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1.
Food Chem ; 420: 136002, 2023 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-37060671

RESUMO

The high ß-glucan content in barley disrupts the gluten network in dough. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and solid-state nuclear magnetic resonance (NMR) techniques were used to clarify how ß-glucan affected the quality of the gluten network structure with ß-glucan contents of 0-2%. The results suggest that the physical hindrance of the ß-glucan gel destroyed the formation of the gluten network structure. When 1.0-2.0% ß-glucan was added, the percentage of α-helical structures increased significantly. When the added amount of ß-glucan reached 2.0%, the sulfhydryl group (SH) content increased from 8.06 to 10.27 µmol/g, and the disulfide bond (SS) content decreased from 240.09 to 217.38 µmol/g. The interaction between ß-glucan and gluten mainly resulted from the interaction of electron-withdrawing groups, such as carbonyl groups (CO) and double bond carbons (CC), and carbon atoms on the side chains of ß-glucan, which play an important role in the central structure of glutenin.


Assuntos
Hordeum , beta-Glucanas , beta-Glucanas/química , Hordeum/química , Varredura Diferencial de Calorimetria/métodos
2.
Braz. J. Pharm. Sci. (Online) ; 59: e21217, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1429971

RESUMO

Abstract Solid dispersions (SDs) of ursolic acid (UA) were developed using polyvinylpyrrolidone K30 (PVP K30) in combination with non-ionic surfactants, such as D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or poloxamer 407 (P407) with the aim of enhancing solubility and in vitro release of the UA. SDs were investigated using a 24 full factorial design, subsequently the selected formulations were characterized for water solubility, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), particle diameter, scanning electron microscopy, drug content, physical-chemical stability and in vitro release profile. SDs showed higher UA water-solubility than physical mixtures (PMs), which was attributed by transition of the drug from crystalline to amorphous or molecular state in the SDs, as indicated by XRD and DSC analyses. SD1 (with P407) and SD2 (with TPGS) were chosen for further investigation because they had higher drug load. SD1 proved to be more stable than SD2, revealing that P407 contributed to ensure the stability of the UA. Furthermore, SD1 and SD2 increased UA release by diffusion and swelling-controlled transport, following the Weibull model. Thus, solid dispersions obtained with PVP k-30 and P407 proved to be advantageous to enhance aqueous solubility and stability of UA.


Assuntos
Polietilenoglicóis/administração & dosagem , Solubilidade , Poloxâmero/efeitos adversos , Difusão , Raios X/efeitos adversos , Técnicas In Vitro , Varredura Diferencial de Calorimetria/métodos , Preparações Farmacêuticas/análise , Microscopia Eletrônica de Varredura/métodos
3.
Braz. J. Pharm. Sci. (Online) ; 59: e22505, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1439507

RESUMO

Abstract Natural products are considered an important source of the therapeutic arsenal currently available. Among these alternatives are the seeds of Ambrosia peruviana (altamisa), whose extract has shown an anti-inflammatory effect. The main objective of this work was to perform a preformulation study of Ambrosia peruviana seeds ethanolic extract, where the main factors that affect the physical, chemical, and pharmacological stability of the extract were evaluated, as well as a compatibility study by differential scanning calorimetry (DSC) analysis against different excipients. A dry extract was obtained by rotary evaporation of the seeds macerated with 96% ethanol. The anti-inflammatory activity was determined by measuring its effect on NO production in RAW 264.7 macrophages, stimulated with LPS. The results showed that the dry extract maintained its stability over time when stored at a temperature of 4 and 25ºC, demonstrating its biological activity, the content of phenolic compounds, and its physicochemical parameters remain practically invariable. However, when exposed to high temperatures (60 ºC) it was affected. The thermal analysis revelated that the behavior of most of the selected excipients and the dry extract was maintained, which indicates that it did not present incompatibilities, therefore they can be candidates for formulating a microemulsion.


