LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
INEB - Institute of Biomedical Engineering Instituto, University of Porto, 4150-180 Porto, Portugal; i3S - Institute for Research & Innovation in Health, University of Porto, 4150-180 Porto, Portugal; CESPU - Institute for Research and Advanced Training in Health Sciences and Technologies, 4585-116 Gandra, Portugal.
Carbohydr Polym. 2022 Feb 1;277:118784. doi: 10.1016/j.carbpol.2021.118784. Epub 2021 Oct 20.
Polysaccharides can be elite carriers for therapeutic molecules due to their versatility and low probability to trigger toxicity and immunogenic responses. Local and systemic therapies can be achieved through particle pulmonary delivery, a promising non-invasive alternative. Successful pulmonary delivery requires particles with appropriate flowability to reach alveoli and avoid premature clearance mechanisms. Polysaccharides can form micro-, nano-in-micro-, and large porous particles, aerogels, and hydrogels. Herein, the characteristics of polysaccharides used in drug formulations for pulmonary delivery are reviewed, providing insights into structure-function relationships. Charged polysaccharides can confer mucoadhesion, whereas the ability for specific sugar recognition may confer targeting capacity for alveolar macrophages. The method of particle preparation must be chosen considering the properties of the components and the delivery device to be utilized. The fate of polysaccharide-based carriers is dependent on enzyme-triggered hydrolytic and/or oxidative mechanisms, allowing their complete degradation and elimination through urine or reutilization of released monosaccharides.
多糖由于其多功能性和低毒性及免疫原性反应的可能性，可作为治疗分子的优秀载体。通过粒子肺部给药可以实现局部和全身治疗，这是一种很有前途的非侵入性替代方法。成功的肺部输送需要具有适当流动性的颗粒到达肺泡并避免过早的清除机制。多糖可以形成微、纳米-微和大孔颗粒、气凝胶和水凝胶。本文综述了用于肺部给药药物制剂的多糖的特性，提供了对结构-功能关系的深入了解。带电荷的多糖可以赋予粘膜粘附性，而特定糖识别的能力可能赋予对肺泡巨噬细胞的靶向能力。必须根据所使用的成分和输送装置的特性来选择颗粒制备方法。多糖载体的命运取决于酶触发的水解和/或氧化机制，允许通过尿液完全降解和消除，或通过释放的单糖再利用。
