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1.
Pharmaceutics ; 15(9)2023 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-37765277

RESUMO

Applying a formulation on the skin represents a patient-acceptable and therapeutically effective way to administer drugs locally and systemically. However, the stratum corneum stands as an impermeable barrier that only allows a very limited number of drugs to be distributed in the underlying tissues, limiting the feasibility of this administration route. Microneedle arrays are minimally invasive platforms that allow the delivery of drugs within/across the skin through the temporary mechanical disruption of the stratum corneum. In this work, microneedle arrays were combined with nanosuspensions, a technology for solubility enhancement of water insoluble molecules, for the skin delivery of diclofenac. Nanosuspensions were prepared using a top-down method and loaded in the tips of 500 µm or 800 µm high microneedles. The quality of the combined platform was assessed using electron microscopy and spectroscopic and calorimetry techniques, demonstrating the ability to load high amounts of the hydrophobic drug and the compatibility between excipients. Lastly, the application of nanosuspension-loaded microneedles on the skin in vitro allowed the delivery of diclofenac within and across the stratum corneum, proving the potential of this combination to enhance skin delivery of scarcely soluble drugs.

2.
Molecules ; 28(16)2023 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-37630267

RESUMO

Polymeric permselective films are frequently used for amperometric biosensors to prevent electroactive interference present in the target matrix. Phenylenediamines are the most commonly used for the deposition of shielding polymeric films against interfering species; however, even phenolic monomers have been utilized in the creation of these films for microsensors and biosensors. The purpose of this paper is to evaluate the performances of electrosynthesized polymers, layered by means of constant potential amperometry (CPA), of naturally occurring compound zingerone (ZING) and its dimer dehydrozingerone (ZING DIM), which was obtained by straight oxidative coupling reaction. The polymers showed interesting shielding characteristics against the main interfering species, such as ascorbic acid (AA): actually, polyZING exhibited an AA shielding aptitude comprised between 77.6 and 99.6%, comparable to that obtained with PPD. Moreover, a marked capability of increased monitoring of hydrogen peroxide (HP), when data were compared with bare metal results, was observed. In particular, polyZING showed increases ranging between 55.6 and 85.6%. In the present work, the molecular structures of the obtained polymers have been theorized and docking analyses were performed to understand their peculiar characteristics better. The structures were docked using the Lamarckian genetic algorithm (LGA). Glutamate biosensors based on those polymers were built, and their performances were compared with biosensors based on PPD, which is the most widespread polymer for the construction of amperometric biosensors.


Assuntos
Ácido Ascórbico , Guaiacol , Ácido Glutâmico , Polímeros
3.
Int J Pharm ; 625: 122079, 2022 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-35932932

RESUMO

Pomalidomide (POM) is an FDA-approved immunomodulatory imide drug (IMiDs) an it is effectively used in the treatment of multiple myeloma. IMiDs are analogs of the drug thalidomide and they have been repurposed for the treatment of several diseases such as psoriatic arthritis and Kaposi Sarcoma. In recent years, IMiDs have been also evaluated as a new treatment for neurological disorders with an inflammatory and neuroinflammatory component. POM draws particular interest for its potent anti-TNF-α activity at significantly lower concentrations than the parent compound thalidomide. However, POM's low water solubility underpins its low gastrointestinal permeability resulting in irregular and poor absorption. The purpose of this work was to prepare a POM nanocrystal-based formulation that could efficiently improve POM's plasma and brain concentration after intraperitoneal injection. POM nanocrystals prepared as a nanosuspension by the media milling method showed a mean diameter of 219 nm and a polydispersity index of 0.21. POM's nanocrystal solubility value (22.97 µg/mL) in phosphate buffer was about 1.58 folds higher than the POM raw powder. Finally, in vivo studies conducted in adult Male Sprague-Dawley rats indicated that POM nanocrystal ensured higher and longer-lasting drug levels in plasma and brain when compared with POM coarse suspension.


