About: A Strategy to Treat COVID-19 Disease with Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Non-clinical Pharmacokinetic Study

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About: A Strategy to Treat COVID-19 Disease with Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Non-clinical Pharmacokinetic Study Goto Sponge NotDistinct Permalink

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Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	A Strategy to Treat COVID-19 Disease with Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Non-clinical Pharmacokinetic Study
Creator	Chen, Yee-Chun Wu, Huey-Dong Shih, Sheue-Fang Tai, Tien-Tzu Tsai, Yi-Chen Wang, An-Min Wang, Hui-Ting Wu, Tzung-Ju
Source	BioRxiv
abstract	Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a newly identified pathogen causing coronavirus disease 2019 (COVID-19) pandemic. Hydroxychloroquine (HCQ), an antimalarial and anti-inflammatory drug, has been shown to inhibit SARS-CoV-2 infection in vitro and tested in clinical studies. However, lung concentration (6.7 µg/mL) to predict the in vivo antiviral efficacy might not be achievable with the currently proposed oral dosing regimen. Further, a high cumulative doses of HCQ may raise concerns of systemic toxicity, including cardiotoxicity. Here, we described a non-clinical study to investigate the pharmacokinetics of a novel formulation of liposomal HCQ administrated by intratracheal (IT) instillation in Sprague-Dawley (SD) rats which achieved 129.4 µg/g (Cmax) in the lung. Compared to unformulated HCQ administered intravenous (IV), liposomal HCQ with normalized dose showed higher (∼30-fold) lung exposure, longer (∼2.5-fold) half-life in lung, but lower blood exposure with ∼20% of Cmax and 74% of AUC and lower heart exposure with 24% of Cmax and 58% of AUC. In conclusion, the pharmacokinetics results in an animal model demonstrate the proof of concept that inhalable liposomal HCQ may provide clinical benefit and serve as a potential treatment for COVID-19.
has issue date	2020-07-10(xsd:dateTime)
bibo:doi	10.1101/2020.07.09.196618
has license	biorxiv
sha1sum (hex)	3d26060058234765d6cbd486736cac0eaeb04fd2
schema:url	https://doi.org/10.1101/2020.07.09.196618
resource representing a document's title	A Strategy to Treat COVID-19 Disease with Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Non-clinical Pharmacokinetic Study
schema:publication	bioRxiv
resource representing a document's body	covid:3d26060058234765d6cbd486736cac0eaeb04fd2#body_text
is schema:about of	named entity 'C max' named entity 'systemic' named entity 'investigate' named entity 'REGIMEN' named entity 'PREDICT' named entity 'ANTIVIRAL' named entity 'IN VIVO' named entity 'PANDEMIC' named entity 'IDENTIFIED' named entity 'INTRATRACHEAL' named entity 'TESTED' named entity 'TO INVESTIGATE' named entity 'ANTI-INFLAMMATORY DRUG' named entity 'Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)' named entity 'anti-inflammatory' named entity 'clinical studies' named entity 'intratracheal' named entity 'cardiotoxicity' named entity 'Severe acute respiratory syndrome coronavirus 2' named entity 'HCQ' named entity 'infection' named entity 'pathogen' named entity 'HCQ' named entity 'antiviral' named entity 'Non-clinical' named entity 'Further' named entity 'acetonitrile' named entity 'rapid heart rate' named entity 'Solidarity Trial' named entity 'internal standard' named entity 'effective dose' named entity 'abnormal heart rhythms' named entity 'anticoagulant' named entity 'antiviral' named entity 'lung' named entity 'formic acid' named entity 'lung disease' named entity 'immunocompromised' named entity 'ng/mL' named entity 'pulmonary disease' named entity 'HCQ' named entity 'liposomal' named entity 'drug delivery' named entity 'lung' named entity 'inhalable' named entity 'liposomal' named entity 'loading dose' named entity 'cardiotoxicity' named entity 'lung' named entity 'COVID' named entity 'lung' named entity 'formic acid' named entity 'lung' named entity 'organ' named entity 'LC-MS/MS' named entity 'FDA' named entity 'HCQ' named entity 'lung' named entity 'effective dose' named entity 'systemic circulation' named entity '0.01' named entity 'liposomal' named entity 'sialic acids' named entity 'sustained release' named entity 'lung' named entity 'inhalable' named entity 'highly contagious' named entity 'organ' named entity 'HCQ' named entity 'azithromycin' named entity 'mobile phase' named entity 'liposomal' named entity 'lung' named entity 'residence time' named entity 'trachea' named entity 'inhalable' named entity 'HCQ'

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