Leach Chet L
Lovelace Respiratory Research Institute, Albuquerque, NM 87108, USA.
Toxicol Pathol. 2007 Jan;35(1):23-6. doi: 10.1080/01926230601072335.
The pulmonary route of drug delivery can provide an excellent alternative to other routes both for local lung disease as well as systemic delivery. The year 2006 marks the 50th year since the invention of metered dose inhalers, yet inhalation is a very much underutilized route of delivery, possibly because inhalation drug development is perceived as being too difficult and expensive. However with proper knowledge these purported difficulties can be overcome. The process begins with identifying the target tissue and then utilizing technologies such as particle size adjustments through formulation techniques and delivery devices to most efficiently deliver the desired dose. There are a variety of new and existing inhaled excipients available to accomplish this goal. The active molecule can also be modified to increase solubility, decrease immunogenicity, and protect it from unwanted metabolism using PEGylation. Sustained release of an inhaled drug is also possible using biocompatible matrices such as oligolactic acid.
药物递送的肺部途径对于局部肺部疾病以及全身给药而言，都是一种优于其他途径的极佳选择。2006年是定量吸入器发明50周年，但吸入给药途径的利用程度仍很低，这可能是因为吸入药物研发被认为难度太大且成本太高。然而，掌握适当的知识，这些所谓的困难是可以克服的。这个过程始于确定靶组织，然后利用诸如通过制剂技术和给药装置调整颗粒大小等技术，最有效地递送所需剂量。有多种新的和现有的吸入用辅料可用于实现这一目标。活性分子也可以进行修饰，通过聚乙二醇化来增加溶解度、降低免疫原性并保护其免受不必要的代谢。使用生物相容性基质如低聚乳酸，吸入药物的缓释也是可能的。