Assuntos
Nanopartículas , Talidomida , Animais , Disponibilidade Biológica , Masculino , Nanopartículas/química , Ratos , Ratos Sprague-Dawley , Roedores , Solubilidade , Talidomida/análogos & derivados , Inibidores do Fator de Necrose Tumoral
4.
Pharmaceutics ; 14(5)2022 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-35631674

RESUMO

Needle-free liquid jet injectors are medical devices used to administer pharmaceutical solutions through the skin. Jet injectors generate a high-speed stream of liquid medication that can puncture the skin and deliver the drug to the underlying tissues. In this work, we investigated the feasibility of using liquid jet injectors to administer nanosuspensions, assessing the impact of the jet injection on their pharmaceutical and physicochemical properties. For this purpose, the model drug diclofenac was used to prepare a set of nanosuspensions, stabilized by poloxamer 188, and equilibrated at different pHs. The hydrodynamic diameter and morphology of the nanocrystals were analyzed before and after the jet injection across porcine skin in vitro, together with the solubility and release kinetics of diclofenac in a simulated subcutaneous environment. The efficacy of the jet injection (i.e., the amount of drug delivered across the skin) was evaluated for the nanosuspension and for a solution, which was used as a control. Finally, the nanosuspension was administered to rats by jet injector, and the plasma profile of diclofenac was evaluated and compared to the one obtained by jet injecting a solution with an equal concentration. The nanosuspension features were maintained after the jet injection in vitro, suggesting that no structural changes occur upon high-speed impact with the skin. Accordingly, in vivo studies demonstrated the feasibility of jet injecting a nanosuspension, reaching relevant plasma concentration of the drug. Overall, needle-free jet injectors proved to be a suitable alternative to conventional syringes for the administration of nanosuspensions.

5.
Spectrochim Acta A Mol Biomol Spectrosc ; 265: 120398, 2022 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-34563743

RESUMO

This paper describes a case study of a linen yarn found inside a spiral bronze necklace fragment during an excavation campaign in la Prisgiona, a Nuragic settlement, near Arzachena, in north-east Sardinia. The site is one of the most interesting settlements of the Nuragic period. Abandoned after a fire, it was no longer inhabited, thus allowing the preservation of the Nuragic stratigraphy. The necklace fragments are part of a votive burial and the yarn is the only known textile material belonging to the Bronze Age period from Sardinia. The uniqueness of the finding, in the rare corpus of prehistoric textile materials, and the small amount of it available do not allow conventional analyses and requires a non-invasive/micro-invasive method. The protocol established to preserve as much as possible the entirety of the object, involving polarize light microscopy, portable ATR-FTIR, SEM-EDS, micro X-ray Computer Tomography and XRD, was successfully used to extend knowledge about the materials and techniques of this civilisation.


Assuntos
Têxteis , História Antiga , Itália
6.
Antioxidants (Basel) ; 10(9)2021 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-34573118

RESUMO

This work provides companies in the fresh-cut produce sector with an Ascorbate Bluetooth© Analyzer (ABA), a screen-printed sensor-based device for ascorbic acid (AA) detection, for quality control all along the supply chain. The amperometric detection of AA on fresh and fresh-cut parsley, under correct and incorrect storage temperature, allowed us to investigate the kinetics of AA decay in response to oxidative stress. The role of ascorbate oxidase (AOx) and ascorbate peroxidase (APx) was studied. ABA was used in situ by unskilled personnel. Treatments influenced AA decay kinetics, which were linear in fresh parsley, and non-linear in fresh-cut. Two hours at 28 °C immediately after chopping, the resilience of the fresh-cut parsley was reduced, even though the cold chain was restored. Two hours at -2 °C caused a rapid loss of AA until its complete decay after 72 h. Significant differences between treatments were observed in both the expression and activity of AOx and APx. ABA registered sudden changes of parsley AA following unpredicted variations of temperature during processing or transport. It was useful to remedy the effects of unexpected flaws in the cold chain, which can be proposed for quality preservation of different fresh-cut produce.

7.
Pharmaceutics ; 13(8)2021 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-34452261

RESUMO

Curcumin has shown a potential extraordinary activity as an add-on ingredient in asthma treatment, due to its immunomodulatory and anti-inflammatory mechanism of action. However, its low water solubility and bioavailability lead to a poor therapeutic effect, which can be overcome by its formulation as nanocrystals. The aim of this study was to prepare a multicomponent formulation for the delivery of curcumin (CUR) and beclomethasone dipropionate (BDP) into the lungs as water-based nanosuspensions (NS). Single component formulations (CUR-NS, BDP-NS) and a multicomponent formulation (CUR+BDP-NS) were prepared through a wet ball media milling technique, using P188 as a non-toxic stabilizer. Characterization was carried out in terms of size, size distribution, zeta potential, nanocrystals morphology, and solid-state properties. Moreover, the inhalation delivery efficiency was studied with Next Generation Impactor (NGI, Apparatus E Ph. Eu). CUR-NS was optimized and showed a long-term stability and improved nanocrystals apparent solubility. The three formulations exhibited a nanocrystal mean diameter in the range of 200-240 nm and a homogenous particle size distribution. Aggregation or sedimentation phenomena were not observed in the multicomponent formulation on 90 days storage at room temperature. Finally, the nebulization tests of the three samples showed optimal aerodynamic parameters and MMAD < 5 µm.

