Lipid nanoparticles as carriers of cyclodextrin inclusion complexes: A promising approach for cutaneous delivery of a volatile essential oil.

Solid inclusion complexes with cyclodextrins (CD) may be used to overcome volatility and solubility problems of essential oils of pharmacological interest. However, they lack the many dermatological advantages of lipid nanoparticles. This study intends to evaluate the ability of nanostructured lipid carriers (NLC) to encapsulate hydroxypropyl-ß-cyclodextrin inclusion complexes of Lippia origanoides essential oil (EO) and to maintain the desirable aspects of lipid colloids interaction with the skin, specifically follicular accumulation and controlled delivery. CD and NLC were also evaluated separately. Thymol (TML) was used as the essential oil marker and to produce control formulations. As expected, CD alone, though effective in overcoming volatility and low aqueous solubility of TML, were ineffective in controlling marker release (˜50% of EO released after 3 h, Hixson-Crowell kinetics). Even though NLC controlled drug release (˜20% EO released after 12 h, zero-order kinetics) enabling TML penetration into the skin (> 40 µg/cm2after 12 h), NLC alone were not efficient in preventing TML volatility, especially at higher temperatures (calculated shelf-life of 2 days at 35 °C). The combined approach resulted in a synergistic effect (˜20% EO released after 12 h; shelf life of 6 days). The lack of statistical difference of TML skin penetration from NLC and NLC-CD suggests the developed system maintained all skin interaction aspects of lipid colloids, including follicular accumulation forming a depot for controlled delivery. In conclusion, lipid nanoparticles demonstrated to be promising carriers for inclusion complexes of this particular volatile essential oil.

GC-MS Chemical Characterization and In Vitro Evaluation of Antioxidant and Toxic Effects Using Drosophila melanogaster Model of the Essential Oil of Lantana montevidensis (Spreng) Briq.

Background and objectives: Natural products such as essential oils with antioxidant potential can reduce the level of oxidative stress and prevent the oxidation of biomolecules. In the present study, we investigated the antioxidant potential of Lantana montevidensis leaf essential oil (EOLM) in chemical and biological models using Drosophila melanogaster. Materials and methods: in addition, the chemical components of the oil were identified and quantified by gas chromatography coupled to mass spectrometry (GC-MS), and the percentage compositions were obtained from electronic integration measurements using flame ionization detection (FID). Results: our results demonstrated that EOLM is rich in terpenes with Germacrene-D (31.27%) and ß-caryophyllene (28.15%) as the major components. EOLM (0.12-0.48 g/mL) was ineffective in scavenging DPPH radical, and chelating Fe(II), but showed reducing activity at 0.24 g/mL and 0.48 g/mL. In in vivo studies, exposure of D. melanogaster to EOLM (0.12-0.48 g/mL) for 5 h resulted in 10% mortality; no change in oxidative stress parameters such as total thiol, non-protein thiol, and malondialdehyde contents, in comparison to control (p > 0.05). Conclusions: taken together, our results indicate EOLM may not be toxic at the concentrations tested, and thus may not be suitable for the development of new botanical insecticides, such as fumigants or spray-type control agents against Drosophila melanogaster.

Prebiotic Carbohydrates: Effect on Reconstitution, Storage, Release, and Antioxidant Properties of Lime Essential Oil Microparticles.

The aim of this study was to include prebiotic biopolymers as wall material in microparticles of lime essential oil. Whey protein isolate (WPI), inulin (IN), and oligofructose (OL) biopolymers were used in the following combinations: WPI, WPI/IN (4:1), and WPI/OL (4:1). The emulsion droplets in the presence of inulin and oligofructose showed larger sizes on reconstitution. There was no significant difference in solubility of the particles, but the wettability was improved on addition of the polysaccharides. The size of the oligofructose chains favored the adsorption of water. Prebiotic biopolymers reduced thermal and chemical stability of the encapsulated oil. Microparticles produced with WPI showed a higher bioactive compound release rate, mainly due to its structural properties, that enabled rapid diffusion of oil through the pores. The use of prebiotic biopolymers can be a good option to add value to encapsulated products, thus promoting health benefits.

