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Item Caracterização farmacognóstica e atividade antimicrobiana da folha e casca do caule da Myrcia rostrata DC(Universidade Federal de Goiás, 2012-02-17) Alcântara, Guizelle Aparecida de; Paula, José Realino de; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4727958Y2; Verde, Giuliana Muniz Vila; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4702170Z2; Paula, Joelma Abadia Marciano de; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4797707D6The family Myrtaceae in Brazil is one of the most important families, comprising about 23 genera and 130 species. The specie Myrcia rostrata DC. popularly known as "folha miúda" or "guamirim chorão" is commonly found in South American forests and in some units that are part of the Federation Cerrado, as in Goias, Distrito Federal, Mato Grosso and other states. The aim of this study was to establish parameters pharmacognostic for quality control of M. rostrata and analyze the antimicrobial activity of the leaves and stem bark of this species. For this, the macroscopic description and implementation of the sections for microscopic analysis, the plant material was used fresh. As for the post microscopy, determination of volatile substances, total ash and acid insoluble, research and quantification of constituent phytochemicals, obtaining of crude ethanol extract and fractions and essential oil extraction, the shells were dried in an oven with forced circulation at 40 ° C and leaves outdoors. The gas chromatography coupled to mass spectrometry (GC / MS) was used to characterize the chemistry composition of essential oils, the test of serial broth microdilution for antimicrobial activity and Minimal Inhibitory Concentration (MIC) and High Performance Liquid Chromatography (HPLC) to obtain the chromatograms of the aqueous fractions (FAqC) and dichloromethane (FDC) from the stem bark of M. rostrata. The leaves of this species are simple menbranacea consistency, with shiny dark green on the adaxial surface dark green and opaque in the abaxial. Microscopically hypostomaticare present numerous unicellular trichomes have secretory cavities and idioblasts with prismatic crystals. The shells are curved stem and appearance of the outer surface is characterized as thick, fissured and striatum of which have dark-brown color. When examined microscopically is possible to visualize the periderm, sclereids and crystal series. Were detect in the phytochemistry essential oil, tannins, flavonoids and terpenes both the leaves and the bark of the stem. The total phenols content, tannins that precipitate proteins, hydrolysable tannins and flavonoids in the leaves were 7,53% ± 0,14, 4,65% ± 0, 65,39% ± 1,70 and 2,83% ± 0, for the stem bark were 10,06% ± 0,06, 9,60% ± 0,60, 29,53% ± 0,52 and 0,38% ± 0,009. In the analysis of essential oils from six constituencies identified spathulenol (51.39%) and globulol (6.88%) were the major components in the shell, together with the -Caryophyllene these compounds also predominated in the leaves, which were identified 32 constituents. Therefore, the sesquiterpene hydrocarbons and oxygenated sesquiterpenes predominated in the essential oils from leaves and bark of M. rostrata. In the analysis of the antimicrobial activity of essential oil extracted from leaves of M. rostrata showed moderate antibacterial activity with minimum inhibitory concentration (MIC) of 250 mg / mL for Gram (-) Enterobacter aerogenes ATCC 13048 and for all Gram (+) tested, the crude extract of leaves inhibited fungi with MIC 31.25 mg / mL for the species Candida parapsilosis ATCC 22019, Candida parapsilosis 11-a, 02 Candida albicans and Cryptococcus gattii L1, Cryptococcus neoformans ATCC 28957 and Cryptococcus neoformans L2 CIM was 15.62 mg / mL. Fractions of the leaves and stem bark tested showed the lowest minimum inhibitory concentration was FAqC against Cryptococcus neoformans ATCC 28957 (7.81 mg / mL) and Cryptococcus gattii L1 (15.62 mg / mL) and the FDC against Gram (-) Enterobacter aerogenes ATCC 13 048 (23.43 mg / mL) and against Gram (+) Bacillus subtilis ATCC 6633 (93.75 mg / mL).The results contribute to the identification of the species M. rostrata and demonstrate its potential for treating diseases caused by micro-organisms.Item Desenvolvimento de modelos de QSAR e análise quimioinformática da sensibilização e permeabilidade da pele(Universidade Federal de Goiás, 2014-03-17) Alves, Vinícius de Medeiros; Andrade, Carolina