Made available in DSpace on 2014-12-17T15:42:08Z (GMT). No. of bitstreams: 1 FabianoESG_TESE.pdf: 2562039 bytes, checksum: f41fc74bb604ad5b4eb0383a80628c68 (MD5) Previous issue date: 2010-03-30 / Conselho Nacional de Desenvolvimento Cient?fico e Tecnol?gico / Among the new drugs launched into the market since 1980, up to 30% of them belong to the class of natural products or they have semisynthetic origin. Between 40-70% of the new chemical entities (or lead compounds) possess poor water solubility, which may impair their commercial use. An alternative for administration of poorly water-soluble drugs is their vehiculation into drug delivery systems like micelles, microemulsions, nanoparticles, liposomes, and cyclodextrin systems. In this work, microemulsion-based drug delivery systems were obtained using pharmaceutically acceptable components: a mixture Tween 80 and Span 20 in ratio 3:1 as surfactant, isopropyl mirystate or oleic acid as oil, bidistilled water, and ethanol, in some formulations, as cosurfactants. Self-Microemulsifying Drug Delivery Systems (SMEDDS) were also obtained using propylene glycol or sorbitol as cosurfactant. All formulations were characterized for rheological behavior, droplet size and electrical conductivity. The bioactive natural product trans-dehydrocrotonin, as well some extracts and fractions from Croton cajucara Benth (Euphorbiaceae), Anacardium occidentale L. (Anacardiaceae) e Phyllanthus amarus Schum. & Thonn. (Euphorbiaceae) specimens, were satisfactorily solubilized into microemulsions formulations. Meanwhile, two other natural products from Croton cajucara, trans-crotonin and acetyl aleuritolic acid, showed poor solubility in these formulations. The evaluation of the antioxidant capacity, by DPPH method, of plant extracts loaded into microemulsions evidenced the antioxidant activity of Phyllanthus amarus and Anacardium occidentale extracts. For Phyllanthus amarus extract, the use of microemulsions duplicated its antioxidant efficiency. A hydroalcoholic extract from Croton cajucara incorporated into a SMEDDS formulation showed bacteriostatic activity against colonies of Bacillus cereus and Escherichia coli bacteria. Additionally, Molecular Dynamics simulations were performed using micellar systems, for drug delivery systems, containing sugar-based surfactants, N-dodecylamino-1-deoxylactitol and N-dodecyl-D-lactosylamine. The computational simulations indicated that micellization process for N-dodecylamino-1- deoxylactitol is more favorable than N-dodecyl-D-lactosylamine system. / Dos novos f?rmacos lan?ados no mercado a partir de 1980, cerca de 30% apresentam origem natural ou semissint?tica. Entre 40 e 70% destes novos prot?tipos de f?rmacos (naturais ou sint?ticos) apresentam baixa solubilidade aquosa, o que pode inviabilizar a sua utiliza??o comercial. Uma das alternativas encontrada pela ind?stria farmac?utica foi a veicula??o dessas subst?ncias a partir de ve?culos ou sistemas de libera??o de f?rmacos, tais como: micelas, microemuls?es, lipossomos, nanopart?culas e ciclodextrinas. Neste trabalho, sistemas microemulsionados biologicamente compat?veis foram obtidos utilizando a mistura Tween 80 e Span 20, na propor??o 3:1, como tensoativo, miristato de isopropila ou ?cido ol?ico como fase oleosa, ?gua bidestilada, e em alguns sistemas, etanol como cotensoativo. Tamb?m foram obtidos sistemas auto-microemulsificantes (SMEDDS) utilizando propilenoglicol ou sorbitol como cotensoativo. As microemuls?es obtidas foram caracterizadas quanto ao comportamento reol?gico, tamanho das got?culas e condutividade el?trica. O produto natural bioativo trans-desidrocrotonina (DCTN), bem como extratos e fra??es das esp?cies vegetais Croton cajucara Benth (Euphorbiaceae), Anacardium occidentale L. (Anacardiaceae) e Phyllanthus amarus Schum. & Thonn. (Euphorbiaceae), foram solubilizados satisfatoriamente nos sistemas microemulsionados obtidos, enquanto que outros produtos tamb?m isolados da esp?cie Croton cajucara, trans-crotonina e ?cido acetilaleurit?lico, n?o apresentaram resultados satisfat?rios em termos de solubilidade. A avalia??o da propriedade antioxidante, pelo m?todo do DPPH, dos extratos vegetais incorporados nos sistemas microemulsionados obtidos evidenciou a capacidade antioxidante dos extratos de Phyllanthus amarus e Anacardium occidentale, bem como a atua??o dos sistemas microemulsionados, que para o caso do extrato etan?lico de Phyllanthus amarus dobrou a sua atividade antioxidante quando solubilizado em microemuls?es. O extrato hidroalco?lico de Croton cajucara incorporado em um sistema auto-microemulsificante mostrou atividade bacteriost?tica frente a col?nias de bact?rias Bacillus cereus e Escherichia coli. Adicionalmente, foi realizado um estudo de simula??o computacional por Din?mica Molecular de sistemas micelares para uso farmacol?gico contendo tensoativos derivados de a??cares, N-dodecilamino-1-deoxilactitol e N-dodecil- -lactosilamina, que indicou que o processo de miceliza??o do primeiro sistema ? mais favor?vel que o segundo.

