The inhalation route, employed primarily for drugs acting in the respiratory tract, is now being expanded for use in systemic drug delivery. A properly designed drug delivery system utilizing the inhalation route can help overcome many of the hurdles associated with conventional therapies: difficult formulation, poor bioavailability, poor patient compliance, and of course, first pass issues. For example, most protein drugs are difficult to deliver through conventional delivery systems because they degrade, either partially or completely, before they reach their therapeutic target. Avoiding the digestive tract not only increases the deliverable therapeutic dose, but also lowers the risk of unintended adverse events such as irritation of the GI tract. Furthermore, by delivering drugs via nanoparticles, one is able to increase the surface-areato-volume ratio, effectively augmenting the drug’s bioavailability through faster dissolution and release rates.