount of energy. The endocytosis pathways of DOC‐LS and LS showed no difference. This study provides a basis for the application of LS being combined with a microneedle system for efficient intracellular drug delivery, targeting cutaneous histocyte disorders.Inspec keywords: drugs, nanoparticles, lipid bilayers, nanomedicine, biomedical materials, electrokinetic effects, biomembrane transport, drug delivery systems, skin, organic compoundsOther keywords: dermal delivery, CCC‐ESF‐1 cells, skin cells, deoxycholate‐mediated liposomes, coumarin 6‐loaded DOC‐LS, endocytosis inhibitors, clathrin‐mediated endocytic pathways, endocytosis pathways, HaCaT cell lines, size distribution, zeta potential, nanocarriers, flow cytometry, pinocytotic vesicles, macropinocytosis, microneedle system, efficient intracellular drug delivery, targeting cutaneous histocyte disorders     

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

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

Docetaxel‐loaded solid lipid nanoparticles: a novel drug delivery system

Over the past few years, taxanes have emerged as a new class of anticancer drugs. Docetaxel (DTX) the prototype of this class has been approved for the treatment of broad range of cancers. However, to date the commercial preparation of DTX (Taxotere^®) is accompanying adverse side effects, intolerance, and poor solubility, which can be overcome by encapsulating them using solid lipid nanoparticles (SLNs). SLNs represent versatile delivery system of drugs with newer forms such as polymer–solid lipid hybrid, surface modified and long circulating nanoparticles bringing forth improved prospects for cancer chemotherapy. In this review, the authors have discussed the current uses of various SLNs formulations of DTX with key emphasis on controlled and site‐specific drug delivery along with enhanced antitumour activity elucidated via in vitro and in vivo studies. Furthermore, the review article highlights few approaches that can be used in combination with existing DTX‐loaded SLNs to supplement DTX drug delivery.Inspec keywords: nanoparticles, nanomedicine, drug delivery systems, biomedical materials, cancer, reviews, tumoursOther keywords: docetaxel‐loaded solid lipid nanoparticles, drug delivery system, taxanes, anticancer drugs, Taxotere, SLN encapsulation, polymer‐solid lipid hybrid, surface modified nanoparticles, long circulating nanoparticles, chemotherapy, review     

RES‐loaded pegylated CS NPs: for efficient ocular delivery

The objective of this study is to develop resveratrol (RES) loaded polyethylene glycols (PEGs) modified chitosan (CS) nanoparticles (NPs) by ionic gelation method for the treatment of glaucoma. While increasing the concentration of PEG, the particle size and polydispersity index of the formulations increased. Entrapment efficiency and RES loading (RL) of NPs decreased while increasing PEG concentration. The in vitro release of NPs showed an initial burst release of RES (45%) followed by controlled release. Osmolality of formulations revealed that the prepared NPs were iso‐osmolar with the tear. Ocular tolerance of the NPs was evaluated using hen''s egg test on the chorioallantoic membrane and it showed that the NPs were non‐irritant. RES‐loaded PEG‐modified CS NPs shows an improved corneal permeation compared with RES dispersion. Fluorescein isothiocyanate loaded CS NPs accumulated on the surface of the cornea but the PEG‐modified CS NPs crossed the cornea and reached retinal choroid. RES‐loaded PEG‐modified CS NPs reduced the intra‐ocular pressure (IOP) by 4.3 ± 0.5 mmHg up to 8 h in normotensive rabbits. These results indicate that the developed NPs have efficient delivery of RES to the ocular tissues and reduce the IOP for the treatment of glaucoma.Inspec keywords: conducting polymers, nanoparticles, nanomedicine, drug delivery systems, particle size, nanofabrication, organic compounds, biomembranes, cellular biophysics, eye, vision defects, biological tissuesOther keywords: RES‐loaded pegylated CS NP, efficient ocular delivery, resveratrol loaded polyethylene glycol modified chitosan nanoparticles, ionic gelation method, glaucoma treatment, particle size, polydispersity index, entrapment efficiency, RES loading, PEG concentration, in vitro release, osmolality formulations, ocular tolerance, hen egg testing, chorioallantoic membrane, improved corneal permeation, RES dispersion, fluorescein isothiocyanate loaded CS NP, cornea surface, reached retinal choroid, intraocular pressure, normotensive rabbits, RES delivery, ocular tissues     

