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1.
Front Nutr ; 11: 1425638, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38903616

RESUMO

L-lysine functionalized gold nanoparticles (AuNPs-Lys) have been widely used for the detection of worldwide interest analytes. In this work, a colorimetric assay for the detection of the carcinogen aflatoxin B1 (AFB1) based on the aggregation of AuNPs-Lys in the presence of copper ions was developed. For this purpose, AuNPs were synthesized in citrate aqueous solution, functionalized, and further characterized by UV-Vis, fluorescence, Fourier transform infrared spectroscopy (FTIR), nanoparticle tracking analysis (NTA), dynamic light scattering (DLS), and transmission electron microscopy (TEM). In general, AuNPS-Lys (~2.73 × 1011 particles) offered a clear colorimetric response in the presence of AFB1 and Cu2+ ions showing linearity in the range of 6.25 to 200 ng AFB1/mL, with a detection limit of 4.18 ng AFB1/mL via photometric inspection. Moreover, the performance of the proposed methodology was tested using the 991.31 AOAC official procedure based on monoclonal antibodies in maize samples artificially contaminated with AFB1. There was a good agreement between the measured AFB1 concentrations in both assays, the average recoveries for the colorimetric and immunoaffinity assays were between 91.2-98.4% and 96.0-99.2%, respectively. These results indicated that the colorimetric assay could be used as a rapid, eco-friendly, and cost-effective platform for the quantification of AFB1 in maize-based products.

2.
Viruses ; 16(3)2024 03 11.
Artigo em Inglês | MEDLINE | ID: mdl-38543796

RESUMO

Porcine epidemic diarrhea virus (PEDV) has affected the pork industry worldwide and during outbreaks the mortality of piglets has reached 100%. Lipid nanocarriers are commonly used in the development of immunostimulatory particles due to their biocompatibility and slow-release delivery properties. In this study, we developed a lipid nanoparticle (LNP) complex based on glycyrrhizinic acid (GA) and tested its efficacy as an adjuvant in mice immunized with the recombinant N-terminal domain (NTD) of porcine epidemic diarrhea virus (PEDV) spike (S) protein (rNTD-S). The dispersion stability analysis (Z-potential -27.6 mV) confirmed the size and charge stability of the LNP-GA, demonstrating that the particles were homogeneously dispersed and strongly anionic, which favors nanoparticles binding with the rNTD-S protein, which showed a slightly positive charge (2.11 mV) by in silico analysis. TEM image of LNP-GA revealed nanostructures with a spherical-bilayer lipid vesicle (~100 nm). The immunogenicity of the LNP-GA-rNTD-S complex induced an efficient humoral response 14 days after the first immunization (p < 0.05) as well as an influence on the cellular immune response by decreasing serum TNF-α and IL-1ß concentrations, which was associated with an anti-inflammatory effect.


Assuntos
Infecções por Coronavirus , Lipossomos , Nanopartículas , Vírus da Diarreia Epidêmica Suína , Doenças dos Suínos , Vacinas Virais , Animais , Suínos , Camundongos , Anticorpos Antivirais , Vírus da Diarreia Epidêmica Suína/genética , Ácido Glicirrízico/farmacologia , Glicoproteína da Espícula de Coronavírus , Adjuvantes Imunológicos , Imunidade , Proteínas Recombinantes , Lipídeos
3.
Eur J Pharm Biopharm ; 193: 262-273, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37944711

RESUMO

This study discusses the lubricant properties of magnesium stearate solid lipid nanoparticles (MgSt-SLN) and their effect on the tabletability, mechanical properties, disintegration, and acetaminophen-model dissolution time of microcrystalline cellulose (MCC) tablets prepared by direct compression. The behavior of MgSt-SLN was compared to reference material (RM) to identify advantages and drawbacks. The nanoprecipitation/ion exchange method was employed to prepare the MgSt-SLN. Particle size, zeta potential, specific surface area, morphology, and true density were measured to characterize the nanosystem. The MgSt-SLN particle sizes obtained were 240 ± 5 nm with a specific surface area of 12.2 m2/g. The MCC tablets with MgSt-SLN presented a reduction greater than 20 % in their ejection force, good tabletability, higher tensile strength, lower disintegration delay, and marked differences in acetaminophen dissolution when compared to the RM. The reduced particle size of the magnesium stearate seems to offer a promising technological advantage as an efficient lubricant process that does not affect the properties of tablets.


