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1.
Int J Biol Macromol ; 274(Pt 2): 133048, 2024 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-38857734

RESUMO

Epiisopiloturine (EPI) is a compound found in jaborandi leaves with antiparasitic activity, which can be enhanced when incorporated into nanoparticles (NP). Cashew Gum (CG), modified by carboxymethylation, is used to produce polymeric nanomaterials with biological activity. In this study, we investigated the antimicrobial potential of carboxymethylated CG (CCG) NP containing EPI (NPCCGE) and without the alkaloid (NPCCG) against bacteria and parasites of the genus Leishmania. We conducted theoretical studies, carboxymethylated CG, synthesized NP by nanoprecipitation, characterized them, and tested them in vitro. Theoretical studies confirmed the stability of modified carbohydrates and showed that the EPI-4A30 complex had the best interaction energy (-8.47 kcal/mol). CCG was confirmed by FT-IR and presented DSabs of 0.23. NPCCG and NPCCGE had average sizes of 221.94 ± 144.086 nm and 247.36 ± 3.827 nm, respectively, with homogeneous distribution and uniform surfaces. No NP showed antibacterial activity or cytotoxicity to macrophages. NPCCGE demonstrated antileishmanial activity against L. amazonensis, both in promastigote forms (IC50 = 9.52 µg/mL, SI = 42.01) and axenic amastigote forms (EC50 = 6.6 µg/mL, SI = 60.60). The results suggest that nanostructuring EPI in CCG enhances its antileishmanial activity.

2.
Chem Biol Interact ; 398: 111115, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-38908811

RESUMO

In the present study, the effect of sulfonamide-chalcone 185 (SSC185) was investigated against B16-F10 metastatic melanoma cells aggressive actions, besides migration and adhesion processes, by in silico and in vitro assays. In silico studies were used to characterize the pharmacokinetic profile and possible targets of SSC185, using the pkCSM web server, and docking simulations with AutoDock Tools. Furthermore, the antimetastatic effect of SSC185 was investigated by in vitro experiments using MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide), colony, scratch, and cell adhesion assays, and atomic force microscopy (AFM). The molecular docking results show better affinity of SSC185 with the metalloproteinases-2 (MMP-2) and α5ß1 integrin. SSC185 effectively restricts the formation of colonies, migration, and adhesion of B16-F10 metastatic melanoma cells. Through the AFM images changes in cells morphology was identified, with a decrease in the filopodia and increase in the average cellular roughness. The results obtained demonstrate the potential of this molecule in inhibit the primordial steps for metastasis, which is responsible for a worse prognosis of late stage cancer, being the main cause of morbidity among cancer patients.


Assuntos
Adesão Celular , Movimento Celular , Chalcona , Simulação de Acoplamento Molecular , Sulfonamidas , Movimento Celular/efeitos dos fármacos , Adesão Celular/efeitos dos fármacos , Sulfonamidas/farmacologia , Sulfonamidas/química , Camundongos , Animais , Linhagem Celular Tumoral , Chalcona/farmacologia , Chalcona/química , Chalcona/análogos & derivados , Metaloproteinase 2 da Matriz/metabolismo , Melanoma Experimental/patologia , Melanoma Experimental/tratamento farmacológico , Melanoma Experimental/metabolismo , Microscopia de Força Atômica , Antineoplásicos/farmacologia , Antineoplásicos/química , Chalconas/farmacologia , Chalconas/química , Humanos
3.
Int J Biol Macromol ; 268(Pt 1): 131661, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38641286

RESUMO

In this study, two nanoemulsions were formulated with essential oil (EO) of Ocimum gratissimum with (EON) or without (EOE) cashew gum (CG). Subsequently, inhibition of melanosis and preservation of the quality of shrimp stored for 16 days at 4 ± 0.5 °C were evaluated. A computational approach was performed to predict the system interactions. Dynamic light scattering (DLS) and atomic force microscopy (AFM) were used for nanoparticle analysis. Gas chromatography and flame ionization detector (GC-FID) determined the chemical composition of the EO constituents. Shrimps were evaluated according to melanosis's appearance, psychrotrophic bacteria's count, pH, total volatile basic nitrogen, and thiobarbituric acid reactive substances. EON exhibited a particle size three times smaller than EOE. The shrimp treated with EON showed a more pronounced sensory inhibition of melanosis, which was considered mild by the 16th day. Meanwhile, in the other groups, melanosis was moderate (EOE) or severe (untreated group). Both EON and EOE treatments exhibited inhibition of psychrotrophic bacteria and demonstrated the potential to prevent lipid oxidation, thus extending the shelf life compared to untreated fresh shrimp. EON with cashew gum, seems more promising due to its physicochemical characteristics and superior sensory performance in inhibiting melanosis during shrimp preservation.


