Ray Animikh, Mandal Abhirup, Mitra Ashim K
University of Missouri Curators' Professor of Pharmacy, Chair, Division of Pharmaceutical Sciences, Vice-Provost for Interdisciplinary Research, University of Missouri-Kansas City, USA.
Recent Pat Drug Deliv Formul. 2015;9(3):225-36. doi: 10.2174/1872211309666150729122231.
Pulmonary delivery is a non-invasive form of delivery that holds tremendous therapeutic promise for topical and systemic administration of several macromolecules. Oral administration of macromolecules has several limitations such as low bioavailability, degradation of drug before reaching circulation and insufficient absorption across intestinal membrane. Administration of macromolecules such as proteins, peptides and nucleic acids via inhalation offers great potential due to the avoidance of first pass metabolism, higher surface area and rapid clinical response. However, delivery of reproducible, uniform and safe doses of inhaled particles remains a major challenge for clinical translation. Recent advances in the fields of biotechnology and particle engineering led to progress in novel pulmonary drug delivery systems. Moreover, significant developments in carriers and delivery devices prevent denaturation of macromolecules and control their release within the lungs. This article reviews the advances in pulmonary drug delivery systems by focusing on the recent patents in delivery of macromolecules. Furthermore, recent patents in gene delivery to the lungs have also been discussed. List of patents included in this review is comprehensive in terms of pulmonary delivery of therapeutics. It includes inventions related to proteins and peptides, DNA therapeutics, siRNA and other genetic materials with therapeutic applications. The diseases targeted by these therapeutic molecules are varied including but not limited to different forms of cancer, respiratory diseases etc.
肺部给药是一种非侵入性给药方式，对于多种大分子药物的局部和全身给药具有巨大的治疗前景。口服大分子药物存在诸多局限性，如生物利用度低、药物在到达循环系统之前降解以及跨肠膜吸收不足等。通过吸入方式给药蛋白质、肽和核酸等大分子药物具有很大潜力，因为可避免首过代谢、具有更大的表面积且临床反应迅速。然而，实现可重复、均匀且安全剂量的吸入颗粒给药仍是临床转化面临的主要挑战。生物技术和颗粒工程领域的最新进展推动了新型肺部药物递送系统的发展。此外，载体和递送装置的重大进展可防止大分子药物变性并控制其在肺部的释放。本文通过聚焦大分子药物递送的近期专利，综述了肺部药物递送系统的进展。此外，还讨论了肺部基因递送的近期专利。本综述中包含的专利列表在治疗性肺部给药方面较为全面。它包括与蛋白质和肽、DNA治疗药物、小干扰RNA（siRNA）以及其他具有治疗应用的遗传物质相关的发明。这些治疗分子所针对的疾病多种多样，包括但不限于不同形式的癌症、呼吸系统疾病等。
