Abstract：
The formulation of microparticles composed of a mixture of carriers represents an innovative approach for lung drug delivery of dry powder. The carriers used can significantly influence the properties of the microparticles, such as size, shape, surface area, hygroscopicity, or aggregation, thus improving the aerosolization of the drugs after inhalation. The properties mentioned above are crucial for effective pulmonary therapy. The combination of carriers of a carbohydrate nature and gelling agents is advantageous for controlled drug release. The experimental work aimed to prepare by spray drying and subsequently evaluate ten batches of microparticles composed of sugar-based carriers (mannitol, maltodextrin, dextran) and gelling polymers (chitosan, chondroitin sulfate) and to select a suitable combination for follow-up experimental work aimed at drug incorporation into the microparticle matrix. The most suitable parameters were exhibited by batches whose aerodynamic diameter was close to 5 µm, particles prepared from a combination of mannitol and dextran, chitosan and chondroitin, or maltodextrin and chondroitin. These batches also showed the highest fine particle fraction value (> 43%). From a processability point of view, the batch with maltodextrin and chondroitin is preferable due to the lower viscosity of the dispersion and the more regular shape of the final microparticles.
摘要：
由载体混合物组成的微粒制剂代表了用于干粉肺部药物递送的创新方法。使用的载体可以显著影响微粒的性质，比如尺寸，形状,表面积,吸湿性,或聚合，从而改善吸入后药物的雾化。上述特性对于有效的肺部治疗至关重要。碳水化合物性质的载体和胶凝剂的组合对于控制药物释放是有利的。实验工作旨在通过喷雾干燥制备，随后评估由糖基载体（甘露醇，麦芽糊精,葡聚糖)和胶凝聚合物(壳聚糖，硫酸软骨素），并选择合适的组合用于后续实验工作，旨在将药物掺入微粒基质中。空气动力学直径接近5µm的批次表现出最合适的参数，由甘露醇和葡聚糖的组合制备的颗粒，壳聚糖和软骨素，或者麦芽糊精和软骨素.这些批次还显示出最高的细颗粒分数值(43%)。从可加工性的角度来看，由于分散体的粘度较低和最终微粒的形状更规则,优选使用麦芽糊精和软骨素的批料。
