Asthma is a chronic inflammatory condition that affects the airways, posing a substantial health threat to a large number of people worldwide. Bronchodilators effectively alleviate symptoms of airway obstruction by inducing relaxation of the smooth muscles in the airways, thereby reducing breathlessness and enhancing overall quality of life. The drug targeting to lungs poses significant challenges; however, this issue can be resolved by employing nano- and micro-particles drug delivery systems. This review provides brief insights about underlying mechanisms of asthma, including the role of several inflammatory mediators that contribute to the development and progression of this disease. This article provides an overview of the physicochemical features, pharmacokinetics, and mechanism of action of particular groups of bronchodilators, including sympathomimetics, PDE-4 inhibitors (phosphodiesterase-4 inhibitors), methylxanthines, and anticholinergics. This study presents a detailed summary of the most recent developments in incorporation of bronchodilators in nano- and micro-particle-based delivery systems which include solid lipid nanoparticles, bilosomes, novasomes, liposomes, polymeric nano- and micro-particles. Specifically, it focuses on breakthroughs in the categories of sympathomimetics, methylxanthines, PDE-4 inhibitors, and anticholinergics. These medications have the ability to specifically target alveolar macrophages, leading to a higher concentration of pharmaceuticals in the lung tissues.