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Obesity and dyslipidemia are the main features of metabolic syndrome, expressed mainly by adipose tissue dysfunction and connected by similar pathways and pharmacotherapy. Conventional drugs used in these two associated disorders are limited due to poor drug efficiency, non-specificity, and toxic side effects. Therefore, novel solutions for tackling obesity-associated diseases and providing insights into the development of innovative or improved therapies are necessary. Targeted nanotherapy is a revolutionary technology, offering a promising solution for combatting the disadvantages of currently available therapies for treating obesity and dyslipidemia due to its superior features, which include specific cell targeting, the protection of drugs against physiological degradation, and sustained drug release. This review presents a brief assessment of obesity and dyslipidemia, their impacts on human health, current treatment, and limitations, and the role and potential use of nanotechnology coupled with targeted drug delivery and nutraceuticals as emerging therapies. To the best of our knowledge, this paper presents, for the first time in the literature, a comparison between obesity and dyslipidemia nano-formulations based on drugs and/or natural extracts applied in experimental studies.