Statins therapy: a review on conventional and novel formulation approaches

Abstract

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.

Tissue Engineered Bio‐Blood‐Vessels Constructed Using a Tissue‐Specific Bioink and 3D Coaxial Cell Printing Technique: A Novel Therapy for Ischemic Disease

“…Some studies have demonstrated microparticles prepared by polyhydroxy acid (e.g., polycaprolactone, polyglycolide, or PLGA) can prolong the release of encapsulated drugs over a month. [13] When exposed to the in vivo conditions, the autocatalytic effect of accumulated acidic products can facilitate the degradation of PLGA, and thus enables and promotes the release of atorvastatin to surroundings. [14] APMS were obtained through an oil/water emulsion solvent evaporation method, which allows us to approximately control the average diameter of microspheres at 10, 50, and 100 µm by adjusting the power of the homogenizer at 15 000, 7000, and 3000 rpm, respectively ( Figure S3, Supporting Information).…”

Rosuvastatin calcium-loaded Solid Lipid Nanoparticles (SLN) using design of experiment approach for oral delivery

“…This can also increase the risk of heart disease, stroke, and other vascular diseases [1]. In this regard, statin drugs are most commonly prescribed to reduce endogenous synthesis of these lipids (cholesterol and triglycerides) and prevent the onset and development of atherosclerosis [2]. Rosuvastatin Calcium (Rst) is a semi-synthetic lipid lowering statin that inhibits HMG-CoA (3-hydroxy3-methyl glutaryl CoA) reductase, which plays a central role in the synthesis of cholesterol [3].…”

Coamorphous Atorvastatin Calcium to Improve its Physicochemical and Pharmacokinetic Properties

“…Statins are a class of cholesterol lowering drugs which have low dissolution rate and bioavailability, warranting the preparation of novel formulations (18). Atorvastatin calcium (ATC), one of the world's top-selling, has an absolute oral bioavailability of 12% (% F) from an oral dosage form.…”

“…Atorvastatin calcium (ATC), one of the world's top-selling, has an absolute oral bioavailability of 12% (% F) from an oral dosage form. In addition, solubilization of ATC is necessary to produce novel formulations of ATC (18).…”