Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, are a well-known class of drug with beneficial therapeutic effects in cardiovascular disease and lipid disorders and have potential use against cancer. However, the bioavailability of statins is hampered due to low aqueous solubility and rapid metabolism. To improve pharmacokinetic profiles of statins, development of drug delivery systems is promising. Hence, the use of liposomes for selective delivery of statins to a selected site or for bioavailability enhancement is an effective strategy to increase statin therapeutic effects. Moreover, liposomal delivery can reduce the required dose of statins especially in terms of antitumor effects. Liposomes, because of their unique properties and biphasic and amphiphilic nature, have attracted much interest and can be considered as a suitable choice for delivery of both hydrophilic and lipophilic statins. In this review article, we focus on liposomes and evaluate the effects of different liposomal delivery systems, based on differences in size, phospholipid composition, circulation half-life, and cholesterol content, on statin function.

译文

他汀类药物是3-羟基-3-甲基戊二酰辅酶a还原酶的抑制剂,是一类著名的药物,在心血管疾病和脂质疾病中具有有益的治疗作用,并且具有潜在的抗癌用途。然而,由于低水溶性和快速代谢,他汀类药物的生物利用度受到阻碍。为了改善他汀类药物的药代动力学特征,药物递送系统的开发是有希望的。因此,使用脂质体将他汀类药物选择性递送至选定部位或增强生物利用度是增加他汀类药物治疗效果的有效策略。此外,脂质体递送可以减少他汀类药物的所需剂量,尤其是在抗肿瘤作用方面。脂质体由于其独特的特性以及双相和两亲性而引起了人们的极大兴趣,可以被认为是递送亲水性和亲脂性他汀类药物的合适选择。在这篇综述文章中,我们专注于脂质体,并基于大小,磷脂组成,循环半衰期和胆固醇含量的差异,评估不同脂质体递送系统对他汀类药物功能的影响。

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