Horta; http://lattes.cnpq.br/2018317447324228; Andrade, Carolina Horta; Ferreira, Elizabeth Igne; Camargo, Ademir J.Repetitive exposure to a chemical agent can induce an immune reaction in inherently susceptible individuals that leads to skin sensitization. Although many chemicals have been reported as skin sensitizers, there have been very few reports analyzing the relationships between their molecular structure and the sensitization potential including the connection to skin permeability, which is widely considered to be mechanistically implicated in sensitization. In this study, we have compiled, curated, and integrated the largest publicly available datasets related to chemically-induced skin sensitization and skin permeability. Unexpectedly, no correlation between sensitization and permeability has been found. Predictive QSAR models have been developed and validated for both skin sensitization and skin permeability using a standardized workflow fully compliant with the OECD guidelines. The classification accuracies of QSAR models discriminating sensitizers from non-sensitizers were 0.68-0.88 when evaluated on several external validation sets. When compared to the predictions generated by the OECD QSAR Toolbox skin sensitization module, our models had significantly higher prediction accuracy for the same sets of external compounds as evaluated by Positive Predicted Rate and Negative Predicted Rate as well as Correct Classification Rate. We have also developed QSAR models of skin permeability measured quantitatively. Cross-species correlation between human and rodent permeability data was found to be low (r²=0.44); thus, skin permeability models were developed using human data only and their external accuracy was q²ext = 0.87 (for 62% of external compounds found within the model applicability domain). Skin sensitization models have been employed to identify putative chemical hazards in the Scorecard database of possible skin or sense organ toxicants that should be regarded as primary candidates for the experimental validation.Item Desenvolvimento tecnológico de extratos vegetais padronizados a partir da Lafoensia pacari A. St.-Hill (Lythraceae)(Universidade Federal de Goiás, 2013-02-28) Cardoso, Natasha Queiroz; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510Lafoensia pacari A. St.-Hill (Lythraceae) popularly known as dedaleiro, didal, or mad-mangabeira pacari, is used by the Brazilian population as a febrifuge, tonic and healing. Studies have shown the antioxidant, anti-inflammatory, and antinoceptiva antiedematogenic extracts from the stem bark, ellagic acid being one of those responsible for the same. This study aimed to obtain dry extract standardized technology from the stem bark of L. pacari. The drug was tested for various quality control tests, according to the Brazilian Pharmacopoeia 5th edition, which ensured the characterization of plant drug and subsequently obtaining the liquid and dry extracts standardized. The extraction method was chosen slow percolation with 80% hydroalcoholic solution as a solvent and velocity of 7 drops per min .. The liquid extract standardized had a density of 0.986 g / mL solids content of 12.49% (w / w), pH 3.53 and an alcohol content of 44.80% (v / v). The content of ellagic acid found in liquid extract was 3.84% (m / m). The spray drying / atomization was performed by experimental design of univariate and then by planning a fractional 5-2 with 2 replicates. During the process the adjuvants were used maltodextrin and aerosil, demonstrating that the optimal conditions found maltodextrin provides greater protection and ellagic acid concentration in the extract.Item Estudo da encapsulação da isotretinoína nas formas livre e associada a ciclodextrinas em niossomas(Universidade Federal de Goiás, 2009-12-15) Rodovalho, Luciana Ferreira Fonseca; Lima, Eliana Martins; http://lattes.cnpq.br/7248774319455970Non-ionic surfactant vesicles (niosomes) and cyclodextrins (CDs) are able to modify physical-chemical properties of incorporated drugs. One of the major challenges for the topical administration of retinoids, such as isotretinoin (31cisRA), is the stability of these compounds in formulations capable of reducing their toxicity during the treatment. The purpose of this research was to develop vesicular carries capable to transport and deliver isotretinoin for topical application during acne treatment. The niosomes were obtained from Bryj®30:Cholesterol:DCP (50:25:10) by the film