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1.
Food Funct ; 11(6): 5357-5376, 2020 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-32463028

RESUMO

The chemical constituents of Allium sativum (garlic) oil were investigated using the GC/MS technique after silylation, and the presence of several fatty acids and their esters was revealed. The most dominant was 9,12-octadecadienoic acid (linoleic acid), a precursor of arachidonic acid, which is essential for brain development. Garlic oil-loaded chitosan nanoparticles (GCNs) were prepared to enhance its cerebral effects, and to mask its odor and taste. Two-level orthogonal factorial design, followed by regression analysis, was used to study the influence of different formulation variables. GCN3, the formula with the smallest particle size and the highest mucoadhesion, was selected as the optimized one. Transmission electron microscopy showed that GCN3 has a short nanorod-shape outline. We aimed to investigate the influence of orally administered GCN3 compared to the plain garlic oil (GO), on ciprofloxacin-induced (CPX) neurotoxicity in rats and the probable underlying mechanisms. The results show the significantly higher neurological curative effect of GCN3 compared to GO, and its greater antidepression-like and antianxiety-like potential via the alteration of brain neurotransmitter levels and inhibition of oxidative stress and inflammatory pathways. The histopathological examination showed the higher capability of GCN3 to repair the damage induced by CPX in the cerebral cortex, hippocampus area and substantia nigra brain sections. Similar results were proved immunohistochemically using Cox-2 antibody. The nanoencapsulation of GO represents a promising strategy for brain-targeting.


Assuntos
Compostos Alílicos/análise , Compostos Alílicos/farmacologia , Quitosana/farmacologia , Alho/química , Nanotubos/química , Sulfetos/química , Sulfetos/farmacologia , Animais , Encéfalo/patologia , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/patologia , Ciprofloxacina/efeitos adversos , Sistemas de Liberação de Medicamentos , Cromatografia Gasosa-Espectrometria de Massas , Hipocampo/efeitos dos fármacos , Hipocampo/patologia , Masculino , Síndromes Neurotóxicas , Estresse Oxidativo/efeitos dos fármacos , Tamanho da Partícula , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Ratos
2.
Int J Pharm ; 569: 118560, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31351180

RESUMO

Arthritis is a chronic degenerative joint disease decreasing the patient's quality of life. Mixed micellar system (MM) was exploited as a nanotechnology platform suitable for the encapsulation of the water-insoluble drug, Resveratrol (RES). MM were prepared using different ratios of poloxamer 188 (P188) and poloxamer 407 (P407), and then subjected to in-vitro evaluation. The selected MM (MM3) composed of P188: P407 in a ratio of 2:1 attained the most compromised properties (Particle size = 52.97 ±â€¯4.52 nm, Encapsulation Efficiency = 76.20 ±â€¯4.51 and Release efficiency = 76.26 ±â€¯6.25), and was coated with poly-lactic acid (PLA). TEM photographs of PLA-coated MM3 showed a polymeric layer surrounding the nanoparticles. Rats with induced arthritis were used to study the curative effect of intra-articularly (IA)-injected MM3, PLA-coated MM3 as well as the drug suspension. All the treated groups showed a significant therapeutic improvement in arthritis proved by measuring rats knee diameter as well as the tumor necrosis factor-alpha (TNF-α). The treatment effectiveness was in the following order: PLA-coated MM3 ˃ MM3 ˃ drug suspension, (p < 0.05). Histological study showed the recovery of the joints and synovial structure by IA administration of the drug-loaded micellar nanosystems, and the PLA-coated MM attained the best effect. This study proves the promising curative effect of the designed nanotechnology-based drug carrier.


Assuntos
Anti-Inflamatórios/administração & dosagem , Artrite Experimental/tratamento farmacológico , Micelas , Nanopartículas/administração & dosagem , Poliésteres/administração & dosagem , Resveratrol/administração & dosagem , Animais , Anti-Inflamatórios/química , Artrite Experimental/patologia , Liberação Controlada de Fármacos , Injeções Intra-Articulares , Articulação do Joelho/efeitos dos fármacos , Articulação do Joelho/patologia , Masculino , Nanopartículas/química , Poliésteres/química , Ratos Wistar , Resveratrol/química
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