Assuntos
Anacardium , Ocimum , Óleos Voláteis , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Ocimum/química , Anacardium/química , Penaeidae/química , Gomas Vegetais/química , Conservação de Alimentos/métodos
4.
J Pharm Pharmacol ; 76(6): 732-742, 2024 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-38546507

RESUMO

OBJECTIVES: Angico gum (AG) (Anadenanthera colubrina var. Cebil [Griseb.] Altschul) is utilized by some Brazilian communities to alleviate symptoms from gastroesophageal reflux disease. Here, we aimed to investigate the "in vitro" topical protective capacity of AG on human esophageal mucosa. METHODS: Biopsies of the distal esophageal mucosa were collected from 35 patients with heartburn (24 non-erosive and 11 with erosive oesophagitis (EE)) and mounted in Üssing chambers. AG was applied topically, followed by exposure with acid solution (pH 2.0 or pH 1.0), where transepithelial electrical resistance (TER) and The transepithelial permeability for fluorescein was assessed. The incubation of the AG labeled with FITC in the esophageal mucosa was localized by fluorescence microscopy. KEY FINDINGS: Pretreatment with AG prevented the drop in TER induced by acid solution, as well as significantly decreases the fluorescein permeability in non-erosive patients. The protective effect of AG was sustained for up to 120 min both in biopsies of non-erosive and erosive esophagitis. Confocal microscope images showed mucosal luminal adherence of FITC-labeled AG. CONCLUSION: AG had a prolonged topical protective effect against acid solution in mucosal biopsies of patients with non-erosive and erosive esophagitis.


Assuntos
Mucosa Esofágica , Refluxo Gastroesofágico , Humanos , Refluxo Gastroesofágico/tratamento farmacológico , Refluxo Gastroesofágico/prevenção & controle , Mucosa Esofágica/efeitos dos fármacos , Mucosa Esofágica/patologia , Mucosa Esofágica/metabolismo , Masculino , Feminino , Pessoa de Meia-Idade , Adulto , Permeabilidade , Impedância Elétrica , Administração Tópica , Biopolímeros , Idoso , Fluoresceína/administração & dosagem , Esôfago/efeitos dos fármacos , Esôfago/patologia , Esôfago/metabolismo , Azia/tratamento farmacológico , Azia/prevenção & controle , Relevância Clínica
5.
Int J Biol Macromol ; 260(Pt 1): 129397, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38219933

RESUMO

Biotechnological advancements require the physicochemical alteration of molecules to enhance their biological efficacy for the effective treatment of gastric ulcers. The study aimed to produce a polyelectrolytic compound from red angico gum (AG) by carboxymethylation, evaluate its physicochemical characteristics and investigate gastric protection against ethanol-induced ulcers. AG and carboxymethylated angico gum (CAG) were characterized by Fourier transform infrared spectroscopy, determination of the degree of substitution and gel permeation chromatography (GPC) and 13C NMR techniques. The results demonstrated that the modification of the polymer was satisfactory, presenting conformational changes e improving the interaction with the gastric mucosa. AG and CAG reduced macroscopic and microscopic damage such as edema, hemorrhage and cell loss caused by exposure of the mucosa to alcohol. Both demonstrated antioxidant activity in vitro, and in vivo, pretreatment with gums led to the restoration of superoxide dismutase and glutathione levels compared to the injured group. Concurrently, the levels of malondialdehyde and nitrite decreased. Atomic force microscopy showed that CAG presented better conformational properties of affinity and protection with the gastric mucosa compared to AG in the acidic pH. Based on our findings, it is suggested that this compound holds promise as a prospective product for future biotechnological applications.