Assuntos
Sementes/metabolismo , Asteraceae/classificação , Ambrosia/efeitos adversos , Produtos Biológicos , Varredura Diferencial de Calorimetria/métodos , Excipientes/administração & dosagem
4.
Int J Mol Sci ; 23(3)2022 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-35163317

RESUMO

Amphiphilic copolymers are appealing materials because of their interesting architecture and tunable properties. In view of their application in the biomedical field, the preparation of these materials should avoid the use of toxic compounds as catalysts. Therefore, enzymatic catalysis is a suitable alternative to common synthetic routes. Pentablock copolymers (CUC) were synthesized with high yields by ring-opening polymerization of ε-caprolactone (ε-CL) initiated by Pluronic (EPE) and catalyzed by Candida antarctica lipase B enzyme. The variables to study the structure-property relationship were EPEs' molecular weight and molar ratios between ε-CL monomer and EPE macro-initiator (M/In). The obtained copolymers were chemically characterized, the molecular weight determined, and morphologies evaluated. The results suggest an interaction between the reaction time and M/In variables. There was a correlation between the differential scanning calorimetry data with those of X-ray diffraction (WAXD). The length of the central block of CUC copolymers may have an important role in the crystal formation. WAXD analyses indicated that a micro-phase separation takes place in all the prepared copolymers. Preliminary cytotoxicity experiments on the extracts of the polymer confirmed that these materials are nontoxic.


Assuntos
Caproatos/química , Lactonas/química , Poloxâmero/química , Polímeros/química , Varredura Diferencial de Calorimetria/métodos , Catálise , Peso Molecular , Polimerização
5.
Carbohydr Polym ; 283: 119148, 2022 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-35153017

RESUMO

In order to provide a theoretical basis on how germination treatment modulated the pasting behaviors of starches from native and germinated waxy brown rice, impacts of germination on the molecular and supramolecular structures and pasting behaviors were evaluated. Multiple analytical methods such as thermodynamics and spectroscopy were applied in this work for investigating the changes in starch multiscale structure and pasting behaviors. The results show that germination treatment contributed to an obvious increase in α- and ß-amylase activities, which could degrade the starch chains and reduce the contents of double helices (50.9%-43.2%), short-range ordered degree (1.054-0.908), relative crystallinity (40.1%-30.5%), and lamellar ordering degree (dc, 6.09-5.46 nm) along with apparent erosion on starch granules. These structural amorphizations at the molecular and supramolecular levels could lead to the weakened entanglements and interactions among molecular chains, eventually reducing the characteristic viscosity (e.g., overall, peak, and final viscosity) of starch. This study may facilitate better development of germinated rice-based products.


Assuntos
Oryza/química , Amido/química , Amilopectina/química , Varredura Diferencial de Calorimetria/métodos , Germinação , Espectroscopia de Ressonância Magnética/métodos , Microscopia Eletrônica de Varredura/métodos , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Temperatura , Termodinâmica , Viscosidade , Ceras/química
6.
J Pharm Pharmacol ; 74(1): 41-56, 2022 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-34986225

RESUMO

OBJECTIVES: In this study, p-sulfonatocalix[6]arenes (SCA6) was proposed to construct a host-guest complexation to carry mitoxantrone (MIT) to maintain its anti-proliferation effect on HepG2 cells as well as to attenuate cardiotoxicity on H9C2 cells as a nano-size drug delivery system. METHODS: SCA6 binding to MIT evidenced through competitive fluorescence titration method. The complex was characterized using UV-visible, Fourier transform infrared, and proton nuclear magnetic resonance (1H-NMR) spectroscopies and differential scanning calorimetry analysis. The cytotoxicity was examined by a cell counting kit-8 assay on six cells. High content analysis, cell apoptosis and cell cycle experiments were measured to investigate the mechanism of detoxification in H9C2. KEY FINDINGS: The host-guest complexation was formed with a stoichiometry ratio of 1:1. Cytotoxicity study demonstrated that MIT/SCA6 complex could improve the cell viability on H9C2, MCF-7, A549, Hek293 and L02 cells and remained cytotoxicity effect on HepG2 cells. High content analysis showed that MIT/SCA6 complex could enhance the cell viability, mitochondrial mass and mitochondrial membrane potential and ameliorate the nuclear swelling on H9C2 cells. Moreover, the complex were arrested in G0/G1 phase of the cell cycle and same with MIT, while the detoxication was attributed to reducing early apoptosis. CONCLUSIONS: The host-guest complexation between SCA6 and MIT had the ability to attenuate cardiotoxicity and provided a potential strategy for the application of soluble calixarenes in chemotherapy.


