About: Macromolecular prodrugs of ribavirin: Polymer backbone defines blood safety, drug release, and efficacy of anti-inflammatory effects

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About: Macromolecular prodrugs of ribavirin: Polymer backbone defines blood safety, drug release, and efficacy of anti-inflammatory effects Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Macromolecular prodrugs of ribavirin: Polymer backbone defines blood safety, drug release, and efficacy of anti-inflammatory effects
Creator	Gajda, Paulina Sørensen, Lise Tolstrup, Martin Zuwala, Kaja Riber, Camilla Zelikin, Alexander Andersen, Anna Løvschall, Kaja
Source	Elsevier; Medline; PMC
abstract	Abstract Macromolecular (pro)drugs hold much promise as broad-spectrum antiviral agents as either microbicides or carriers for intracellular delivery of antiviral drugs. Intriguing opportunity exists in combining the two modes of antiviral activity in the same polymer structure such that the same polymer acts as a microbicide and also serves to deliver the conjugated drug (ribavirin) into the cells. We explore this opportunity in detail and focus on the polymer backbone as a decisive constituent of such formulations. Fourteen polyanions (polycarboxylates, polyphosphates and polyphosphonates, and polysulfonates) were analyzed for blood pro/anti coagulation effects, albumin binding and albumin aggregation, inhibitory activity on polymerases, cytotoxicity, and anti-inflammatory activity in stimulated macrophages. Ribavirin containing monomers were designed to accommodate the synthesis of macromolecular prodrugs with disulfide-exchange triggered drug release. Kinetics of drug release was fast in all cases however enhanced hydrophobicity of the polymer significantly slowed release of ribavirin. Results of this study present a comprehensive view on polyanions as backbone for macromolecular prodrugs of ribavirin as broad-spectrum antiviral agents.
has issue date	2018-04-10(xsd:dateTime)
bibo:doi	10.1016/j.jconrel.2018.02.012
bibo:pmid	29432822
has license	els-covid
sha1sum (hex)	73bef56a5413095ad768aa4118258686618ae229
schema:url	https://doi.org/10.1016/j.jconrel.2018.02.012
resource representing a document's title	Macromolecular prodrugs of ribavirin: Polymer backbone defines blood safety, drug release, and efficacy of anti-inflammatory effects
has PubMed Central identifier	PMC7114659
has PubMed identifier	29432822
schema:publication	Journal of Controlled Release
resource representing a document's body	covid:73bef56a5413095ad768aa4118258686618ae229#body_text
is schema:about of	named entity 'POLYANIONS' named entity 'BROAD' named entity 'DELIVERY' named entity 'PROMISE' named entity 'CARRIERS' named entity 'RELEASE' named entity 'HOLD' named entity 'ACTS' named entity 'COMBINING' named entity 'BACKBONE' named entity 'CONSTITUENT' covid:arg/73bef56a5413095ad768aa4118258686618ae229 named entity 'ANTI-INFLAMMATORY' named entity 'POLYMER' named entity 'STRUCTURE' named entity 'PRODRUGS' named entity 'RESULTS' named entity 'PRODRUGS' named entity 'ANTIVIRAL ACTIVITY' named entity 'MACROPHAGES' named entity 'TRIGGERED' named entity 'RIBAVIRIN' named entity 'DRUG RELEASE' named entity 'BACKBONE' named entity 'BLOOD SAFETY' named entity 'EFFECTS' named entity 'EFFICACY' named entity 'OPPORTUNITY' named entity 'COMPREHENSIVE' named entity 'PRESENT' named entity 'DRUG RELEASE' named entity 'SPECTRUM' named entity 'MICROBICIDES' named entity 'FOURTEEN' named entity 'HYDROPHOBICITY' named entity 'BINDING' named entity 'CASES' named entity 'KINETICS' named entity 'AGGREGATION' named entity 'CELLS' named entity 'TO DELIVER' named entity 'EFFECTS' named entity 'ALBUMIN' named entity 'POLYMER' named entity 'BLOOD' named entity 'ENHANCED' named entity 'ANALYZED' named entity 'RIBAVIRIN' named entity 'ANTI-INFLAMMATORY ACTIVITY' named entity 'FOCUS' named entity 'MICROBICIDE' named entity 'PRO' named entity 'POLYPHOSPHATES' named entity 'ANTIVIRAL DRUGS' named entity 'VIEW' named entity 'EXCHANGE' named entity 'MUCH' named entity 'STUDY' named entity 'SYNTHESIS' named entity 'MONOMERS' named entity 'EITHER' named entity 'INHIBITORY ACTIVITY' named entity 'DISULFIDE' named entity 'POLYMERASES' named entity 'CONJUGATED' named entity 'CONTAINING' named entity 'INTRACELLULAR' named entity 'ANTIVIRAL AGENTS' named entity 'DRUG' named entity 'S T' named entity 'STIMULATED' named entity 'CYTOTOXICITY' named entity 'COAGULATION' named entity 'SLOWED'

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