University of Bonn, Institute of Pharmacy, Laboratory of Pharmaceutical Technology and Biopharmaceutics , Bonn , Germany
Expert Opin Drug Deliv. 2015 Jun;12(6):929-45. doi: 10.1517/17425247.2015.993968. Epub 2014 Dec 23.
Respiratory infections and diseases are accompanied by or exhibit inflammation. Recent advances in nanoparticle engineering technology, together with the increased knowledge of inflammatory pathophysiology, have ignited interest in the pulmonary delivery of anti-inflammatory agents (AIAs) to achieve local treatment of pulmonary inflammatory disorders.
This review summarizes and discusses the investigated formulation approaches for the pulmonary delivery of AIAs, including: inhalation of actives as suspensions or dry powder formulations, with polymeric micro- and nano-delivery carriers, or within liposomes and lipid nanoparticles. Some recent approaches for targeting AIAs to the pulmonary endothelium have also been reviewed. The discussion focuses on finding out whether the investigated approaches were really able to achieve lung targeting and reduce the side effects associated with the systemic administration of AIAs.
The use of the inhalation route for the pulmonary delivery of AIAs is facing several challenges. Some of the investigated formulation approaches appear to be promising in overcoming these challenges. However, in order to create products that reach patients, more therapeutically oriented studies are still needed to ensure formulation stability, in-vivo sustained release behavior, pulmonary retention, and bypassing lung clearance mechanisms.
呼吸道感染和疾病伴随着或表现出炎症。纳米颗粒工程技术的最新进展，以及对炎症病理生理学认识的提高，激发了人们对将抗炎剂（AIAs）肺部递送来实现肺部炎症性疾病局部治疗的兴趣。
本综述总结和讨论了用于肺部递送 AIAs 的研究制剂方法，包括：将活性物质作为混悬剂或干粉制剂吸入，使用聚合物微载体和纳米载体，或在脂质体和脂纳米粒内。还综述了一些最近针对肺部内皮细胞靶向 AIAs 的方法。讨论的重点是确定所研究的方法是否真的能够实现肺部靶向并减少与全身给予 AIAs 相关的副作用。
使用吸入途径肺部递送 AIAs 面临着一些挑战。一些研究的制剂方法似乎有希望克服这些挑战。然而，为了开发出能惠及患者的产品，仍需要进行更多以治疗为导向的研究，以确保制剂的稳定性、体内持续释放行为、肺部保留和绕过肺部清除机制。
