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可吸入微粒作为干粉制剂中肺部给药系统。

Inhalable microparticles as drug delivery systems to the lungs in a dry powder formulations.

作者信息

Knap Karolina, Kwiecień Konrad, Reczyńska-Kolman Katarzyna, Pamuła Elżbieta

机构信息

Department of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, 30-059 Krakow, Poland.

出版信息

Regen Biomater. 2022 Dec 8;10:rbac099. doi: 10.1093/rb/rbac099. eCollection 2023.

Abstract

Inhalation-administrated drugs remain an interesting possibility of addressing pulmonary diseases. Direct drug delivery to the lungs allows one to obtain high concentration in the site of action with limited systemic distribution, leading to a more effective therapy with reduced required doses and side effects. On the other hand, there are several difficulties in obtaining a formulation that would meet all the criteria related to physicochemical, aerodynamic and biological properties, which is the reason why only very few of the investigated systems can reach the clinical trial phase and proceed to everyday use as a result. Therefore, we focused on powders consisting of polysaccharides, lipids, proteins or natural and synthetic polymers in the form of microparticles that are delivered by inhalation to the lungs as drug carriers. We summarized the most common trends in research today to provide the best dry powders in the right fraction for inhalation that would be able to release the drug before being removed by natural mechanisms. This review article addresses the most common manufacturing methods with novel modifications, pros and cons of different materials, drug loading capacities with release profiles, and biological properties such as cytocompatibility, bactericidal or anticancer properties.

摘要

吸入给药仍然是治疗肺部疾病的一个有吸引力的选择。将药物直接输送到肺部可以在全身分布有限的情况下在作用部位获得高浓度,从而以更低的所需剂量和更少的副作用实现更有效的治疗。另一方面,要获得一种符合所有与物理化学、空气动力学和生物学性质相关标准的制剂存在诸多困难,这就是为什么只有极少数被研究的系统能够进入临床试验阶段并最终投入日常使用的原因。因此,我们专注于由多糖、脂质、蛋白质或天然及合成聚合物组成的微粒形式的粉末,这些粉末作为药物载体通过吸入输送到肺部。我们总结了当今研究中最常见的趋势,以提供最适合吸入的正确粒度的最佳干粉,使其能够在被自然机制清除之前释放药物。这篇综述文章探讨了最常见的制造方法及其新颖改进、不同材料的优缺点、具有释放曲线的载药量以及生物学性质,如细胞相容性、杀菌或抗癌特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a80/9845529/3cb7ab87827f/rbac099f13.jpg

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