Assuntos
Calixarenos/farmacologia , Cardiotoxicidade , Estabilidade de Medicamentos , Mitoxantrona , Fenóis/farmacologia , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Varredura Diferencial de Calorimetria/métodos , Cardiotoxicidade/etiologia , Cardiotoxicidade/prevenção & controle , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/farmacologia , Sistemas de Liberação de Medicamentos , Células Hep G2 , Humanos , Mitoxantrona/farmacologia , Mitoxantrona/toxicidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
7.
Carbohydr Polym ; 275: 118682, 2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-34742412

RESUMO

Layer-by-layer three-dimensional nanofibrous scaffolds (3DENS) were produced using the electrospinning technique. Interest in using biopolymers and application of electrospinning fabrication techniques to construct nanofibers for biomedical application has led to the development of scaffolds composed of PVA, keratin, and chitosan. To date, PVA/keratin blended nanofibers and PVA/chitosan blended nanofibers have been fabricated and studied for biomedical applications. Electrospun scaffolds comprised of keratin and chitosan have not yet been reported in published literature, thus a novel nanofibrous PVA/keratin/chitosan scaffold was fabricated by electrospinning. The resulting 3DENS were characterized using fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning colorimetry (DSC), and thermogravimetric analysis (TGA). Physiochemical properties of the polymer solutions such as viscosity (rheology) and conductivity were also investigated. The 3DENS possess a relatively uniform fibrous structure, suitable porosity, swelling properties, and degradation which are affected by the mass ratio of keratin, and chitosan to PVA. These results demonstrate that PVA/keratin/chitosan 3DENS have the potential for biomedical applications.


Assuntos
Quitosana/química , Queratinas/química , Nanofibras/química , Álcool de Polivinil/química , Tecidos Suporte/química , Animais , Materiais Biocompatíveis/química , Biopolímeros/química , Varredura Diferencial de Calorimetria/métodos , Condutividade Elétrica , Microscopia Eletrônica de Varredura/métodos , Porosidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Termogravimetria/métodos , Engenharia Tecidual/métodos , Viscosidade
8.
Carbohydr Polym ; 276: 118788, 2022 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-34823798

RESUMO

The purpose of this study was to investigate the potential of bacterial cellulose nanofiber suspension (BCNs) as stabilizer in anti-solvent precipitation and its effect on improving bioavailability of coenzyme Q10. Bacterial cellulose (BC) was hydrolyzed by sulfuric acid followed by the oxidation with hydrogen peroxide to prepare BCNs. The suspension of BCNs-loaded CoQ10 (CoQ10-BCNs) were prepared by antisolvent precipitation. The zeta potential of CoQ10-BCNs was about -36.01 mV. The properties of CoQ10, BCNs and CoQ10-BCNs were studied by scanning electron microscopy, transmission electron microscope, Fourier-transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry and thermo gravimetric analysis. The crystallinity of CoQ10 decreased in CoQ10-BCNs compared with the raw CoQ10, and CoQ10-BCNs have good physicochemical stability. In oral bioavailability studies, the area under curve (AUC) of CoQ10-BCNs was about 3.62 times higher than the raw CoQ10 in rats.


Assuntos
Celulose/química , Nanofibras/química , Polissacarídeos Bacterianos/química , Ubiquinona/análogos & derivados , Água/química , Administração Oral , Animais , Disponibilidade Biológica , Varredura Diferencial de Calorimetria/métodos , Gluconacetobacter xylinus/metabolismo , Microscopia Eletrônica de Varredura/métodos , Ratos , Ratos Sprague-Dawley , Solubilidade , Solventes/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Suspensões , Termogravimetria/métodos , Ubiquinona/química , Ubiquinona/farmacocinética , Difração de Raios X/métodos
9.
Braz. J. Pharm. Sci. (Online) ; 58: e19723, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1394035

RESUMO

Abstract Passiflora nitida Kunth, an Amazonian Passiflora species, is little studied, although the specie's high biological potential. Herein the plant's pharmacognostic characterization, extract production, antioxidant potential evaluation, and application of this extract in cosmetic products is reported. The physical chemical parameters analyzed were particle size by sieve analysis, loss through drying, extractive yield, total ash content, laser granulometry, specific surface area and pore diameter (SBET), differential scanning calorimetry, thermogravimetry (TG), and wave dispersive X-Ray fluorescence (WDXRF). Total phenol/flavonoid content, LC-MS/MS analysis, DPPH and ABTS antioxidant radical assays, cytotoxicity, melanin, and tyrosinase inhibition in melanocytes test provided evidence to determine the content of the major constituent. P. nitida dry extract provided a fine powder with mesopores determined by SBET, with the TG curve showing five stages of mass loss. The antioxidant potential ranged between 23.5-31.5 mg∙mL-1 and tyrosinase inhibition between 400-654 µg∙mL-1. The species presented an antimelanogenic effect and an inhibitory activity of cellular tyrosinase (26.6%) at 25 µg/mL. The LC-MS/MS analysis of the spray-dried extract displayed the main and minor phenolic compounds constituting this sample. The results indicate that P. nitida extract has promising features for the development of cosmetic formulations