Assuntos
Colubrina , Fabaceae , Úlcera Gástrica , Estudos Prospectivos , Estômago , Antioxidantes/efeitos adversos , Mucosa Gástrica , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Extratos Vegetais/química
6.
Saúde Soc ; 33(1): e220584pt, 2024. tab, graf
Artigo em Português | LILACS-Express | LILACS | ID: biblio-1536866

RESUMO

Resumo Centrando-se no impacto que a comunicação de risco emitida pelas organizações de saúde pública tem na mudança dos comportamentos da sociedade, esta investigação pretende analisar as mensagens-chave que a Organização Mundial de Saúde (OMS) definiu para promover o programa de vacinação contra a covid-19. Para cumprir este objetivo, enveredou-se por uma metodologia de estudo qualitativa, que privilegiou o uso da análise do conteúdo publicado nas páginas de Facebook e de Instagram da OMS, no período de 1 de abril a 31 de agosto de 2021. No total, foram analisadas 62 publicações. Os resultados mostraram que a OMS utilizou quatro eixo de comunicação para promover a importância da vacinação na sociedade: garantir a credibilidade e a transparência da informação transmitida; certificar a segurança e a eficácia da vacina; apelar ao sentido de responsabilidade coletiva; e associar a vacina à solução para pôr fim à pandemia. As conclusões do estudo mostram que, embora a equidade no acesso à vacina ainda seja uma realidade em construção, os quase 70% da população mundial vacinada sugerem que as mensagens enviadas pela OMS no contexto de comunicação de risco podem ter contribuído para a construção de uma imagem positiva do programa de vacinação.


Abstract Focusing on the impact that risk communication issued by public health organizations brings to changing societal behaviors, this research aimed to analyze the key messages that the World Health Organization (WHO) has defined to promote the COVID-19 vaccination program. In order to achieve this goal, a qualitative study methodology was used to analyze the content published on the WHO's Facebook and Instagram pages from April 1 to August 31, 2021. In total, 62 publications were analyzed. The results showed that the WHO used four key communication messages to promote the importance of vaccination in society: ensuring the credibility and transparency of the information transmitted; certifying the safety and efficacy of the vaccine; appealing to a sense of collective responsibility; and associating the vaccine with the solution to end the pandemic were the chosen communication axes. The conclusions of this study show that, although fair access to the vaccine is still a reality in the making, the fact that almost 70% of the world's population has been vaccinated suggests that the messages sent by the WHO in the context of risk communication may have contributed to building a positive image of the vaccination program.

7.
Int J Biol Macromol ; 253(Pt 6): 127281, 2023 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-37806422

RESUMO

Hydrogels made with depolymerized guar gum, oxidized with theoretical oxidation degrees of 20, 35 and 50 %, were obtained via Schiff's base reaction with N-succinyl chitosan. The materials obtained were subjected to characterization by FT-IR, rheology, swelling, degradation, and morphology. Additionally, their gelation time categorized all three hydrogels as injectable. The materials' swelling degrees in Phosphate-Buffered Saline (PBS) were in the range of 26-35 g of fluid/g gel and their pore size distribution was heterogeneous, with pores varying from 67 to 93 µm. All hydrogels degraded in PBS solution, but maintained around 40 % of their initial mass after 28 days, which was more than enough time for wound healing. The biomaterials were also flexible, self-repairing, adhesive and cytocompatible and presented intrinsic actions, regardless of the presence of additives or antibiotics, against gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and gram-negative bacteria (Escherichia coli). However, the most pronounced bactericidal effect was against resistant Staphylococcus aureus - MRSA. In vivo assays, performed with 50 % oxidized gum gel, demonstrated that this material exerted anti-inflammatory effects, accelerating the healing process and restoring tissues by approximately 99 % within 14 days. In conclusion, these hydrogels have unique characteristics, making them excellent candidates for wound-healing dressings.


