Central properties of the essential oil and the crude ethanol extract from aerial parts of Artemisia annua L.

The present study evaluated the central activity of the essential oil and the ethanolic extract from Artemisia annua L. in animals as a part of a psychopharmacological screening of this plant. The extract was prepared with fresh leaves in ethanol (AEE) and the essential oil (AEO) was obtained by hidrodestilation. The ED50 and the LD50 obtained for the essential oil were 470 mg/kg (correlation coefficient r = 0.97333 and linear regression y = -26.52x + 0.158) and 790 mg/kg, and for the extract, 450 mg/kg (correlation coefficient r = 0.99266 and linear regression y = -27.34 + 0.156) and more than 2 g/kg, respectively. The doses increased the latency time to convulsions induced by picrotoxin and pilocarpine but prevented the onset of pentylenotetrazol and strychnine induced seizures. In addition to, the products have caused marked inhibition in the Rota-rod assay. According to the results, the AEO has a high acute toxicity and a possible cholinergic action, and the AEE showed a possible central activity as dopaminergic and cholinergic agents, and did not present a significant acute toxicity. These differences should be due to chemical substances present in each product. These products had no significant effect as an anticonvulsant, while exhibited a strong depressant activity on the CNS. (C) 2003 Elsevier Ltd. All rights reserved.48549750

Effect of Artemisia annua L. leaves essential oil and ethanol extract on behavioral assays

Artemisia annua has been used as a traditional plant for the treatment of malaria and fever in China because of the presence of its active compound, artemisinin. The present study evaluated the central activity of the essential oil and the crude ethanol extract of A. annua L. in animals as a part of a psychopharmacological screening of this plant. The extract was prepared in ethanol (AEE) and the essential oil (AEO) obtained by hydrodistillation, both with fresh leaves. Induced immobility, the forced swimming test (FST) and the open-field test (OFT) are well-known animal models to study drug-induced depression. The administration of A. annua essential oil or crude ethanol extract increased the immobility time in the FST and decreased other activities (ambulation, exploration, rearing and grooming) in the OFT in animals. Both AEO and AEE prolonged pentobarbital-induced sleep as well, but the essential oil had a marked effect. Observing these results, it is possible to suggest that A. annua crude ethanol extract and essential oil could act as depressors on the Central Nervous System (CNS).1868668

Design of indomethacin-loaded nanoparticles: effect of polymer matrix and surfactant

Danay Dupeyrón,1,2 Monique Kawakami,1 Adriana M Ferreira,1 Paolin Rocio Cáceres-Vélez,3 Jacques Rieumont,4 Ricardo Bentes Azevedo,3 José Carlos T Carvalho1 1Laboratório de Pesquisa em Fármacos, Centro de Ciências Biológicas e da Saúde, Colegiado de Farmácia, Universidade Federal do Amapá, Brazil; 2Programa de Pós-Graduação em Biodiversidade Tropical, Universidade Federal do Amapá, Brazil; 3Departamento de Genética e Morfologia, Instituto de Ciências Biológicas, Universidade de Brasília, Brazil; 4Departamento de Química – Física, Facultad de Química, Universidad de la Habana, Cuba Abstract: Despite recent advances in nonsteroidal anti-inflammatory drug (NSAID) formulations, the design of targeted delivery systems to improve the efficacy and reduce side effects of NSAIDs continues to be a focus of much research. Enteric nanoparticles have been recognized as a potential system to reduce gastrointestinal irritations caused by NSAIDs. The aim of this study was to evaluate the effect of EUDRAGIT® L100, polyethylene glycol, and polysorbate 80 on encapsulation efficiency of indomethacin within enteric nanoparticles. Formulations were developed based on a multilevel factorial design (three factors, two levels). The amount of polyethylene glycol was shown to be the factor that had the greatest influence on the encapsulation efficiency (evaluated response) at 95% confidence level. Some properties of nanoparticles like process yield, drug–polymer interaction, particle morphology, and in vitro dissolution profile, which could affect biological performance, have also been evaluated. Keywords: nonsteroidal anti-inflammatory, indomethacin, enteric polymer, polyethylene glycol, nanoparticle

Design of indomethacin-loaded nanoparticles: effect of polymer matrix and surfactant

Despite recent advances in nonsteroidal anti-inflammatory drug (NSAID) formulations, the design of targeted delivery systems to improve the efficacy and reduce side effects of NSAIDs continues to be a focus of much research. Enteric nanoparticles have been recognized as a potential system to reduce gastrointestinal irritations caused by NSAIDs. The aim of this study was to evaluate the effect of EUDRAGIT® L100, polyethylene glycol, and polysorbate 80 on encapsulation efficiency of indomethacin within enteric nanoparticles. Formulations were developed based on a multilevel factorial design (three factors, two levels). The amount of polyethylene glycol was shown to be the factor that had the greatest influence on the encapsulation efficiency (evaluated response) at 95% confidence level. Some properties of nanoparticles like process yield, drug-polymer interaction, particle morphology, and in vitro dissolution profile, which could affect biological performance, have also been evaluated

Preliminary studies of analgesic and anti-inflammatory properties of Caesalpinia ferrea crude extract

The crude aqueous extract of the fruits of Caesalpinia ferrea Mart. (Leguminosae) has been investigated for possible anti-inflammatory and analgesic properties. The carrageenan induced rat hind paw edema was significantly inhibited (P < 0.05) by oral administration of 300 mg/kg of this extract. A centrally mediated analgesic effect was not observed, however, there was a dose dependent reduction in the number of total writhes induced by acetic acid

Investigation of anti-inflammatory and antinociceptive activities of trans-dehydrocrotonin, a 19-nor-clerodane diterpene from Croton cajucara .1.

The anti-inflammatory and antinociceptive effects of trans-dehydrocrotonin, isolated from the bark of Croton cajucara (Euphorbiaceae), were investigated using several animal models. The trans-dehydrocrotonin produced a significant inhibition of carrageenin-induced paw edema and cotton pellet granuloma in rats. It also inhibited the writhings in mice induced by acetic acid, but did not show a significant effect in the hot-plate test in mice. The LD(50) of t-DCTN was 555.0 mg/kg (p.o.) for mice

Anti-inflammatory and analgesic activities of the crude extracts from stem bark of Bauhinia guianensis

Methylene chloride, ethyl acetate and methanolic extracts front the stem bark of Bauhinia guianensis (Leguminosae, Caesalpinoideae) were obtained. These extracts were evaluated for antiinflammatory activity which was conducted using carrageenin, dextran and histamine-induced paw edema in rats. The extracts of B. guianensis were also assessed for analgesic activity which was conducted using the writhing test in mouse. The different animal groups were treated with these extracts (100 mg/kg i.p. and p.o, IC50) 30 min prior to the application of stimuli. The methanolic extract demonstrated significant inhibition in the carrageenin-induced edema model. In the dextran-induced edema model, all three extracts inhibited the inflammatory process significantly with the methanolic extract being the most active. The ethyl acetate extract was the only one shown to be effective in the histamine-induced edema model. Finally all extracts inhibited effectively the algogenic process in the writhing test induced by acetic acid