Eficiencia de la desingección con aceites esenciales y ultrasonido sobre Escherichia coli inoculada en frutos de tomate y el impacto sobre la actividad antioxidante / Efficacy of disinfection treatments using essential oils and ultrasound on tomato fruits inoculated with escherichia coli and impact on antioxidant activity

La creciente demanda de frutos frescos puede constituir un riesgo para la salud de los consumidores, teniendo en cuenta la gran variedad de microorganismos que estos suelen albergar. El objetivo del presente estudio fue evaluar la eficacia de varios procedimientos de desinfección sobre Escherichia coli enterotoxigénica (enterotoxigenic E. coli [ETEC]) inoculada en tomate y la conservación de las propiedades antioxidantes de los frutos desinfectados. Los frutos fueron sumergidos durante 5 o 10min en dispersiones de aceites esenciales de orégano o tomillo (5 o 10ppm), combinados o no con la aplicación de ultrasonido. La actividad antioxidante se determinó por la neutralización del radical 2,2-difenil-1-pricrilhidrazil (DPPH) y se reportó como porcentaje de inhibición (%I). Los tratamientos de desinfección más eficaces para una significativa reducción log10 UFG/g (S) de ETEC fueron con 10ppm de aceite de orégano durante 10min, con reducciones S=3,05 en tratamientos individuales y S=4,03 en mixtos. Los %I más altos se lograron con tratamientos individuales con sonicación (69,52 y 72,48) y en tratamientos combinados con aceite de tomillo 5ppm y ultrasonido durante 5 y 10min, con valores de 51,27 y 53,31%, respectivamente

Fresh produce often harbors a great number of microorganisms; hence, its growing demand may constitute a risk for consumers. The aim of this study was to evaluate the efficacy of several disinfection procedures against enterotoxigenic Escherichia coli (ETEC) inoculated on tomato fruits and the conservation of the antioxidant properties of these disinfected fruits. Fruits were immersed for 5 or 10min in oregano or thyme essential oil dispersions (5, 10ppm), with or without ultrasound treatment. Antioxidant activity of disinfected fruits was determined as the ability to scavenge 2,2-diphenyl-1-pricrylhydrazyl (DPPH) radicals and was reported as percentage of inhibition (%I). The most efficient disinfectant treatments showing significant differences (p≤.05) between the reductions log10 CFU/g (S) of ETEC were those using 10ppm oregano for 10min, with S=3.05 in individual treatments and S=4.03 in mixed treatments. The highest %I was obtained with individual sonication treatments (69.52 and 72.48), while in combined treatments the %I values increased with thyme oil 5ppm and ultrasound for 5min (51.27%) and 10min (53.31%)

Atividade antimicrobiana do óleo essencial de Cymbopogon citratus / Antimicrobial activity of Cymbopogon citratus essential oil / Actividad antimicrobiana del aceite esencial de Cymbopogon citratus

O Cymbopogon citratus é uma planta originária da Índia, pertencente à família Poaceae e facilmente adaptada em regiões tropicais como o Brasil. Este trabalho avaliou a atividade antimicrobiana do óleo essencial (OE) obtido por hidrodestilação das folhas de C. citratus. A concentração inibitória mínima (CIM) foi determinada pela técnica de microdiluição em caldo para as bactérias Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa e a levedura Candida albicans. O menor CIM foi de 7,81 µg mL-1 para S. aureus, a média de 15,62µg mL-1 para P. aeruginosa e C. albicans e a maior de 62,50µg mL-1 para E. coli. O óleo essencial de C. citratus apresentou atividade antimicrobiana para todos os micro-organismos testados. O óleo mostrou potencial aplicabilidade no controle microbiano e sugerem-se novos estudos para auxiliar na ampliação das aplicações desta planta.(AU)