Assuntos
Quitosana , Staphylococcus aureus Resistente à Meticilina , Hidrogéis/farmacologia , Quitosana/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Bandagens , Bactérias , Antibacterianos/farmacologia , Staphylococcus aureus
8.
Medicina (Kaunas) ; 59(8)2023 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-37629700

RESUMO

Background: Noninvasive ventilation (NIV) provides positive pressure through different interfaces. A multifunctional full-face mask prototype was developed to provide NIV from three sources: ICU ventilators, portable ventilators, and high-flow medical gas pipeline systems. This study aimed to evaluate the usability of this prototype mask. Methods: This was a quantitative experimental study, conducted in two phases: the development of a full-face mask prototype NIV interface, and the evaluation of its usability by health professionals (evaluators) using a heuristic approach. The Wolf Mask prototype is a multifunctional full-face mask that makes it possible to deliver positive pressure from three different sources: microprocessor-controlled ICU ventilators, portable ventilators with single-limb circuits, and high-flow medical gas. The evaluation was conducted in three stages: presentation of the prototype to the evaluators; skills testing via simulation in a clinical environment; and a review of skills. Results: The prototype was developed by a multidisciplinary team and patented in Brazil. The evaluators were 10 health professionals specializing in NIV. Seven skills related to handling the prototype were evaluated. Three of the ten evaluators called for (non-urgent) changes to improve recognition of the components of the prototype. Only one evaluator called for (non-urgent) changes to improve recognition of the pieces, assembly, and checking the mask. Conclusions: The newly developed multifunctional full-face mask prototype demonstrated excellent usability for providing noninvasive ventilation from multiple sources. Minor modifications may further improve the design.


Assuntos
Ventilação não Invasiva , Máscaras , Respiração Artificial , Brasil , Simulação por Computador
9.
Braz J Microbiol ; 54(3): 2319-2331, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37578738

RESUMO

Sulfentrazone (STZ) is an efficient tool for the pre- and post-emergence control of monocotyledonous and dicotyledonous weeds in fields of crops such as pineapple, coffee, sugarcane, citrus, eucalyptus, tobacco, and soybean. However, this herbicide persists in the soil, causing phytotoxicity in the subsequent crop. Therefore, it is important to use efficient strategies for the remediation of STZ-contaminated areas. The aim of this study was to evaluate the effects of Crotalaria juncea L. on the remediation of STZ-contaminated soil and on the microbial activity and bacterial community structure therein. The study was conducted in three stages: (i) cultivation of C. juncea in soil contaminated with 200, 400, and 800 g ha-1 STZ; (ii) determination of the soil microbial activity (basal respiration, microbial biomass carbon, and bacterial community structure); and (iii) cultivation of a bioindicator species and determination of the residual fraction of STZ. The soil microbial activity was impacted by the soil type and STZ dose. Soil previously cultivated with C. juncea (rhizospheric soil) displayed higher CO2 and lower qCO2 values than non-rhizospheric soil (no previous C. juncea cultivation). Increasing doses of STZ reduced the activity and lowered the diversity indices of the soil microorganisms. The bacterial community structure was segregated between the rhizospheric and non-rhizospheric soils. Regardless of soil type, the bioindicator of remediation (Pennisetum glaucum R.Br.) grew only at the STZ dose of 200 g ha-1, and the plant intoxication level was also lower in rhizospheric soil treated with this herbicide dose. All P. glaucum plants died in the soils treated with 400 and 800 g ha-1 STZ. Previous cultivation of C. juncea in soils contaminated with 200, 400, and 800 g ha-1 STZ reduced the residual fraction of the herbicide by 4.8%, 12.5%, and 17.4%, respectively, compared with that in the non-rhizospheric soils. In conclusion, previous cultivation with C. juncea promoted increases in the soil bacterial activity and diversity indices, mitigated the deleterious effects of STZ on the bioindicator crop, and reduced the residual fraction of the herbicide in the soil.


Assuntos
Crotalaria , Microbiologia do Solo , Sulfonamidas , Triazóis , Crotalaria/metabolismo , Biodegradação Ambiental , Sulfonamidas/metabolismo , Triazóis/metabolismo
10.
Front Public Health ; 11: 1215574, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37457260

