Pneumonia is an inflammatory condition of the lung and it is caused by infection with viruses, bacteria, parasites or fungi. As pulmonary infections are often persistent and recurrent, a rise in drug-resistant strains of infectious organisms, such as Streptococcus pneumoniae, poses great challenges in the treatment of pneumonia in the clinical practice. In order to overcome this inconvenient, a potential therapeutic approach is to target the delivery of drugs directly to the site of infection. Nanocarriers for pulmonary application have been a popular topic within the last two decades and different systems have been investigated including liposomes, polymeric micelles, dendrimers, mezoporous silica nanoparticles, nanostructured lipid carriers, micro/nanoparticles. Lung-targeted drug delivery systems can be administrated via intravenous route or via pulmonary inhalation. Lung endothelial cells have unique cell surface molecular characteristics that allow the binding of specific peptides. Antimicrobial peptides have been widely exploited for their important antimicrobial activity towards bacteria, viruses, and fungi. The preparation of biocompatible and biodegradable polymeric drug-loaded particles functionalized with two specific peptides will enhance not only the efficiency of the treatment of pulmonary infections but also will provide an experimental blueprint to development of ligand-active targeting carriers for other diseases.