Acaricide potencial of andiroba (Carapa guianensis Aubl.) oil on engorged adult females of Anocentor nitens (Neumann, 1897) and Rhipicephalus sanguineus (Latreille, 1806)

In vitro acaricide potential of the oil from andiroba seed (Carapa guianensis) was evaluated on engorged females of Anocentor nitens (n=210) and Rhipicephalus sanguineus (n=140) manually collected, from horses and dogs naturally infested, respectively. Five dilutions, 100%, 50%, 30%, 25%, and 10% of andiroba seed oil in deionized water, using tween 80 as dispersant, were employed for the engorged females immersion test. For A. nitens test, three repetitions were made with each dilution, using 10 engorged females for each treatment, and two repetitions for R. sanguineus test. Two control groups were used for each tick species, one with deionized water and another one with tween 80 and deionized water. After the tests, the females were kept in the laboratory under room temperature. Engorged female mortality and oviposition reduction were observed with infertile eggs, showing 100% of efficacy in the two species in all tested dilutions. The obtained data demonstrated the potential use of andiroba seed extract against A. nitens and R. sanguineus.Avaliou-se o potencial acaricida in vitro do óleo da semente da andiroba (Carapa guianensis) sobre fêmeas ingurgitadas de Anocentor nitens (n=210) e Rhipicephalus sanguineus (n=140), coletadas manualmente, respectivamente, de equinos e de cães naturalmente infestados. Para o teste de imersão, empregaram-se cinco diluições do óleo de andiroba, 100%, 50%, 30%, 25% e 10%, em água destilada, utilizando-se tween 80 como dispersante. No teste com A. nitens, foram usadas três repetições para cada diluição, utilizando-se 10 fêmeas ingurgitadas para cada tratamento. No teste com R. sanguineus, usaram-se duas repetições, e formaram-se, ainda, dois grupos-controle para cada espécie de ixodídeo, um com água destilada e outro com tween 80 mais água destilada. Após os testes, as fêmeas foram mantidas em laboratório sob temperatura ambiente. Observou-se mortalidade das fêmeas ingurgitadas e redução de postura, neste caso, com ovos inférteis, demonstrando eficácia de 100% nas duas espécies em todas as diluições testadas. Os dados obtidos evidenciaram a potencialidade do uso do extrato de andiroba contra A. nitens e R. sanguineus

Preliminary development of lapachol gel: in vitro permeation study

O objetivo do presente estudo foi desenvolver formulações geleificadas do lapachol, substância de conhecida atividade antiinflamatória. Para otimização das formulações, foi verificada a influência da resina de Carbopol® empregada (934P, 940 e 941), do pH da formulação (5, 7 e 8), da concentração do princípio ativo (0,2%, 0,5% e 1,0%) bem como da incorporação de um promotor de absorção (Polissorbato 80) na liberação in vitro do lapachol utilizando células de difusão tipo Franz. Para tanto foram usadas como barreiras membrana sintética Durapore® e pele de rato albino tipo Wistar. Os resultados demonstraram que a adição do Polissorbato 80 na formulação promoveu aumento significativo na permeação do princípio ativo através da pele estudada, exceto para os géis contendo 0,2% de lapachol utilizando Carbopol® 934P como agente geleificante. Estes géis apresentaram as melhores taxas difusionais de lapachol, principalmente quando incorporados em formulações com pH 8, nas concentrações de 0,5% ou 1,0% de princípio ativo. Todavia as preparações contendo 1,0 % de princípio ativo apresentaram pequenos cristais de lapachol não solubilizados.The scope of this work was to develop two gel formulations containing lapachol, substance with known anti-inflammatory activity. In order to achieve a more effective topical delivery, the effects of vehicles and enhancers were evaluated. The influence of the Carbopol® resin (934P, 940 and 941), the pH of the formulation (5, 7 and 8), the concentration of the active (0.2%, 0.5% and 1.0%) and the incorporation of Tween® 80 were investigated. A series in vitro permeation studies were conduct in classical Franz-type diffusion cells using Durapore® synthetic membranes and Wistar mouse skins as barriers. Through the careful analyse of the data obtained, we could observe that the addition of Tween® 80 leads to a significant increase in the in vitro diffusion of the active, except for the formulations containing Carbopol® 934P and 0.2% of lapachol. The formulations assayed presented best in vitro diffusion rates of lapachol at pH 8 when 0.5% or 1.0% of the active was added. However, the preparations containing 1.0% of drug presented little insoluble crystals of lapachol

Nanostructured polymeric system based of cashew gum for oral admnistration of insulin