RESUMO

Recurrent outbreaks of zoonotic infectious diseases highlight the importance of considering the interconnections between human, animal, and environmental health in disease prevention and control. This has given rise to the concept of One Health, which recognizes the interconnectedness of between human and animal health within their ecosystems. As a contribution to the One Health approach, this study aims to develop an indicator system to model the facilitation of the spread of zoonotic diseases. Initially, a literature review was conducted using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) statement to identify relevant indicators related to One Health. The selected indicators focused on demographics, socioeconomic aspects, interactions between animal and human populations and water bodies, as well as environmental conditions related to air quality and climate. These indicators were characterized using values obtained from the literature or calculated through distance analysis, geoprocessing tasks, and other methods. Subsequently, Multi-Criteria Decision-Making (MCDM) techniques, specifically the Entropy and Technique for Order of Preference by Similarity to Ideal Solution (TOPSIS) methods, were utilized to combine the indicators and create a composite metric for assessing the spread of zoonotic diseases. The final indicators selected were then tested against recorded zoonoses in the Valencian Community (Spain) for 2021, and a strong positive correlation was identified. Therefore, the proposed indicator system can be valuable in guiding the development of planning strategies that align with the One Health principles. Based on the results achieved, such strategies may prioritize the preservation of natural landscape features to mitigate habitat encroachment, protect land and water resources, and attenuate extreme atmospheric conditions.


Assuntos
Ecossistema , Saúde Única , Animais , Humanos , Zoonoses/prevenção & controle , Surtos de Doenças , Atenção à Saúde
11.
Polymers (Basel) ; 15(13)2023 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-37447501

RESUMO

Tree-exuded gums are natural polymers that represent an abundant raw material in the food and pharmaceutical industries. The cashew gum can be obtained by exudation of trees of the genus Anacardium, a native species of the Brazilian northeast; its polymer consists of monosaccharide units propitious to the action of chemical reactions that tend to improve their intrinsic characteristics among them, as the degree of hydro-solubility. The objective of this work was to modify the exudate gum of Anacardium occidentale (cashew gum (CG)) through an amine reaction. The modification was confirmed by Nuclear Magnetic Resonance (1H NMR), infrared spectroscopy (FTIR), gel permeation chromatography (GPC), zeta potential, and thermogravimetric analysis (TG). In addition, the chemical modification altered the molar mass and surface charge of the CG, and the amino group binding to the CG polymers was confirmed by FTIR spectra. In addition, cytotoxicity tests were performed where cell viability was estimated by an MTT assay on RAW 264.7 macrophages. Through these tests, it was found that the amine caused an increase in the thermal stability of the amino compounds and did not present cytotoxic potential at concentrations below 50.0 mg/L.

12.
Int J Biol Macromol ; 243: 125254, 2023 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-37295699

RESUMO

The present work explores the esterification reaction in the polysaccharide extracted from the seaweed Gracilaria birdiae and investigates its antioxidant potential. The reaction process was conducted with phthalic anhydride at different reaction times (10, 20 and 30 min), using a molar ratio of 1:2 (polymer: phthalic anhydride). Derivatives were characterized by FTIR, TGA, DSC and XRD. The biological properties of derivatives were investigated by assays of cytotoxicity and antioxidant activity (2,2-diphenyl-1-picrylhydroxyl - DPPH and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt - ABTS). The results obtained by FT-IR confirmed the chemical modification, there was a reduction related to the presence of carbonyl and hydroxyl groups when compared to the in nature polysaccharide spectrum. TGA analysis showed a change in the thermal behavior of the modified materials. X-ray diffraction, it was shown that the in nature polysaccharide appeared as an amorphous material, while the material obtained after the chemical modification process had increased crystallinity, due to the introduction of phthalate groups. For the biological assays, it was observed that the phthalate derivative was more selective than the unmodified material for the murine metastatic melanoma tumor cell line (B16F10), revealing a good antioxidant profile for DPPH and ABTS radicals.


Assuntos
Antineoplásicos , Gracilaria , Animais , Camundongos , Antioxidantes/química , Anidridos Ftálicos , Galactanos , Espectroscopia de Infravermelho com Transformada de Fourier , Antineoplásicos/química , Polissacarídeos/química
13.
Pharmaceutics ; 15(3)2023 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-36986777

