Maloney Norcross Sara E, Levin Leanna P K, Hickey Anthony J, Hill David B
Technology Advancement and Commercialization, RTI International, Research Triangle Park, Durham, NC 27709, USA.
Joint Department of Biomedical Engineering, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Pharmaceuticals (Basel). 2024 Dec 4;17(12):1628. doi: 10.3390/ph17121628.
Natural and synthetic biopolymers are gaining popularity in the development of inhaled drug formulations. Their highly tunable properties and ability to sustain drug release allow for the incorporation of attributes not achieved in dry powder inhaler formulations composed only of micronized drugs, standard excipients, and/or carriers. There are multiple physiological barriers to the penetration of inhaled drugs to the epithelial surface, such as the periciliary layer mucus mesh, pulmonary macrophages, and inflammation and mucus compositional changes resulting from respiratory diseases. Biopolymers may facilitate transport to the epithelial surface despite such barriers. A variety of categories of biopolymers have been assessed for their potential in inhaled drug formulations throughout the research literature, ranging from natural biopolymers (e.g., chitosan, alginate, hyaluronic acid) to those synthesized in a laboratory setting (e.g., polycaprolactone, poly(lactic-co-glycolic acid)) with varying structures and compositions. To date, no biopolymers have been approved as a commercial dry powder inhaler product. However, advances may be possible in the treatment of respiratory diseases and infections upon further investigation and evaluation. Herein, this review will provide a thorough foundation of reported research utilizing biopolymers in dry powder inhaler formulations. Furthermore, insight and considerations for the future development of dry powder formulations will be proposed.
天然和合成生物聚合物在吸入药物制剂的开发中越来越受到关注。它们具有高度可调节的特性以及维持药物释放的能力，使得仅由微粉化药物、标准辅料和/或载体组成的干粉吸入剂制剂无法实现的特性得以融入。吸入药物穿透到上皮表面存在多种生理屏障，如纤毛周围层黏液网、肺巨噬细胞以及呼吸系统疾病导致的炎症和黏液成分变化。尽管存在这些屏障，生物聚合物仍可能促进药物向 上皮表面的转运。在整个研究文献中，已经评估了各种类别的生物聚合物在吸入药物制剂中的潜力，从天然生物聚合物（如壳聚糖、藻酸盐、透明质酸）到在实验室环境中合成的（如聚己内酯、聚（乳酸 - 乙醇酸）），其结构和组成各不相同。迄今为止，尚无生物聚合物被批准作为商业干粉吸入剂产品。然而，经过进一步的研究和评估，在治疗呼吸系统疾病和感染方面可能会取得进展。在此，本综述将为在干粉吸入剂制剂中使用生物聚合物的已报道研究提供全面的基础。此外，还将对干粉制剂的未来发展提出见解和考虑因素。