8.
Pest Manag Sci ; 77(7): 3508-3518, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33837628

RESUMO

BACKGROUND: Low water solubility of pesticide requires formulations with high levels of stabilizers and organic solvents. Moreover, only 0.1% of the applied pesticides formulation reaches the target, while 99.9% spreads in the surrounding environment. Therefore, there is the need for more efficient and environmentally sustainable alternatives. RESULTS: Zoxamide (ZO) nanosuspension was prepared through a media milling technique by using the stabilizer polysorbate 80. The thin and acicular crystals obtained, showed particle size of 227 nm, polydispersion index of 0.247 and zeta potential of -28 mV. Dimensional data and morphology of ZO nanocrystals alone, on tomato leaves and berries, were confirmed by scanning electron microscopy. The reduction in size for ZO crystals obtained after the milling process increased pesticide water solubility till 39.6 mg L-1 , about 1.6 the solubility obtained with a conventional commercial formulation. Field and dip contamination trials performed on tomato plants showed the nanosuspension's ability to increase ZO deposition and accumulation versus a coarse ZO suspension and commercial formulation, respectively. CONCLUSIONS: The nanoformulation proposed, resulted in low cost and was easy to make. Moreover, the organic solvent-free composition together with a low surfactant addition assured a minor environmental impact. Finally, the increased retention and deposition of the fungicide can reduce the amounts of ZO formulation applied to tomatoes. © 2021 Society of Chemical Industry.


Assuntos
Nanopartículas , Solanum lycopersicum , Amidas , Tamanho da Partícula , Solubilidade , Suspensões , Tecnologia
9.
Pharmaceutics ; 12(12)2020 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-33255623

RESUMO

Topical application of the anti-inflammatory drug diclofenac (DCF) reduces the severity of systemic unwanted effects compared to its oral administration. A number of transdermal formulations are available on the market and routinely used in clinical and home-care settings. However, the amount of DCF delivered across the skin remains limited and often insufficient, thus making the oral route still necessary for achieving sufficient drug concentration at the inflamed site. In attempting to improve the transdermal penetration, we explored the combined use of DCF nanosuspensions with a microneedle roller. Firstly, DCF nanosuspensions were prepared by a top-down media milling method and characterized by spectroscopic, thermal and electron microscopy analyses. Secondly, the pore-forming action of microneedle rollers on skin specimens (ex vivo) was described by imaging at different scales. Finally, DCF nanosuspensions were applied on newborn pig skin (in vitro) in combination with microneedles roller treatment, assessing the DCF penetration and distribution in the different skin layers. The relative contribution of microneedle length, nanosuspension stabilizer and application sequence could be identified by systemically varying these parameters.

10.
Food Microbiol ; 87: 103386, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31948627

RESUMO

Contamination by Listeria monocytogenes is a particularly challenging problem in the food industry due to the ability of the bacterium to develop under conditions normally used for food preservation. Here, we show that the gaseous phase of Citrus limon var pompia leaf essential oil (hereafter PLEO) exerts specific anti-Listeria activity on ricotta salata cheese stored at 5 °C. The synergic effect of gaseous PLEO treatment and refrigeration was first confirmed in vitro on L. monocytogenes strains treated for 3 h with gaseous PLEO and then stored at 5 °C. Ricotta cheese was then inoculated with L. monocytogenes strains and subjected to hurdle technology with different concentrations of gaseous PLEO. Cell counts revealed gaseous PLEO to exert a bactericidal effect on L. monocytogenes 20600 DSMZ and a bacteriostatic effect on a mix of L. monocytogenes strains. Scanning and transmission electron microscopy analyses of L. monocytogenes cells suggested that gaseous PLEO targets the bacterial cell wall and plasma membrane. Chemical analyses of the liquid and vapor phases of PLEO indicated linalyl acetate to be the predominant compound, followed by limonene and the two isomers of citral, whereas EO composition analysis, although generally in line with previous findings, showed the presence of linalyl acetate for the first time. Solid-phase microextraction coupled with gas chromatography confirmed the presence of all crude oil components in the headspace of the box.


