Nanotechnological delivery systems for the oral administration of active molecules: Polymeric microparticles and microemulsions applied to anti-inflammatory and anti-infectious drugs

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

Análise multitemporal dos elementos geoambientais da região da Ponta do Tubarão, área de influência dos campos petrolíferos de Macau e Serra, município de Macau/RN

The study area is inserted in Ponta do Tubarão region, Macau City, setentrional littoral of Rio Grande do Norte State, composed of Tertiary and Quatemary sedimentary rocks and sediments. This region is characterized for the intense action of the coastal processes, causing the morphologic instability in part of the area, beyond the interference of human activities, as the Petroliferous Industrial Polo, salt companies and shrimp farms. This justifies the integration of multidisciplinary and multitemporal detailed scientific studies dealing with the evaluation of the changing behavior of this coastal environment by geoenvironments elements characterization, identifying protected and recuperation areas, mainly those under socioeconomic intervention. The main objective was the coastal monitoring using geoprocessing techniques to prepare thematic maps useful for oil spilling environment risk areas survey. The methodology was based on multitemporal interpretation of remote sensing images and field checking, integrated in a Geographical Information System (GIS). The Geologic, Geomorphologic, Vegetation, Soil and Land Use maps were prepared, and later on they allowed the generation of the Natural Vulnerability and Environmental Vulnerability maps. These maps had been classified in accordance with vulnerability degrees: very low, low, medi um, high and very high. Beyond these maps the GIS allowed the analysis of the shoreline evolution for 10 distinct dates, using Landsat 5 TM and 7 ETM+ and SPOT-HRVIR images. This analysis made possible the attendance of the coastal morphodynamic evolution, where the results had been represented by areasof erosion and accretion (or deposition) of sediments, pointing critical areas under erosive process to the petroliferous industry (Macau and Serra fields). The GIS also provided to prepare the Environmental Sensitivity Maps of Oil Spill (SAO Maps) in operational scale (1: 10.000), according to the norms ofthe Ministério do Meio Ambiente (MMA 2002). The SAO Map in operational scale was based on IKONOS images mosaic where the ESI (Environmental Sensitivity Index) was represented according with two tides phases of theregion. Therewere recognizedfiveESI (3, 4,7,9, 1O) for the low tide; to the high tide the ESI number increased to seven (3, 4, 5, 7, 8, 9, 10). All these information are necessary to the decisions making about oi! spill and its derivatives containment. These techniques application makes possible the optimization and implantation ofnew socioeconomics activities of low environmental impact, indicates areas for better productivity and security exploration, and benefits local communities with fauna and flora preservation. The development of these activities is inserted in the scope of Monitoramento Ambiental de Áreas de Risco a Derrames de Petróleo e Seus Derivados Cooperation Project (Rede 05/01 - PETRORISCO, FINEP/CTPETRO/PETROBRAS) of multidisciplinary and interinstitucional characteristics dealing with subjects involving the environmental monitoring and the petroliferous activity