Cymbopogon citratus is an Indian plant belonging to the Poaceae family, easily adapted to tropical regions such as Brazil. This study assesses the antimicrobial activity of essential oil from C. citratus leaves obtained by hydro-distillation. The minimum inhibitory concentration (MIC) was determined by broth micro-dilution technique for Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans. The lowest MIC was 7.81 µg ml-1 for S. aureus, the medium was 15,62 µg mL-1 for P. aeruginosa and C. albicans and the highest was 62.50 µg mL-1 for E. coli. The C. citratus essential oil presented antimicrobial activity against all microorganisms. The essential oil showed potential applicability in microbial control and further studies are suggested to expand the application of this plant.(AU)

Cymbopogon citratus es una planta originaria de India, perteneciente a la familia Poaceae y fácilmente adaptable en las regiones tropicales como Brasil. Este estudio evaluó la actividad antimicrobiana del aceite esencial de las hojas de C. citratus obtenido por hidrodestilación. La concentración inhibidora mínima (CIM) se ha determinado por la técnica de microdilución en caldo para las bacterias Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa y la levadura Candida albicans. La CIM más baja fue 7.81 µg mL-1 para S. aureus, la media de 15.62µg mL-1 para P. aeruginosa y C. albicans y la mayor de 62.50 µg mL-1 para E.coli. El aceite esencial de C. citratus presentó actividad antimicrobiana para todos los microorganismos testados. El aceite mostró potencial de aplicabilidad en el control microbiano y se sugieren nuevos estudios para ampliar las aplicaciones de esta planta.(AU)

Atividade antimicrobiana do óleo essencial de Cymbopogon citratus / Antimicrobial activity of Cymbopogon citratus essential oil / Actividad antimicrobiana del aceite esencial de Cymbopogon citratus

O Cymbopogon citratus é uma planta originária da Índia, pertencente à família Poaceae e facilmente adaptada em regiões tropicais como o Brasil. Este trabalho avaliou a atividade antimicrobiana do óleo essencial (OE) obtido por hidrodestilação das folhas de C. citratus. A concentração inibitória mínima (CIM) foi determinada pela técnica de microdiluição em caldo para as bactérias Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa e a levedura Candida albicans. O menor CIM foi de 7,81 µg mL-1 para S. aureus, a média de 15,62µg mL-1 para P. aeruginosa e C. albicans e a maior de 62,50µg mL-1 para E. coli. O óleo essencial de C. citratus apresentou atividade antimicrobiana para todos os micro-organismos testados. O óleo mostrou potencial aplicabilidade no controle microbiano e sugerem-se novos estudos para auxiliar na ampliação das aplicações desta planta...

Cymbopogon citratus is an Indian plant belonging to the Poaceae family, easily adapted to tropical regions such as Brazil. This study assesses the antimicrobial activity of essential oil from C. citratus leaves obtained by hydro-distillation. The minimum inhibitory concentration (MIC) was determined by broth micro-dilution technique for Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans. The lowest MIC was 7.81 µg ml-1 for S. aureus, the medium was 15,62 µg mL-1 for P. aeruginosa and C. albicans and the highest was 62.50 µg mL-1 for E. coli. The C. citratus essential oil presented antimicrobial activity against all microorganisms. The essential oil showed potential applicability in microbial control and further studies are suggested to expand the application of this plant...

Cymbopogon citratus es una planta originaria de India, perteneciente a la familia Poaceae y fácilmente adaptable en las regiones tropicales como Brasil. Este estudio evaluó la actividad antimicrobiana del aceite esencial de las hojas de C. citratus obtenido por hidrodestilación. La concentración inhibidora mínima (CIM) se ha determinado por la técnica de microdilución en caldo para las bacterias Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa y la levadura Candida albicans. La CIM más baja fue 7.81 µg mL-1 para S. aureus, la media de 15.62µg mL-1 para P. aeruginosa y C. albicans y la mayor de 62.50 µg mL-1 para E.coli. El aceite esencial de C. citratus presentó actividad antimicrobiana para todos los microorganismos testados. El aceite mostró potencial de aplicabilidad en el control microbiano y se sugieren nuevos estudios para ampliar las aplicaciones de esta planta...