Assuntos
Antibacterianos/farmacologia , Queijo/microbiologia , Citrus/química , Listeria monocytogenes/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Antibacterianos/química , Membrana Celular/efeitos dos fármacos , Parede Celular/efeitos dos fármacos , Listeria monocytogenes/crescimento & desenvolvimento , Óleos Voláteis/química , Folhas de Planta/química , Óleos de Plantas/química
11.
Biosensors (Basel) ; 9(3)2019 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-31366026

RESUMO

The use of amperometric biosensors has attracted particular attention in recent years, both from researchers and from companies, as they have proven to be low-cost, reliable, and very sensitive devices, with a wide range of uses in different matrices. The continuous development of amperometric biosensors, since their use involves an enzyme, is specifically aimed at keeping and increasing the catalytic properties of the loaded protein, so as to be able to use the same device over time. The present study aimed to investigate the impact of glycerol and polysaccharides, in the presence of polycationic substances to constitute a hydrogel, in enhancing the enzymatic and analytic performance of a glucose biosensor. Initially, it was possible to verify how the deposition of the starch-based hydrogel, in addition to allowing the electropolymerization of the poly(p-phenylenediamine) polymer and the maintenance of its ability to shield the ascorbic acid, did not substantially limit the permeability towards hydrogen peroxide. Moreover, different biosensor designs, loading a mixture containing all the components (alone or in combination) and the enzyme, were tested in order to evaluate the changes of the apparent enzyme kinetic parameters, such as VMAX and KM, and analytical response in terms of Linear Region Slope, highlighting how the presence of all components (starch, glycerol, and polyethyleneimine) were able to substantially enhance the performance of the biosensors. The surface analysis of the biosensors was performed by scanning electron microscope (SEM). More, it was shown that the same performances were kept unchanged for seven days, proving the suitability of this biosensor design for short- and mid-term use.


Assuntos
Glucose/análise , Glicerol/química , Polissacarídeos/química , Técnicas Biossensoriais , Estabilidade Enzimática , Enzimas Imobilizadas/química , Glucose/química , Hidrogéis/química , Cinética , Polietilenoimina , Fatores de Tempo
12.
Sensors (Basel) ; 19(11)2019 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-31141953

RESUMO

A preliminary assessment of properties of the commercial product Chemiplus 2DS HB (BI-QEM Specialties SpA) is proposed. Cyclic voltammetry of this oligomer containing sulfate/sulfone groups shows a single oxidative peak at +0.866 V vs. Ag/AgCl, and its passivating process on Pt electrode suggests the formation of a non-conductive layer. Electrode modification was achieved by exploiting the constant potential amperometry setting potential at +0.900 V vs. Ag/AgCl. A substantial change in the oxidative currents from electroactive species H2O2 and ascorbic acid (AA) were observed on Pt/Chemiplus 2DS HB sensors compared to unmodified Pt. Furthermore, the influence of different storage conditions on modified sensors was examined. A storage solution containing AA concentration from 0.1 until 10 mM maintained effective AA rejection of Pt/Chemiplus 2DS HB after 7 days from construction; H2O2 oxidation capability was also retained. Sulfone and sulfonate groups of Chemiplus 2DS HB are likely responsible for the dimensionality of the film and the electrostatic interaction leading to a self-blocking/self-rejection of AA. The way Pt/Chemiplus can reveal the AA presence depends on the maintaining of AA rejection, and this peculiarity can distinguish it from other sensors or biosensors.