Assuntos
Extratos Vegetais/análise , Folhas de Planta/efeitos adversos , Cosméticos/classificação , Passiflora/classificação , Termogravimetria/métodos , Raios X/efeitos adversos , Varredura Diferencial de Calorimetria/métodos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Compostos Fenólicos , Melaninas , Antioxidantes/efeitos adversos
10.
Braz. J. Pharm. Sci. (Online) ; 58: e21131, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1420447

RESUMO

Abstract The study is aimed to develop a monolithic controlled matrix transdermal patches containing Metoclopramide as a model drug by solvent casting method. Eudragit L100, Polyvinylpyrrolidone K-30, and Methylcellulose were used in different ratios and Polyethylene glycol 400 added as a plasticizer. Resulting patches were evaluated for their physicochemical characters like organoleptic characters, weight variation, folding endurance, thickness, swelling index, flatness, drug content, swelling index, percentage erosion, moisture content, water vapor transmission rate and moisture uptake. Formed patches were also evaluated through Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning calorimetry (DSC) and Scanning Electron Microscopy (SEM). Results of SEM unveiled smooth surface of drug-loaded patches. In-vitro dissolution studies were conducted by using dissolution medium phosphate buffer saline pH 7.4. Effect of natural permeation enhancers was elucidated on two optimized formulations (Z4 and Z9). Different concentrations (5%-10 %) of permeation enhancers i.e. Olive oil, Castor oil and Eucalyptus oil were evaluated on Franz diffusion cell using excised abdominal rat skin. Z4-O2 (Olive oil 10%) had enhanced sustain effect and flux value (310.72) close to the desired flux value. Z4-O2 followed Higuchi release model (R2= 0.9833) with non-fickian diffusion release mechanism (n=0.612)


Assuntos
Análise Espectral/métodos , Óleos Voláteis/análise , Metoclopramida/agonistas , Difração de Raios X/instrumentação , Varredura Diferencial de Calorimetria/métodos , Microscopia Eletrônica de Varredura/métodos
11.
Braz. J. Pharm. Sci. (Online) ; 58: e18946, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1364411

RESUMO

Abstract To investigate structure-property relationship of polymer-based curcumin solid dispersion (SD), three acrylic polymers were used to formulate curcumin SD by solvent evaporation method. Curcumin Eudragit EPO SD (cur@EPO), curcumin Eudragit RS PO SD (cur@RSPO) and curcumin Eudragit RL PO SD (cur@RLPO) showed deep red, golden orange and reddish orange color, respectively. Cur@RSPO entrapped 15.42 wt% of curcumin followed by cur@RL PO and cur@EPO. FTIR spectra indicated that in cur@EPO, curcumin may transfer hydrogen to the dimethylaminoethyl methacrylate group and thus change its color to red. In contrast, curcumin may form hydrogen bonding with Eudragit RS PO and Eudragit RL. Curcumin exists in amorphous state in three SDs as proved by differential scanning calorimetry and X-Ray diffraction measurement. In vitro digestion presented that lower pH value in simulated gastric fluid (SGF) stimulates the curcumin release from cur@EPO while permeability influences the release profile in other two SDs. When in simulated intestinal fluid (SIF), first order release model governs the release behaviors of all three SDs which showed sustained release pattern. Our results are helpful to elucidate how structure of polymer may impact on the major properties of curcumin contained SD and will be promising to broaden its therapeutic applications.


