Hydrophilic or Lipophilic Statins?

Abstract

Drugs can be classified as hydrophilic or lipophilic depending on their ability to dissolve in water or in lipid-containing media. The predominantly lipophilic statins (simvastatin, fluvastatin, pitavastatin, lovastatin and atorvastatin) can easily enter cells, whereas hydrophilic statins (rosuvastatin and pravastatin) present greater hepatoselectivity. Although the beneficial role of statins in primary and secondary cardiovascular prevention has been unequivocally confirmed, the possible superiority of one statin or other regarding their solubility profile is still not well-established. In this respect, although some previously published observational studies and clinical trials observed a superiority of lipophilic statins in cardiovascular outcomes, these results could also be explained by a greater low-density lipoprotein cholesterol reduction with this statin type. On the other hand, previous studies reported conflicting results as to the possible superiority of one statin type over the other regarding heart failure outcomes. Furthermore, adverse events with statin therapy may also be related to their solubility profile. Thus, the aim of the present review was to collect clinical evidence on possible differences in cardiovascular outcomes among statins when their solubility profile is considered, and how this may also be related to the occurrence of statin-related adverse effects.

Organic Anion Transporting Polypeptide 2B1 in Human Fetal Membranes: A Novel Gatekeeper for Drug Transport During Pregnancy?

“…We further validated the functional role of OATP2B1 in crossing the feto-maternal interface by using an exogenous substrate (rosuvastatin) and siRNA silencing of OATP2B1 in CTCs in our previously developed feto-maternal interface-OOC device. Rosuvastatin is more hydrophilic than other statins (such as pravastatin) and requires protein transporters such as OATP2B1 to enter the cell to inhibit the HMG-CoA reductase enzyme (Climent et al, 2021). Therefore, it is an ideal candidate to use as a substrate for characterizing the functions of transporter proteins.…”

“…We used stain as the model drug, since they are competitive inhibitors of 3-hydroxy-3methylglutaryl-coenzyme-A reductase (HMG-CoA reductase) and have been tested in multiple models of pregnancy complications, such as preterm birth and preeclampsia (Istvan, 2003;Basraon et al, 2012). Specifically, we selected rosuvastatin because it is more hydrophilic than other statins (such as pravastatin) and requires protein transporters such as OATP2B1 to enter the cell to inhibit the HMG-CoA reductase enzyme (Climent et al, 2021). This drug was loaded into the DEC chamber (innermost chamber) and its propagation throughout the FM layers measured using mass spectrometry (Figure 6A).…”

Osteopontin Gene Polymorphisms Are Associated with Cardiovascular Risk Factors in Patients with Premature Coronary Artery Disease

“…ApoB has been related to dyslipidemia processes and it is considered a significant predictor of cardiovascular diseases such as myocardial infarction [ 68 ]. In this sense, our control group was not under a lipid-lowering treatment, this was probably why we found an association between the rs11730582 polymorphism and elevated ApoB levels [ 69 ].…”

Simvastatin Inhibits NLRP3 Inflammasome Activation and Ameliorates Lung Injury in Hyperoxia-Induced Bronchopulmonary Dysplasia via the KLF2-Mediated Mechanism

“…As an HMG-CoA reductase inhibitor, simvastatin is a widely used drug for treating dyslipidemia and cardiovascular diseases [ 26 – 29 ]. In addition, simvastatin demonstrates vascular protective effects by inducing KLF2 expression [ 30 ].…”