Assuntos
Acetaminofen , Lubrificantes , Lubrificantes/química , Ácidos Esteáricos/química , Excipientes/química , Comprimidos/química , Resistência à Tração
4.
Int J Mol Sci ; 24(19)2023 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-37834378

RESUMO

Bisphenols such as bisphenol A (BPA), S (BPS), C (BPC), F (BPF), AF (BPAF), tetrabromobisphenol, nonylphenol, and octylphenol are plasticizers used worldwide to manufacture daily-use articles. Exposure to these compounds is related to many pathologies of public health importance, such as infertility. Using a protector compound against the reproductive toxicological effects of bisphenols is of scientific interest. Melatonin and vitamins have been tested, but the results are not conclusive. To this end, this systematic review and meta-analysis compared the response of reproductive variables to melatonin and vitamin administration as protectors against damage caused by bisphenols. We search for controlled studies of male rats exposed to bisphenols to induce alterations in reproduction, with at least one intervention group receiving melatonin or vitamins (B, C, or E). Also, molecular docking simulations were performed between the androgen (AR) and estrogen receptors (ER), melatonin, and vitamins. About 1234 records were initially found; finally, 13 studies were qualified for review and meta-analysis. Melatonin plus bisphenol improves sperm concentration and viability of sperm and increases testosterone serum levels compared with control groups; however, groups receiving vitamins plus bisphenols had lower sperm concentration, total testis weight, and testosterone serum levels than the control. In the docking analysis, vitamin E had the highest negative MolDock score, representing the best binding affinity with AR and ER, compared with other vitamins and melatonin in the docking. Our findings suggest that vitamins could act as an endocrine disruptor, and melatonin is most effective in protecting against the toxic effects of bisphenols.


Assuntos
Disruptores Endócrinos , Melatonina , Masculino , Ratos , Animais , Melatonina/farmacologia , Vitaminas , Simulação de Acoplamento Molecular , Sêmen/metabolismo , Compostos Benzidrílicos/toxicidade , Compostos Benzidrílicos/química , Reprodução , Receptores de Estrogênio , Vitamina A , Vitamina K , Testosterona/metabolismo , Disruptores Endócrinos/toxicidade , Disruptores Endócrinos/química
5.
Int J Mol Sci ; 24(17)2023 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-37686226

RESUMO

Food bioactive peptides are well recognized for their health benefits such as antimicrobial, antioxidant, and antihypertensive benefits, among others. Their drug-like behavior has led to their potential use in targeting skin-related aging factors like the inhibition of enzymes related with the skin-aging process. In this study, canary seed peptides (CSP) after simulated gastrointestinal digestion (<3 kDa) were fractioned by RP-HPLC and their enzyme-inhibition activity towards elastase and tyrosinase was evaluated in vitro. CSP inhibited elastase (IC50 = 6.2 mg/mL) and tyrosinase (IC50 = 6.1 mg/mL), while the hydrophobic fraction-VI (0.2 mg/mL) showed the highest inhibition towards elastase (93%) and tyrosinase (67%). The peptide fraction with the highest inhibition was further characterized by a multilevel in silico workflow, including physicochemical descriptor calculations, antioxidant activity predictions, and molecular dynamics-ensemble docking towards elastase and tyrosinase. To gain insights into the skin permeation process during molecular dynamics simulations, based on their docking scores, five peptides (GGWH, VPPH, EGLEPNHRVE, FLPH, and RPVNKYTPPQ) were identified to have favorable intermolecular interactions, such as hydrogen bonding of polar residues (W, H, and K) to lipid polar groups and 2-3 Å van der Waals close contact of hydrophobic aliphatic residues (P, V, and L). These interactions can play a critical role for the passive insertion of peptides into stratum corneum model skin-membranes, suggesting a promising application of CSP for skin-aging treatments.


