Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes

Although phosphodiesterase type 5 inhibitors are widely used and well-studied drugs, the potential benefits of their application in the treatment of various diseases and new drug delivery systems, including liposome forms, are still being discussed. In this regard, the role of the lipid matrix of ce...

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Autores principales:	Anastasiia A. Zakharova, Svetlana S. Efimova, Olga S. Ostroumova
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	phosphodiesterase type 5 inhibitors sildenafil vardenafil tadalafil lipid bilayers liposomes Chemical technology TP1-1185 Chemical engineering TP155-156
Acceso en línea:	https://doaj.org/article/d9e8fb21a21a41f3a9501598481b7058
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spelling	oai:doaj.org-article:d9e8fb21a21a41f3a9501598481b70582021-11-25T18:20:08ZPhosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes10.3390/membranes111108932077-0375https://doaj.org/article/d9e8fb21a21a41f3a9501598481b70582021-11-01T00:00:00Zhttps://www.mdpi.com/2077-0375/11/11/893https://doaj.org/toc/2077-0375Although phosphodiesterase type 5 inhibitors are widely used and well-studied drugs, the potential benefits of their application in the treatment of various diseases and new drug delivery systems, including liposome forms, are still being discussed. In this regard, the role of the lipid matrix of cell membranes in the pharmacological action of the inhibitors is of special interest. It was shown that sildenafil, vardenafil, and tadalafil caused a significant decrease in the boundary potential of model membranes composed of palmitoyloleoylphosphatidylcholine or its mixture with cholesterol, by 70–80 mV. The reduction in the membrane dipole potential induced by inhibitors led to a 20–25% increase in the conductance of cation-selective pores formed by the antimicrobial peptide gramicidin A. The addition of sildenafil or vardenafil also led to a significant decrease in the temperature of the main phase transition of dipalmytoylphosphatidylcholine, by about 1.5 °C, while tadalafil did not change the melting temperature. Sildenafil, vardenafil, and tadalafil enhanced the pore-forming activity of the antifungal polyene antibiotic nystatin by 11, 13, and 2 times, respectively. This fact might indicate the induction of membrane curvature stress by the inhibitors. The data obtained might be of special interest for the development of lipid-mediated forms of drugs.Anastasiia A. ZakharovaSvetlana S. EfimovaOlga S. OstroumovaMDPI AGarticlephosphodiesterase type 5 inhibitorssildenafilvardenafiltadalafillipid bilayersliposomesChemical technologyTP1-1185Chemical engineeringTP155-156ENMembranes, Vol 11, Iss 893, p 893 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	phosphodiesterase type 5 inhibitors sildenafil vardenafil tadalafil lipid bilayers liposomes Chemical technology TP1-1185 Chemical engineering TP155-156
spellingShingle	phosphodiesterase type 5 inhibitors sildenafil vardenafil tadalafil lipid bilayers liposomes Chemical technology TP1-1185 Chemical engineering TP155-156 Anastasiia A. Zakharova Svetlana S. Efimova Olga S. Ostroumova Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
description	Although phosphodiesterase type 5 inhibitors are widely used and well-studied drugs, the potential benefits of their application in the treatment of various diseases and new drug delivery systems, including liposome forms, are still being discussed. In this regard, the role of the lipid matrix of cell membranes in the pharmacological action of the inhibitors is of special interest. It was shown that sildenafil, vardenafil, and tadalafil caused a significant decrease in the boundary potential of model membranes composed of palmitoyloleoylphosphatidylcholine or its mixture with cholesterol, by 70–80 mV. The reduction in the membrane dipole potential induced by inhibitors led to a 20–25% increase in the conductance of cation-selective pores formed by the antimicrobial peptide gramicidin A. The addition of sildenafil or vardenafil also led to a significant decrease in the temperature of the main phase transition of dipalmytoylphosphatidylcholine, by about 1.5 °C, while tadalafil did not change the melting temperature. Sildenafil, vardenafil, and tadalafil enhanced the pore-forming activity of the antifungal polyene antibiotic nystatin by 11, 13, and 2 times, respectively. This fact might indicate the induction of membrane curvature stress by the inhibitors. The data obtained might be of special interest for the development of lipid-mediated forms of drugs.
format	article
author	Anastasiia A. Zakharova Svetlana S. Efimova Olga S. Ostroumova
author_facet	Anastasiia A. Zakharova Svetlana S. Efimova Olga S. Ostroumova
author_sort	Anastasiia A. Zakharova
title	Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
title_short	Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
title_full	Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
title_fullStr	Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
title_full_unstemmed	Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes
title_sort	phosphodiesterase type 5 inhibitors greatly affect physicochemical properties of model lipid membranes
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/d9e8fb21a21a41f3a9501598481b7058
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Phosphodiesterase Type 5 Inhibitors Greatly Affect Physicochemical Properties of Model Lipid Membranes

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