Abstract
The water-in-water emulsion method has been reported as a technique able to prepare microparticles without using harmful solvents. However, there are few reports showing the encapsulation of small molecules into microparticles produced within this technique. The probable reason relays on the rapid diffusion of these molecules from the discontinuous phase to the continuous phase. In the present study, xylan microparticles containing mesalamine were produced and the doubled crosslinking approach, used to promote higher encapsulation rates, was disclosed. To achieve this goal, a 23 full factorial design was carried out. The results revealed that all formulations presented spherical-shaped microparticles. However, at specific conditions, only few formulations reached up to 50% of drug loading. In addition, the new xylan-based microparticles formulation retained almost 40% of its drug content after 12 h of a dissolution assay likely due to the degree of crosslinking. Thus, the doubled crosslinking approach used was effective on the encapsulation of mesalamine and may pave the way to successfully produce other polysaccharide-based carriers for clinical use.
Highlights
The preparation of microparticles based on hydrophilic polymers, such as polysaccharides derivatives, using techniques based on emulsion templates, majorly requires the use of organic solvents in order to form the hydrophilic and hydrophobic phases in which the internal hydrophilic phase contains the polymer [1,2,3]
Stenekes and Hennink, still in the 1990s, showed that the average size of the particles prepared using the water-in-water emulsion method depends on the volume ratio of the discontinuous/continuous phase, the viscosity of the solutions, and the molecular weight of the polymers [20]
The kinetic release of the 5-ASA was linked to the relaxation of the xylan chains
Summary
The preparation of microparticles based on hydrophilic polymers, such as polysaccharides derivatives, using techniques based on emulsion templates, majorly requires the use of organic solvents in order to form the hydrophilic and hydrophobic phases in which the internal hydrophilic phase contains the polymer [1,2,3]. Together with the use of crosslinkers such as glutaraldehyde and terephthaloyl chloride, the microparticles produced by this way may present an important degree of toxicity [1,4]. The use of xylan for biomedical applications is based on its important biocompatibility and selective degradation in the gastrointestinal. Sci. 2019, 9, 3519 tract, which occurs in the colon through enzymatic hydrolysis by the microbiota. Our group has lately exploited this feature in order to develop colon-specific drug delivery systems [6,7,8]
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