Assuntos
Monofenol Mono-Oxigenase , Phalaris , Simulação de Dinâmica Molecular , Elastase Pancreática , Sementes , Antioxidantes/farmacologia
6.
Int J Cosmet Sci ; 45(6): 699-724, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37402111

RESUMO

The term biopolymer refers to materials obtained by chemically modifying natural biological substances or producing them through biotechnological processes. They are biodegradable, biocompatible and non-toxic. Due to these advantages, biopolymers have wide applications in conventional cosmetics and new trends and have emerged as essential ingredients that function as rheological modifiers, emulsifiers, film-formers, moisturizers, hydrators, antimicrobials and, more recently, materials with metabolic activity on skin. Developing approaches that exploit these features is a challenge for formulating skin, hair and oral care products and dermatological formulations. This article presents an overview of the use of the principal biopolymers used in cosmetic formulations and describes their sources, recently derived structures, novel applications and safety aspects of the use of these molecules.


Le terme biopolymère fait référence aux matériaux obtenus par modification chimique des substances biologiques naturelles ou ceux qui surviennent des processus biotechnologiques. Ils sont biodégradables, biocompatibles, et non-toxiques. Du à leur avantages, les biopolymères ont de larges applications dans les cosmétiques conventionnels ainsi que dans les nouvelles tendances, et se placent comme des ingrédients essentiels qui peut être utilise comme modificateurs rhéologiques, émulsifiants, producteurs de films, humectants, hydratants, antimicrobiens, et, plus récemment, comme matériaux avec activité métabolique sur la peau. Le développement d'approches compte tenu de ces caractéristiques constitue un défi pour la création de produits de soins capillaires, dermatologiques et buccodentaires. Cet article présente une vision sur l'utilisation des principaux biopolymères dans les produits cosmétiques, et décrit leurs sources, leur structures dérivées, les nouvelles applications, ainsi que les aspects de sécurité lies à leur utilisation comme molécules cosmétiques.


Assuntos
Cosméticos , Biopolímeros/química , Emulsificantes
7.
Polymers (Basel) ; 15(5)2023 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-36904450

RESUMO

Solid lipid nanoparticles (SLN) based on candelilla wax were prepared using the hot homogenization technique. The resulting suspension had monomodal behavior with a particle size of 809-885 nm; polydispersity index < 0.31, and zeta potential of -3.5 mV 5 weeks after monitoring. The films were prepared with SLN concentrations of 20 and 60 g/L, each with a plasticizer concentration of 10 and 30 g/L; the polysaccharide stabilizers used were either xanthan gum (XG) or carboxymethyl cellulose (CMC) at 3 g/L. The effects of temperature, film composition, and relative humidity on the microstructural, thermal, mechanical, and optical properties, as well as the water vapor barrier, were evaluated. Higher amounts of SLN and plasticizer gave the films greater strength and flexibility due to the influence of temperature and relative humidity. The water vapor permeability (WVP) was lower when 60 g/L of SLN was added to the films. The arrangement of the SLN in the polymeric networks showed changes in the distribution as a function of the concentrations of the SLN and plasticizer. The total color difference (ΔE) was greater when the content of the SLN was increased, with values of 3.34-7.93. Thermal analysis showed an increase in the melting temperature when a higher SLN content was used, whereas a higher plasticizer content reduced it. Edible films with the most appropriate physical properties for the packaging, shelf-life extension, and improved quality conservation of fresh foods were those made with 20 g/L of SLN, 30 g/L of glycerol, and 3 g/L of XG.

8.
Molecules ; 27(23)2022 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-36500284

RESUMO

Consumers today demand the use of natural additives and preservatives in all fresh and processed foods, including meat and meat products. Meat, however, is highly susceptible to oxidation and microbial growth that cause rapid spoilage. Essential oils are natural preservatives used in meat and meat products. While they provide antioxidant and antimicrobial properties, they also present certain disadvantages, as their intense flavor can affect the sensory properties of meat, they are subject to degradation under certain environmental conditions, and have low solubility in water. Different methods of incorporation have been tested to address these issues. Solutions suggested to date include nanotechnological processes in which essential oils are encapsulated into a lipid or biopolymer matrix that reduces the required dose and allows the formation of modified release systems. This review focuses on recent studies on applications of nano-encapsulated essential oils as sources of natural preservation systems that prevent meat spoilage. The studies are critically analyzed considering their effectiveness in the nanostructuring of essential oils and improvements in the quality of meat and meat products by focusing on the control of oxidation reactions and microbial growth to increase food safety and ensure innocuity.


