Patton John S, Byron Peter R
Nektar Therapeutics, 150 Industrial Road, San Carlos, California 94070, USA.
Nat Rev Drug Discov. 2007 Jan;6(1):67-74. doi: 10.1038/nrd2153.
Remarkably, with the exception of anaesthetic gases, the ancient human practice of inhaling substances into the lungs for systemic effect has only just begun to be adopted by modern medicine. Treatment of asthma by inhaled drugs began in earnest in the 1950s, and now such 'topical' or targeted treatment with inhaled drugs is considered for treating many other lung diseases. More recently, major advances have led to increasing interest in systemic delivery of drugs by inhalation. Small molecules can be delivered with very rapid action, low metabolism and high bioavailability; and macromolecules can be delivered without injections, as highlighted by the recent approval of the first inhaled insulin product. Here, we review these advances, and discuss aspects of lung physiology and formulation composition that influence the systemic delivery of inhaled therapeutics.
值得注意的是，除了麻醉气体外，古代人类将物质吸入肺部以产生全身效应的做法直到现代医学才刚刚开始采用。吸入药物治疗哮喘始于20世纪50年代，如今这种吸入药物的“局部”或靶向治疗被考虑用于治疗许多其他肺部疾病。最近，重大进展引发了人们对通过吸入进行药物全身递送的兴趣日益浓厚。小分子可以快速起效、低代谢且生物利用度高；而大分子可以无需注射进行递送，首个吸入胰岛素产品的近期获批就凸显了这一点。在此，我们回顾这些进展，并讨论影响吸入治疗药物全身递送的肺生理学和制剂组成方面的问题。