Assuntos
Polímeros , Curcumina/análise , Métodos , Solventes/administração & dosagem , Difração de Raios X/instrumentação , Técnicas In Vitro/métodos , Varredura Diferencial de Calorimetria/métodos , Evaporação/classificação , Espectroscopia de Infravermelho com Transformada de Fourier , Cor , Citrus sinensis/classificação , Concentração de Íons de Hidrogênio
12.
São Paulo; s.n; s.n; 2022. 80 p. tab, graf.
Tese em Português | LILACS | ID: biblio-1415544

RESUMO

O objetivo deste trabalho foi preparar e caracterizar nanocarreadores via auto-organização a partir da pectina de citros e lisozima para o encapsulamento da ß-lactose. Foram estudadas três condições de interação entre os biopolímeros variando a razão molar pectina/lisozima (3:1, 2:1, 1:1, 1:2 e 1:3), o pH e o tempo de aquecimento. A confirmação da interação foi determinada por espectroscopia no infravermelho por transformada de Fourier (FTIR) e por calorimetria de varredura diferencial (DSC). Os espectros de infravermelho evidenciaram que ligações de hidrogênio foram as principais forças envolvidas na formação dos nanocarreadores e sugeriram a ausência de ß-lactose livre na superfície das nanopartículas. Os termogramas evidenciaram que as nanopartículas formadas na presença de ß-lactose têm maior estabilidade térmica do que as nanopartículas sem ß-lactose. Para ambas as formulações estudadas, na presença e na ausência de ß-lactose, a formação das nanopartículas ocorreu entre os valores de pKa e ponto isoelétrico (pI) da pectina e lisozima, respectivamente, sendo a melhor razão de interação pectina/lisozima 1:2, em pH 10, a 80 ºC por 30 min. As nanopartículas foram formadas via auto-organização e todos as partículas apresentaram distribuição de tamanho homogênea, formato esférico, diâmetro inferior a 100 nm e carga superficial negativa. A morfologia e o tamanho das partículas pouco alteraram com a incorporação da -lactose. A eficiência de encapsulação (EE) da ß-lactose foi superior a 96% para as concentrações estudadas. Ensaios preliminares in vitro, em células epiteliais de câncer de cólon (HCT-116), evidenciaram que as nanopartículas formadas são capazes de adentrar no meio intracelular, possivelmente, por via endocitose


This work aimed to prepare and characterize nanocarriers via self-assembly using citrus pectin and lysozyme for ß-lactose encapsulation. Three interaction conditions between the biopolymers were studied, varying the pectin/lysozyme molar ratio (3:1, 2:1, 1:1, 1:2 and 1:3), pH and heating time. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) determined the interaction's confirmation. The infrared spectra showed that hydrogen bonds were the main forces involved in the formation of nanocarriers and suggested the absence of free ß-lactose on the surface of the nanoparticles. The thermograms showed that nanoparticles formed in the presence of ß-lactose have greater thermal stability than nanoparticles without ß-lactose. For both formulations studied, in the presence and absence of lactose, the formation of nanoparticles occurred between the pKa and isoelectric point (pI) values of pectin and lysozyme, respectively, with the best pectin/lysozyme interaction molar ratio 1:2, at pH 10, at 80 °C for 30 min. Nanoparticles were formed via self-assembly, and all particles presented homogeneous size distribution, spherical shape, diameter less than 100 nm, and negative surface charge. The morphology and size of the particles changed little with the incorporation of ß-lactose. The encapsulation efficiency (EE) of ß-lactose was higher than 96% for the concentrations studied. Preliminary in vitro assays in colon cancer epithelial cells (HCT-116) showed that the nanoparticles formed are capable of entering the intracellular medium, possibly via endocytosis


Assuntos
Muramidase/análise , Pectinas/análise , Biopolímeros/efeitos adversos , Calorimetria , Varredura Diferencial de Calorimetria/métodos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Neoplasias do Colo , Nanopartículas , Concentração de Íons de Hidrogênio , Lactose
13.
Cell Mol Biol (Noisy-le-grand) ; 67(1): 64-72, 2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-34817366