Assuntos
Anti-Infecciosos , Produtos da Carne , Óleos Voláteis , Óleos Voláteis/farmacologia , Conservantes de Alimentos/farmacologia , Carne/análise , Anti-Infecciosos/farmacologia , Conservação de Alimentos/métodos
9.
Intervirology ; 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36455522

RESUMO

BACKGROUND: Emerging virus infections provoke health problems in people and animals, which generate social, and economic issues worldwide. This has spurred the search for new pharmacological strategies to confront them. SUMMARY: The purpose of this review is to draw the reader's attention to pharmacological evaluations of glycyrrhizic acid (GA) and its analogs on the broad range of viruses known in human and veterinary medicine. GA is the main water-soluble constituent extracted from the roots of plants from the genus Glycyrrhiza, commonly known as licorice root. It has long been used due to its broad spectrum of bioactivities, including anti-inflammatory, antiulcer, and antitumor properties. It has also been proposed as an antiviral agent. Medicines derived from GA are currently being used to combat acute and chronic hepatitis and herpes viruses. KEY MESSAGES: This review suggests that GA could be a new broad-spectrum antiviral due to its ability to inhibit DNA or RNA viruses both in vitro and in vivo. GA could be a potential drug for preventing and/or treating various viral diseases.

10.
Polymers (Basel) ; 14(22)2022 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-36433107

RESUMO

Polymeric nanoparticles have attracted much attention as pharmaceutical delivery vehicles to prolong residence time and enhance the bioavailability of therapeutic molecules through the mucoadhesive phenomenon. In this study, chitosan:TPP nanoparticles were synthetized using the ionic gelation technique to analyze their mucoadhesive interaction with reconstituted porcine gastrointestinal mucus from a triborheological point of view under different pH conditions (pH = 2.0, 4.0, 6.0 and 7.0). The triborheological profile of the reconstituted mucus was evaluated at different pH environments through the oscillation frequency and the flow sweep tests, demonstrating that the reconstituted mucus exhibits shear thinning behavior regardless of pH, while its viscoelastic properties showed a change in behavior from a polymeric solution performance under neutral pH conditions to a viscoelastic gel under acidic conditions. Additionally, a rheological synergism analysis was performed to visualize the changes that occur in the viscoelastic properties, the viscosity and the coefficient of friction of the reconstituted mucus samples as a consequence of the interaction with the chitosan:TPP nanoparticles to determine or to discard the presence of the mucoadhesion phenomenon under the different pH values. Mucoadhesiveness evaluation revealed that chitosan:TPP exhibited strong mucoadhesion under highly acidic pH conditions, below its pKa value of 6.5. In contrast, at neutral conditions or close to its pKa value, the chitosan:TPP nanoparticles' mucoadhesiveness was negligible.

11.
Int J Vet Sci Med ; 10(1): 72-79, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36259046

RESUMO

Both Gram-negative and Gram-positive bacteria have recently developed antibiotic resistance to treatments for bovine mastitis, creating a serious concern for public and animal health. The objective of this study was to analyse in vitro microbicidal activity of tea tree oil, thymol and carvacrol (composed of oregano and thyme essential oils) on bacteria isolated from clinical mastitis. Field isolates and ATCC strains of the Staphylococcus spp, Streptococcus spp, Escherichia coli, Klebsiella pneumoniae, and Candida albicans genera were analysed. The agar diffusion technique was used to test bactericidal susceptibility and plate microdilution was utilized to determine the minimum inhibitory, bactericidal, and fractional inhibitory concentrations. Thymol alone and the combinations of thymol-carvacrol and thymol-TTO obtained the highest inhibition diameters for Gram-negative bacteria, while for Gram-positive bacteria and C. albicans, thymol and the combination thymol-carvacrol obtained the highest indices. TTO, thymol, and carvacrol had MIC values of 1.56-25 mg/ml, 0.05-0.4 mg/ml, and 0.02-0.2 mg/ml, respectively. CMB results for the Gram-negative and gram-positive groups were 0.39-0.78 mg/ml, and for C. albicans, 0.78-1.56 mg/ml. Results for the fractional inhibitory concentrations show that the TTO+thymol and thymol+carvacrol combinations had additive activity against groups of Gram-negative bacteria and C. albicans. These natural components, evaluated individually and in combinations, have an effectiveness above 70%.

