Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Anti-Doping Laboratory Qatar, Life Sciences Research Division, Doha, Qatar.
J Cell Physiol. 2019 Feb;234(2):1219-1229. doi: 10.1002/jcp.27121. Epub 2018 Sep 10.
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.
他汀类药物是羟甲基戊二酰辅酶 A 还原酶的抑制剂，属于一类众所周知的药物，在心脑血管疾病和脂质紊乱方面具有有益的治疗效果，并且具有抗肿瘤的潜力。然而，由于低水溶解度和快速代谢，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性，开发药物传递系统是很有前途的。因此，使用脂质体将他汀类药物选择性递送至特定部位或提高生物利用度是一种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，特别是在抗肿瘤效果方面。脂质体由于其独特的性质和两亲性，已经引起了广泛的关注，并可以被认为是亲水和亲脂性他汀类药物递送的合适选择。在这篇综述文章中，我们重点关注脂质体，并根据其大小、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。