13.
Talanta ; 186: 53-59, 2018 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-29784398

RESUMO

Interference rejection in amperometric biosensors can be more effective introducing some modifiers during electro-deposition of permselective film. Addition of ß-cyclodextrin (ßCD), a cyclic oligosaccharide composed of seven glucose units, to the ortho-phenylendiamine (oPD) monomer were already demonstrated to provide an enhancement in ascorbic acid (AA) rejection. Here we evaluated the improvement in permselectivity of poly-eugenol and poly-magnolol films electro-polymerized in presence of different amounts of ßCD or eugenol-ßCD inclusion complex for amperometric biosensor application. Starting from Pt-Ir wire as transducer several microsensors were covered with polymeric films doped with ßCD-based modifiers through constant potential amperometry. Characterization of modified polymers was achieved by scanning electron microscopy and permselectivity analysis. Poly-magnolol film in combination with ßCD showed a worsening in permselectivity compared to poly-magnolol alone. In contrast, the introduction of ßCD-based modifier enhanced the interference rejection toward the archetypal interferent AA, while slightly affecting permeability toward H2O2 compared to the poly-eugenol without modifier. The AA rejection seems to be influenced by the availability of ßCD cavity as well as film performance due to concentration of ßCD-Eugenol inclusion complex. A poly-eugenol film co-polymerized with 2 mM ßCD-eugenol inclusion complex showed a permselectivity equal to poly-orthophenylendiamine film (PPD), with a lower permeability to AA, likely to be related with a self-blocking mechanism. Based on these results, a biosensor for glutamate was constructed with a poly-eugenol doped with ßCD-eugenol as permselective layer and its permselectivity, stability and lifetime were determined.


Assuntos
Ácido Ascórbico/química , Técnicas Biossensoriais , Técnicas Eletroquímicas , Ácido Glutâmico/análise , beta-Ciclodextrinas/química , Compostos de Bifenilo/química , Eugenol/química , Lignanas/química , Polímeros/química
14.
Hepatol Res ; 48(8): 664-674, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29330965

RESUMO

AIM: The etiopathogenesis of non-syndromic biliary atresia (BA) is obscure. The primary aim was to investigate intrahepatic bile duct cilia (IHBC) in BA at diagnosis and its correlation with clinical outcome. The secondary aim was to analyze IHBC in routine paraffin-embedded liver biopsies using conventional scanning electron microscopy (SEM). METHODS: Surgical liver biopsies taken at diagnosis from 22 BA infants (age range, 39-116 days) and from eight children with non-BA chronic cholestasis (age range, 162 days -16.8 years) were evaluated for IHBC by immunofluorescence (IF) and SEM. A minimum 18-month follow-up after surgery was available for all patients. RESULTS: By IF, cilia were present in 6/8 (75%) non-BA but only in 3/22 (14%) BA cases, and cilia were reduced or absent in 19/22 (86%) BA and 2/8 (25%) non-BA livers (P < 0.01). In BA, cilia presence was found to be associated with clearance of jaundice at 6-month follow-up (P < 0.05). However, high overall survival rates with native liver, >90% at 12 months, and >70% at 24 months post-surgery, were recorded regardless of cilia presence/absence at diagnosis. Electron microscopy was able to detect bile ducts and cilia in routine liver biopsies, revealing significant abnormalities in 100% BA livers. CONCLUSIONS: The presence of IHBC in BA livers at the diagnosis was associated with resolution of cholestasis, although was not predictive of short-term survival with native liver. Scanning electron microscopy represents a powerful new tool to study routine liver biopsies in biliary disorders. Cilia dysfunction in BA pathogenesis and/or disease progression warrants further investigation.

15.
Int J Pharm ; 524(1-2): 1-8, 2017 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-28336458

RESUMO

The strategy of formulating poorly soluble actives as nanosuspension has been explored by more than a thousand research papers, with some medicinal products for oral and intravenous use having reached the market or advanced clinical trials. Interestingly, there is a limited number of reports of nanosuspensions formulated for dermal and transdermal drug delivery. In the present work, a nanocrystals suspension of the fluorescent, water-insoluble dye Nile Red, is prepared through a media milling technique and exploited to characterize the fate of the nanosuspended drug when applied on the skin. More in detail, the accumulation of Nile Red nanocrystals inside the hair follicles is evidenced by scanning electron microscopy, and the diffusion of drug molecules in the different skin layers is evaluated by confocal microscopy and skin permeation studies. Overall, the combination of the analytical techniques provide a description of the mechanisms underlying dermal accumulation, and transdermal penetration of a drug formulated as a nanosuspension.