12.
Foods ; 11(14)2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35885393

RESUMO

Due to their high water, lipid, and protein content, meat and meat products are highly perishable. The principal spoilage mechanisms involved are protein and lipid oxidation and deterioration caused by microbial growth. Therefore, efforts are ongoing to ensure food safety and increase shelf life. The development of low-cost, innovative, eco-friendly approaches, such as nanotechnology, using non-toxic, inexpensive, FDA-approved ingredients is reducing the incorporation of chemical additives while enhancing effectiveness and functionality. This review focuses on advances in the incorporation of natural additives that increase the shelf life of meat and meat products through the application of nanosystems. The main solvent-free preparation methods are reviewed, including those that involve mixing organic-inorganic or organic-organic compounds with such natural substances as essential oils and plant extracts. The performance of these additives is analyzed in terms of their antioxidant effect when applied directly to meat as edible coatings or marinades, and during manufacturing processes. The review concludes that nanotechnology represents an excellent option for the efficient design of new meat products with enhanced characteristics.

13.
Nanomaterials (Basel) ; 11(12)2021 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-34947551

RESUMO

The aim of this work was to obtain pH-dependent nanofibers with an electrospinning technique as a novel controlled release system for the treatment of periodontal disease (PD). Cellulose acetate phthalate (CAP) was selected as a pH-sensitive and antimicrobial polymer. The NF was optimized according to polymeric dispersion variables, polymer, and drug concentration, and characterized considering morphology, diameter, entrapment efficiency (EE), process efficiency (PE), thermal properties, and release profiles. Two solvent mixtures were tested, and CHX-CAP-NF prepared with acetone/ethanol at 12% w/v of the polymer showed a diameter size of 934 nm, a uniform morphology with 42% of EE, and 55% of PE. Meanwhile, CHX-CAP-NF prepared with acetone/methanol at 11% w/v of polymer had a diameter of 257 nm, discontinuous nanofiber morphology with 32% of EE, and 40% of PE. EE and PE were dependent on the polymer concentration and the drug used in the formulation. Studies of differential scanning calorimetry (DSC) showed that the drug was dispersed in the NF matrix. The release profiles of CHX from CHX-CAP-NF followed Fickian diffusion dependent on time (t0.43-0.45), suggesting a diffusion-erosion process and a matrix behavior. The NF developed could be employed as a novel drug delivery system in PD.

14.
Drug Dev Ind Pharm ; 47(8): 1302-1309, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34719999

RESUMO

In this study, a Venturi tube is proposed as an efficient static mixer incorporated into a continuous recirculation system for obtaining solid lipid nanoparticles (SLN) of monoolein. The device's operating principle consists of producing a turbulent flux in the throat of a Venturi tube. Taking advantage of this effect SLN of monoolein were obtained by rapid diffusion of the organic phase into the aqueous phase (stabilizer), causing lipid aggregation on the nanometric particles. The main aim of the present study was to evaluate the critical factors for obtaining the SLN of monoolein in order to control the independent variables of this methodology. A Box-Behnken design was used to study such independent variables (factors) as injection rate (X1), recirculation rate (X2), and stabilizer (X3) on the dependent variables; namely, process yield (Y1), particle size (Y2), polydispersity index (Y3) and zeta potential (Y4). The optimum operating conditions for preparing SLN were: injection rate, 1.6 mL/min; recirculation rate, 4.2 L/min; and stabilizer concentration, 1.0 w/v, with a value of D = 0.84. The predicted responses of the particle size were 212.0 nm, with a polydispersity index of 0.21, a zeta potential of -19.9 mV, and a process yield of 96.0%. Under the same operating condition, SLN formed with different lipids and stabilizers were obtained with nanometric size and zeta potential of ∼ -30.0 mV. Results show that the Venturi tube method is an innovative and versatile technique for preparing SLN of nanometric size with high process yields through a turbulent flow.