Ketoconazole‐conjugated ZnO nanoparticles based semi‐solid formulation and study their impacts on skin disease

In this study, the ketoconazole‐conjugated zinc oxide (ZnO) nanoparticles were prepared in a single‐step approach using dextrose as an intermediate compound. The physical parameters confirmed the drug conjugation with ZnO and their size was around 70–75 nm. The drug loading and in vivo drug release studies indicated that the –CHO group from the dextrose increase the drug loading up to 65% and their release kinetics were also studied. The anti‐fungal studies indicated that the prepared nanoparticles exhibit strong anti‐fungal activity and the minimum concentration needed is 10 mg/ml. The nanoparticles loaded semi‐solid gel was prepared using carbopol, methylparaben, propyl paraben and propylene glycol. The in vitro penetration of the ketoconazole‐conjugated nanoparticles was studied using the skin. The results indicated that the semi‐solid gel preparations influenced the penetration and also favoured the accumulation into the skin membrane. The veterinary clinical studies indicated that the prepared gel is highly suitable for treatment of Malassezia.Inspec keywords: II‐VI semiconductors, skin, biomedical materials, antibacterial activity, wide band gap semiconductors, drug delivery systems, nanomedicine, drugs, diseases, gels, nanofabrication, nanoparticles, zinc compounds, biomembranes, veterinary medicineOther keywords: strong anti‐fungal activity, propyl paraben, propylene glycol, semisolid gel preparations, skin membrane, veterinary clinical studies, semisolid formulation, skin disease, ketoconazole‐conjugated zinc oxide nanoparticles, single‐step approach, physical parameters, drug conjugation, drug loading, release kinetics, dextrose, in vivo drug release studies, carbopol, methylparaben, in vitro penetration, Malassezia, ZnO     

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     

Poly (vinyl alcohol)/poly (acrylamide‐ co ‐diallyldimethyl ammonium chloride) semi‐IPN hydrogels for ciprofloxacin hydrochloride drug delivery

Herein, the authors developed a new and potential semi‐interpenetrating polymer network (semi‐IPN) hydrogels of poly vinyl alcohol (PVA), acryl amide and diallyldimethyl ammonium chloride employing chemical cross‐linker N, N''‐methylene bisacrylamide (NNMBA) and ammonium persulphate as an initiator by radical polymerisation. To analyse the copolymer formation between two monomers and IPN cross‐linking reaction, the resulting hydrogel was characterised by Fourier transform infrared spectroscopy and the surface morphology was analysed using scanning electron microscopy. Differential scanning calorimetry and X‐ray diffraction studies were also carried out for investigating drug loading and distribution and swelling experiments were carried out for the uptake of water. In vitro release of ciprofloxacin hydrochloride from hydrogel was performed at intestinal conditions. The amount of PVA, NNMBA and total monomer concentration was found to strongly control the drug release behaviour from the hydrogels.Inspec keywords: hydrogels, polymer blends, biomedical materials, drug delivery systems, polymerisation, Fourier transform infrared spectra, surface morphology, scanning electron microscopy, differential scanning calorimetry, X‐ray diffraction, swelling, biological organs, ammonium compoundsOther keywords: PVA‐poly(acrylamide‐co‐diallyldimethyl ammonium chloride) semiIPN hydrogels, ciprofloxacin hydrochloride drug delivery, semiinterpenetrating polymer network hydrogels, polyvinyl alcohol, acryl amide, diallyldimethyl ammonium chloride, chemical crosslinker N,N''‐methylene bisacrylamide, ammonium persulphate, radical polymerisation initiator, NNMBA, copolymer formation, IPN crosslinking reaction, Fourier transform infrared spectroscopy, surface morphology, scanning electron microscopy, differential scanning calorimetry, X‐ray diffraction, drug loading, drug distribution, swelling, water uptake, in vitro ciprofloxacin hydrochloride release, intestinal conditions, total monomer concentration, drug release behaviour