RESUMO

Docetaxel (DTX) is a non-selective antineoplastic agent with low solubility and a series of side effects. The technology of pH-sensitive and anti-epidermal growth factor receptor (anti-EGFR) immunoliposomes aims to increase the selective delivery of the drug in the acidic tumor environment to cells with EFGR overexpression. Thus, the study aimed to develop pH-sensitive liposomes based on DOPE (dioleoylphosphatidylethanolamine) and CHEMS (cholesteryl hemisuccinate), using a Box-Behnken factorial design. Furthermore, we aimed to conjugate the monoclonal antibody cetuximab onto liposomal surface, as well as to thoroughly characterize the nanosystems and evaluate them on prostate cancer cells. The liposomes prepared by hydration of the lipid film and optimized by the Box-Behnken factorial design showed a particle size of 107.2 ± 2.9 nm, a PDI of 0.213 ± 0.005, zeta potential of -21.9 ± 1.8 mV and an encapsulation efficiency of 88.65 ± 20.3%. Together, FTIR, DSC and DRX characterization demonstrated that the drug was properly encapsulated, with reduced drug crystallinity. Drug release was higher in acidic pH. The liposome conjugation with the anti-EGFR antibody cetuximab preserved the physicochemical characteristics and was successful. The liposome containing DTX reached an IC50 at a concentration of 65.74 nM in the PC3 cell line and 28.28 nM in the DU145 cell line. Immunoliposome, in turn, for PC3 cells reached an IC50 of 152.1 nM, and for the DU145 cell line, 12.60 nM, a considerable enhancement of cytotoxicity for the EGFR-positive cell line. Finally, the immunoliposome internalization was faster and greater than that of liposome in the DU145 cell line, with a higher EGFR overexpression. Thus, based on these results, it was possible to obtain a formulation with adequate characteristics of nanometric size, a high encapsulation of DTX and liposomes and particularly immunoliposomes containing DTX, which caused, as expected, a reduction in the viability of prostate cells, with high cellular internalization in EGFR overexpressing cells.

14.
Int J Biol Macromol ; 232: 123058, 2023 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-36669633

RESUMO

Lemon gum (LG) obtained from Citrus × latifolia in Brazil was isolated and characterized. In addition, gum biocompatibility was evaluated in vitro and in vivo by Galleria mellonella and mice model. The cytotoxicity against tumor cells was also evaluated. The ratio of arabinose:galactose: rhamnose:4-OMe-glucuronic acid was 1:0.65:0.06:0.15. Small traces of protein were detected, emphasizing the isolate purity. Molar mass was 8.08 × 105 g/mol, with three different degradation events. LG showed antiproliferative activity against human prostate adenocarcinoma cancer cells, with percentage superior to 50 %. In vivo toxicity models demonstrated that LG is biocompatible polymer, with little difference in the parameters compared to control group. These results demonstrate advance in the study of LG composition and toxicity, indicating a potential for several biomedical and biotechnological future applications.


Assuntos
Adenocarcinoma , Citrus , Masculino , Animais , Camundongos , Humanos , Próstata , Galactanos , Adenocarcinoma/tratamento farmacológico
15.
Int J Biol Macromol ; 230: 123272, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36649864

RESUMO

Nanotechnology is a crucial technology in recent years has resulted in new and creative applications of nanomedicine. Polymeric nanoparticles have increasing demands in pharmaceutical applications and require high reproducibility, homogeneity, and control over their properties. Work explores the use of cashew phthalate gum (PCG) as a particle-forming polymer. PCG exhibited a pH-sensitive behavior due to the of acid groups on its chains, and control drug release. We report the development of nanoparticles carrying benznidazole. Formulations were characterized by DLS, encapsulation efficiency, drug loading, FTIR, pH-responsive behavior, release, and in vitro kinetics. Interaction between polymer and drug was an evaluated by molecular dynamics. Morphology was observed by SEM, and in vitro cytotoxicity by MTT assay. Trypanocidal effect for epimastigote and trypomastigote forms was also evaluated. NPs responded to the slightly basic pH, triggering the release of BNZ. In acidic medium, they presented small size, spherical shape, and good stability. It was indicated NP with enhanced biological activity, reduced cytotoxicity, high anti T. cruzi performance, and pH-sensitive release. This work investigated properties related to the development and enhancement of nanoparticles. PCG has specific physicochemical properties that make it a promising alternative to drug delivery, however, there are still challenges to be overcome.