hydration method. The HP CDs:isotretinoin complex was obtained by agitation for 8 days in phosphate buffer pH 7.4. The vesicles were characterized and it was possible to encounter a large amount of morphological varieties, flexible structures and fluid membrane, after inclusion of free isotretinoin. The fluidness of the membrane that contains isotretinoin allowed leaking of the drug when in concentration above 5 mM. The HP CDs:Isotretinoin (20:1) increased the vesicle size considerably, also allowing drug leaking. The systems developed presented themselves as potential carries of isotretinoin for topical application and played the roll of drug delivery system,Item Nanopartículas lipídicas sólidas contendo genisteína para uso tópico(Universidade Federal de Goiás, 2012-02-28) Silva, Lorena Maione; Taveira, Stephânia Fleury; http://lattes.cnpq.br/0382450621383005; Lima, Eliana Martins; http://lattes.cnpq.br/7248774319455970Genistein (GEN), isoflavone contained in soybeans, shows activity against a large number of cancers, including skin cancer. However, to be used topically it is essential the association of GEN in an appropriate formulation. The aim of this study was the development and characterization of solid lipid nanoparticles (SLN) contends genistein for topical application. A bioanalytical method was developed and validated for GEN quantification in skin layers with High Performance Liquid Chromatographer (HPLC) with UV detection. The SLN was obtained with glyceryl behenate, polysorbate 80, sorbitan trioleate and different amounts of cetylpyridinium chloride (CPC) (0.5 - 0.05%). The characteristics in terms of particle size, size distribution, zeta potential, entrapment efficiency and drug recovery were evaluated. In vitro release, passive and iontophoretic, skin permeation studies were performed. Cytotoxicity studies were carried out in melanoma cells (B16F10) with free drug and SLN with and without GEN. The analytical method was linear in the concentration range of 0.1 to 60 mg/mL. Limit of quantification was 100 ng/mL for both skin layers. Recovery of the drug ranged from 95.57 to 97.57%. The method was able to analyze the GEN without suffering interference from endogenous skin components. SLN loaded with GEN showed positive surface (+ 23 mV) and average size of 343 nm. Particles were obtained with high entrapment efficiency (93%) and drug load was 5.45%. In vitro release studies demonstrated that the release of GEN from SLN occurs in two stages with a large amount of drug released within the first six hours, followed by a slow release of the remaining drug in the lipid matrix of SLN in the following hours. When administered in the skin, during in vitro passive permeation studies, the SLN increased retention of GEN in stratum corneum and remaining skin compared with free GEN. After iontophoresis application in formulation of SLN containing GEN thirteen times more GEN was retained on stratum corneum and three times more drug was retained on remaining skin. In cellular cytotoxicity studies SLN favored the increase of interaction of drug with the cells and the cytotoxicity was concentration-dependent. Thus, GEN loaded SLN increased drug skin permeation and retention and shows to be a potential formulation for topical application.Item Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados(Universidade Federal de Goiás, 2013-03-18) Silva, Luis Antônio Dantas; Taveira, Stephânia Fleury; Marreto, Ricardo Neves; Cutaneous retentio.; http://lattes.cnpq.br/6127043775208484; Marreto, Ricardo Neves; Gratieri, Taís; Taveira, Stephânia FleuryClobetasol propionate is one of the most potent topical corticosteroids usually available and has been established the use in treatment of various skin pathology. However its systemic absorption may cause serious side effects. The use of lipids nanocarriers and application of iontophoretic current shown potential to further controlled release of clobetasol propionate and increase their retention in the stratum corneum, thus making its management more effective and safe. In this study an analytical method was developed and validated for quantification of clobetasol propionate in nanocarriers and pig skin, used as model membranes in vitro permeation studies. Nanostructured lipid carriers (NLC) were obtained by dilution of microemulsion and chitosan-coated NLC (NLC-Ch) by the dripping of NLC in chitosan solution. The developed nanocarriers were characterized to mean diameter, polydispersity index, zeta