Abstract
In 10% to 40% of the cases of coronary stent implantation, patients face in-stent restenosis due to an inflammatory response, which induces artery thickening. Everolimus, a drug that inhibits growth factor-stimulated cell proliferation of endothelial cells, represents a promising alternative to prevent in-stent restenosis. In this study, everolimus was encapsulated by a film hydration technique in liposomes by using phosphatidylcholine and cholesterol at different ratios. As the ratio of cholesterol increases, it modulates the rigidity of the structure which can affect the encapsulation efficiency of the drug due to steric hindrance. Moreover, various lipid : drug ratios were tested, and it was found that as the lipid : drug ratio increases, the encapsulation efficiency also increases. This behavior is observed because everolimus is a hydrophobic drug; therefore, if the lipidic region increases, more drug can be entrapped into the liposomes. In addition, stability of the encapsulated drug was tested for 4 weeks at 4°C. Our results demonstrate that it is possible to prepare liposomal everolimus by film hydration technique followed by extrusion with high entrapment efficiency as a viable drug delivery system.
Highlights
Cardiovascular disease remains the leading cause of morbidities and mortality worldwide
We found that the formulation with the highest %EE (95%) was a liposome with a lipid : drug 60 : 1 ratio and with a lipid composition with POPC Chol 9 : 1. It was found that the %EE of everolimus is directly proportional to the lipid : drug ratio and inversely proportional to the amount of cholesterol and double bonds present in PC
This finding could be relevant for the encapsulation of other hydrophobic drugs in liposomes following similar compositions
Summary
Cardiovascular disease remains the leading cause of morbidities and mortality worldwide. It encompasses a broad range of conditions that affect the heart and blood vessels, many of which are related to a process called atherosclerosis. Up to 4 out of 10 people with coronary stents present in-stent restenosis, a decrease in the diameter of the arterial lumen [2]. This phenomenon is caused by neointimal proliferation, that is an excessive propagation of the endothelial tissue in the interior area of the stent or by new atherosclerotic plaques [3]. There are several excipients that can be used for drug release, including polymeric, nanoparticle, and liposomal coatings
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