Following COVID-19, people’s lives have altered significantly, with people spending less time exercising and more time on electronic devices. Furthermore, urbanization and globalization have changed lifestyles, leading to the emergence of several lifestyle disorders that are generally referred to as metabolic syndrome (MetS). Diabetes, glucose intolerance, insulin resistance, dyslipidemia, obesity, non-alcoholic fatty liver disease (NAFLD), hypertension, and other metabolic abnormalities are hallmarks of metabolic syndrome, which predisposes people to cardiovascular and neurological disorders. The pathophysiological causes of metabolic syndrome are widely understood. However, a few drawbacks, including limited effectiveness, low bioavailability, lack of target selectivity, and dose-dependent adverse effects, make the currently available medicines ineffective. Fresh hope in the fight against metabolic syndrome is provided by targeted nanotherapy. Nanomaterials are constantly changing, and efficient drug delivery strategies that manage the intricate relationships between molecules and technology guarantee medication safety, effectiveness, and targeting. A few nano-drug delivery systems have been developed for bioactive substances, including liposomes, hydrogel nanocomposites, nanomicelles, nanoemulsions, core-shell nanoparticles, and metallic nanoparticles. Bioactive substances’ nano-encapsulation has transformed the clinical and pharmaceutical sectors and aided in the creation of innovative treatments for metabolic syndrome and related conditions like Alzheimer’s disease. Metabolic syndrome may be diagnosed and treated with carbon nanoparticles. In those with metabolic syndrome, it can be utilized as a nanosensor to monitor blood pressure, blood glucose levels, and dyslipidemia. Nanozymes can be tailored in such a way as to enhance their catalytic efficiency, targeting ability, and ability to eliminate ROS and alleviate oxidative stress, thereby promising potential for preventing metabolic syndrome and improving treatment efficacy. The major challenges for nanomaterials used for drug delivery systems are their optimization to check their cellular uptake and/or targeting the desired tissue without any side effects. This chapter briefly assesses metabolic syndrome, and the potential use of nanomaterial coupled with targeted drug delivery of bioactive compounds as emerging therapies and challenges.