Submitted by Sandra Pereira (srpereira@ufrrj.br) on 2016-09-15T12:14:46Z No. of bitstreams: 1 2011 - Daiane Ouvernay Fernandes da Silva.pdf: 7586481 bytes, checksum: 5a97593f1df40687d3039aaf482f7a65 (MD5) / Made available in DSpace on 2016-09-15T12:14:46Z (GMT). No. of bitstreams: 1 2011 - Daiane Ouvernay Fernandes da Silva.pdf: 7586481 bytes, checksum: 5a97593f1df40687d3039aaf482f7a65 (MD5) Previous issue date: 2011-06-21 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES / This study investigated the relationship between species of frogs, lizards, gradients environmental and insularity. We could detect a strong relationship between lizards in open habitats and anthropic as well as a strong influence of the area to the richness and abundance of lizards, rather than habitat heterogeneity. The community was the most diverse State Park Cunhambebe. The lizards of island environments of the Sepetiba Bay showed a strong relationship between abundance and area, supporting the hypothesis of Ecological Release. The species Cycloramphus sp., Thoropa miliaris, Hylodes asper, H. phyllodes, Phasmahyla cruzi and Scinax trapicheiroi are those with lower values of tolerance of distance from this physiognomy and sometimes only occur in this environment. / Neste estudo foram investigadas as rela??es entre esp?cies de anf?bios anuros, lagartos, gradientes ambientais e insularidade. Nota-se uma forte rela??o dos lagartos com ambientes abertos e antr?picos, bem como uma forte influ?ncia da ?rea para a riqueza e abund?ncia dos lagartos, mais que a heterogeneidade de habitats. A comunidade mais diversa foi a do Parque Estadual do Cunhambebe. Os lagartos de ambientes insulares da Ba?a de Sepetiba demonstraram forte rela??o entre abund?ncia e ?rea, corroborando com a hip?tese de Libera??o ecol?gica. As esp?cies Cycloramphus sp., Thoropa miliaris, Hylodes asper, H. phyllodes, Phasmahyla cruzi e Scinax trapicheiroi s?o as que possuem menores valores de toler?ncia de dist?ncia da cachoeira e, algumas vezes, s? ocorrem neste ambiente

Made available in DSpace on 2014-12-17T14:13:33Z (GMT). No. of bitstreams: 1 ElquioEO_TESE.pdf: 1649953 bytes, checksum: 1098cd34b1d3e6c9a180949d25fa8185 (MD5) Previous issue date: 2010-06-07 / Universidade Federal do Rio Grande do Norte / The aim of this work was to perform the extraction and characterization of xylan from corn cobs and prepare xylan-based microcapsules. For that purpose, an alkaline extraction of xylan was carried out followed by the polymer characterization regarding its technological properties, such as angle of repose, Hausner factor, density, compressibility and compactability. Also, a low-cost and rapid analytical procedure to identify xylan by means of infrared spectroscopy was studied. Xylan was characterized as a yellowish fine powder with low density and poor flow properties. After the extraction and characterization of the polymer, xylan-based microcapsules were prepared by means of interfacial crosslinking polymerization and their characterization was performed in order to obtain gastroresistant multiparticulate systems. This work involved the most suitable parameters of the preparation of microcapsules as well as the study of the process, scale-up methodology and biological analysis. Magnetic nanoparticles were used as a model system to be encapsulated by the xylan microcapsules. According to the results, xylan-based microcapsules were shown to be resistant to several conditions found along the gastrointestinal tract and they were able to avoid the early degradation of the magnetic nanoparticles / O presente trabalho teve como objetivo a extra??o e caracteriza??o do pol?mero de xilana a partir de res?duos de sabugo de milho e a produ??o de microc?psulas a partir deste pol?mero. O primeiro passo foi a extra??o da xilana em meio alcalino e caracteriza??o deste pol?mero quanto as suas propriedades tecnol?gicas (?ngulo de repouso, fator de Hausner, densidade, compressibilidade e compactabilidade), bem como a elabora??o de uma procedimento r?pido e barato para a identifica??o deste pol?mero atrav?s de espectroscopia de absor??o na regi?o do infravermelho. O pol?mero de xilana foi caracterizado como sendo um p? de cor amarelada de baixa densidade e com propriedades de escoamento pouco favor?veis. Ap?s a obten??o e caracteriza??o do pol?mero, microc?psulas de xilana foram preparadas atrav?s da reticula??o polim?rica interfacial e caracterizadas a fim de se obter sistemas multiparticulados gastroresistentes. O trabalho foi delineado buscando-se os melhores fatores na t?cnica de prepara??o das microc?psulas, assim como o estudo do processo, aumento de escala e avalia??o biol?gica. Nanopart?culas magn?ticas foram utilizadas como sistema modelo a ser encapsulado pelas microc?psulas ? base de xilana. Os resultados obtidos demonstraram que as microc?psulas de xilana s?o resistentes ?s diversas condi??es encontradas ao longo do trato gastrintestinal e foram capazes de evitar a degrada??o pr?via das nanopart?culas magn?ticas in vitro

