The present study was an attempt to develop galactosylated albumin nanoparticles of Simvastatin for treatment of hypercholesterolemia. By developing the galactosylated nanoparticulated delivery, the required action of the drug at the target site at the liver can be provided. The advantage of targeting helps to reduce the systemic side effects that may occur due to the distribution of the drug to the other organs and thus helps in maintaining the required concentration of drug at the desired site. The galacotsylated albumin nanoparticles were prepared for the selective delivery of a Simvastatin to the 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) the rate-limiting enzyme in the pathway of cholesterol biosynthesis that is particularly presents on hepatocytes. The asialoglycoprotein receptor (ASGP-R) which is particularly presents on mammalian hepatocytes can be utilize for active targeting by using its natural and synthetic ligands. By utilizing this receptors can provides a unique means for the development of liver-specific carriers, such as liposomes, recombinant lipoproteins, and polymers for drug or gene delivery to the liver, especially to hepatocytes. These receptors recognize the ligands with terminal galactose or N-acetylgalactosamine residues, and endocytose the ligands for an intracellular degradation process. The albumin nanoparticles (NPs) were prepared by using desolvation method and efficiently conjugated with galactose. Various parameters such as particle size, zeta potential, percentage entrapment efficiency and drug loading efficiency, percentage yield, in-vitro drug release were determined. The size of nanoparticles (both plain and coated NPs) was 200 and 250 nm. The zeta potential of plain nanoparticles was -3.61 and that of galactose-coated nanoparticles was 64.1. The maximum drug content was in between 79.98% to 79.8 % respectively in plain, and galactose coated nanoparticles while the maximum entrapment efficiency was 70.10% and 71.03% in plain and coated nanoparticles. It was found that coating of nanoparticles increases the size of nanoparticles.