Pharmacokinetics and tissue distribution of the sesquiterpene alpha-humulene in mice.

A quantitative study was undertaken to assess the plasma and tissue levels, tissue distribution and skin (ear) absorption of the sesquiterpene alpha-humulene, the main active constituent isolated from the plant Cordia verbenacea (Boraginaceae ), after oral, intravenous and topical administration in mice. The alpha-humulene levels were quantified by GC-MS analysis. The peak alpha-humulene concentration was achieved 15 min following its oral administration (150 mg/kg). Then, the alpha-humulene plasma concentration gradually decreased and it was almost undetectable at 2 hours after intravenous administration and 12 hours after oral administration. When the oil of C. verbenacea was given orally (1 g/kg), the peak alpha-humulene plasma concentration was observed after 30 min, being detectable only up to 2 h. The oral bioavailability of alpha-humulene was found to be 18 %. The half-lives of alpha-humulene were very short, 16.8 min after oral administration and 1.8 min after intravenous administration. However, the elimination half-lives were longer, 118.2 min and 55 min, for oral and intravenous routes, respectively. We also assessed the amount of alpha-humulene in some selected tissues at 0.5 and at 4 h after oral administration. We found a high amount of the compound in the liver, followed by the kidneys, heart, lungs, spleen and brain, 0.5 h after oral administration. Notably, the yield of alpha-humulene decreased significantly in all analyzed tissues, especially in the liver, 4 h after oral administration. Of note, 30 minutes after topical administration of Acheflan formulations (cream and aerosol) containing 0.5 % of C. verbenacea essential oil, a schedule of treatment that produces marked and similar topical anti-inflammatory activity, the amount of alpha-humulene absorbed in the ear was very similar (about 2 microg/ear). It is concluded that alpha-humulene exhibited a rapid onset and relatively good absorption following oral and topical administration. Taken together, these findings further contribute to an explanation of the topical and systemic anti-inflammatory and antinociceptive properties previously reported for the essential oil and for alpha-humulene obtained from Cordia verbenacea, they also provide support for the clinical studies conducted with the phytomedicine Acheflan.

Chemotherapeutic potential of the volatile oils from Zanthoxylum rhoifolium Lam leaves.

In this work, the anti-tumor properties of the volatile oil from Zanthoxylum rhoifolium Lam leaves and some terpenes (alpha-humulene, beta-caryophyllene, alpha-pinene and beta-pinene) were investigated in vitro and in vivo using the Ehrlich ascites tumor model. Treatment of Ehrlich ascites tumor-bearing mice with 20 mg/kg of the volatile oil and beta-caryophyllene for 4 days has significantly increased survival, whereas administration of alpha-humulene, alpha-pinene and beta-pinene were ineffective in affording protection. Volatile oil and beta-caryophyllene exhibited little direct activity against Ehrlich tumor cells in vitro, while alpha-humulene, alpha-pinene and beta-pinene did not such activity. Investigation of the effects of the volatile oil (and terpenes) treatment on total natural killer cells (NK cell) activity from tumor-bearing mice as a possible mechanism of these compounds in vivo revealed that volatile oil and beta-caryophyllene significantly improved NK cell cytotoxicity against YAC-1, a Moloney virus-induced mouse T-cell lymphoma of A/SN origin and Ehrlich ascites cells. As expected, tumor growth in non-treated mice markedly suppressed NK cell cytolysis while the volatile oil and beta-caryophyllene reversed this effect when mice were treated with 20-mg/kg dosages of these compounds for 4 days. Summing up, volatile oil exhibits anti-tumor efficacy and significative immunomodulatory action in vivo, which may be related to beta-caryophyllene associated to the synergism of other natural compounds presented in volatile oil from Z. rhoifolium Lam leaves.