RESUMO

The purpose of our study was to obtain new wound dressings in the form of hydrogels that promote wound healing taking advantage of the broad activities of elastin (ELT) in physiological processes. The hydrogel of ELT and polyvinylpyrrolidone (PVP; ELT-PVP) was obtained by cross-linking induced by gamma irradiation at a dose of 25 kGy. The physicochemical changes attributed to cross-linking were analyzed through scanning electron microscopy (SEM), infrared spectroscopy analysis with Fourier transform (FTIR), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). Furthermore, we performed a rheological study to determine the possible changes in the fluidic macroscopic properties produced by the cross-linking method. Finally, we accomplished viability and proliferation analyses of human dermal fibroblasts in the presence of the hydrogel to evaluate its biological characteristics. The hydrogel exhibited a porous morphology, showing interconnected porous with an average pore size of 16 ± 8.42 µm. The analysis of FTIR, DSC, and TGA revealed changes in the chemical structure of the ELT-PVP hydrogel after the irradiation process. Also, the hydrogel exhibited a rheological behavior of a pseudoplastic and thixotropic fluid. The hydrogel was biocompatible, demonstrating high cell viability, whereas ELT presented low biocompatibility at high concentrations. In summary, the hydrogel obtained by gamma irradiation revealed the appropriate morphology to be applied as a wound dressing. Interestingly, the hydrogel exhibited a higher percentage of cell viability compared with ELT, suggesting that the cross-linking of ELT with PVP is a suitable strategy for biological applications of ELT without generating cellular damage.


Assuntos
Materiais Biocompatíveis/metabolismo , Elastina/metabolismo , Curativos Oclusivos , Polimerização/efeitos da radiação , Povidona/metabolismo , Materiais Biocompatíveis/química , Materiais Biocompatíveis/farmacologia , Varredura Diferencial de Calorimetria/métodos , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Elastina/química , Elastina/ultraestrutura , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Humanos , Hidrogéis/química , Hidrogéis/metabolismo , Hidrogéis/farmacologia , Microscopia Eletrônica de Varredura , Povidona/química , Povidona/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Termogravimetria/métodos , Cicatrização/efeitos dos fármacos
14.
Int J Biol Macromol ; 193(Pt B): 2260-2270, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34793812

RESUMO

This study aimed to evaluate the effects of insoluble dietary fiber (IDF) and ferulic acid (FA) on the properties of rice starch (RS), including gelatinization, thermodynamic, rheological parameters, and freeze-thaw stability. Rapid viscosity analysis (RVA), differential scanning calorimetry (DSC), rheological analysis, and freeze-thaw stability analysis were performed. The results showed that the presence of IDF and FA could significantly delay the short-term retrogradation of RS, especially at high FA concentrations. Rheological tests showed that IDF was not conducive for the elasticity, viscosity enhancement, and system stability of the starch gels. However, FA could offset the deterioration of the system caused by IDF and further improve the gel properties. The presence of IDF and FA weakened the freeze-thaw stability of the starch gel, unlike their single action on the starch gel, correspondingly. The results show that FA could alleviate the degradation of RS gel performance caused by IDF in the ternary system. The findings provide potential possibilities for improvements in the quality of rice starch gel-based products.


Assuntos
Ácidos Cumáricos/química , Oryza/química , Amido/química , Varredura Diferencial de Calorimetria/métodos , Fibras na Dieta , Elasticidade , Congelamento , Gelatina/química , Géis/química , Reologia , Temperatura , Viscosidade
15.
Eur J Pharm Biopharm ; 169: 125-133, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34655768

RESUMO

Understanding drug miscibility in pharmaceutically relevant systems is essential for the development and optimisation of pharmaceutical dosage forms. This is particularly true for film forming systems which are designed to become supersaturated with drug, following application on the skin surface, whilst maintaining the physical stability of the drug for a suitable period to enhance drug delivery. For such formulations, chemical penetration enhancers as well as the drug are absorbed from the formulation into the skin, making understanding drug delivery from the films challenging. This study investigated the use of an optical differential scanning calorimetry (DSC) to understand drug miscibility in polymeric film forming systems and explain drug transport behaviour from film forming formulations, containing ibuprofen, a copolymer based on dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate (Eudragit® E, EuE), a copolymer based on ethyl acrylate, methyl methacrylate and methacrylic acid ester with quaternary ammonium groups (Eudragit® RS, EuRS) and a copolymer based on methacrylic acid and methyl methacrylate (Eudragit® S, EuS), with and without the chemical penetration enhancer propylene glycol, across a model membrane. The optical DSC enabled the rapid screening of not only drug-polymer miscibility, but also drug-vehicle miscibility, while considering both the melting-point depression and melting enthalpy of the drug due to the presence of the polymer/polymer-based vehicle, obtained via thermal analysis by structural characterisation (TASC) and DSC analysis, respectively. The results obtained enable the polymers studied to be ranked in the order of EuE > EuRS > EuS, with EuE being more miscible with ibuprofen, and the incorporation of a penetration enhancer in the film forming system formulation was found to increase ibuprofen solubility in EuE- and EuRS- based films. The drug-polymer/vehicle miscibility information obtained via optical DSC provided understanding of drug transport from film forming systems with the higher miscibility of ibuprofen with EuE reducing drug transport through decreasing drug saturation in the film. The higher drug transport from films containing EuRS and EuS could also be linked to drug miscibility with the polymer and showed dependence on ibuprofen loading in the formulation. Overall optical DSC has been demonstrated to be a valuable tool for determining drug-vehicle miscibility for pharmaceutical product development.