Made available in DSpace on 2014-12-17T14:13:48Z (GMT). No. of bitstreams: 1 AcariliaES_TESE.pdf: 9221805 bytes, checksum: 71876e327362584aeb9dcac7d3652c4d (MD5) Previous issue date: 2013-04-05 / Conselho Nacional de Desenvolvimento Cient?fico e Tecnol?gico / This thesis was devoted to the development of innovative oral delivery systems for two different molecules. In the first part, microparticles (MPs) based on xylan and Eudragit? S- 100 were produced and used to encapsulate 5-aminosalicylic acid for colon delivery. Xylan was extracted from corn cobs and characterized in terms of its physicochemical, rheological and toxicological properties. The polymeric MPs were prepared by interfacial cross-linking polymerization and spray-drying and characterized for their morphology, mean size and distribution, thermal stability, crystallinity, entrapment efficiency and in vitro drug release. MPs with suitable physical characteristics and satisfactory yields were prepared by both methods, although the spray-dried systems showed higher thermal stability. In general, spraydried MPs would be preferable systems due to their thermal stability and absence of toxic agents used in their preparation. However, drug loading and release need to be optimized. In the second part of this thesis, oil-in-water microemulsions (O/W MEs) based on mediumchain triglycerides were formulated as drug carriers and solubility enhancers for amphotericin B (AmB). Phase diagrams were constructed using surfactant blends with hydrophiliclipophilic balance values between 9.7 and 14.4. The drug-free and drug-loaded MEs presented spherical non-aggregated droplets around 80 and 120 nm, respectively, and a low polydispersity index. The incorporation of AmB was high and depended on the volume fraction of the disperse phase. These MEs did not reduce the viability of J774.A1 macrophage-like cells for concentrations up to 25 μg/mL of AmB. Therefore, O/W MEs based on propylene glycol esters of caprylic acid may be considered as suitable delivery systems for AmB / Esta tese teve como objetivo o desenvolvimento de novos sistemas de libera??o para duas mol?culas distintas. Na primeira parte, micropart?culas ? base de xilana e Eudragit? S-100 foram produzidas para encapsular ?cido 5-aminosalic?lico visando ? libera??o c?lonespec?fica. A xilana foi extra?da de sabugos de milho e caracterizada quanto ?s suas propriedades f?sico-qu?micas, reol?gicas e toxicol?gicas. Em seguida, dois m?todos de microencapsula??o foram utilizados: reticula??o interfacial polim?rica e secagem por aspers?o. Os sistemas produzidos foram caracterizados quanto ? morfologia, tamanho m?dio e distribui??o, estabilidade t?rmica, cristalinidade, taxa de encapsula??o e libera??o do f?rmaco in vitro. Foram obtidas micropart?culas com adequadas caracter?sticas f?sicas e rendimentos satisfat?rios atrav?s dos dois m?todos, embora os sistemas aspergidos tenham apresentado maior estabilidade t?rmica e sejam considerados mais interessantes devido a sua maior estabilidade t?rmica e aus?ncia de agentes t?xicos. No entanto, ajustes precisam ser feitos para melhorar a encapsula??o e libera??o do f?rmaco. Na segunda parte, microemuls?es do tipo ?leo em ?gua (MEs O/A) com base em triglicer?deos de cadeia m?dia (MCT) foram produzidas visando ao carreamento de anfotericina B (AmB) e aumento da sua solubilidade. Foram obtidas MEs O/A sem e com AmB com got?culas em torno de 80 e 120 nm, respectivamente, e ?ndices de polidispers?o de 0,25 e 0,31, respectivamente. A taxa de incorpora??o da AmB foi alta e dependente do volume da fase dispersa. A viabilidade celular n?o foi afetada at? 25 μg/mL da AmB. Portanto, MEs O/A a partir de MCT podem ser promissores sistemas de libera??o para AmB

This thesis, bearing the name "The crime of drunkenness according to § 360 of Act No. 40/2009Coll., Criminal Code" aims to analyse and understand deeper the crime of drunkenness in all its aspects. Initially, it deals with the historical kontext of this crime and the development of its conception through history to this day. The thesis also describes terms of diminished sanity and insanity as well as other terms related to the crime including the institute actio libera in causa in both of its forms. This crime is indeed an atypical one, whilst being one of the methods of dealing with illegal deeds committed by inflicted insanity. Such crime lies in the fact that the offender of an act otherwise criminal (one lacking an important sign of a crime) had, prior to such act, induced himself to a state of insanity by culpable consuming or applicating an addictive substance. Insanity as itself exclude criminal culpability of the offender, however not in cases hen offender self-inducing it by consuming or applicating an addictive substance, which makes the crime of drunkenness unique. No less interesting is that, in a way, the crime of drunkenness overcomes the principle nullum crimen sine culpa, or no crime without culpability, since it is composed of two separate actions, while culpability revers only to...