Design and optimization of selfnanoemulsifying drug delivery systems for enhanced dissolution of gemfibrozil

Self-nanoemulsifying drug delivery systems of gemfibrozil were developed under Quality by Design approach for improvement of dissolution and oral absorption. Preliminary screening was performed to select proper components combination. BoxBehnken experimental design was employed as statistical tool to optimize the formulation variables, X1 (Cremophor® EL), X2 (Capmul® MCM-C8), and X3 (lemon essential oil). Systems were assessed for visual characteristics (emulsification efficacy), turbidity, droplet size, polydispersity index and drug release. Different pH media were also assayed for optimization. Following optimization, the values of formulation components (X1, X2, and X3) were 32.43%, 29.73% and 21.62%, respectively (16.22% of gemfibrozil). Transmission electron microscopy demonstrated spherical droplet morphology. SNEEDS release study was compared to commercial tablets. Optimized SNEDDS formulation of gemfibrozil showed a significant increase in dissolution rate compared to conventional tablets. Both formulations followed Weibull mathematical model release with a significant difference in td parameter in favor of the SNEDDS. Equally amodelistic parameters were calculated being the dissolution efficiency significantly higher for SNEDDS, confirming that the developed SNEDDS formulation was superior to commercial formulation with respect to in vitro dissolution profile. This paper provides an overview of the SNEDDS of the gemfibrozil as a promising alternative to improve oral absorption.

Mouthrinses: a comparative microbiological study

This study was performed in order to evaluate the efficacy of different mouthrinses whose use is extended in Spain. Six different antiseptic mouthrinses were studied by means of determination of Minimal Inhibitory Concentration (MIC) values against Klebsiella pneumoniae, Serratia marcescens, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhimurium, Bacillus subtilis, Streptococcus mutans, Prevotella intermedia, Porphyromonas gingivalis and Actinobacillus actinomycetemcomitans. Also in vivo experiments were carried out in volunteers by the use of mouthrinses and evaluation of bacterial populations before and after the treatment. Finally, the kinetics of bacterial death was determined. Results suggested that the determination of MIC values is not a reliable method to evaluate the antibacterial effect of such products. On the other hand those rinsing solutions based on the effect of oxygen, such as those containing carbamide peroxide have a greater efficacy against anaerobic bacteria compared with rinses whose active molecule is a disinfectant. Finally, the kinetics of bacterial death demonstrates that the essential oil rinse kills bacteria much faster. All tested mouthrinses were active as antibacterial although those based on oxygen production or essential oils were more active than solutions based on chlorhexidine and Triclosan

Quantificação do linalol no óleo essencial da Aniba duckei Korstermans utilizando uma nova coluna capilar POLYH4-MD em Cromatografia Gasosa

In the present work a polyurethane polymer derived from castor oil was used as stationary phase for capillary gas chromatography. The polymer was obtained by reaction of hydroxylated compound and isocynate (NCO), forming urethane. Columns of 7 m x 0,25 mm were then coated with this stationary phase (film thickness of 0,25 µm) using static coating method. The Grob test was also performed. Samples of essential oil of the Aniba duckei Korstermans was then analysed in POLYH4-MD capillary column in order to evaluate its chromatographic perfomance. The linalool was found to be the major component and has been used as compound of departure for many important syntheses. Results show that the experimental columns give higher resolution and can be employed for analysis of essentials oils.

Produtos naturais para o controle da transmissão da dengue: atividade larvicida de Myroxylon balsamum (óleo vermelho) e de terpenóides e fenilpropanóides

The bioassay-guided fractionation of the hexane extract obtained from the medicinal plant Myroxylon balsamum (red oil) was conducted in preparative thin layer chromatography on silica gel. The obtained fractions and some terpenoids and phenylpropanoids were assayed as larvicidal on third instar Aedes aegypti larvae, NPPN colony. The results indicate that the sesquiterpene nerolidol was the active constituent in the extract and that the sesquiterpenes were more active than the monoterpenes and phenylpropanoids utilized in this study. Lipophilicity seems to be an important property for the activity since the compounds with hydroxyl, carbonyl and methoxyl groups were less active. The results confirm also that essential oils can be a good tool for the control of dengue.

