Emergence of hyperlipidemia in urban population of India and the world at large is very high and accounts to several fatal diseases. This condition is known to manifest elevated levels of lipids and/or lipoproteins. Serious limitations like inadequate solubility, less absorption, less bioavailability, ineffectiveness in lowering of cholesterol levels, patient incompliance and so on are noticed with majority of anti-hyperlipidemic drugs and dosage forms, which are used conventionally. To overcome these shortcomings, building technology platforms for development of appropriate dosage forms is the need of the hour. These efforts are required to maximize patient acceptability while maintaining safety, efficacy, accessibility and affordability. Hyperlipidemia, its types, etiology, pathophysiology and conventional dosage forms are discussed here. The current approaches and novel developments which illustrate controlled drug release and sustained therapeutic effect along with site specific and target oriented drug delivery with better patient compliance are also reviewed critically. Despite the incentives provided by the efforts of formulation scientists, there is still a need for implementation of pharmaceutical technologies that enable to combat limitations of anti-hyperlipidemic drugs and conventional dosage forms associated with it. The present review emphasize on applications of novel drug delivery systems in pharmacotherapy of anti-hyperlipidemic drugs demonstrating the advantages and disadvantages.