Estandarización de Mentha arvensis L. medicamento herbario con actividad antihistamínica / Standardization of Mentha Arvensis L. Herbal drug with antihistaminic activity

Se hizo un estudio macro y micromorfológico, además del tamizaje fitoquímico y la determinación del contenido de mentol por cromatografía en capa delgada. Al mismo tiempo se realizó un estudio de conservación de la droga en condiciones de humedad y temperatura ambiental durante un año. El porcentaje de aceite esencial se mantuvo alto en todos los lotes analizados, sin verse influenciado por el tipo de secado ni por la procedencia de las muestras. El contenido de mentol determinado fue aproximadamente del 60 porciento. Los demás índices numéricos determinados se encontraron dentro de los rangos que se reportan para drogas vegetales. Se concluye que la droga puede almacenarse hasta un año en frascos de vidrio, latas compuestas y sobres de polietileno, sin que se afecte su calidad (AU)

Estudio farmacognóstico de Ocimum gratissimum L. (Orégano cimarrón) / Pharmacognostic study of Ocimum gratissimum (Oregano cimarrón)

Se realizó el estudio farmacognóstico de Ocimum gratissimum L. (Orégano cimarrón), para lo cual se realizaron determinaciones macro y micromorfólogicas. Se determinó el porcentaje de humedad, cenizas totales, sustancias extractivas en agua, aceite esencial y contenido de timol a la droga secada a la sombra, al sol y en estufa de recirculación de aire a 40 0C. Se realizó el tamizaje fitoquímico y el estudio de conservación por un año en frascos de vidrio, latas compuestas y sobres de papel. Las 3 formas de secado estudiadas resultaron satisfactorias, esta droga responde a los requerimientos organolépticos. El secado no influyó de forma significativa en la mayoría de los índices numéricos. Las características macro y micromorfológicas se correspondieron con las que se reportan para esta especie o para otras pertenecientes al mismo género. El tamizaje fitoquímico evidenció la presencia de aminas, esteroides y triterpernoides, fenoles, flavonoides, azúcares reductores, aceite esencial, saponinas y quinonas. Con el estudio de conservación es posible almacenar la droga durante 6 meses en frascos de vidrio y latas compuestas, no se recomienda la utilización de sobres de papel. Se logró la estandarización de la droga cruda, lo que permitió proponer las especificaciones de calidad para este medicamento herbario (AU)

Estudio farmacognóstico de Ocimum gratissimum L (Orégano cimarrón) / Pharmacognostic study of Ocimum gratissimum (Oregano cimarrón)

Se realizó el estudio farmacognóstico de Ocimum gratissimum L. (Orégano cimarrón), para lo cual se realizaron determinaciones macro y micromorfólogicas. Se determinó el porcentaje de humedad, cenizas totales, sustancias extractivas en agua, aceite esencial y contenido de timol a la droga secada a la sombra, al sol y en estufa de recirculación de aire a 40 0C. Se realizó el tamizaje fitoquímico y el estudio de conservación por un año en frascos de vidrio, latas compuestas y sobres de papel. Las 3 formas de secado estudiadas resultaron satisfactorias, esta droga responde a los requerimientos organolépticos. El secado no influyó de forma significativa en la mayoría de los índices numéricos. Las características macro y micromorfológicas se correspondieron con las que se reportan para esta especie o para otras pertenecientes al mismo género. El tamizaje fitoquímico evidenció la presencia de aminas, esteroides y triterpernoides, fenoles, flavonoides, azúcares reductores, aceite esencial, saponinas y quinonas. Con el estudio de conservación es posible almacenar la droga durante 6 meses en frascos de vidrio y latas compuestas, no se recomienda la utilización de sobres de papel. Se logró la estandarización de la droga cruda, lo que permitió proponer las especificaciones de calidad para este medicamento herbario