Assuntos
Lipídeos , Nanopartículas , Excipientes , Lipossomos , Tamanho da Partícula
15.
Gels ; 7(4)2021 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-34842688

RESUMO

The nanoencapsulation of thyme essential oil has been greatly important in food science, given its remarkable antioxidant and antimicrobial capacity. However, its analysis in storage has not been established in terms of physical stability, antioxidant capacity, and release studies. In this paper, chitosan-thyme oil nanocapsules were prepared by the ionic gelation method. These were characterized for differential calorimetry, release kinetic, and infrared spectroscopy. The chitosan-thyme oil nanocapsules were stored at 4 and 25 °C for 5 weeks, the changes in particle size, zeta potential, stability (diffuse reflectance), and antioxidant capacity were analyzed and associated with nanocapsules' functionality. The results show that the storage time and temperature significantly modify the particle size (keeping the nano-size throughout the storage), the release of the bioactive was Fickian with t0.193 according to Korsmery & Peppas and best described by Higuchi model associated with changes in the zeta potential from 8 mV to -11 mV at 4 °C. The differential scanning calorimetry and infrared spectroscopy results confirm the good integration of the components. The antioxidant capacity revealed a direct relationship with residual oil concentration with a decrease in the ABTS test of 15% at 4 °C and 37% at 25 °C. The residual bioactive content was 77% at 4 °C and 62% at 25 °C, confirming nanoencapsulation effectiveness. The present investigation provides helpful information so that these systems can be applied in food conservation.

16.
Polymers (Basel) ; 13(21)2021 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-34771260

RESUMO

The objective of this study was to evaluate the effectiveness of a combination of UV-C disinfection treatment and a nano-coating lemon essential oil nanocapsules. The nanocapsules were prepared by ionic gelation with an alginate-pectin wall and the lemon essential oil had a particle size of 219 ± 22 nm and a zeta potential of -7.91 ± 0.18 mV. The lemon essential oil had an encapsulation efficiency of 68.19 ± 1.18%. The fresh-cut cucumber was stored for 15 days at 4 °C. Six formulations of nanocapsules were evaluated, and hydroxypropyl methylcellulose was used as matrix polysaccharide in four coatings. Three formulations were treated with UV-C at 4.5 kJ/m2. The results showed that the combination of UV-C and nano-coatings (lemon essential oil = 200 mg/L) increased the shelf life by up to 15 days. Using UV-C and nano-coatings, the ∆E value was 7.12 at the end of the storage period, while the Control samples had an ∆E of 28.1. With nano-coating treatment, the amount of polyphenols decreased by 23% within 9 days. In contrast, with combined UV-C and nano-coating treatment, the amount of polyphenols was reduced by 38.84% within 15 days. The antioxidant capacity remained stable at 459 µmol TE/100 g for the fresh product when the combined treatment was used. A good correlation was also observed between the increasing of the fruit's shelf life and decreasing of its enzymatic activity. The inclusion of UV-C treatment contributed to the reduction in the initial total bacteria at 3.30 log CFU/g and its combination with nano-coatings helped in the control of microbial growth during storage.

17.
J Pharm Pharm Sci ; 24: 509-532, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34644523

RESUMO

Nanoparticles have shown overall beneficial effects in drug administration. Specifically, solid lipid nanoparticles (SLN) have emerged as an alternative to polymer-based systems. However, the oral administration of SLN, the first choice for conventional medications, has not been addressed due to the taboo surrounding the complicated transit that this delivery route entails. This review focuses on the encapsulation of drugs into SLN as a strategy for improving oral administration. Examples of applications of SLN to enhance the absorption and bioavailability of poorly-soluble drugs and protect acid-labile active molecules are discussed. This work also emphasizes the importance of developing SLN-based systems to treat health issues such as neurological diseases and cancer, and combat antibiotic resistance, three significant and increasingly common current public health problems. The review sections clarify how SLN can improve bioavailability, target therapeutic agents, and reduce side effects.


Assuntos
Administração Oral , Lipossomos/administração & dosagem , Sistemas de Liberação de Fármacos por Nanopartículas/administração & dosagem , Nanopartículas/administração & dosagem , Animais , Disponibilidade Biológica , Humanos , Solubilidade
18.
Molecules ; 26(7)2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33917445

