Over the past decades, research on nanomedicines as innovative tools in combating complex pathologies has increased tenfold, spanning fields from infectiology and ophthalmology to oncology. This process has further accelerated since the introduction of SARS-CoV-2 vaccines. When it comes to human health, nano-objects are designed to protect, transport, and improve the solubility of compounds to allow the delivery of active ingredients on their targets. Nanomedicines can be administered by different routes, such as intravenous, oral, intramuscular, or pulmonary routes. In the latter route, nanomedicines can be aerosolized or nebulized to reach the deep lung. This review summarizes existing nanomedicines proposed for inhalation administration, from their synthesis to their potential clinical use. It also outlines the respiratory organs, their structure, and particularities, with a specific emphasis on how these factors impact the administration of nanomedicines. Furthermore, the review addresses the organs accessible through pulmonary administration, along with various pathologies such as infections, genetic diseases, or cancer that can be addressed through inhaled nanotherapeutics. Finally, it examines the existing devices suitable for the aerosolization of nanomedicines and the range of nanomedicines in clinical development.