Assuntos
Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Oxazinas/análise , Absorção Cutânea , Administração Cutânea , Animais , Técnicas In Vitro , Pele/efeitos dos fármacos , Suínos
16.
Talanta ; 162: 151-158, 2017 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-27837811

RESUMO

First-generation amperometric biosensors are often based on the electro-oxidation of oxidase-generated H2O2. At the applied potential used in most studies, other molecules such as ascorbic acid or dopamine can be oxidized. Phenylenediamines are commonly used to avoid this problem: when these compounds are electro-deposited onto the transducer surface in the form of poly-phenylenediamine, a highly selective membrane is formed. Although there is no evidence of toxicity of the resulting polymer, phenylenediamine monomers are considered carcinogenic. An aim of this work was to evaluate the suitability of natural phenols as non-toxic alternatives to the ortho isomer of phenylenediamine. Electrosynthesis over Pt-Ir electrodes of 2-methoxy phenols (guaiacol, eugenol and isoeugenol), and hydroxylated biphenyls (dehydrodieugenol and magnolol) was achieved. The potentials used in the present study are significantly lower than values commonly applied during electro-polymerization. Polymers were obtained by means of constant potential amperometry, instead of cyclic voltammetry, in order to achieve multiple polymerizations, hence decreasing the time of realization and variability. Permselective properties of natural phenols were significantly improved at low polymerization potentials. Among the tested compounds, isoeugenol and magnolol, polymerized respectively at +25mV and +170mV against Ag/AgCl reference electrode, proved as permselective as poly-ortho-phenylenediamine and may be considered as effective polymeric alternatives. The natural phenol-coated electrodes were stable and responsive throughout 14 days. A biosensor prototype based on acetylcholine esterase and choline oxidase was electro-coated with poly-magnolol in order to evaluate the interference-rejecting properties of the electrosynthesized film in an amperometric biosensor; a moderate decrease in ascorbic acid rejection was observed during in vitro calibration of biosensors.


Assuntos
Técnicas Biossensoriais/métodos , Técnicas Eletroquímicas/métodos , Fenóis/química , Polímeros/química , Acetilcolina/química , Acetilcolina/metabolismo , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Oxirredutases do Álcool/química , Oxirredutases do Álcool/metabolismo , Ácido Ascórbico/química , Técnicas Biossensoriais/instrumentação , Compostos de Bifenilo/química , Técnicas Eletroquímicas/instrumentação , Eugenol/análogos & derivados , Eugenol/química , Lignanas/química , Microscopia Eletrônica de Varredura , Fenilenodiaminas/química , Polimerização , Polímeros/síntese química , Reprodutibilidade dos Testes
17.
Bioresour Technol ; 225: 90-98, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27886634

RESUMO

The ability of two municipal solid waste composts (MSW-C) to sorb As(V) in the presence of Pb(II) and in acidic conditions was investigated. Sorption isotherms and kinetics showed that both MSW-C were able to sorb As(V) in a similar way (∼0.24mmolg-1 MSW-C), but only when Pb(II) was present (0.45mmolL-1). The concomitant sorption of Pb(II) by both MSW-C (∼0.40mmolg-1) suggested that the metal cation was likely acting as bridging element between the negatively charged functional groups of composts and As(V). SEM-EDX analysis of the MSW-C+Pb(II)+As(V) systems supported the association between Pb(II) and As(V), while sequential extraction procedures and organic acids treatment showed that As(V) was strongly retained by MSW-C+Pb(II) and suggested the presence of different interaction types between As(V) and Pb(II). Plant growth experiments highlighted the key role of Pb(II) in the reduction of As(V)-phytotoxicity for triticale plants (×Triticosecale Wittm.) in the presence of MSW-C.


Assuntos
Arseniatos/química , Chumbo/química , Eliminação de Resíduos/métodos , Solo/química , Resíduos Sólidos , Arseniatos/toxicidade , Fracionamento Químico/métodos , Ácido Cítrico/química , Concentração de Íons de Hidrogênio , Cinética , Malatos/química , Microscopia Eletrônica de Varredura , Poluentes do Solo/química , Testes de Toxicidade/métodos , Triticale/efeitos dos fármacos , Triticale/crescimento & desenvolvimento
18.
Mater Sci Eng C Mater Biol Appl ; 68: 594-602, 2016 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-27524059

RESUMO

The bioactive flavonoid fisetin (FS) is a diet-derived antioxidant that is being increasingly investigated for its health-promoting effects. Unfortunately, the poor physicochemical and pharmacokinetic properties affect and limit the clinical application. In this study, novel polymeric nanoparticles (NPs), based on Poly-(ε-caprolactone) (PCL) and PLGA-PEG-COOH, encapsulating FS were formulated as suitable oral controlled release systems. Results showed NPs having a mean diameter of 140-200nm, and a percent loading of FS ranging from 70 to 82%. In vitro release studies revealed that NPs are able to protect and preserve the release of FS in gastric simulated conditions, also controlling the release in the intestinal medium. Moreover, the DPPH and ABTS scavenging capacity of FS, as well as α-glucosidase inhibition activity, that resulted about 20-fold higher than commercial Acarbose, were retained during nanoencapsulation process. In summary, our developed NPs can be proposed as an attractive delivery system to control the release of antioxidant and anti-hyperglycemic FS for nutraceutical and/or therapeutic application.


