Overactive bladder syndrome (OAB) is characterised by urgency symptoms, with or without urgency incontinence, usually with frequency and nocturia and severely affects the quality of life. This systematic review evaluates the various drug delivery strategies used in practice to manage OAB. Advanced drug delivery strategies alongside traditional strategies were comprehensively analysed and comparatively evaluated. The present review was conducted according to the preferred reporting items for systematic reviews and meta-analyses guidelines. A total of 24 studies reporting the development of novel formulations for the treatment of OAB were considered eligible and were further categorised according to the route of drug administration. The review found that various drug delivery routes (transdermal, intravesicular, oral, vaginal and intramuscular) are used for the administration of drugs for managing OAB, however, the outcomes illustrated the marked potential of transdermal drug delivery route. The findings of the current review are expected to be helpful for pharmaceutical scientists to better comprehend the existing literature and challenges and is anticipated to provide a basis for designing and fabricating novel drug delivery systems to manage OAB.