Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone(r) R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1st, 7th, 15th, and 30th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear.Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona(r) R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (

ATIVIDADE DE UM NOVO DERIVADO PIRAZOLÍNICO (LQFM 021) EM MODELO DE ARTRITE INDUZIDA POR ADJUVANTE COMPLETO DE FREUND (CFA)

Introdu&ccedil;&atilde;o e objetivos: Os compostos pirazol&iacute;nicos s&atilde;o conhecidos por apresentar atividade anti-inflamat&oacute;ria, analg&eacute;sica e antipir&eacute;tica. O objetivo deste trabalho foi avaliar o derivado pirazol&iacute;nico LQFM 021, em testes nociceptivos cr&ocirc;nicos de artrite induzida por CFA. Metodologia: Grupos de ratas (n=7) pr&eacute;-sensibilizados foram tratados (v.o.) com ve&iacute;culo (10 mL/kg 1 vez/dia), LQFM 021 (15 mg/kg 2 vezes/dia) ou LQFM 021 (30 mg/kg 1 vez/dia). Uma hora ap&oacute;s os tratamentos foi feito uma inje&ccedil;&atilde;o intra-articular de CFA. Medidas do tempo de eleva&ccedil;&atilde;o da pata (TEP) e do di&acirc;metro articular foram realizadas at&eacute; o 6&deg; dia. Resultados e discuss&otilde;es: Tratamento com LQFM 021 30 mg/kg 1 vez/dia promoveu uma redu&ccedil;&atilde;o progressiva e permanente do TEP a partir do 2&deg; dia, em 26,3; 31,4; 31,3; 41,8 e 47,0 %. A forma&ccedil;&atilde;o do edema foi reduzida a partir do 1&deg; dia de tratamento em 29,6; 15,6; 21,2; 29,2 e 29,5 %. Na migra&ccedil;&atilde;o celular, houve uma redu&ccedil;&atilde;o do n&uacute;mero de leuc&oacute;citos em 34,2 % e polimorfonucleares em 54,3%. J&aacute; o tratamento com 15 mg/kg 2 vezes/dia, reduziu o TEP em 29,6; 15,6; 21,2; 29,2 e 29,5 %. No entanto, n&atilde;o inibiu a forma&ccedil;&atilde;o do edema ou n&uacute;mero de leuc&oacute;citos totais, mas reduziu polimorfonucleares em 33,8 %. Conclus&otilde;es: O derivado LQFM 021 apresentou efeito antinoceptivo e anti-inflamat&oacute;rio em modelo cr&ocirc;nico

Anti-inflammatory effect of Spiranthera odoratissima A. St.-Hil. leaves involves reduction of TNF-alpha

Spiranthera odoratissima A. St.-Hil., 'manaca', is a medicinal species used in Brazil, especially in central region, for the treatment of several diseases such as pain and inflammation. In this study, the methanol/aqueous phase of the ethanol extract of the leaves of 'manaca' (MAP), at the doses of 50, 150 and 500 mg/kg was used to evaluate the anti-inflammatory and/or antinociceptive effects and the possible anti-inflammatory mechanism. The antinociceptive and anti-inflammatory activities of MAP were assessed using formalin test, carrageenan-induced paw oedema. The myeloperoxidase activity, capillary permeability, leukocyte migration and tumour necrosis factor alpha (TNF-alpha) levels were evaluated in pleural exudate. The MAP reduced the licking time only in the later phase of formalin test, and showed anti-inflammatory activity by reducing the paw oedema, migration cell, myeloperoxidase activity, capillary permeability and TNF-alpha levels. In conclusion, we confirmed the inflammatory activity of MAP and affirm that this effect involves the reduction of TNF-alpha level.FUNAPE/UFGFUNAPE/UFGPRPPG/UFGPRPPG/UFGFAPEGFAPEGCAPESCAPESCNPqCNP

Anti-inflammatory and opioid-like activities in methanol extract of Mikania lindleyana, sucuriju

Mikania lindleyana DC., Asteraceae (sucuriju), grows in the Amazon region, where is frequently used to treat pain, inflammatory diseases and scarring. This study was carried out to investigate phytochemical profile accompanied by in vivo antinociceptive and anti-inflammatory screening of n-hexane (HE), dichloromethane (DME) and methanol (ME) extracts obtained from the aerial parts of the plant. The oral administration of ME (0.1, 0.3, 1 g/kg) caused a dose-related reduction (16.2, 42.1 e 70.2%) of acetic acid-induced abdominal writhing while HE and DME (1 g/kg, p.o.) were ineffective. In the hot plate test, ME (300 mg/kg, p.o.) increased the latency of heat stimulus between 30 and 120 min and inhibited the first (45%) and second (60%) phases of nociception in the formalin test. The antinociception induced by ME or positive control fentanyl (150 µg/kg, s.c.) in hot plate and formalin tests was prevented by naloxone (3 mg/kg, s.c.). When submitted to the carrageenan-induced peritonitis test, ME (0.5, 1.0, 2.0 g/kg, p.o.) impaired leukocyte migration into the peritoneal cavity by 46.8, 59.4 and 64.8% respectively, while positive control dexamethasone (2 mg/kg, s.c.), inhibited leukocyte migration by 71.1%. These results indicate that the antinociception obtained after oral administration of methanol extract of M. lindleyana involves anti-inflammatory mechanisms accompanied with opioid-like activity which could explain the use of the specie for pain and inflammatory diseases