Abstract: Disorders in lipid metabolism are one of the key mechanisms driving the development of metabolic syndrome such as obesity, diabetes, and atherosclerosis. Recent studies have shown that drug targeting to critical steps in lipid metabolism demonstrated potentially enhanced therapeutic efficacy compared to conventional therapies. This review article first briefly summarizes the lipid metabolism pathway targets associated with metabolic syndrome. Subsequently, we systematically elaborate on emerging targeted delivery strategies directed toward active sites of lipid metabolism such as the liver, adipose tissue, macrophages, and atherosclerotic plaques. The article aims to provide insights developing safer and more effective new therapies against metabolic diseases.