The subcutaneous administration of insulin has been the treatment of millions of diabetics in the world.However, for such via insulin is invasive and not mimics the physiological action causing side effects. Theoral route would be the most physiological and comfortable option, but the oral bioavailability of insulin islow by proteolytic activity and reduced permeability of the gastrointestinal tract. The aim of the study was todevelop a nanostructured system integrating biomaterials for oral insulin delivery. Cashew gum (CG) is apolysaccharide extracted from the exudate of the plant Anacardium occidentale. It is a biopolymer composedof simple sugars and glucuronic acid and it can be used in nanostructured systems for the incorporation ofmolecules. The exudate was isolated, dissolved in water, filtered, precipitated in ethanol and purified. TheCG was characterized by infrared spectroscopy and molecular weight by size exclusion chromatography.Nanoparticles were prepared through ionotropic gelation integrating cashew gum, dextran sulfate and poloxamercontaining insulin stabilized with chitosan, poly(ethyleneglycol) and coated with albumin. The particleswere analyzed for particle size, zeta potential and insulin entrapment efficiency. The FTIR spectrum for CGshowed a band at 3395 cm-1 due to the stretching vibration of O-H, a band at 2926 cm-1 of C-H vibrations;absorption at 1639 cm-1 of O-H type from bound water molecules and bands at 1143, 1073 and 1024 cm-1 duevibrations of the C-O-C from glycosidic bonds and O-H of alcohols. The peak molar mass of GC was 2.35 ×104 g/mol. The particles had a size of 156 nm and after coating, size of 5387 nm with 92% insulin entrapmentefficiency and zeta potential of -51 mV indicating electrostatic stabilization. The results suggest an innovativecashew gum base system for oral insulin administration.Keywords: Nanostructures, biomaterials, cashew gum, insulin, oral delivery

Repeated-Doses Toxicity Study of the Essential Oil of Hyptis martiusii

Hyptis martiusii Benth. (Lamiaceae) is found in abundance in Northeastern Brazil where it is used in traditional medicine to treat gastric disorders. Since there are no studies reporting the toxicity and safety profile of this species, we investigated repeated-doses toxicity of the essential oil of Hyptis martiusii (EOHM). Swiss mice of both sexes were orally treated with EOHM (100 and 500 mg/kg) for 30 days, and biochemical, hematological, and morphological parameters were determined. No toxicity signs or deaths were recorded during the treatment with EOHM. The body weight gain was not affected, but there was an occasional variation in water and food consumption among mice of both sexes treated with both doses. The hematological and biochemical profiles did not show significant differences except for a decrease in the MCV and an increase in albumin, but these variations are within the limits described for the species. The microscopic analysis showed changes in liver, kidneys, lungs, and spleen; however, these changes do not have clinical relevance since they varied among the groups, including the control group. The results indicate that the treatment of repeated-doses with the essential oil of Hyptis martiusii showed low toxicity in mice

Spondias purpurea

Spondias purpurea is used in folk medicine to treat diarrhea and diuresis. The objective of this study was to evaluate the phytochemical profile and antioxidant and antiulcer activities of the hexane extract of the leaves of S. purpurea (SpHE). Phytochemical profile was evaluated via thin layer chromatography (TLC) and HPLC. SpHE was screened for antioxidant activities using DPPH, ABTS, FRAP, and phosphomolybdenum assays. To determine its antiulcer properties, animals were pretreated with injured control, lansoprazole, ranitidine, carbenoxolone, or SpHE (12.5, 25, and 50 mg/kg) and were screened; acute ulcers were induced by HCl/ethanol, absolute ethanol, and nonsteroidal anti-inflammatory drug (NSAID). TLC revealed the presence of flavonoids, whereas HPLC analysis showed the presence of caffeic acid and epigallocatechin. The phenolic compounds and in vitro assays showed antioxidant activity. After gastric ulcer induction by using HCl/ethanol, SpHE reduced the area of ulcerative lesions by 82, 91, and 88%, respectively. In ethanol, SpHE reduced the area of ulcerative lesions by 77, 93, and 92%, respectively. In the NSAID, the percentages of protection were 70, 76, and 78%, respectively. SpHE promoted the minimization of ulcers, increased the levels of reduced glutathione, and decreased tumor necrosis factor. S. purpurea has antioxidant and antiulcer properties

Efeito da ouabaína no ducto deferente de rato: sensibilização pela metoxamina e imidazolinas

BV UNIFESP: Teses e dissertaçõe

Efeito inibitório do clorobutanol no útero e ducto deferente de rato

BV UNIFESP: Teses e dissertaçõe

Intervenções a partir da análise custo-benefício em prescrições de estatinas e fibratos do Componente Especializado de Assistência Farmacêutica

O objetivo deste estudo foi avaliar a qualidade das intervenções interdisciplinares médico-farmacêutico a partir da análise custo-benefício das prescrições de estatinas e fibratos em uma unidade pública estadual, dispensadora de medicamentos especializados da alta complexidade. Trata-se um estudo de intervenção, prospectivo longitudinal com 502 pacientes, no período de janeiro a setembro de 2009. A maioria das prescrições realizadas para o tratamento de dislipidemias em 2008 estava relacionados com atorvastatina (72,3%) e o custo anual do medicamento foi de aproximadamente R$ 1,9 milhões. Na análise custo-benefício, 272 (54%) prescrições apresentaram a indicação da atorvastatina como fármaco de 1ª escolha terapêutica. Após as intervenções, 81% dos problemas encontrados foram resolvidos, consistindo em geral, em ações interdisciplinares médico-farmacêutico. As intervenções trouxeram mudanças significativas nas prescrições, reduzindo gastos com a farmacoterapia e maior economia aos cofres públicos