Assuntos
Varredura Diferencial de Calorimetria/métodos , Sistemas de Liberação de Medicamentos/métodos , Ibuprofeno/farmacologia , Ácidos Polimetacrílicos/farmacologia , Administração Tópica , Anti-Inflamatórios não Esteroides/farmacologia , Química Farmacêutica/métodos , Análise Diferencial Térmica/métodos , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Humanos , Absorção Cutânea/efeitos dos fármacos , Solubilidade
16.
Food Funct ; 12(20): 10008-10022, 2021 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-34505612

RESUMO

The active compounds in star anise alcohol extractives (SAAE) have potent bioactivity. However, their poor solubility and stability limit their applications. In this study, SAAE/hydroxypropyl-ß-cyclodextrin (HP-ß-CD) inclusion complexes were prepared as a strategy to overcome the abovementioned disadvantages. The phase solubility results indicated that the solubility of the inclusion complex was enhanced. Complexation was confirmed by complementary methods, including Fourier-transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, scanning electron microscopy, and transmission electron microscopy, which proved to be extremely insightful for studying the inclusion formation phenomenon between SAAE and HP-ß-CD. Despite there being no apparent improvements in the antioxidant capacity and antimicrobial activity, the results of the stability studies presented higher thermal, volatile, and photostability after encapsulation. Further, molecular modeling was used to investigate the factors influencing complex formation and provide the most stable molecular conformation. Thus, based on the obtained results, this study strongly demonstrates the potential of the SAAE/HP-ß-CD inclusion complex in the food industry.


Assuntos
2-Hidroxipropil-beta-Ciclodextrina/química , Illicium/química , Extratos Vegetais/química , 2-Hidroxipropil-beta-Ciclodextrina/análise , Antioxidantes/química , Varredura Diferencial de Calorimetria/métodos , Etanol/química , Espectroscopia de Ressonância Magnética/métodos , Microscopia Eletrônica de Varredura/métodos , Microscopia Eletrônica de Transmissão/métodos , Modelos Moleculares , Extratos Vegetais/análise , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
17.
Int J Mol Sci ; 22(17)2021 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-34502506

RESUMO

Poultry feathers are among the most abundant and polluting keratin-rich waste biomasses. In this work, we developed a one-pot microwave-assisted process for eco-friendly keratin extraction from poultry feathers followed by a direct electrospinning (ES) of the raw extract, without further purification, to obtain keratin-based bioplastics. This microwave-assisted keratin extraction (MAE) was conducted in acetic acid 70% v/v. The effects of extraction time, solvent/feathers ratio, and heating mode (MAE vs. conventional heating) on the extraction yield were investigated. The highest keratin yield (26 ± 1% w/w with respect to initial feathers) was obtained after 5 h of MAE. Waste-derived keratin were blended with gelatin to fabricate keratin-based biodegradable and biocompatible bioplastics via ES, using 3-(Glycidyloxypropyl)trimethoxysilane (GPTMS) as a cross-linking agent. A full characterization of their thermal, mechanical, and barrier properties was performed by differential scanning calorimetry, thermogravimetric analysis, uniaxial tensile tests, and water permeability measurements. Their morphology and protein structure were investigated using scanning electron microscopy and attenuated total reflection-infrared spectroscopy. All these characterizations highlighted that the properties of the keratin-based bioplastics can be modulated by changing keratin and GPTMS concentrations. These bioplastics could be applied in areas such as bio-packaging and filtration/purification membranes.