Teor e composição do óleo essencial de cinco acessos de mentrasto

This study aimed to analyse the content and the composition of the essential oil of five accesses of mentrasto (Ageratum conyzoides). Five accesses of mentrasto with three repetitions were used. The accesses were obtained in Mariana-MG (AMA), Piranga-MG (API), Visconde do Rio Branco (ARB) and Viçosa-MG (AVB and AVP). The essential oil was obtained by hydrodistillation and the identification of the oil components by CG and GC/MS. The ARB access presented the higher essential oil content, that is 0.70% (P < 0.05). Eleven chemical compounds were identified. The precocene I was the main constituent in the access API, and the precocene II was the main constituent in the accesses AMA, ARB, AVB and AVP.

Constituintes químicos de Ottonia corcovadensis Miq. da floresta Amazônica: atribuição dos deslocamentos químicos dos átomos de hidrogênio e carbono

In an ethanolic extract of leaves of Ottonia corcovadensis (Piperaceae) were identified sixteen terpenoids of essential oil and the three flavonoids 3',4',5,5',7-pentamethoxyflavone (1), 3',4',5,7-tetramethoxyflavone (2) and 5-hydroxy-3',4',5',7-tetramethoxyflavone (3) and cafeic acid (4). Two amides (5 and 6) were isolated from an ethanolic extract of the roots. The structures were established by spectral analysis, meanly NMR (1D and 2D) and mass spectra. Extensive NMR analysis was also used to complete ¹H and 13C chemical shift assignments of the flavonoids and amides. The components of the essential oil were identified by computer library search, retention indices and visual interpretation of mass spectra.

Constituintes químicos voláteis das flores e folhas do pau-brasil (Caesalpinia echinata, Lam.)

The volatile constituents obtained from a static cryogenic headspace of Caesalpinia echinata Lam. (Leguminosae) showed E-beta-ocimene as the major compound (57.2%), beside other monoterpenes, C6 derivatives like n-hexanal and (E)-2-hexenal and nitrogen compounds such as indole and methyl anthranilate. From the essential oil of the leaves obtained by hydrodistillation in a Clevenger apparatus, (E)-3-hexen-1-ol was identified as the major constituent while phenolic compounds were the most representative class of secondary metabolites.

Óleos voláteis de espécies de Myrcia nativas do Rio Grande do Sul

Essential oils from M. richardiana, M. arborescens, M. selloi, M. oligantha, M. rostrata, M. lajeana, M. obtecta, M. pubipetala and M. hatschbachii were obtained by hydrodistillation and analyzed by GC and GC/MS. Sixty-seven compounds have been identified ranging from 90-99% of the oil contents. All analyzed species were rich in cyclic sesquiterpenes (66-99%), mainly those from the cadinane, caryophyllane and germacrane cyclization pathway, among them b-caryophyllene, germacrene D, bicyclogermacrene, d-cadinene, spathulenol, caryophyllene oxide, globulol and a-cadinol. The acyclic sesquiterpene series was well represented by M. lajeana (32.1%), with 25,3% of (E)-nerolidyl acetate.

Avaliação do óleo essencial de Aloysia sellowii (Briquet) moldenke (Verbenaceae) do Sul do Brasil

This work was performed with the aim of evaluating the chemical variability among samples of Aloysia sellowii (Verbenaceae) collected in different geographical regions as well as the application of supercritical CO2 for obtaining essential oil. Thus, samples were collected in different localities and oils were isolated by hydrodistillation and supercritical CO2. Results showed existence of two chimiotypes in the species (cineole and sabinene). The supercritical CO2 extraction process was appropriate for extraction of A. sellowii essential oil at 40 ºC, 110 bar, 2 mL/min of flow and 10 min of extraction time.

