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1.
Eur J Pharm Biopharm ; 200: 114307, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38685438

RESUMO

Herein, we report the properties of nanostructured lipid carriers (NLCs) prepared with a gradient concentration of Bergenin (BGN) isolated from Pentaclethra macrophylla stem bark powder. A gradient concentration of BGN (BGN 0, 50, 100, 150, and 200 mg) was prepared in a 5 % lipid matrix consisting of Transcutol HP (75 %), Phospholipon 90H (15 %), and Gelucire 43/01 (10 %) to which a surfactant aqueous phase consisting of Tween 80, sorbitol, and sorbic acid was dissolved. The NLCs were evaluated by size, polydispersity index (PDI), zeta potential, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), encapsulation efficiency, and in vitro drug release. The result shows polydispersed nanoparticles with high drug encapsulation (94.26-99.50 %). The nanoparticles were mostly spherical, but those from the 50 mg BGN batch were more cuboidal than spherical. The drug release was highest from the latter to the tune of 40 % compared to the pure BGN solution, which released about 15 % BGN. The anti-inflammatory activity of the BGN-NLC and total plant extract was studied on lipopolysaccharide (LPS)-inflamed macrophages. The cell study showed that BGN and plant extract had low cytotoxicity on macrophages and exhibited a dose-dependent anti-inflammatory effect on the LPS-induced inflammatory process in macrophages.


Assuntos
Anti-Inflamatórios , Benzopiranos , Portadores de Fármacos , Lipídeos , Lipopolissacarídeos , Macrófagos , Nanopartículas , Lipopolissacarídeos/farmacologia , Animais , Camundongos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Portadores de Fármacos/química , Benzopiranos/farmacologia , Benzopiranos/administração & dosagem , Benzopiranos/química , Nanopartículas/química , Lipídeos/química , Células RAW 264.7 , Liberação Controlada de Fármacos , Nanoestruturas/química , Saxifragaceae/química , Tamanho da Partícula , Inflamação/tratamento farmacológico , Inflamação/induzido quimicamente , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química
2.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wpr-819541

RESUMO

OBJECTIVE@#To evaluate the possible antiulcer effect of the African garden egg, Solanum aethiopicum (S. aethiopicum) (a domestic vegetable) experimentally in rats.@*METHODS@#A methanol extract of the plant fruit was prepared by maceration. Twenty five overnight fasted rats for each model were divided randomly into five groups of five rats. Groups 1, 2, 3, 4 and 5 received normal saline, extract dose levels of 100, 200 and 400 mg/kg and 100 mg/kg of ranitidine respectively. All administrations were given orally. For the indomethacin and aspirin models, ulcerogenic agents (indomethacin, 50 mg/kg and aspirin 200 mg/kg) were given thirty minutes after extract treatments and animals sacrificed 8 h later. The acidified ethanol model (ethanol 60% + 0.1 mol/L HCl) was given 1 hr after extract treatment and animals sacrificed 1 h later. Ulcer index was checked and analysed with appropriate statistical tools.@*RESULTS@#Extract of S. aethiopicum showed positive effect on all the models used. It produced higher ulcer inhibition than ranitidine in the indomethacin and acid-ethanol models. All the anti-ulcer effects of the extract at different doses were dose dependent but only in indomethacin model did it produce statistically significant (P<0.05) ulcer reduction in all doses compared to control.@*CONCLUSIONS@#Garden egg, a readily cultivated crop vegetable possesses ulcer protective properties against ulcers induced experimentally making it a cheap source of natural anti-ulcer remedy.


Assuntos
Animais , Ratos , Antiulcerosos , Modelos Animais de Doenças , Extratos Vegetais , Ratos Wistar , Solanum , Química , Úlcera Gástrica , Tratamento Farmacológico , Resultado do Tratamento
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