<p>The non-ergot dopamine receptor agonist known as rotigotine (RGT) marketed as NEUPRO is an efficacious remedy for the ailment known as Parkinson’s disorder. By activating the body’s natural dopamine agonists, RGT imitates the actions of the dopamine neurotransmitter. Despite its small size and unique physicochemical properties enabling it to cross the blood–brain barrier, its limited aqueous solubility and low oral bioavailability hinder its therapeutic efficacy. To address these limitations, delivering RGT via nanosystems appears to be a promising approach. This review centers its attention on the advancement of RGT nanoparticle formulation to enhance its therapeutic index by augmenting solubility, enabling direct localization to specific areas, and improving bioavailability. The feasibility of nanoformulation in delivering RGT and investigation into the chemistry, physicochemical properties, and pharmacological characteristics of RGT used to enhance therapeutic efficacy are covered in this review. The transformation of RGT into nanosized particles as a formulation could diminish the necessary therapeutic dosages and subsequently mitigate its toxicity. These nanoparticles possess the capability to deliver RGT locally to the brain. Nonetheless, the potential toxicity of nanocarriers in the context of RGT delivery represents a crucial concern that necessitates careful consideration during the nanoformulation process.</p> Graphical Abstract <p></p>