A convenient method for the determination of moisture in aromatic plants

A method is proposed for the determination of the moisture content of aromatic plants. This method is based on the co-distillation of the starting material in a modified Clevenger apparatus with four organic solvents (toluene, cyclohexane, dichloromethane and carbon tetrachloride). The results were compared with those obtained by oven drying at 105 ºC and steam distillation of the essential oil. The efficiencies of the methods were shown to be equivalent. The solvent distillation method was more practical, especially with respect to operating time (2 h).

Atividade antioxidante de óleos essenciais de espécies de Croton do nordeste do Brasil

Three Croton species, C. zenhtneri, C. nepetaefolius and C. argyrophylloides, were collected at two different times, 6:00 and 13:00 h, their essential oils were extracted by steam distillation and analyzed by gas Chromatography / Mass Spectrometry. The percentage yield of oil constituents changes along the day. The oils were submitted to the antioxidant test thiobarbituric acid reactive species, using BHT and a-tocoferol as the reference compounds. All oils exhibited good antioxidant activities. In general, C. zenhtneri and C. argyrophylloides essential oils showed higher antioxidant activity than C. nepetaefolius.

Óleo essencial de Gochnatia polymorpha (Less) Cabr. ssp floccosa Cabr.

The essential oil isolated by hydrodistillation from flowers and root bark of Gochnatia polymorpha (Less) Cabr. ssp floccosa Cabr. (Asteraceae) was analyzed by capillary GC/MS. Thirty components were identified in oil of flowers. The composition depends on the stage of flowering. At the beginning of flowering, the main components were (E)-nerolidol (20,4%) and eugenol (17,9%) whereas at the end they were phenylacetaldehyde (14,6%) and tricosane (12,0%). In the essential oil of root bark ten sesquiterpenes were identified. The major components were beta-bisabolene (31,0%) and beta-bisabolol (21,5%). This paper describes for the first time the composition of essential oil in the genus Gochnatia.

Variação química do óleo essencial de Hyptis suaveolens (L.) Poit., sob condições de cultivo

This study was performed to establish the correlation between the growth conditions and essential oil composition of Hyptis suaveolens from Alfenas (MG), Brazil. The plants were grown in a greenhouse, four treatments were used and they were harvested at two different periods of time (60 and 135-day-old plants). The essential oil composition was determined by GC-MS analysis. The terpenes spathulenol, globulol, dehydroabietol, a-cadinol and beta-phellandrene were the major constituents found in the essential oil. Oxygenated sesquiterpenes represented the main group of constituents in most of the treatments. The major changes in the essential oil composition were found in 135-day-old plants grown under NPK deficiency. We also identified three groups of volatile components that have not been previously described in H suaveolens.

Influência da temperatura do ar de secagem sobre o teor e a composição química do óleo essencial de Lippia alba (Mill) N. E. Brown

Leaves of Lippia alba were submitted to six different drying treatments, using air at ambient temperature and heated up to 80 °C. The essential oil was extracted by steam distillation and analyzed by GC-MS. For the dried leaves, the oil content was reduced by 12 to 17% when compared with the fresh plant (0.66%). The major oil component was citral, representing 76% for the fresh plant, and varying from 82 to 84% for the dried material. These results showed that L. alba can be submitted to a drying process of up to 80 ºC without degradation and/or loss of the major, [LC1] active component.

Evaluation of seasonal changes in chemical composition and antibacterial activity of Elyonurus muticus (sprengel) O. Kuntze (Gramineae)

Aerial parts of Elyonurus muticus were collected in the four seasons of the year in the Brazilian Pantanal and subjected to extractrion with cold ethanol and to hydrodistillation. Sesquiterpenoids (E)-caryophyllene, bicyclogermacrene, spathulenol and caryophyllene oxide were the main components identified in the essential oils and their concentrations varied according to the plant collection period. The essential oils and the ethanolic crude extracts were active against Bacillus cereus MIP 96016, Pseudomonas aeruginosa ATCC 27853 and Staphylococcus aureus ATCC 25923 and were not active against Escherichia coli ATCC 25922. The antibacterial activities varied according to the plant collection period.