Abstract

Proliferative vitreoretinopathy (PVR) with rhegmatogenous retinal detachment (RRD) is a complex inflammatory ocular disease. Statins are widely used cholesterol-lowering drugs with putative anti-inflammatory properties. In this study, we have explored their efficacy in controlling post-surgical PVR formation. Simvastatin (SIM), atorvastatin (ATV), or rosuvastatin (RSV) were added to cultures of human retinal pigment epithelial cells (ARPE-19) prior to exposure with the bacterial lipopolysaccharide (LPS), and the production of pro-inflammatory cytokines (IL-6, IL-8, MCP-1) was examined using an enzyme-linked immunosorbent assay. In addition, the concentrations of simvastatin, atorvastatin, rosuvastatin, and their metabolites were measured from the vitreal samples of 20 patients undergoing vitrectomy (16 of them receiving oral statin therapy) using an ultra-performance liquid chromatography-tandem mass spectrometer technique. All statins alleviated LPS-induced inflammation at 5 µM concentration in the ARPE-19 cell cultures. Statin levels in the vitreous samples ranged from 6 to 316 pg/mL (ca. 0.1–7 M−10). Vitreal statin concentrations were similar to the typical steady-state unbound statin concentrations in plasma, indicating that only the unbound drug distributes from the blood circulation into the vitreous. Pharmacokinetic simulations of the intravitreal delivery of statins indicate that the measured clinical statin concentrations could be maintained with existing drug delivery technologies for months. Our results suggest that intravitreal statin therapy may have the potential in alleviating the risk of post-surgical PVR.

Details

Title
Statins for the prevention of proliferative vitreoretinopathy: cellular responses in cultured cells and clinical statin concentrations in the vitreous
Author
Yashavanthi, Mysore 1 ; del Amo Eva M 1 ; Loukovaara Sirpa 2 ; Hagström Marja 3 ; Urtti Arto 4 ; Kauppinen Anu 1 

 University of Eastern Finland, School of Pharmacy, Faculty of Health Sciences, Kuopio, Finland (GRID:grid.9668.1) (ISNI:0000 0001 0726 2490) 
 University of Helsinki, Department of Ophthalmology, Unit of Vitreoretinal Surgery, Helsinki University Central Hospital, and Individualized Drug Therapy Research Program, Helsinki, Finland (GRID:grid.7737.4) (ISNI:0000 0004 0410 2071) 
 University of Helsinki, School of Pharmacy, Helsinki, Finland (GRID:grid.7737.4) (ISNI:0000 0004 0410 2071) 
 University of Eastern Finland, School of Pharmacy, Faculty of Health Sciences, Kuopio, Finland (GRID:grid.9668.1) (ISNI:0000 0001 0726 2490); University of Helsinki, School of Pharmacy, Helsinki, Finland (GRID:grid.7737.4) (ISNI:0000 0004 0410 2071); St. Petersburg State University, Institute of Chemistry, Petergof, Russian Federation (GRID:grid.15447.33) (ISNI:0000 0001 2289 6897) 
Publication year
2021
Publication date
2021
Publisher
Nature Publishing Group
e-ISSN
20452322
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2477375960
Copyright
© The Author(s) 2021. This work is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.