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Application of nanotechnology to improve the therapeutic benefits of statins
Drug Discovery Today ( IF 7.4 ) Pub Date : 2018-10-05 , DOI: 10.1016/j.drudis.2018.09.023
Shahla Korani , Mitra Korani , Samira Bahrami , Thomas P. Johnston , Alexandra E . Butler , Maciej Banach , Amirhossein Sahebkar

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.



中文翻译:

纳米技术改善他汀类药物的治疗作用

高脂血症被定义为血液中脂质和脂蛋白水平的升高,被认为是加速动脉粥样硬化以及心血管疾病进程的重要危险因素。胆固醇,尤其是低密度脂蛋白胆固醇(LDL-C)的水平通常在高脂血症中升高,并且代表了主要的治疗靶点。他汀类药物是一组通过抑制3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶起作用的药物,在减少血清中升高的LDL-C和预防动脉粥样硬化性心血管疾病方面极为有效。但是,他汀类药物具有一些局限性,例如水溶性差,口服吸收低,因此通过口服途径给药时生物利用度有限。纳米技术领域现已发展成熟,其中一些较新的纳米技术策略为他汀类药物的水溶性增加,吸收,生物利用度提高以及他汀类药物在给药部位的受控释放提供了系统。在这里,我们讨论了纳米尺寸的药物输送系统,以增强他汀类药物的治疗潜力。

更新日期:2018-10-05
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