Assuntos
Anacardium , Nanopartículas , Trypanosoma cruzi , Reprodutibilidade dos Testes , Nanopartículas/química , Liberação Controlada de Fármacos , Polímeros/farmacologia , Concentração de Íons de Hidrogênio , Portadores de Fármacos/farmacologia
16.
AAPS PharmSciTech ; 23(6): 212, 2022 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-35918472

RESUMO

Squamous cell carcinoma (SCC) represents 20% of cases of non-melanoma skin cancer, and the most common treatment is the removal of the tumor, which can leave large scars. 5-Fluorouracil (5FU) is a drug used in the treatment of SCC, but it is highly hydrophilic, resulting in poor skin penetration in topical treatment. Some strategies can be used to increase the cutaneous penetration of the drug, such as the combination of liposomes containing penetration enhancers, for instance, surfactants, associated with the use of microneedling. Thus, the present work addresses the development of liposomes with penetration enhancers, such as sorbtitan monolaurate, span 20, for topical application of 5-FU and associated or not with the use of microneedling for skin delivery. Liposomes were developed using the lipid film hydration, resulting in particle size, polydispersity index, zeta potential, and 5-FU encapsulation efficiency of 88.08 nm, 0.169, -12.3 mV, and 50.20%, respectively. The presence of span 20 in liposomes potentiated the in vitro release of 5-FU. MTT assay was employed for cytotoxicity evaluation and the IC50 values were 0.62, 30.52, and 24.65 µM for liposomes with and without span 20 and 5-FU solution, respectively after 72-h treatment. Flow cytometry and confocal microscopy analysis evidenced high cell uptake for the formulations. In skin penetration studies, a higher concentration of 5-FU was observed in the epidermis + dermis, corresponding to 1997.71, 1842.20, and 2585.49 ng/cm2 in the passive penetration and 3214.07, 2342.84, and 5018.05 ng/cm2 after pretreatment with microneedles, for solution, liposome without and with span 20, respectively. Therefore, herein, we developed a nanoformulation for 5-FU delivery, with suitable physicochemical characteristics, potent skin cancer cytotoxicity, and cellular uptake. Span 20-based liposomes increased the skin penetration of 5-FU in association of microneedling. Altogether, the results shown herein evidenced the potential of the liposome containing span 20 for topical delivery of 5-FU.


Assuntos
Fluoruracila , Neoplasias Cutâneas , Hexoses , Humanos , Lipossomos/metabolismo , Tamanho da Partícula , Pele/metabolismo , Absorção Cutânea , Neoplasias Cutâneas/tratamento farmacológico , Neoplasias Cutâneas/metabolismo
17.
Phys Chem Chem Phys ; 23(48): 27484-27497, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34873605

RESUMO

We report on single- and double-charge photofragment formation by synchrotron radiation, following C 1s core excitation and ionization and Cl 2p inner excitation and ionization of chlorobenzene, C6H5Cl. From a comparison of experimental near-edge X-ray absorption fine structure spectra and theoretical ab initio calculations, the nature of various core and inner shell transitions of the molecule and pure atomic features were identified. To shed light on the normal Auger processes following excitation or ionization of the molecule at the Cl 2p or C 1s sites, we addressed the induced ionic species formation. With energy resolved electron spectra and ion time-of-flight spectra coincidence measurements, the ionic species were correlated with binding energy regions and initial states of vacancies. We explored the formation of the molecular dication C6H5Cl2+, the analogue benzene dication C6H42+, and the singly charged species produced by single loss of a carbon atom, C5HnCl+. The appearance and intensities of the spectral features associated with these ionic species are shown to be strongly site selective and dependent on the energy ranges of the Auger electron emission. Unexpected intensities for the analogue double charged benzene C6H42+ ion were observed with fast Auger electrons. The transitions leading to C6H5Cl2+ were identified from the binding energy representation of high resolution electron energy spectra. Most C6H5Cl2+ ions decay into two singly charged moieties, but intermediate channels are opened leading to other heavy dicationic species, C6H42+ and C6H4Cl2+, the channel leading to the first of these being much more favored than the other.