potential, drug loading, recovery and encapsulation efficiency. The in vitro release and permeation profile of clobetasol free and nanoencapsulated was evaluated using Franz cells. The nanocariers obtained of 125 nm and uniform size distribution, whit PdI 0,25. The increase in size of NLC-Ch and the inverting the value of zeta potential, suggest that there was a coating of the CLN by chitosan, though interaction of charges. The NLC and NLC-Ch showed recovery values greater than 80% and encapsulation efficiency than 90%. The release profile of clobetasol from the developed formulations showed a controlled release with 35% in 24 hours of study. The nanoenapsulation of clobetasol in the NLC-Ch and NLC resulted in retention increased in the stratum corneum of 9.2 an 7.8 fold, respectively, compared to free drug. The retention of the clobetasol in the stratum corneum was 4 and 2 times higher when electric current was applied to the formulation CLNQ, compared to the free drug and encapsulated in NLC, respectively. The accumulation of the drug in the stratum corneum, promoted by lipid carriers, shows that these systems are effective for potential topical delivery to minimize the permeation of the drug into the bloodstream and reduces the side effects.Item Planejamento, síntese, caracterização e avaliação de um novo composto candidato a protótipo de fotoprotetor(Universidade Federal de Goiás, 2012) Vinhal, Daniela Cristina; Bozinis, Marize Campos Valadares; http://lattes.cnpq.br/6157755243167018; Gil, Éric de Souza; http://lattes.cnpq.br/3218622824233303In Brazil, the estimates for the year 2012 point to approximately 134,000 new cases of skin cancer, being mostly related to exposure to ultraviolet radiation. According to current consensus, such damage can be minimized by prophylactic use of sunscreens, which aims to protect human skin against harmful effects of UV radiation. This way, this study proposed to plan, synthesize, characterize and evaluate a new compound to be a sunscreen (17). The structural planning is made from photoprotective triazona ethylhexyl prototypes (12) and cinnamate (4) having the compound 15 which was produced from vanillin, a natural abundant and low cost product. In addition, 17 compound has molecular weight above 800 Daltons, which is in accordance with the photoprotective recently launched on the market, because it minimizes or even prevents its absorption through the skin. The synthetic route proposal consisted of two stages, which after optimized lead to obtain the 17 compound in 78.6% overall yield. It is noteworthy that the 15 compound was obtained in quantitative yield and the 17 compound was purified by Soxhlet extractor, using amyl alcohol as solvent. These facts make its synthesis a bit laborious and inexpensive, fundamental characteristics of a technological product, from the financial point of view. All the synthesized compounds were characterized by spectrometric techniques of nuclear magnetic resonance of hydrogen-dimensional and two-dimensional, infrared, mass and ultraviolet, in equal ways. From the spectrophotometric absorption technique it was identified that 17 compound had two peaks of maximum absorption (λmax.) in the UV, and 306 nm in the region of UVB and 344 nm for UVA. It is also possible to calculate the parameters of the molar absorptivity (ε) and specific extinction coefficient (E), whose values were above 104 -1 cm-1 for ε and 5,843 4,337 for E. Moreover, the 15 and 17 compounds were also M evaluated on their redox profile using the technique of cyclic voltammetry which showed that the 17 compound keeps stable considering the applied potential. The thermogravimetric thermal analysis the 17 compound showed a weight loss of 47.88% in the range of 330 °C under an atmosphere of synthetic air, characterized as a stable compound at high temperatures. From the in vitro evaluation by the spectrophotometric method described by Mansur it presented SPF equal to 4.58, while under the same conditions the methoxycinnamato of octyl (4), sunscreen sold worldwide, presented SPF equal to 2.79. At the end of this work it is possible to observe that the proposed synthetic route to obtain the 17 compound was effective, given the obtained high yields, laborious and low cost steps. Finally, we conclude that the structural planning employee was ratified, since the described physical-chemicals organic evaluated had great similarities with the prototype sunscreen (12) and (4) used in its planning.