Biopharmaceuticals including recombinant proteins, monoclonal antibody and nucleic acid based therapeutics have become more and more important to improve the quality of life of patients. However, the administration of biopharmaceuticals was mainly limited to parenteral routes and their delivery remains the most significant challeng to their clinical adoption due to their unfavorable intrinsic physicochemical properties. Among noninvasive administration routes the lung has been attempted intensively to be an alternative to injection to deliver the biopharmaceuticals, and has shown to be promising. In this review we discussed the formulation strategies and particle engineering technologies to improve the efficiency of pulmonary delivery of biopharmaceutical, with a focus on systemic therapy of pharmaceutical proteins/peptides and local delivery of siRNA via the lung administration.