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.