Estandarización de Mentha arvensis L medicamento herbario con actividad antihistamínica / Standardization of Mentha Arvensis L Herbal drug with antihistaminic activity

Se hizo un estudio macro y micromorfológico, además del tamizaje fitoquímico y la determinación del contenido de mentol por cromatografía en capa delgada. Al mismo tiempo se realizó un estudio de conservación de la droga en condiciones de humedad y temperatura ambiental durante un año. El porcentaje de aceite esencial se mantuvo alto en todos los lotes analizados, sin verse influenciado por el tipo de secado ni por la procedencia de las muestras. El contenido de mentol determinado fue aproximadamente del 60 porciento. Los demás índices numéricos determinados se encontraron dentro de los rangos que se reportan para drogas vegetales. Se concluye que la droga puede almacenarse hasta un año en frascos de vidrio, latas compuestas y sobres de polietileno, sin que se afecte su calidad

Estudo histológico das lesöes renais produzidas pelo B-Mirceno e d-Limoneno em ratos / Histologyc study of the renal lesions produced by B-mirceno and d-limoneno in mices

O B-mirceno (7-metil-3-metileno-1,6-octadieno) (MIR) é um monoterpeno olefínico encontrado nos óleos essenciais de uma grande variedade de plantas tais como o capim-limäo (Cymbopogon citratus Stapf), lúpulo, verbena, louro e outras. MIR e óleos essenciais contendo este monoterpeno hidrocarboneto acíclico säo amplamente usados como fragrâncias em cosméticos, como essência em saböes e detergentes, e como aditivos aromatizantes de alimentos. Apesar da importância da exposiçäo humana ao MIR, o seu potencial nefrotóxico ainda näo havia sido estudado. Por outro lado tem sido relatado que a exposiçäo crônica ao d-limoneno (p-menta-1,8-dieno) (LIM), um monoterpeno hidrocarboneto monocíclico,causa uma "nefropatia tubular hialina" sexo-específica e uma maior incidência de tumores renais em ratos machos. O presente estudo foi realizado para investigar se o tratamento sub-crônico de MIR causa lesäo renal em ratos. Um grupo de animais näo-tratados (controle negativo) e um grupo exposto ao d-limoneno (controle positivo) também foram incluídos neste experimento. MIR (1000 mg.kg-1.dia-1) ou óleo de milho (controle-veículo) foram administrados por gavagem a grupos de 10 ratos Wistar adultos machos, e 10 fêmeas, durante 15 dias. Alteraçöes de peso corporal e quaisquer sinais clínicos de toxicidade foram registrados durante o tratamento. Todos os animais foram sacrificados por inalaçäo de éter etílico e necropsiados ca de 24 horas após a última dose. Näo ocorreram alteraçöes significativas de peso corporal. Exceto por um aumento de peso de fígado e rins nos ratos tratados com MIR e LIM, näo foram evidenciadas alteraçöes dignas de nota por ocasiäo da necrópsia. Cortes de rins (5µm de espessura) foram corados pela Hematoxilina-Eosina (HE) ou pelo método de Mallory-Heidenhain, para avaliaçäo histopatológica. A intensidade da nefropatia tubular hialina (graus de 0 a +++++) foi quantificada por um patologista que ignorava o tratamento prévio do animal. Ratos machos expostos ao MIR (mediana 2,5) e ao LIM (mediana 4,5) apresentaram uma típica nefropatia tubular hialina. A nefropatia tubular hialina näo foi observada nas fêmeas tratadas com MIR ou LIM, e nos machos e fêmeas dos grupos controle-veículo e näo-tratado. Nossos resultados demonstraram que o MIR causa uma nefropatia tubular hialina sexo-específica em ratos machos.