Assuntos
Antioxidantes , Suplementos Nutricionais , Flavonoides , Inibidores de Glicosídeo Hidrolases , Nanocápsulas/química , Antioxidantes/química , Antioxidantes/farmacocinética , Flavonoides/química , Flavonoides/farmacocinética , Flavonóis , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacocinética , Saccharomyces cerevisiae/enzimologia , Proteínas de Saccharomyces cerevisiae/química , Proteínas de Saccharomyces cerevisiae/metabolismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
19.
J Med Chem ; 59(11): 5209-20, 2016 06 09.
Artigo em Inglês | MEDLINE | ID: mdl-27139920

RESUMO

Pancreatic ductal adenocarcinoma (PDAC) is an aggressive disease with poor prognosis and limited therapeutic options. Therefore, there is an urgent need to identify new, safe, and targeted therapeutics for effective treatment of late as well as early stage disease. Plectin-1 (Plec-1) was recently identified as specific biomarker for detecting PDAC at an early stage. We envisioned that multivalent attachment of nanocarriers incorporating certain drugs to Plec-1-derived peptide would increase specific binding affinity and impart high specificity for PDAC cells. Previously, we discovered a novel class of compounds (e.g., quinazolinediones, QDs) that exert their cytotoxic effects by modulating ROS-mediated cell signaling. Herein, we prepared novel QD242-encapsulated polymeric nanoparticles (NPs) functionalized with a peptide to selectively bind to Plec-1. Similarly, we prepared QD-based NPs densely decorated with an isatoic anhydride derivative. Furthermore, we evaluated their impact on ligand binding and antiproliferative activity against PDAC cells. The targeted NPs were more potent than the nontargeted constructs in PDAC cells warranting further development.


Assuntos
Antineoplásicos/farmacologia , Carcinoma Ductal Pancreático/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Neoplasias Pancreáticas/tratamento farmacológico , Quinazolinonas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Carcinoma Ductal Pancreático/patologia , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Portadores de Fármacos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Neoplasias Pancreáticas/patologia , Quinazolinonas/síntese química , Quinazolinonas/química , Relação Estrutura-Atividade
20.
Int J Food Microbiol ; 217: 29-34, 2016 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-26485316

RESUMO

Grape juice can be easily contaminated with ochratoxin A (OTA), one of the known mycotoxins with the greatest public health significance. Among the different approaches to decontaminate juice from this mycotoxin, microbiological methods proved efficient, inexpensive and safe, particularly the use of yeast or yeast products. To ascertain whether immobilisation of the yeast biomass would lead to successful decontamination, alginate beads encapsulating Candida intermedia yeast cells were used in our experiments to evaluate their OTA-biosorption efficacy. Magnetic calcium alginate beads were also prepared by adding magnetite in the formulation to allow fast removal from the aqueous solution with a magnet. Calcium alginate beads were added to commercial grape juice spiked with 20 µg/kg OTA and after 48 h of incubation a significant reduction (>80%), of the total OTA content was achieved, while in the subsequent phases (72-120 h) OTA was slowly released into the grape juice by alginate beads. Biosorption properties of alginate-yeast beads were tested in a prototype bioreactor consisting in a glass chromatography column packed with beads, where juice amended with OTA was slowly flowed downstream. The adoption of an interconnected scaled-up bioreactor as an efficient and safe tool to remove traces of OTA from liquid matrices is discussed.


Assuntos
Candida/metabolismo , Microbiologia de Alimentos/métodos , Micotoxinas/metabolismo , Ocratoxinas/metabolismo , Vitis/microbiologia , Adsorção , Alginatos , Bebidas/microbiologia , Reatores Biológicos/microbiologia , Descontaminação/métodos , Contaminação de Alimentos/prevenção & controle , Ácido Glucurônico , Ácidos Hexurônicos , Nanopartículas de Magnetita/microbiologia , Vitis/química
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