Assuntos
Plumas/química , Queratinas/química , Queratinas/isolamento & purificação , Ácido Acético/química , Animais , Varredura Diferencial de Calorimetria/métodos , Microscopia Eletrônica de Varredura/métodos , Micro-Ondas , Solventes , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
18.
Carbohydr Polym ; 270: 118373, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34364617

RESUMO

Dual-drug delivery systems were constructed through coaxial techniques, which were convenient for the model drugs used the present work. This study aimed to fabricate core-shell electrospun nanofibrous membranes displaying simultaneous cell proliferation and antibacterial activity. For that purpose, phenytoin (Ph), a well-known proliferative agent, was loaded into a polycaprolactone (PCL) shell membrane, and as-prepared silver-chitosan nanoparticles (Ag-CS NPs), as biocidal agents, were embedded in a polyvinyl alcohol (PVA) core layer. The morphology, chemical composition, mechanical and thermal properties of the nanofibrous membranes were characterized by FESEM/STEM, FTIR and DSC. The coaxial PVA-Ag CS NPs/PCL-Ph nanofibers (NFs) showed more controlled Ph release than PVA/PCL-Ph NFs. There was notable improvement in the morphology, thermal, mechanical, antibacterial properties and cytobiocompatibility of the fibers upon incorporation of Ph and Ag-CS NPs. The proposed core-shell PVA/PCL NFs represent promising scaffolds for tissue regeneration and wound healing by the effective dual delivery of phenytoin and Ag-CS NPs.


Assuntos
Quitosana/química , Sistemas de Liberação de Medicamentos/métodos , Nanofibras/química , Nanopartículas/química , Fenitoína/química , Prata/química , Antibacterianos/farmacologia , Varredura Diferencial de Calorimetria/métodos , Proliferação de Células/efeitos dos fármacos , Quitosana/farmacologia , Escherichia coli/efeitos dos fármacos , Microscopia Eletrônica de Varredura/métodos , Fenitoína/farmacologia , Poliésteres/química , Álcool de Polivinil/química , Prata/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Staphylococcus aureus/efeitos dos fármacos , Cicatrização/efeitos dos fármacos
19.
Carbohydr Polym ; 270: 118378, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34364622

RESUMO

The effects of gelatinization degree (GD) and octenyl succinic anhydride (OSA) esterification in the sorption-desorption characteristics of normal corn starch (NCS) were studied. NCS was subjected to different GD (53, 70, and 96%) with an extruder and lyophilized. FTIR analysis revealed that GD increased the hydrated (995/1022 ratio) and decreased the short-range ordered (1022/1047 ratio). The equilibrium sorption-desorption curve of starches was obtained for water activities up to 0.95 and fitted with the Guggenheim-Anderson-de Boer (GAB) model. Gelatinization of corn starch decreased its water sorption capacity, increased its sorption hysteresis and decreased its monolayer moisture content. OSA treatment of NCS reduced the water sorption capacity, hysteresis, and monolayer moisture content as reflected by slight variations of these parameters with the GD. A principal component analysis showed that GD and OSA esterification are mutually independent treatments, which can provide different effects on the water sorption characteristics of NCS.


Assuntos
Amido/química , Anidridos Succínicos/química , Zea mays/química , Varredura Diferencial de Calorimetria/métodos , Esterificação , Gelatina/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Amido/análogos & derivados , Água/química
20.
Mol Pharm ; 18(8): 3050-3062, 2021 08 02.
Artigo em Inglês | MEDLINE | ID: mdl-34250800

RESUMO

In this work, we employed broad-band dielectric spectroscopy to determine the solubility limits of nimesulide in the Kollidon VA64 matrix at ambient and elevated pressure conditions. Our studies confirmed that the solubility of the drug in the polymer matrix decreases with increasing pressure, and molecular dynamics controls the process of recrystallization of the excess of amorphous nimesulide from the supersaturated drug-polymer solution. More precisely, recrystallization initiated at a certain structural relaxation time of the sample stops when a molecular mobility different from the initial one is reached, regardless of the temperature and pressure conditions. Finally, based on the presented results, one can conclude that by transposing vertically the results obtained at elevated pressures, one can obtain the solubility limit values corresponding to low temperatures. This approach was validated by the comparison of the experimentally determined points with the theoretically obtained values based on the Flory-Huggins theory.


Assuntos
Química Farmacêutica/métodos , Espectroscopia Dielétrica/métodos , Composição de Medicamentos/métodos , Polímeros/química , Pressão , Sulfonamidas/química , Temperatura , Varredura Diferencial de Calorimetria/métodos , Cristalização , Estabilidade de Medicamentos , Pirrolidinas/química , Solubilidade , Soluções , Compostos de Vinila/química
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