Statins therapy: a review on conventional and novel formulation approaches

BACKGROUND AND OBJECTIVE: High levels of cholesterol lead to atherosclerosis, a factor predisposing to the development of coronary artery disease. Statin drugs, i.e. HMG-CoA reductase inhibitors, have been known since the end of the last century for their benefits against cardio- and cerebrovascular diseases and are widely used clinically. This review aims at compiling the research inputs being made for developing therapeutically efficacious dosage forms that have the potential to surmount the limitations of conventional dosage forms of statins. KEY FINDINGS: Statin drugs can reduce the endogenous synthesis of cholesterol and prevent the onset and development of atherosclerosis, and are therefore used as an effective treatment against primary hypercholesterolemia. At present, statin drugs are most often administered orally, on a daily basis. After administration, the bioavailability and the general circulation of statin drugs is fairly low due to the first-pass metabolism in the liver and clearance by the digestive system. Extensive pharmaceutical research in understanding the causes of low oral bioavailability has led to the development of novel technologies to address these challenges. SUMMARY: These technologies vary from conventional dosage forms to nanoparticulate drug-delivery systems, and have the potential to cause improvements in bioavailability and consequently therapeutic efficacy.