18.
An Acad Bras Cienc ; 94(1): e20191320, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34787289

RESUMO

The present study was based on the analysis of 10,467 trawls of the industrial piramutaba (Brachyplatystoma vaillantii) fishing fleet of the Brazilian state of Pará, which were mapped by onboard GPS loggers (between February 2008 and September 2011) and the PREPS data from 40 vessels which were tracked by this system between 2008 and 2011. The variation in the mean monthly CPUE, based on Lomb's periodogram, revealed a well-defined and constant cycle with a duration of approximately one year. Three environmental factors influenced this cycle. The El Niño 3.4 index had a negative correlation with the CPUE of the piramutaba fishery, with a time lag of 15 months, while monthly rainfall and the mean discharge of the Amazon River correlated strongly (r=0.89 and 0.87, respectively; p<0.001) with the CPUE, with time lags of 12 and 11 months, respectively. The spatiotemporal analysis of the distribution of the activity of the piramutaba fishing fleet indicated that the most intense area of operation of the fleet lies between latitudes 00º N and 02° N, and longitudes 047º40' W and 049º40' W. This area was divided into four geographic quadrants, although fishery operations were concentrated in only three of these quadrants. The study proposed a quadrimester fishing cycle with zoning in three of the quadrants, where fishing would be permitted for four months (occupation period), followed by an 8-month rest period for the recuperation of stocks, aiming at the sustainability of this fishing exploration.


Assuntos
Peixes-Gato , Pesqueiros , Animais , Brasil , Conservação dos Recursos Naturais , Rios
19.
Int J Biol Macromol ; 193(Pt A): 450-456, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34688680

RESUMO

Enoxaparin is an effective biological molecule for prevention and treatment of coagulation disorders. However, it is poorly absorbed in the gastrointestinal tract. In this study, we developed an Eudragit® L100 coated chitosan core shell nanoparticles for enoxaparin oral delivery (Eud/CS/Enox NPs) through a completely eco-friendly method without employing any high-energy homogenizer technique and any organic solvents. Spherical nanocarriers were successfully prepared with particle size lower than 300 nm, polydispersity index about 0.12 and zeta potential higher than +25 mV, entrapment efficiency greater than 95% and the in vitro release behavior confirms the good colloidal stability and the successful Eudragit® L100 coating process demonstrated by negligible cumulative enoxaparin release (<10%) when the particles are submitted to simulated gastric fluid conditions. Finally, we demonstrated that the core-shell structure of the particle influenced the drug release mechanism of the formulations, indicating the presence of the Eudragit® L100 on the surface of the particles. These results suggested that enteric-coating approach and drug delivery nanotechnology can be successfully explored as potential tools for oral delivery of enoxaparin.


Assuntos
Quitosana/química , Portadores de Fármacos/química , Enoxaparina/química , Nanopartículas/química , Liberação Controlada de Fármacos , Tamanho da Partícula
20.
Int J Biol Macromol ; 193(Pt A): 100-108, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34627848

RESUMO

In this study, nanoemulsions of essential oil from Ocimumgratissimum (Linn) (EO) were produced using low and high energy techniques using cashew gum (CG) as a co-surfactant. The main constituents of the EO were determined by Gas Chromatography coupled with Mass Spectrometry (GC-MS), and their presence in the EO and in the formulations verified by Fourier Transform Infrared Spectroscopy (FTIR) and UV-visible spectrophotometry was observed the encapsulation efficiency (EE%), with colloidal stability. Nuclear magnetic resonance (NMR) was used to study cashew gum. Dynamic light scattering analysis (DLS) determined the nanoemulsion Z means, polydispersity index and the Zeta potential value, nanoparticle tracking analysis (NTA) were determined. The nanostructured EO showed better antibacterial action against the pathogenic gastroenteritis species Staphylococcus aureus, Escherichia coli and Salmonella enterica when compared to free EO. Atomic Force Microscopy (AFM) was used for morphological analysis of the nanoparticle and study of the action of the nanoemulsion through images of the cellular morphology of S. enterica. The antioxidant activity was evaluated against the ABTS radical (2,2'-azino-bis diazonium salt (3-ethylbenzothiazoline-6-sulfonic acid)). The encapsulation of EO in a nanostructured system improved its antibacterial and antioxidant activity, the low energy synthesis showed greater storage stability, remaining stable for 37 days.


Assuntos
Antibacterianos/química , Emulsões/química , Ocimum/metabolismo , Óleos Voláteis/química , Gomas Vegetais/química , Folhas de Planta/metabolismo
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