RESUMO

The purpose of the study was to develop a novel, directly compressible, co-processed excipient capable of providing a controlled-release drug system for the pharmaceutical industry. A co-processed powder was formed by adsorption of solid lipid nanoparticles (SLN) as a controlled-release film onto a functional excipient, in this case, dicalcium phosphate dihydrate (DPD), for direct compression (Di-Tab®). The co-processed excipient has advantages: easy to implement; solvent-free; industrial scaling-up; good rheological and compressibility properties; and the capability to form an inert platform. Six different batches of Di-Tab®:SLN weight ratios were prepared (4:0.6, 3:0.6, 2:0.6, 1:0.6, 0.5:0.6, and 0.25:0.6). BCS class III ranitidine hydrochloride was selected as a drug model to evaluate the mixture's controlled-release capabilities. The co-processed excipients were characterized in terms of powder rheology and dissolution rate. The best Di-Tab®:SLN ratio proved to be 2:0.6, as it showed high functionality with good flow and compressibility properties (Carr Index = 16 ± 1, Hausner Index = 1.19 ± 0.04). This ratio could control release for up to 8 h, so it fits the ideal profile calculated based on biopharmaceutical data. The compressed systems obtained using this powder mixture behave as a matrix platform in which Fickian diffusion governs the release. The Higuchi model can explain their behavior.


Assuntos
Preparações de Ação Retardada/farmacologia , Excipientes/química , Lipídeos/química , Nanopartículas/química , Força Compressiva , Liberação Controlada de Fármacos , Nanopartículas/ultraestrutura , Tamanho da Partícula , Pós , Ranitidina/farmacologia , Reologia
19.
Biometals ; 34(3): 687-700, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33900531

RESUMO

Neurodegenerative disorders have been linked to the decrease of copper concentrations in different regions of the brain. Therefore, intake of micronutrient supplements could be a therapeutic alternative. Since the copper distribution profile has not been elucidated yet, the aim of this study was to characterize and to analyze the concentration profile of a single administration of copper gluconate to rats by two routes of administration. Male Wistar rats were divided into three groups. The control group received vehicle (n = 5), and the experimental groups received 79.5 mg/kg of copper orally (n = 4-6) or 0.64 mg/kg of copper intravenously. (n = 3-4). Blood, striatum, midbrain and liver samples were collected at different times. Copper concentrations were assessed using atomic absorption spectrophotometry. Copper concentration in samples from the control group were considered as baseline. The highest copper concentration in plasma was observed at 1.5 h after oral administration, while copper was quickly compartmentalized within the first hour after intravenous administration. The striatum evidenced a maximum metal concentration at 0.25 h for both routes of administration, however, the midbrain did not show any change. The highest concentration of the metal was held by the liver. The use of copper salts as replacement therapy should consider its rapid and discrete accumulation into the brain and the rapid and massive distribution of the metal into the liver for both oral and intravenous routes. Development of controlled-release pharmaceutical formulations may overcome the problems that the liver accumulation may imply, particularly, for hepatic copper toxicity.


Assuntos
Gluconatos/farmacocinética , Administração Oral , Animais , Relação Dose-Resposta a Droga , Gluconatos/administração & dosagem , Gluconatos/sangue , Injeções Intravenosas , Masculino , Ratos , Ratos Wistar , Distribuição Tecidual
20.
RSC Adv ; 11(4): 2226-2234, 2021 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-35424190

RESUMO

From an integral perspective, nanotechnology can be used to care for the environment by improving current preparation methods and facilitating industrial scale-up. This article discusses the implementation of techniques for obtaining polystyrene nanoparticles (PSN), as an added value, using an emulsification and solvent displacement method (EDSD); the solvent displacement is a novel modification to the emulsion-diffusion methodology, where the diffusion is done directly on the emulsion, which allows concentrated dispersions that facilitate direct use to be obtained, eliminating the dilution with water and the recovery of water by additional processes. The solvent was recovered by reduced pressure, which is class 3, conforming to ICH, and making this method sustainable. The optimization of this process has not been reported elsewhere. This approach made it possible to obtain highly-concentrated nanoparticles while allowing the reuse of the solvent. A scaling proposal is presented that integrates the conditioning of the solid urban waste material called expanded polystyrene (EPS) foam that constitutes a serious environmental problem both nationally and globally. Hence, the article presents an alternative to the recycling of EPS, and a methodology in the context of green chemistry, because solvent is recovered to prepare other batches. The PSN obtained from this waste material had a minimum particle size of 225.8 nm, with a polydispersion index of 0.158. Process performance was 97.1%, and the solvent was recovered at a maximum rate of 85%. The morphology of the PSN was spherical and uniform, with a smooth surface.

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