Desenvolvimento de uma formulação cólon específica visando o tratamento da colite ulcerativa

Micro and nanoparticulate systems as drug delivery carriers have achieved successful therapeutic use by enhancing efficacy and reducing toxicity of potent drugs. The improvement of pharmaceutical grade polymers has allowed the development of such therapeutic systems. Microencapsulation is a process in which very thin coatings of inert natural or synthetic polymeric materials are deposited around microsized particles of solids or around droplets. Products thus formed are known as microparticles. Xylan is a natural polymer abundantly found in nature. It is the most common hemicellulose, representing more than 60% of the polysaccharides existing in the cell walls of corn cobs, and is normally degraded by the bacterial enzymes present in the colon of the human body. Therefore, this polymer is an eligible material to produce colon-specific drug carriers. The aim of this study was to evaluate the technological potential of xylan for the development of colon delivery systems for the treatment of inflammatory bowel diseases. First, coacervation was evaluated as a feasible method to produce xylan microcapsules. Afterwards, interfacial cross-linking polymerization was studied as a method to produce microcapsules with hydrophilic core. Additionally, magnetic xylan-coated microcapsules were prepared in order to investigate the ability of producing gastroresistant systems. Besides, the influence of the external phase composition on the production and mean diameter of microcapsules produced by interfacial cross-linking polymerization was investigated. Also, technological properties of xylan were determined in order to predict its possible application in other pharmaceutical dosage forms

Obtenção e caracterização de extrato microencapsulado de resíduo agroindustrial de acerola

Acerola (Malpighia emarginata D.C.) is a red fruit widely cultivated in Brazil, especially in the Northeastern region. Its increasing demand is attributed to its high ascorbic acid contents. Besides ascorbic acid, widely known by its health-benefit effects, acerola is rich in anthocyanins, which contribute for the antioxidant power of the fruit. Acerola processing produces a bright-red pomace, usually discarded. The further processing of this pomace, in order to explore its antioxidant compounds, could enhance acerola market value and rentability of its processing. Both ascorbic acid and anthocyanins are highly susceptible to degradation, that can be delayed by microencapsulation, which consists on packing particles (core) in an edible matrix (wall material). This work has been made with the purpose of producing a microencapsulated acerola pomace extract, which could be used by the food industry as a functional ingredient with antioxidant and coloring properties. Antioxidant compounds were recovered by pressing the pomace diluted in a solvent (a citric acid aqueous solution), by using a central composite design, with two variables: citric acid concentration in the solvent (0-2%), and solvent: pomace mass ratio (2:1-6:1). The acerola pomace extract was then microencapsulated by spray drying. A central composite design was adopted, with three variables: inlet temperature of the spray dryer (170o-200oC), wall material: acerola solids mass ratio (2:1-5:1), and degree of maltodextrin replacement by cashew tree gum as wall material (0-100%). The cashew tree gum was used because of its similarity to arabic gum, which is regarded as the wall material by excellence. The following conditions were considered as optimal for extraction of anthocyanins and ascorbic acid: solvent/pomace ratio, 5:1, and no citric acid in the solvent. 82.47% of the anthocyanins were recovered, as well as 83.22% of the ascorbic acid. Anthocyanin and ascorbic acid retentions were favored by lower inlet temperatures, higher wall material: acerola solids mass ratio and higher maltodextrin replacement by cashew tree gum, which was presented as a promising wall material. The more adequate microencapsulation conditions, based not only on retention of antioxidant compounds but also on physical properties of the final powder, were the following: inlet temperature, 185oC; wall material: acerola solids mass ratio, 5:1, and minimum degree of maltodextrin replacement by cashew tree gum, 50%

Desenvolvimento de sistemas micro e nanoestruturados de quitosana/MDI para aplicações cosméticas

Currently, studies in the area of polymeric microcapsules and nanocapsules and controlled release are considerably advanced. This work aims the study and development of microcapsules and nanocapsules from Chitosan/MDI, using a new technique of interfacial polycondensation combined to spontaneous emulsification, for encapsulation of BZ-3. It was firstly elaborated an experimental design of 23 of the particle in white without the presence of BZ-3 and Miglyol, where the variables were the concentrations of MDI, chitosan and solvent. Starting from the data supplied by the experimental design was chosen the experiment with smaller particle diameter and only added like this BZ-3 and Miglyol. The suspension containing concentrations of 6.25 mg/mL, 12.5 mg/mL, 18.75 mg/mL, 25 mg/mL of BZ-3 were prepared, nevertheless, during the storage time, these formulations presented drug precipitates in the suspensions of 18.75 mg/mL and 25 mg/mL of BZ-3. This apparition of precipitate was attributed to the diffusion of BZ-3 for the aqueous phase without any encapsulation, suggesting so the use of the smaller concentrations of the BZ-3. The suspension containing 6.25mg/mL of BZ3 presented average size of 1.47μm, zeta potential of 61 mV, pH 5.64 and this sample showed an amount of BZ-3 and drug entrapment of 100 %. The suspension containing 12.5mg/mL of BZ-3 presented average size of 1.76μm, zeta potential of 47.4 mV, pH 5.71 and this sample showed an amount of BZ-3 and drug entrapment of 100 %. Then, showing such important characteristics, these two formulations were chosen for futher continuity to the study. These formulations were also characterized by the morphology, FTIR, stability for Turbiscan, DSC and a study of controlled release of the BZ-3 was elaborated in different receiving means

Desenvolvimento de microcápsulas contendo as antocianinas presentes no corante do extrato do jambo por polimerização interfacial

The industries of food, medicine and cosmetic apply microencapsulation for many reasons, among them, stabilize the active, control the release of encapsulated and separate incompatible components of the formulation. In this context, microencapsulation techniques have been used in the food industry to provide stable liquid and solid ingredients. Anthocyanins have high antioxidant potential, but they are photodegradable. The challenges are therefore directed to the research for techniques that could make this potential remaining active and bioavailable and could be used as a vehicle for the delivery release of bioactive and micronutrients in appropriate conditions and levels. This work has as main objective to propose a method to encapsulate the anthocyanins in the extract of mountain apple using the interfacial polymerization technique. As well as to define the ideal conditions of temperature and agitation system for this procedure. The microparticles were characterized for size, morphology, active distribution, surface charge, degradation, composition and stability. The results, like particle diameter of 5.94 μm and Zeta potential of 7.03 mV, showed that the technique used to obtain these microparticles was satisfactory and has potential for application in cosmetics and food