Novel chitosan microsphere-templated microcapsules suitable for spontaneous loading of heparin

Abstract This report aimed to describe a novel type of core–shell-structured microcapsules suitable for spontaneous loading of anticoagulant heparin. Chitosan (CS) microspheres were fabricated by a sodium sulfate-based precipitation process. The microspheres were approximately 1 μm in size and applied as templates for microcapsules prepared by the layer-by-layer (LbL) self-assembly technique. Polyelectrolytes including polyanion poly(styrene sulfonate) and polycation CS were alternately deposited on CS microsphere templates, monitored by flow cytometry and zeta potential analysis. Scanning electron microscopy, confocal laser scanning microscopy, fluorescence microscopy, flow cytometry and laser particle size analysis were used to characterize the microcapsules. The resulted microcapsules were about 1 μm in average diameter, and allowed spontaneous loading of heparin through electrostatic interaction, with the encapsulation efficiency and loading capacity of 74.4% and 10.0%, respectively. Moreover, heparin could be released from the microcapsules in phosphate buffered saline at pH 7.4. It is suggested that the type of microcapsules may provide a new and effective system of heparin delivery for pharmaceutical use.