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Application of nanotechnology to improve the therapeutic benefits of statins

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DRUG DISCOVERY TODAY
卷 24, 期 2, 页码 567-574

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ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2018.09.023

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Hyperlipidemia is defined as an elevated level of lipids and lipoproteins in the blood and is considered to be a significant risk factor for accelerating the process of atherosclerosis and, consequently, cardiovascular disease. The level of cholesterol, especially low-density lipoprotein cholesterol (LDL-C), is commonly elevated in hyperlipidemia and represents the primary therapeutic target. Statins are a group of drugs that function by inhibiting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and are extremely efficacious in reducing elevated LDL-C in the serum and preventing atherosclerotic cardiovascular disease. However, statins have some limitations, such as poor aqueous solubility, low oral absorption, and, consequently, limited bioavailability when administered by the oral route. The field of nanotechnology is now well developed and some of these newer nanotechnology strategies offer systems with enhanced aqueous solubility of the statin, increased absorption, bioavailability, and controlled release of the statin at the site of administration. Here, we discuss nano-sized drug delivery systems to enhance the therapeutic potential of statins.

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