2014
DOI: 10.1002/cmdc.201300563
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Delivery of Suramin as an Antiviral Agent through Liposomal Systems

Abstract: Norovirus RNA-dependent RNA polymerase (RdRp) is a promising target enzyme for the development of new antiviral drugs. Starting from the crystal structure of norovirus RdRp, we had previously performed an in silico docking search using a library of low-molecular-weight compounds that enabled us to select molecules with predicted enzyme inhibitory activity. Among these, the polysulfonated naphthylurea suramin proved to inhibit in vitro both murine and human norovirus polymerases, with IC50 values in the low mic… Show more

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Cited by 30 publications
(25 citation statements)
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“…However, following the administration of suramin, we did not observe any difference in intracellular CHIKV RNA after CHIKV entry. Suramin bears strongly hydrophilic polysulfonate groups, which might limit accessibility across cellular membranes [ 49 ].…”
Section: Discussionmentioning
confidence: 99%
“…However, following the administration of suramin, we did not observe any difference in intracellular CHIKV RNA after CHIKV entry. Suramin bears strongly hydrophilic polysulfonate groups, which might limit accessibility across cellular membranes [ 49 ].…”
Section: Discussionmentioning
confidence: 99%
“…19 Given the release data, we hypothesize that the immediate microenvironment will be affected by low concentrations of the drug over the first 30 days, with much of the suramin release being dictated by cellular adhesion to MDP hydrogels, mediated by an –RGDS terminal sequence, and degradation of MDP matrix, mediated by MMP-susceptible –LRG– domain. Sustained and targeted delivery of suramin has been a goal of several groups, liposomal encapsulation of suramin for antiviral applications, 20 encapsulation of suramin/paclitaxel into PLLA/PLGA microparticles for cancer treatment, 21 and local delivery to inhibit neointimal hyperplasia postangioplasty, 22 to name a few. However, of primary concern with any of these techniques is the release, detailed above, and bioavailability, detailed below, of the suramin after loading into the carrier.…”
Section: Controlled Release Of An Ionically Sequestered Drugmentioning
confidence: 99%
“…Highly pure phosphatidylcholine (PC) 90% from soybean (Phospholipon 90G Lipoid, Germany); cholesterol 97% (Fluka, Germany); dimethyldioactdecylammonium bromide (DDAB) (Sigma-Aldrich, UK); dimethyldioctadecylammonium chloride (DDAC) (Sigma-Aldrich, UK); and ivermectin (Sigma-Aldrich, UK) are used. The determination of entrapment efficiency was conducted with Sepharose 4B (Pharmacia, Uppsala, Sweden) and Isotonic Palitzsch Buffer (pH 7.44) as previously described [ 11 ]. For TLC analysis, iodine was used (Fluka, Germany).…”
Section: Methodsmentioning
confidence: 99%