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Previous issue date: 2017-05-31 / ?, ? amirina (ABAM) ? uma mistura natural de triterpenos pentac?clicos que possui v?rias atividades biol?gicas, incluindo o efeito anti-inflamat?rio. ? isolada das esp?cies da fam?lia Burseraceae, nas quais a esp?cie Protium heptaphyllum ? a esp?cie mais comumente encontrada na Amaz?nia brasileira. A forma??o de complexo de inclus?o (CI) com a ciclodextrina (CD) e dispers?es s?lidas (DS) com pol?meros hidrof?licos t?m sido aplicadas como alternativas para resolver algumas limita??es que novas entidades qu?micas (NEQ) t?m em comum, principalmente a baixa solubilidade em meios aquosos. Ent?o, o objetivo deste trabalho foi desenvolver CI?s da ABAM (ABAM) com a ?-ciclodextrina (?CD) e com a hidroxipropil-?-ciclodextrina (HP?CD) e DS com a hidroximetilcelulose (HPMC), polietilenoglicol (PEG 6000) e a polivinilpirrolidona (PVP k-30) a fim de melhoras suas propriedades f?sico-qu?mica para torna-la vi?vel numa futura formula??o. Inicialmente, para os CI, foram realizados estudos te?ricos computacionais nos quais foram calculadas as energias de intera??o entre a ?CD e a ABAM e HP?CD e ABAM. Em seguida, foram desenvolvidos os CI?s com ?CD e HP?CD pelos m?todos de mistura f?sica (MF) e malaxagem (MAL). Foi realizada a caracteriza??o f?sico-qu?mica dos CI atrav?s de espectroscopia de infravermelho com transformada Fourier (FTIR), microscopia eletr?nica de varredura (MEV), difra??o de raio-X de p? (DRX), an?lise termogravim?trica (ATG) e calorimetria explorat?ria diferencial (DSC). As DS foram obtidas atrav?s da MF, MAL e RE com o HPMC, PEG e o PVP. Foram utilizadas as mesmas t?cnicas de caracteriza??o que foram realizadas para os CI. Al?m da caracteriza??o para as DS, realizou-se a atividade anti-inflamat?ria in vitro e foram comparadas em rela??o ? suas atividades anti-inflamat?rias com a ABAM. Os estudos de caracteriza??o mostraram a forma??o de CI entre a ABAM e as CD e a forma??o de dispers?es s?lidas entre a ABAM e os pol?meros hidrof?licos. No ensaio de atividade das DS, verificou-se que comparando o efeito, mesma dose da ABAM e mesma dose da DS, tanto as DS quanto a ABAM tiveram atividade anti-inflamat?ria sobre macr?fagos ativados por LPS. Portanto, as DS e CI com ABAM s?o alternativas eficazes para modificar suas caracter?sticas, melhorando propriedades que possam interferir numa futura formula??o terap?utica. / ?, ? amyrin (ABAM) is a natural mixture of triterpenes pentacyclis which has various biological activities, including the anti-inflammatory effect. Are isolated from the species in the family Burseraceae, in which the species Protium heptaphyllum is more commonly found in the brazilian Amazon. The inclusion complexes formation (IC) with the cyclodextrin (CD) and solid dispersions (SD) with hydrophilic polymers have been applied as alternatives to solve some limitations that new chemical entities (NCE) have in common, mainly the low solubility in aqueous environments. So, the objective of this work was to develop IC's the ABAM (ABAM) with ?-cyclodextrin (?CD) and hydroxypropyl-?-cyclodextrin (HP?CD) and SD with the hidroximetilcelulose (HPMC), polyethylene glycol (PEG 6000) and polyvinylpyrrolidone (PVP-30 k). Initially, for the IC, computational theoretical studies were carried out in which interaction energies were calculated between the ?CD and the ABAM and HP?CD and ABAM. Then, the IC's have been developed with ?CD and HP?CD by mixing physical methods (MF) and kneading (KND). The physical and chemical characterization of IC's using Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), x-ray diffraction (DRX), thermogravimetric analysis (TG) and differential scanning calorimetry (DSC). The DS were obtained through the MF, KND and RE with HPMC, PEG and the PVP. Held the same characterization techniques that were held for the IC. Beyond characterization to the DS, the anti-inflammatory activity in vitro and were compared with respect to their anti-inflammatory activities with the ABAM. The characterization studies showed the formation of CI between the ABAM and the CD and the formation of solid dispersions between the ABAM and hydrophilic polymers. In the activity of DS, it was found that comparing the effect, the same dose of ABAM and same dose of the DS, the DS as the ABAM had anti-inflammatory activity on macrophages activated by LPS. Therefore, the DS and CI with ABAM are effective alternatives to modify their characteristics, improving properties that may interfere in a future therapeutic formulation.
| Identifer | oai:union.ndltd.org:IBICT/oai:repositorio.ufrn.br:123456789/23709 |
| Date | 31 May 2017 |
| Creators | Silva J?nior, Walter Ferreira da |
| Contributors | 99328976472, http://lattes.cnpq.br/4061809277935577, Damasceno, Bolivar Ponciano Goulart de Lima, 91616751487, http://lattes.cnpq.br/6407334157973308, Veiga J?nior, Valdir Florencio da, 01872867790, http://lattes.cnpq.br/0581412073128121, Lima, Adley Antonini Neves de |
| Publisher | PROGRAMA DE P?S-GRADUA??O EM CI?NCIAS FARMAC?UTICAS, UFRN, Brasil |
| Source Sets | IBICT Brazilian ETDs |
| Language | Portuguese |
| Detected Language | English |
| Type | info:eu-repo/semantics/publishedVersion, info:eu-repo/semantics/masterThesis |
| Source | reponame:Repositório Institucional da UFRN, instname:Universidade Federal do Rio Grande do Norte, instacron:UFRN |
| Rights | info:eu-repo/semantics/openAccess |
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